Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 546/285)
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Publication number: 20030216571Abstract: The present invention is to provide novel tricyclic compounds having leukotriene antagonistic action and represented by the formula: 1Type: ApplicationFiled: July 31, 2002Publication date: November 20, 2003Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Takashi Ikuta
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Publication number: 20030195200Abstract: The present invention relates to compounds of the general formula (I) 1Type: ApplicationFiled: February 20, 2003Publication date: October 16, 2003Inventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
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Patent number: 6630492Abstract: Mevinolin compounds for use in the treatment or prevention of autoimmune diseases, inflammation, ischemia/reperfusion injury and graft rejection. Such compounds bind to the LFA-1 I-domain and thereby inhibit LFA-1/ICAM-1 or LFA-1/ICAM-3 interactions.Type: GrantFiled: February 24, 2000Date of Patent: October 7, 2003Assignee: Novartis AGInventors: Wilfried Bauer, Sylvain Cottens, Dieter Geyl, Gabriele Weitz-Schmidt, Jörg Kallen, Ulrich Hommel
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Publication number: 20030187031Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: ApplicationFiled: December 6, 2002Publication date: October 2, 2003Inventors: Lilian Alcaraz, Mark Furber
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Publication number: 20030181489Abstract: In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment and/or prevention of cough in warm-blooded animals, including humans, such as compounds of formula Y—J—E An− (I), wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).Type: ApplicationFiled: February 14, 2003Publication date: September 25, 2003Inventors: Lewis Siu Leung Choi, Gregory N Beatch, Clive Page
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Publication number: 20030158127Abstract: The present invention discloses novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest.Type: ApplicationFiled: July 3, 2001Publication date: August 21, 2003Applicant: MALLINCKRODT INC.Inventors: Raghavan Rajagopalan, Gary L. Cantrell, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
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Publication number: 20030130515Abstract: Compounds of the formula 1Type: ApplicationFiled: January 2, 2003Publication date: July 10, 2003Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
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Publication number: 20030120081Abstract: A process for preparing a compound of the formula 1Type: ApplicationFiled: October 15, 2002Publication date: June 26, 2003Inventors: Jerry A. Murry, Timothy D. White
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Publication number: 20030114674Abstract: 1 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infections.Type: ApplicationFiled: October 4, 2002Publication date: June 19, 2003Inventors: Gerald Brooks, Eric Hunt, Steven Howard
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Patent number: 6521646Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.Type: GrantFiled: October 15, 2001Date of Patent: February 18, 2003Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
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Publication number: 20030027830Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, incluidng angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.Type: ApplicationFiled: July 18, 2002Publication date: February 6, 2003Applicant: University of Georgia Research Foundation, Inc.Inventors: J. Phillip Bowen, Thomas Philip Robinson, Tedman Ehlers, David Goldsmith, Jack Arbiser
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Publication number: 20030018218Abstract: A novel arylamine compound represented by the following general formula (1): 1Type: ApplicationFiled: July 12, 2002Publication date: January 23, 2003Applicant: Idemitsu Kosan Co., Ltd.Inventors: Chishio Hosokawa, Masakazu Funahashi
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Publication number: 20030008889Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: ApplicationFiled: July 19, 2002Publication date: January 9, 2003Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
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Patent number: 6492355Abstract: The invention provides compounds of general formula in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2000Date of Patent: December 10, 2002Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Michael P. Mortimore
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Publication number: 20020165402Abstract: Novel compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.Type: ApplicationFiled: May 13, 2002Publication date: November 7, 2002Inventors: Gregory N. Beatch, Lewis S. L. Choi, Clive P. Page, Bertrand M. C. Plouvier, Yuzhong Liu
