Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/586)
  • Patent number: 5770378
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Youssef L. Bennani, Stacie S. Canan Koch, Beth Ann Badea, Jonathan J. Hebert, Alex M. Nadzan
  • Patent number: 5770382
    Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 23, 1998
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Chan Kou Hwang, Steven K. White, Beth Ann Badea, Alex M. Nadzan
  • Patent number: 5741789
    Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 21, 1998
    Assignee: Eli Lilly and Company
    Inventors: David J. Hibschman, Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson
  • Patent number: 5736538
    Abstract: 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: Grant
    Filed: April 25, 1996
    Date of Patent: April 7, 1998
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Xuemei Du
  • Patent number: 5731307
    Abstract: The instant invention is directed to compounds, compositions and antipsychotic methods of use wherein the compounds are of formula I: ##STR1## wherein Y is an imide or benzoyl alkyl group and X is a cycloalkyl, phenyl or dibenzoazepinyl group.
    Type: Grant
    Filed: June 16, 1997
    Date of Patent: March 24, 1998
    Assignee: Pfizer, Inc.
    Inventor: Kishor A. Desai
  • Patent number: 5723633
    Abstract: A pyran derivative has a structure ofR.sup.2 R.sup.3 C.dbd.(C.sub.5 H.sub.2 R.sup.1 O)--(CH.dbd.CH).sub.n --C.sub.6 H.sub.2 R.sup.6 R.sup.7 --NR.sup.4 R.sup.5wherein n is 3 or 4; R.sup.1 is a proton, alkyl or phenyl group; each of R.sup.2 and R.sup.3 is independently a cyano, alkoxycarbonyl having an alkyl, acyl having an alkyl, aracyl having phenyl, sulfonyl, aryl, or aryloxy; each of R.sup.4 and R.sup.5 is an alkyl group; and each of R.sup.6 and R.sup.7 is a proton, provided that R.sup.4 and R.sup.5 are alkyl groups, and a pair of R.sup.4 and R.sup.6 as well as a pair of R.sup.5 and R.sup.7 can be bonded to each other to form a heterocycle.A photosensitive composition comprises a polymerizable compound, a polymerization initiator and a photosensitizer which is the pyran derivative. A photosensitive resin composition comprises a crosslinkable polymer, a crosslinking agent and the photosensitizer.
    Type: Grant
    Filed: December 20, 1995
    Date of Patent: March 3, 1998
    Assignee: Canon Kabushiki Kaisha
    Inventors: Shin Kobayashi, Susumu Matsumura, Naosato Taniguchi, Yoko Yoshinaga, Toshiyuki Sudo, Hideki Morishima, Tadashi Kaneko
  • Patent number: 5705498
    Abstract: Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl;A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms;R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl;R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy;R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy,Y is O or NH, or CO--Y together are a heterocyclic bioisostere;Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; andR.sub.6 is hydrogen or C.
    Type: Grant
    Filed: May 4, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham plc.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5693635
    Abstract: 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: Grant
    Filed: June 13, 1996
    Date of Patent: December 2, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Marvin Fred Reich
  • Patent number: 5616575
    Abstract: Ibogaine analogs are provided, which are phenyl-substituted-hexahydroazepino[4,5-b]indoles useful to treat cocaine addiction and the use of other addictive substances.
    Type: Grant
    Filed: December 4, 1995
    Date of Patent: April 1, 1997
    Assignees: Regents of the University of Minnesota, University of Miami
    Inventors: S. Mbua N. Efange, Deborah C. Mash
  • Patent number: 5594152
    Abstract: This invention comprises a process for production of a compound of the formula: ##STR1## in which R.sup.1 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), bromo, chloro, fluoro, iodo, --COlower alkyl(C.sub.1 -C.sub.3), and --CF.sub.3 ;R.sup.2 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), amino, bromo, chloro, fluoro, iodo, and --COlower alkyl(C.sub.1 -C.sub.3);or R.sup.1 and R.sup.2 taken together are methylenedioxy or ethylenedioxy;R.sup.3 is an aldehyde or carboxcylic acid moiety;the moiety ##STR2## wherein Z represents substituted or unsubstituted phenyl ring or an optionally substituted 5 or 6-membered aromatic heterocyclic ring.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: January 14, 1997
    Assignee: American Cyanamid Company
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright
  • Patent number: 5545636
    Abstract: The present invention discloses compounds of the general formula: ##STR1## The compounds are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.
