Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/557)
- The additional cyclo has at least six ring members (Class 540/559)
- Chalcogen in the tricyclo ring system (Class 540/560)
- The additional cyclo consists of one nitrogen and four carbons (e.g., diazepinoindoles, etc.) (Class 540/561)
- The additional cyclo consists of two nitrogens and three carbons (e.g., imidazobenzodiazepines, etc.) (Class 540/562)
- s-Triazolo(4,3-a)(1,4)-benzodi-azepines (including hydrogenated) (Class 540/563)
- Chalcogen, nitrogen, cyano or halogen bonded directly to ring carbon of the triazolo ring (Class 540/564)
- Nitrogen attached indirectly to ring carbon of the triazolo ring by acyclic nonionic bonding (Class 540/565)
- The unshared ring carbon of the triazolo ring is unsubstituted or alkyl substituted only (Class 540/566)
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Publication number: 20010039272Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 and R3 independently represent a hydrogen atom or a C1-6 alkyl group, or R2 and R3 may combine together to represent a 5- or 6-membered cycloalkyl group; R4 represents, for example, a hydrogen atom or a C1-6 alkyl group; R5 represents, for example, a hydrogen atom or a C1-6 alkyl group; R6 represents a hydrogen atom or a C-1-6 alkyl group; X represents —NR7—, —O—, —CHR7— or —S— in which R7 represents, for example, a hydrogen atom or a C1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.Type: ApplicationFiled: April 20, 2001Publication date: November 8, 2001Inventor: Koichi Shudo
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Patent number: 6268360Abstract: The present invention provides compounds of the general formula: wherein Y is a moiety selected independently, from NH or —(CH2)n— wherein n is 1; m is an integer from 1 to 2; and the moiety represents: (1) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is nitrogen, and B and C are CH), (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is carbon, B is nitrogen, and C is —CH—CH—), (3) a 6-membered aromatic (unsaturated) ring (wherein A is carbon, B is CH, and C is —CH—CH—); as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.Type: GrantFiled: October 27, 2000Date of Patent: July 31, 2001Assignee: American Home Products CorporationInventors: Amedeo A. Failli, David K. Williams, Thomas J. Caggiano, Jay S. Shumsky, Mark A. Ashwell
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Patent number: 6251895Abstract: The present invention provides the novel Dihydrate D 2-methyl-thieno-benzodiazepine and a formulation therefor.Type: GrantFiled: September 23, 1997Date of Patent: June 26, 2001Assignee: Eli Lilly and CompanyInventors: Samuel Dean Larsen, John Richard Nichols, Susan Marie Reutzel, Gregory Alan Stephenson
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Patent number: 6194407Abstract: The present invention provides compounds of the general formula: wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.Type: GrantFiled: July 24, 1998Date of Patent: February 27, 2001Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Jay S. Shumsky, Robert J. Steffan
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Patent number: 6174882Abstract: Methods and compositions are disclosed utilizing 2-hydroxymethylolanzapine for the treatment of psychosis in humans. 2-Hydroxymethylolanzapine exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. 2-Hydroxymethylolanzapine is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse, depressive signs and symptoms, tic disorder, functional bowel disorder and fungal dermatitis.Type: GrantFiled: November 22, 1999Date of Patent: January 16, 2001Assignee: Sepracor Inc.Inventor: William E. Yelle
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Patent number: 6169084Abstract: The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.Type: GrantFiled: September 30, 1998Date of Patent: January 2, 2001Assignee: Eli Lilly and CompanyInventors: Charles Arthur Bunnell, Thomas Harry Ferguson, Barry Arnold Hendriksen, Manuel Vicente Sanchez-Felix, David Edward Tupper
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Patent number: 6150354Abstract: A method of treating Alzheimer's disease and related dementias by treatment with analogs of galanthamine, particularly those wherein the methoxy and hydroxy substituents are replaced by, for example carbamate groups, the methoxy is replaced by hydroxy and esters of galanthamine and O-desmethyl galanthamine. Many of the useful compounds are novel.Type: GrantFiled: October 19, 1993Date of Patent: November 21, 2000Assignee: Bonnie DavisInventors: Bonnie Davis, Madeleine M. Joullie