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Publication number: 20020111335Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.Type: ApplicationFiled: June 29, 2001Publication date: August 15, 2002Inventors: Mark L. Nelson, Darrell Koza
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Publication number: 20020091264Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: 1Type: ApplicationFiled: December 17, 2001Publication date: July 11, 2002Applicant: SmithKline Beecham CorporationInventors: William E. Bondinell, William H. Miller, Dirk Heerding, James M. Samanen
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Publication number: 20020087005Abstract: A process for preparing a compound of the formula 1Type: ApplicationFiled: October 22, 2001Publication date: July 4, 2002Inventors: Jerry A. Murry, Timothy D. White
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Patent number: 6399606Abstract: Neuroprotective agents are disclosed having the following structure: wherein R1, R2, R3, R4 and R5 are as defined herein. Such compounds have utility in the treatment of conditions which benefit from administration of neuroprotective agents generally, including treatment of central and peripheral nervous condition as well as for promoting nerve cell differentiation. Methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more of the compounds of this invention.Type: GrantFiled: November 27, 2000Date of Patent: June 4, 2002Assignee: Nippon Kayaku Co., Ltd.Inventors: Moorthy S. S. Palanki, Shripad S. Bhagwat, Hiroshi Sato, Paul E. Erdman, Mary Doubleday
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Publication number: 20020042517Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: September 10, 2001Publication date: April 11, 2002Applicant: BAYER CORPORATIONInventors: Khire Uday, Jacques Dumas, Bernd Riedl, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Renick Joel, Robert N. Sibley
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Publication number: 20020040029Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.Type: ApplicationFiled: December 26, 2000Publication date: April 4, 2002Inventors: J. Phillip Bowen, Thomas Philip Robinson, Tedman Ehlers, David Goldsmith, Jack Arbiser
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Publication number: 20020010337Abstract: The invention relates to novel stilbene compounds having the general formula (I): 1Type: ApplicationFiled: February 21, 2001Publication date: January 24, 2002Inventors: Jean-Michel Bernardon, Bruno Charpentier
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Patent number: 6319948Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation. Also provided by the invention are certain novel substituted (5,6)-dihydronaphthalenyl compounds which are retinoid antagonists and possess the above-mentioned property in addition to their use as antiinflammatory agents for chronic skin inflammatory diseases, as agents for the treatment of rheumatic diseases and as agents for the treatment of various tumors as well as non-malignant proliferative skin conditions.Type: GrantFiled: December 8, 2000Date of Patent: November 20, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Tramposch, Xina Nair, Anne Marinier, Fred Christopher Zusi
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Patent number: 6268362Abstract: A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.Type: GrantFiled: September 7, 2000Date of Patent: July 31, 2001Assignee: Pharmacia & Upjohn SpAInventors: Tiziano Bandiera, Daniele Fancelli, Mario Varasi, Michele Caruso, Jacqueline Lansen, Antonino Suarato
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Publication number: 20010008941Abstract: A subject of the invention is the compounds of formula (I): 1Type: ApplicationFiled: January 10, 2001Publication date: July 19, 2001Applicant: Hoechst Marion RousselInventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
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Publication number: 20010005756Abstract: A subject of the invention is the compounds of formula (I): 1Type: ApplicationFiled: January 10, 2001Publication date: June 28, 2001Applicant: Hoechst Marion RousselInventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
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Publication number: 20010003121Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: ApplicationFiled: December 26, 2000Publication date: June 7, 2001Applicant: AstraZeneca UK LimitedInventors: Andrew Baxter, Thomas Mcinally, Michael Mortimore, David Cladingooel
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Patent number: 6239148Abstract: 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: April 6, 1998Date of Patent: May 29, 2001Assignee: Novo Nordisk A/SInventors: Florenzio Zaragossa Dörwald, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh Jørgensen, Uffe Bang Olsen, Henrik Sune Andersen, Svend Treppendahl, Polivka Zdenék, Silhánková Alexandra, Sindelár Karel