    Type: Grant
    Filed: October 18, 1994
    Date of Patent: August 13, 1996
    Assignee: Eli Lilly and Company
    Inventors: William F. Heath, Jr., John H. McDonald, III, Michael Paal, Gerd R uhter, Theo Schotten, Wolfgang Stenzel
  • Patent number: 5512562
    Abstract: Tricyclic benzazepines having the general formula ##STR1## wherein A together with the .alpha.- and .beta.-marked carbon atoms is a cyclopentene, cyclohexene, furan, dihydrofuran, pyran, dihydropyran, thiophene, oxazole, pyrrole, pyrroline, tetrahydropyridine or dioxole ring, R.sup.1 is H or alkyl, R.sup.2 and R.sup.3 independently are H, alkoxy, halogen, nitro, cyano or hydroxy, or R.sup.2 and R.sup.3 together may form a furan, dihydrofuran, cyclopentene or dioxole ring and R.sup.4 is H, alkoxy, nitro, cyano, hydroxy or halogen, or a pharmaceutically acceptable salt thereof, are useful in treatment of certain disorders in the central nervous system, e.g., psychosis, pain, depression, sleep disturbances, dyskinesia, Parkinson's disease, stroke.
    Type: Grant
    Filed: February 24, 1994
    Date of Patent: April 30, 1996
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Erik B. Nielsen
  • Patent number: 5512563
    Abstract: 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: Grant
    Filed: June 13, 1994
    Date of Patent: April 30, 1996
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Fuk-Wah Sum, Xuemei Du
  • Patent number: 5478845
    Abstract: Piperidine derivatives of formula ##STR1## wherein A is straight or branched alkyl, alkoxy-alkyl, or alkenyl; X is O or NH; Y is O, S, NH, NCN, or N-alkyl; R.sup.1 is 6-fluoro-1,2-benzisoxazol-3-yl, 6-fluoro-1H-indazol-3-yl, or 6-fluoro-1-methyl-1H-indazol-3-yl; R.sup.2 is alkyl or phenyl; and R.sup.3 is phenyl optionally substituted, or R.sup.3 is ##STR2## wherein Z represents a 5- or 6-membered heterocyclic ring; or R.sup.2 and R.sup.3 together with the nitrogen atom form a fused heterocyclic ring system; or pharmaceutically acceptable salts thereof are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: December 26, 1995
    Assignee: Novo Nordisk A/S
    Inventors: John B. Hansen, Frederik C. Gronvald, John P. Mogensen
  • Patent number: 5457122
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: October 10, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5436333
    Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, amino, bromo, chloro, fluoro, iodo, C.sub.1 -C.sub.3 alkylcarbonyl or trifluoromethyl; R.sup.2 is H, C.sub.1 -C.sub.3 alkyl, C.sub.1 --C.sub.3 alkoxy, bromo, chloro, fluoro, iodo, or C.sub.1 -C.sub.3 alkylcarbonyl; or R.sup.1 and R.sup.2 taken together are methylenedioxy or ethylenedioxy; the structure ##STR2## represents, as described in the specification, an ortho-fused phenyl moiety; an aromatic 5-membered heterocycle containing N, O, or S; or an aromatic 6-membered heterocycle containing N; all of which may be optionally substituted, are produced by reaction of ##STR3## where R.sup.3 is a masked aldehyde or carboxyl group, with 2-nitro-benzyl bromide followed by removal of the mask, reduction and cyclization.
    Type: Grant
    Filed: August 8, 1994
    Date of Patent: July 25, 1995
    Assignee: American Cyanamid Company
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright
  • Patent number: 5399553
    Abstract: A tricyclic compound represented by the general formula (1) and salts thereof are disclosed. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.