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Patent number: 6103715Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof.Type: GrantFiled: August 25, 1998Date of Patent: August 15, 2000Assignee: Allelix Biopharmaceuticals Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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Patent number: 6075018Abstract: The invention relates to new 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof and pharmaceutical compositions comprising them. The new 1-[2-(substituted vinyl)]-3,4-dihidro-5H-2,3-benzodiazepine derivatives according to the invention correspond to the general formula (I), ##STR1## wherein the variables are hereinbelow defined: The new compounds according to the invention affect the central nervous system and can be used to advantage in the therapy.Type: GrantFiled: February 9, 1996Date of Patent: June 13, 2000Assignee: Egis Gyogyszergyar Rt.Inventors: Pal Vago, Jozsef Reiter, Istvan Gyertyan, Gabor Gigler, Ferenc Andrasi, Anna Bakonyi, Pal Berzsenyi, Peter Botka, deceased, Erszebet Birkas, Tamas Hamori, Edit Horvath, Katalin Horvath, Jeno Korosi, deceased, Gyorgyne Mate, Imre Moravcsik, Gyorgy Somogyi, Eszter Szentkuti, Gabor Zolyomi
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Patent number: 6034078Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or halo, and R.sup.2 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-6 cycloalkyl optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl in which the cycloalkyl group is optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, or optionally substituted phenyl-C.sub.1-4 alkyl; or a salt thereof. Such compounds are useful for treating a disorder of the central nervous system which is associated with the modulation of a 5-HT.sub.3 receptor.Type: GrantFiled: July 1, 1997Date of Patent: March 7, 2000Assignees: Eli Lilly and Company Limited, Eli Lilly and CompanyInventors: John Fairhurst, Terrence Michael Hotten, David Edward Tupper, David Taiwai Wong
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Patent number: 6020487Abstract: The present invention provides a process for preparing olanzapine and intermediates therefor.Type: GrantFiled: September 23, 1997Date of Patent: February 1, 2000Assignee: Eli Lilly and CompanyInventors: Charles Arthur Bunnell, Samuel Dean Larsen, John Richard Nichols, Susan Marie Reutzel, Gregory Alan Stephenson
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Patent number: 6008213Abstract: Compounds of formula (I) ##STR1## wherein A.sub.1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R.sup.3 or R.sup.4 ; X.sup.1 --X.sup.2 is CHR.sup.1 --CH, CR.sup.1 .dbd.CH, NR.sup.1 --CH, S(O).sub.u --CH or O--CH; X.sup.3 is CR.sup.5 R.sup.5 ', NR.sup.5, S(O).sub.u or O; R.sup.2 is --OR', --NR'R", --NR'SO.sub.2 R'", --NR'OR', --OCR'.sub.2 C(O)OR', --OCR'.sub.2 OC(O)--R', --OCR'.sub.2 C(O)NR'.sub.2, CF.sub.3 or --COCR'.sub.2 R.sup.2 '; R.sup.3, R.sup.4 and R.sup.7 are independently H, halo, --OR.sup.12, --SR.sup.12, --CN, --NR'R.sup.12, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R', --CONR'.sub.2, R.sup.14 --C.sub.0-6 alky-, R.sup.14 --C.sub.1-6 oxoalkyl-, R.sup.14 --C.sub.2-6 alkenyl-, R.sup.14 --C.sub.2-6 alkynyl-, R.sup.14 --C.sub.0-6 alkyloxy-, R.sup.14 --C.sub.0-6 alkylamino- or R.sup.14 --C.sub.0-6 alkyl--S(O).sub.r --; R.sup.6 is W--(CR'.sub.2).sub.q --Z--(CR'R.sup.10)--U--(CR'.sub.2).sub.s --V-- or W'--(CR'.sub.2).sub.Type: GrantFiled: December 19, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, William H. Miller
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Patent number: 6008216Abstract: 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system.Type: GrantFiled: July 24, 1998Date of Patent: December 28, 1999Assignee: Eli Lilly And Company and LimitedInventors: Jiban Kumar Chakrabarti, Terrence Michael Hotten, David Edward Tupper
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Patent number: 5985869Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.Type: GrantFiled: July 15, 1997Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5962449Abstract: The present invention relates to novel N-substituted amino acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 28, 1996Date of Patent: October 5, 1999Assignee: Novo Nordisk A/SInventors: Peter Madsen, Knud Erik Andersen, Rolf Hohlweg, Florenzio Zaragossa Dorwald, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen, Henrik Sune Andersen