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Patent number: 6225328Abstract: Pharmaceutically/cosmetically-active adamantyl-substituted retinoid compounds have the structural formula (I): wherein Ar is a radical having one of the formulae (a)-(d): and are useful for the treatment of disorders and/or ailments manifesting an overregulation of PAR receptors and/or a hypervitaminosis A.Type: GrantFiled: April 23, 1999Date of Patent: May 1, 2001Assignee: Centre International de Recherches DermatologiquesInventor: Jean-Michel Bernardon
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Patent number: 6201024Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: January 26, 1999Date of Patent: March 13, 2001Assignee: AstraZeneca UK LimitedInventors: Andrew Baxter, Thomas McInally, Michael Mortimore, David Cladingboel
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Patent number: 6143751Abstract: Compounds of the formula (I) wherein X, R.sup.1, R.sup.2, and Ar.sup.1 as defined in the specification. The compounds are useful medicaments, particularly in the treatment of asthma or rhinitis.Type: GrantFiled: May 11, 1998Date of Patent: November 7, 2000Assignee: AstraZeneca UK LimitedInventors: David Cheshire, David Cladinggboel, Martin Cooper, David Hardern, Simon Hirst, Carol Manners, Michael Stocks
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Patent number: 6096888Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.Type: GrantFiled: September 14, 1999Date of Patent: August 1, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Antonino Suarato, Jacqueline Lansen, Michele Caruso, Dario Ballinari, Tiziano Bandiera
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Patent number: 6072068Abstract: The present invention relates to certain 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medicinal therapy, particularly in the treatment or prophylaxis of glucocorticoid dependent diseases or symptoms.Type: GrantFiled: July 14, 1999Date of Patent: June 6, 2000Assignee: Akzo Nobel N.V.Inventors: Marinus Bernard Groen, Ronald Gebhard
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Patent number: 6048877Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.Type: GrantFiled: January 20, 1998Date of Patent: April 11, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
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Patent number: 6015811Abstract: Chrysene derivatives having the formula ##STR1## have been found to have antitumor activity. In the above formula, at least one of R.sub.1 -R.sub.12 is --R.sub.13 Z, where R.sub.13 is a substituted or unsubstituted amino or amido group having from 1-12 carbon atoms, and Z is a substituted or unsubstituted heterocyclic group having from 1-12 carbon atoms; and the remainder of R.sub.1 -R.sub.12 are independently selected from the group consisting of hydrogen, substituted or unsubstituted amino or amido groups having 1-12 carbon atoms, nitro, and substituted or unsubstituted hydrocarbyl groups having from 1-12 carbon atoms.Type: GrantFiled: October 27, 1998Date of Patent: January 18, 2000Assignee: Board of Regents, The University of Texas SystemInventors: Frederick F. Becker, Bimal K. Banik
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Patent number: 6015900Abstract: Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents; A is an optionally substituted alkylene; R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents; R.sub.5 is hydrogen or lower alkyl; R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members; Z is nitrogen or carbon; and W is optionally susbtituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: November 23, 1998Date of Patent: January 18, 2000Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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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: 6001860Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.17, R.sup.18 and R.sup.1 are as defined below. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.Type: GrantFiled: January 17, 1995Date of Patent: December 14, 1999Assignee: Pfizer Inc.Inventor: Ernest S. Hamanaka
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Patent number: 5998615Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.Type: GrantFiled: October 7, 1997Date of Patent: December 7, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Antonino Suarato, Jacqueline Lansen, Michele Caruso, Dario Ballinari, Tiziano Bandiera
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Patent number: 5945561Abstract: Certain novel substituted (5,6)-dihydroanthracenyl compounds of the general formula ##STR1## wherein A, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined in the specification exhibit retinoid-like properties and are particularly useful in the prevention of post-surgical adhesions.Type: GrantFiled: April 24, 1998Date of Patent: August 31, 1999Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., Kenneth M. Tramposch, Xina Nair, Peter R. Reczek, Anna Ericsson, Anne Marinier, Alain Martel, Fred C. Zusi
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Patent number: 5932734Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: August 7, 1997Date of Patent: August 3, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5922879Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy; --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1 R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.Type: GrantFiled: December 22, 1997Date of Patent: July 13, 1999Assignee: Neurogen CorporationInventors: Xi Chen, Jan William Francis Wasley