    Type: Grant
    Filed: June 16, 1993
    Date of Patent: March 21, 1995
    Assignees: Wakunaga Seiyaku Kabushiki Kaisha, Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Masaharu Yokomoto, Akira Yazaki, Norihiro Hayashi, Shunso Hatono, Satoshi Inoue, Yasuhiro Kuramoto
  • Patent number: 5393764
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5378701
    Abstract: A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m -- wherein m is an integer of 0 to 2; W represents ##STR2## and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.CH or CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2, ##STR3## and Q represents N or CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents CH.sub.2 CH.sub.2 ; and Z.sup.1 --Z.sup.2 represents N--(CH.sub.2).sub.n -- wherein n is an integer of 1 to 3 or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 25, 1993
    Date of Patent: January 3, 1995
    Assignee: Kyowa Hakko Kogyo
    Inventors: Etsuo Ohshima, Fumihiko Kanai, Hideyuki Sato, Hiroyuki Obase, Toshiaki Kumazawa, Shiho Takahara, Tetsuji Ohno, Tomoko Ishikawa, Koji Yamada
  • Patent number: 5369084
    Abstract: Isonicotinic acid derivatives and related furo-, thieno- and pyrrolo[3,4-c]pyridin-1(3H)-one, -thione and -imine compounds having the formula ##STR1## wherein R is ##STR2## Q is O, S or NR.sup.7 ; Y is O, S or NR.sup.8 ; L is COOR.sup.9, CONR.sup.10 R.sup.11, C(.dbd.S)NR.sup.10 R.sup.11, CN, or a radical of formula ##STR3## the acceptable addition salts, the stereochemically isomeric forms and the N-oxides thereof, having herbicidal properties, compositions containing the same and methods for controlling weeds.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: November 29, 1994
    Assignee: Janssen Pharmaceutical N.V.
    Inventors: Hans-Rudolf Waespe, Guy R. E. Van Lommen, Victor K. Sipido
  • Patent number: 5362728
    Abstract: Novel benzazepines of the formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R represents H, alkyl, allyl or ##STR2## A represents --[CR.sup.1 R.sup.2].sub.n --; n represents 3 or 4; R.sup.1 and R.sup.2 may be the same or different and each independently represents H, OH, atkyl, alkoxy, phnenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.2 on the same carbon atom are not both OH, or R.sup.1 and R.sup.2 on the same carbon atom together represent=O;G represents H, R.sup.3 (CO)-- or ArNHCO--;R.sup.3 represents H, alkyl, alkoxy, phenyl or substituted phenyl;Ar represents phenyl or substituted phenyl; andY and Z may be the same or different and each is independently selected from H, halo, alkyl, alkoxy or halpalkyl;the pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, useful in the treatment of psychoses, drug dependence, D1 dependent neurological disorder or pain are disclosed.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: November 8, 1994
    Assignee: Schering Corporation
    Inventors: Theodros Asberom, Edward O'Connor, Joel G. Berger, John W. Clader
  • Patent number: 5296483
    Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.
    Type: Grant
    Filed: September 27, 1991
    Date of Patent: March 22, 1994
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5250681
    Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.
    Type: Grant
    Filed: February 15, 1991
    Date of Patent: October 5, 1993
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura
  • Patent number: 5241065
    Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: August 31, 1993
    Assignee: Schering Corporation
    Inventors: Joel G. Berger, Wei K. Chang, Joseph A. Kozlowski, Guowei Zhou
  • Patent number: 5223613
    Abstract: An azatetracycle compound of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.
    Type: Grant
    Filed: June 19, 1992
    Date of Patent: June 29, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Roger Nosal, Dale P. Spangler, Daniel L. Zabrowski
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5104868
    Abstract: This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this invention are substituted at the 7-position by vinyl, W--CH.dbd.CH--, CH.sub.3 C.tbd.C--, W--CH.sub.2 C.tbd.C-- or ##STR1## where W is selected from certain substituted alkyl groups. This invention also relates to antibacterial compositions containing the compounds and methods of using the compounds to treat bacterial disease.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: April 14, 1992
    Assignee: Pfizer Inc.