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Patent number: 5929069Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R.sup.1 represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.3 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; x represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.Type: GrantFiled: September 20, 1996Date of Patent: July 27, 1999Assignee: Institute of Medicinal Molecular Design, Inc.Inventor: Koichi Shudo
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Patent number: 5919780Abstract: Compounds of formula I ##STR1## wherein X is N or C--R.sup.9, Y is N--R.sup.10, CH.sub.2, O, S, SO, SO.sub.2, C.dbd.O or CH--OH,R is H or alkyl,R.sup.1 is heteroaryl,n is 1-5, andR.sup.2 -R.sup.10 are H or various substituents,are useful as inhibitors of protein farnesyl transferase and for the treatment of proliferative diseases including cancer, restenosis and psoriasis, and as antiviral agents.Type: GrantFiled: December 11, 1997Date of Patent: July 6, 1999Assignee: Warner Lambert CompanyInventors: Gary L. Bolton, Annette M Doherty, James S. Kaltenbronn, John Quin, III, Jeffrey D. Scholten, Judith Sebolt-Leopold, Harold Zinnes
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Patent number: 5917033Abstract: The present invention pertains to a method for designing inhibitors of enzyme human immunodeficiency virus type 1 reverse transcriptase which comprises the steps of:(a) providing a three dimensional model of the receptor site in the prepolymerization complex of the p66 subunit of enzyme human immunodeficiency virus type 1 reverse transcriptase and a known nonnucleoside inhibitor;(b) locating the conserved residues in the p66 subunit which constitute the nonnucleoside inhibitor binding pocket; and(c) designing a new nonnucleoside inhibitor which possesses complementary structural features and binding forces to the residues in the p66 subunit nonnucleoside inhibitor binding pocket.Type: GrantFiled: October 31, 1995Date of Patent: June 29, 1999Assignee: University of Medicine & Dentistry of New JerseyInventors: Mukund J. Modak, Prem N. S. Yadav, Janardan S. Yadav
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Patent number: 5886016Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A, wherein X, m, n, p, B, R.sup.1, R.sup.2, and R.sup.4 are as described in the specification.Type: GrantFiled: June 9, 1997Date of Patent: March 23, 1999Assignee: G.D. Searle & Co.Inventors: John J Talley, Stephen R Bertenshaw, Donald J Rogier, Jr., Matthew J Graneto
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Patent number: 5854236Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: April 1, 1997Date of Patent: December 29, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Xuemei Du
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Patent number: 5849735Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.Type: GrantFiled: December 22, 1995Date of Patent: December 15, 1998Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Aranapakam M. Venkatesan, Efren G. Delos Santos
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Patent number: 5837704Abstract: Novel compounds for the treatment of HIV-1 infection. These are 2-heteroary-5,11-dihydro-6H-dipyrido?3,2-b:2',3'-e!?1,4!diazepines of the formula ##STR1## wherein Z is oxygen, sulfur, .dbd.NCN or .dbd.NOR.sup.Type: GrantFiled: August 1, 1996Date of Patent: November 17, 1998Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl Hargrave, John Proudfoot, Usha Patel, Suresh Kapadia, Terence Kelly, Daniel McNeil, Mario Cardozo
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Patent number: 5834463Abstract: Compounds represented by the formula: ##STR1## wherein ring A is benzene; Ar is aromatic group; R.sup.1, R.sup.2 and R.sup.3 each stands for H, acyl, hydrocarbon or heterocyclic, or R.sup.2 and R.sup.3, taken together, may form non-aromatic cyclic hydrocarbon; X is methylene or carbonyl; ......... is single bond or double bond; when ......... is single bond, Y is --NR.sup.4 -- (R.sup.4 is H, acyl, hydrocarbon or heterocyclic), when ......... is double bond, Y is N; n is 1-3, provided that, X is carbonyl and, at the same time, R.sup.2 and R.sup.3, taken together, form non-aromatic cyclic hydrocarbon, ......... is double bond or R.sup.4 is a heterocyclic or --Z(CH.sub.2).sub.m --W (Z is methylene or carbonyl, W is optionally substituted amino, and m denotes 0-5), or salts thereof have an excellent GnRH receptor antagonistic action and/or an action of improving sleep disturbances.Type: GrantFiled: June 26, 1995Date of Patent: November 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Nobuhiro Fujii, Koichi Kato, Masaomi Miyamoto