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Patent number: 5908851Abstract: Compounds of formula (I), ##STR1## wherein X is a --CO.sub.2 H or --CONHOH group; R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.Type: GrantFiled: October 7, 1997Date of Patent: June 1, 1999Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Andrew Miller, Zoe Marie Spavold, Mark Whittaker
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Patent number: 5883257Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: December 19, 1997Date of Patent: March 16, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5856497Abstract: This invention relates to process for asymmetrically producing enantiomerically pure .alpha.-cycloalkylalkyl substitututed methanamines from .alpha.-pinene. One key step of the process of this invention utilizes the oxidation product of .alpha.-pinene, hydroxy pinanone, as a chiral auxiliary to direct the stereoselective alkylation of the corresponding ketimine. This invention also relates to key intermediates useful in the processes referred to herein.Type: GrantFiled: November 22, 1996Date of Patent: January 5, 1999Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Gregory Roth, John Landi
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Patent number: 5807889Abstract: Compounds of formula I ##STR1## wherein R1=(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2=H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5=H, halo, alkyl, alkoxy, etc.; R6,R7=H, alkyl; R6R7=atoms to complete a ring; R8,R9=groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other=CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8-OH DPAT cue agonism test in rats.Type: GrantFiled: June 6, 1995Date of Patent: September 15, 1998Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard
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Patent number: 5780486Abstract: 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 27, 1997Date of Patent: July 14, 1998Assignee: 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: 5770737Abstract: A two-photon absorbing chromophore of the formulaD--Ar--Awherein Ar is selected from the group consisting of ##STR1## D is selected from the group consisting of ##STR2## and A is selected from the group consisting of ##STR3## wherein R.sub.1 and R.sub.2 are alkyl groups having 8 to 12 carbon atoms, and wherein R.sub.1 and R.sub.2 are the same or different.Type: GrantFiled: September 18, 1997Date of Patent: June 23, 1998Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Bruce A. Reinhardt, Jayprakash C. Bhatt, Lawrence L. Brott, Stephen J. Clarson
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Patent number: 5763719Abstract: A fullerene derivative of the formula I ##STR1## where the symbols and indices have the following meanings: F is a fullerene radical of the formula (C.sub.20+2m), where m is a number from 1 to 50R.sup.1 to R.sup.8 are identical or different and are each H, CO.sub.2 R.sup.9, CN, COR.sup.10, Cl, Br, I, F, OR.sup.11, C.sub.1 -C.sub.20 -alkyl, phenyl or H, R.sup.1 -R.sup.4 and/or R.sup.5, R.sup.7 can also be part of a cycloalipathic, cycloaromatic or cycloheteroaromatic system which in turn is substituted by C.sub.1 -C.sub.20 -alkyl, aryl, carboxyl, carbonyl, alkoxy, aryloxy, halogen, nitro, alcohol or amine, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, R.sup.3 and R.sup.4 can together be ##STR2## where R.sup.15 -R.sup.18 are each H, C.sub.1 -C.sub.20 -alkyl, F, Cl, Br, I or phenyl, andAR is the radical of a fused cyclo-aromatic system, and n is from 1 to 20 and a process for its preparation.Type: GrantFiled: September 15, 1995Date of Patent: June 9, 1998Assignee: Hoechst AGInventors: Andreas Gugel, Pavel Belik, Klaus Mullen
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Patent number: 5698559Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man, such as in Alzheimer's disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.The compounds of this invention can be described as shown in Formula I ##STR1## where Q is ##STR2## R.sup.1 is 4-, 3-, or 2-pyridyl, pyrimidyl, pyrazinyl, or fluoro-4-pyridyl;R.sup.2 and R.sup.3 are independently H, F, Cl, Br, NO.sub.2, OH, --R.sup.4, --O--R.sup.4, --CO.sub.2 R.sup.4, --COR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sub.4 R.sup.4', --S(O).sub.m2 --R.sup.4, NH.sub.2, CF.sub.3, NHR.sup.4, NR.sup.4 R.sup.4' ;R.sup.4 and R.sup.4' are independently H, alkyl of 1 to 4 carbons, CH.sub.2 Phe-W or Phe-W;Phe is a phenyl group;R.sup.5 is --(CH.sub.2).sub.n --Y or --OCOR.sup.4 ;Y is H, OH, NH.sub.2, NHR.sup.4, NR.sup.4 R.sup.4', NHCOR.sup.4, NHCO.sub.2 R.sup.4, NHS(O).sub.2 R.sup.4 ; F, Cl, Br, OR.sup.Type: GrantFiled: March 25, 1996Date of Patent: December 16, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Wendell Wilkie Wilkerson, Christopher Allan Teleha