    Inventor: Paul R. McGuirk
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 5066800
    Abstract: A novel process and intermediates used therein for linking a cephalosporin compound to a quinolone are disclosed. According to the disclosed process, the 2-carboxylic acid moiety of the cephalosporin compound is treated with an organic base. The resulting salt is then reacted with a quinolone compound which has been activated using a haloformate. The reaction is run in a non-aqueous organic solvent. 4-Dimethylaminopyridine is used to promote the reaction between the cephalosporin salt and the activated quinolone.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: November 19, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Masami Okabe
  • Patent number: 5026696
    Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene chain and R.sup.3 is a hydrogen atom; orR.sup.1 and R.sup.3 together form a C.sub.2-4 alkylene chain and R.sup.2 is a hydrogen atom;A-B represents the group R.sup.4 R.sup.5 C--CH.sub.2 or R.sup.4 C.dbd.CH;R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or a C.sub.1-6 alkyl group; andIm represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.6, R.sup.7 and R.sup.8 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.
    Type: Grant
    Filed: July 18, 1990
    Date of Patent: June 25, 1991
    Assignee: Glaxo Group Limited
    Inventors: Peter C. North, Alexander W. Oxford, David J. Cavalla
  • Patent number: 4985420
    Abstract: The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of these receptors.
    Type: Grant
    Filed: December 7, 1988
    Date of Patent: January 15, 1991
    Assignee: Duphar International Research B.V.
    Inventors: Derk Hamminga, Hans H. Haeck, Ineke Van Wijngaarden, Wouter Wouters
  • Patent number: 4959374
    Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereif, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents o or NR.sup.o wherein R.sup.0 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3,andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: September 25, 1990
    Assignee: Beecham Group P.L.C.
    Inventor: John M. Berge
  • Patent number: 4957914
    Abstract: 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: September 18, 1990
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, Jacob Berger, Klaus K. Weinhardt
  • Patent number: 4952587
    Abstract: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted circle represents one or two double bonds in any position in the 5-membered ring;X, Y and Z independently represent oxygen, sulphur, nitrogen or carbon, provided that at least one of X, Y and Z represents oxygen, sulphur or nitrogen;A represents a group of formula II: ##STR2## in which R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, hydroxy(C.sub.1-6)alkyl, halogen, amino, cyano, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylcarbonyl;V represents nitrogen, ##STR3## and W represents oxygen, sulphur or ##STR4## in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.
    Type: Grant
    Filed: February 3, 1989
    Date of Patent: August 28, 1990
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, John Saunders, Christopher Swain
  • Patent number: 4942231
    Abstract: The invention relates to a method of preparing a chlorinated, brominated, radiobrominated, iodinated and/or radioiodinated aromatic or heteroaromatic compound, in which the (hetero)aromatic nucleus optionally comprises one or more additional substituents, by reacting the corresponding halogenated or diazonium-substituted compound in the presence of a water-soluble acid and of copper ions as a catalyst with a likewise water-soluble chloride, bromide radiobromide, iodide or radio-iodide, in which the reaction is carried out in the presence of one or more reduction agents, which are stable in acid medium, in a quantity exceeding the quantity of catalyst. The invention also relates to a composition suitable for diagnostic examination and to a kit for the preparation thereof. The invention further relates to a method and an equipment for the preparation of said composition.
    Type: Grant
    Filed: May 17, 1985
    Date of Patent: July 17, 1990
    Assignee: Mallinckrodt, Inc.
    Inventor: John Mertens
  • Patent number: 4897391
    Abstract: Isoquinolinone and isothiochromone derivatives of the general formula ##STR1## are disclosed. These compounds display anti-allergy, antiinflammatory and anti-hyperproliferative activity, which makes them useful for treating related disorders.
    Type: Grant
    Filed: June 17, 1988
    Date of Patent: January 30, 1990
    Assignee: Schering Corporation
    Inventor: Richard J. Friary
  • Patent number: 4885278
    Abstract: Compounds of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and A have the meanings stated in the specification, as well as the use thereof for controlling diseases, are described.