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Patent number: 5834459Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O);Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which D4 receptor stimulation is implicated, such as schizophrenia, is also described.Type: GrantFiled: April 1, 1996Date of Patent: November 10, 1998Assignee: Allelix Biopharmaceuticals Inc.Inventor: Jian-Min Fu
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Patent number: 5814628Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCI, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.Type: GrantFiled: December 10, 1996Date of Patent: September 29, 1998Assignee: Allelix Biopharmaceuticals Inc.Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
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Patent number: 5801174Abstract: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof whereinR.sup.1 is hydrogen, alkyl or benzyl;X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl;Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl;n is 0 or 1;R.sup.6 is phenyl which is substituted one or more times with substituents selected from the group consisting of SO.sub.2 NR'R", CONR'R", and COR'"wherein R' and R" each independently are hydrogen, alkyl, or --(CH.sub.2).sub.p --W, wherein p is 0, 1, 2, 3, 4, 5, or 6, and W is hydroxy, amino, alkoxycarbonyl, or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy or methylenedioxy; or wherein R' and R" together is (CH.sub.2).sub.r Z(CH.sub.2).sub.s wherein r and s each independently are 0, 1, 2, 3, 4, 5, or 6 and Z is O, S, CH.sub.2 or NR"" wherein R"" is hydrogen, alkyl, or --(CH.sub.2).sub.Type: GrantFiled: May 20, 1997Date of Patent: September 1, 1998Assignee: Neurosearch A/SInventors: Peter Moldt, Frank Watjen
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Patent number: 5795886Abstract: Compounds having general formula (I) wherein R is hydrogen or C.sub.1 -C.sub.10 alkyl; X is an aromatic moiety selected from phenyl, thienyl, furyl, pyridyl, imidazolyl, benzimidazolyl, benzothiazolyl and phthalazinyl which is unsubstituted or substituted with one or more moieties chosen from the group consisting of halogen, hydroxy, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, carboxy, C.sub.1 -C.sub.6 alkoxycarbonyl, acetyl, formyl, carboxymethyl, hydroxymethyl, amino, aminomethyl, methylenedioxy and trifluoromethyl; and "Aryl" represents p-nitrophenyl, p-aminophenyl or p-(protected amino) phenyl; or a pharmaceutically acceptable salt thereof, are useful as anticonvulsants.Type: GrantFiled: February 11, 1997Date of Patent: August 18, 1998Assignee: Eli Lilly and CompanyInventors: Benjamin A. Anderson, Marvin M. Hansen, Nancy K. Harn
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Patent number: 5756729Abstract: A multistep process for producing 8-chloro-6-(2-fluorophenyl)-1-methyl-4-H-imidazo?1,5a!?1,4! benzodiazepine (midazolam) comprises treating a compound of Formula II with a lower alkyl dithiol to produce a compound of Formula III, wherein n=2 or 3, converting the compound of Formula III to a compound of Formula VII, and then treating the compound of Formula VII with a deprotecting agent, thereby producing midazolam. Novel intermediate compounds are also disclosed.Type: GrantFiled: October 9, 1996Date of Patent: May 26, 1998Assignee: Ranbaxy Laboratories, Ltd.Inventors: Jag Mohan Khanna, Naresh Kumar, Chandrahas Khanduri, Mukesh Kumar Sharma, Pankaj Sharma, Swargam Sathyanarayan, Girij Pal Singh
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Patent number: 5756495Abstract: New 3-substituted 3H-2,3-benzodiazepine derivatives of general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and n have the meanings indicated in the description, their production as well as their use as pharmaceutical agents are described.Type: GrantFiled: January 31, 1997Date of Patent: May 26, 1998Assignee: Schering AktiengesellschaftInventors: Tamas Hamori, Istvan Tarnawa, Sandor Solyom, Pal Berzsenyi, Erzsebet Birkas, Ferenc Andrasi, Istvan Ling, Tibor Hasko, Gabor Kapus, Emese Csuzdl, Marta Szollosy, Franciska Erdo, Antal Simay, Gabor Zolyomi
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Patent number: 5753643Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 22, 1997Date of Patent: May 19, 1998Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen
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Patent number: 5739128Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: April 24, 1996Date of Patent: April 14, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Xuemei Du
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Patent number: 5736541Abstract: The invention provides Form II, a pharmaceutically elegant, stable polymorph of olanzapine useful for treating a condition selected from the group consisting of a psychotic condition, mild anxiety and gastrointestinal conditions.Type: GrantFiled: July 25, 1996Date of Patent: April 7, 1998Assignees: Eli Lilly and Company, Eli Lilly and CompanyInventors: Charles Arthur Bunnell, Barry Arnold Hendriksen, Samuel Dean Larsen
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Patent number: 5703232Abstract: The invention provides lower alcohol solvates of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno?2,3-b!?1,5!benzodiazepine (olanzapine) and a process for making such lower alcohol solvates of olanzapine. The invention provides a method for using such solvates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.Type: GrantFiled: January 16, 1996Date of Patent: December 30, 1997Assignee: Eli Lilly and CompanyInventors: Charles A. Bunnell, Terrence Michael Hotten, Samuel D. Larsen, David Edward Tupper
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Patent number: 5698551Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 29, 1996Date of Patent: December 16, 1997Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Patent number: 5665878Abstract: A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.Type: GrantFiled: March 28, 1995Date of Patent: September 9, 1997Assignee: Eli Lilly and CompanyInventors: Benjamin A. Anderson, Marvin M. Hansen, David L. Varie, Jeffrey T. Vicenzi, Milton J. Zmijewski
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Patent number: 5637584Abstract: The invention provides a methylene chloride solvate of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine. The invention provides a method for using such solvate.Type: GrantFiled: March 24, 1995Date of Patent: June 10, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventor: Samuel D. Larsen
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Patent number: 5631250Abstract: The invention provides lower alcohol solvates of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine (olanzapine) and a process for making such lower alcohol solyates of olanzapine. The invention provides a method for using such solyates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.Type: GrantFiled: March 24, 1995Date of Patent: May 20, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Charles A. Bunnell, Terrence M. Hotten, Samuel D. Larsen, David E. Tupper
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Patent number: 5624922Abstract: Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II ##STR1## .delta.-aminoamides of formula III and aryldimethanamines of formula XXXVII ##STR2## wherein A is an aryl or hetaryl ring;R.sup.1 is hydrogen, alkyl, aryl or hetaryl;R.sup.2 is hydrogen, alkyl, substituted alkyl, or aryl;R.sup.3 is alkyl, aryl, aralkyl or heteroatom substituted alkyl or aralkyl;R.sup.4 is hydrogen or alkyl;R.sup.5 is hydrogen, alkyl, aryl or hetaryl;R.sup.6 is hydrogen, alkyl, alkoxy, halogen or a fused benzene ring;R.sup.9 is hydrogen, alkyl, or substituted alkyl; andR.sup.10 is hydrogen, alkyl, or substituted alkyl the invention further relates to processes for the preparation of, pharmaceutical compositions containing, and methods of treating cardiac arrhythmia with the compounds of formulas XXXVI, XXX, II, III, and XXXVII.Type: GrantFiled: May 24, 1995Date of Patent: April 29, 1997Assignee: Sterling Winthrop Inc.Inventors: Robert E. Johnson, Donald C. Schlegel, Alan M. Ezrin
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Patent number: 5620974Abstract: Disclosed are novel 5,11-dihydro-6H-dipyrido[3,2-b; 2',3'-e][1,4]diazepines. These are useful in the prevention or treatment of HIV infection.Type: GrantFiled: July 22, 1994Date of Patent: April 15, 1997Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, John R. Proudfoot, Julian Adams, Karl G. Grozinger, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
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Patent number: 5602121Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 . . . is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.Type: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventor: Jian-Min Fu
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Patent number: 5602113Abstract: Disclosed are novel pyrido[2,3,-b][1,5]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.Type: GrantFiled: December 29, 1994Date of Patent: February 11, 1997Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
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Patent number: 5602120Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.Type: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
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Patent number: 5602124Abstract: Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ;and acid addition salts, solvates and hydrates thereof.Type: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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Patent number: 5593979Abstract: Disclosed are novel pyrido[2,3-b][1,4]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.Type: GrantFiled: December 29, 1994Date of Patent: January 14, 1997Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
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Patent number: 5571809Abstract: Disclosed are novel pyridodiazepines. These compounds, as well certain known 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-ones are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.Type: GrantFiled: August 17, 1994Date of Patent: November 5, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
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Patent number: 5561127Abstract: Described herein are D4 receptor-selective compounds of the general formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--NEt.sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2; andZ is selected from C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.Type: GrantFiled: December 19, 1994Date of Patent: October 1, 1996Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Ashok Tehim, Sumanas Rakhit
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Patent number: 5550117Abstract: Disclosed are novel dipyrido[3,2-b:2',3'-e][1,4]diazepines and their use in the treatment of HIV-1 infection.Type: GrantFiled: December 29, 1994Date of Patent: August 27, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
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Patent number: 5536832Abstract: The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I)R stands for a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group, or by one or more halogen(s); or R is a benzoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.1 means hydrogen; or R.sup.1 is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.2 means a C.sub.1-3 alkyl group; orR.sup.1 and R.sup.2 together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms;R.sup.3 means hydrogen or a C.sub.1-4 alkanoyl group;R.sup.4 represents hydrogen; a C.sub.Type: GrantFiled: April 17, 1995Date of Patent: July 16, 1996Assignee: Gyogyszerkutato Intezet KFTInventors: Ferenc Andrasi, Pal Berzsenyi, Peter Botka, Sandor Farkas, Katalin Goldschmidt, Tamas Hamori, Jeno Korosi, Imre Moravcsik, Istvan Tarnawa
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Patent number: 5532235Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.Type: GrantFiled: January 17, 1995Date of Patent: July 2, 1996Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Efren G. Delos Santos, Xuemei Du, Marvin E. Reich, Aranapakam M. Venkatesan
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Patent number: 5521174Abstract: The invention relates to novel N-acyl-2,3-benzodiezapine derivatives and a method of treating spasms of the skeletal musculature therewith.Type: GrantFiled: June 7, 1995Date of Patent: May 28, 1996Assignee: Gyogyszerkutato Intezet Kv.Inventors: Ferenc Andrasi, Pal Berzsenyi, Peter Botka, Sandor Farkas, Katalin Goldschmidt, Tamas Hamori, Jeno Korosi, Imre Moravcsik, Istvan Tarnawa