    Type: Grant
    Filed: May 20, 1988
    Date of Patent: December 5, 1989
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Hans-Juergen Teschendorf, Liliane Unger, Rudolf Binder
  • Patent number: 4871735
    Abstract: The present invention relates to new naphthyl derivatives of general formula ##STR1## wherein N represents the number 1 or 2,A represents a --CH.sub.2 --, --CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## while the atom marked with an x is linked to the phenyl nucleus, E represents a straight chained alkylene group optionally substituted by an alkyl group,G represents a straight chained alkylene group optionally substituted by an alkyl group,L represents a bond or an oxygen atom, if G represents a straight chained alkylene group with 2 to 5 carbon atoms optionally substituted by an alkyl group,R.sub.1 and R.sub.2, which may be identical or different, represent alkyl or alkoxy groups or R.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, or an alkyl or an allyl group,R.sub.4, R.sub.5 and R.sub.
    Type: Grant
    Filed: September 11, 1987
    Date of Patent: October 3, 1989
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Joachim Heider, Manfred Psiorz, Andreas Bomhard, Norbert Hauel, Berthold Narr, Klaus Noll, Christian Lillie, Walter Kobinger, Jurgen Dammgen
  • Patent number: 4833244
    Abstract: Novel ethanobenzazepines, processes for the preparation thereof, and a method of alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: October 1, 1987
    Date of Patent: May 23, 1989
    Assignee: Hoechst-Rouseel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Bernhard Seuring
  • Patent number: 4824472
    Abstract: Novel herbicidal 1-cyclyl or polycyclyl substituted 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Processes for making these novel compounds.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: April 25, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren, William R. Lutz
  • Patent number: 4820818
    Abstract: The muscle relaxant (E)-3-(9-chloro-5,6-dihydro-11H-pyrrolo[2,1-b][3]benzazepin-11-ylidene-N,N -dimethyl-1-propanamine is prepared by the geometric stereoselective dehydration of the intermediate carbinol with acidic agents and organic bases and low temperatures.
    Type: Grant
    Filed: May 2, 1988
    Date of Patent: April 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ruth V. Wattley, Gerard R. Kieczykowski
  • Patent number: 4816453
    Abstract: Compounds of formula (i) and pharmaceutically acceptable salts thereof: ##STR1## wherein: m and n are independently 1 or 2 and p is 0, 1 or 2 such that m+n+p.gtoreq.3;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group of formula (a): ##STR2## wherein either R.sub.3 is hydrogen or C.sub.1-7 alkanoyl; and X is chloro, bromo, methylthio or nitro; having gastric motility enhancing activity, anti-emetic activity and/or 5-HT antagonist activity, a process for their preparation, and their use as pharmaceuticals.
    Type: Grant
    Filed: September 17, 1986
    Date of Patent: March 28, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Eric A. Watts
  • Patent number: 4788203
    Abstract: Novel cyclized N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.
    Type: Grant
    Filed: November 26, 1985
    Date of Patent: November 29, 1988
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Wasyl Halczenko
  • Patent number: 4769368
    Abstract: 2,3,4,8,9,9a-Hexahydro-4-aryl-1H-indeno[1,7-cd;]-azepines are selective dopamine receptor site binding agents.
    Type: Grant
    Filed: February 10, 1986
    Date of Patent: September 6, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Hye-Ja Oh, Joseph Weinstock
  • Patent number: 4745111
    Abstract: Compounds of the formula ##STR1## where R and A have the meanings given in the description, and their use in the treatment of disorders are described.
    Type: Grant
    Filed: July 9, 1986
    Date of Patent: May 17, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Hans-Juergen Teschendorf, Liliane Unger
  • Patent number: 4741765
    Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: May 3, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4723009
    Abstract: Novel ethanobenzazepines, processes for the preparation thereof, and a method of alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: February 2, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bernhard Seuring
  • Patent number: 4678499
    Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.
    Type: Grant
    Filed: January 30, 1986
    Date of Patent: July 7, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan