Tricyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/547)
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Publication number: 20020006921Abstract: Polycondensated heterocycles with a pyrrole[2,1-b][1,3]benzothiazepine structure of the following formula (I) 1Type: ApplicationFiled: January 26, 2001Publication date: January 17, 2002Inventors: Giuseppe Campiani, Vito Nacci, Patrizia Minetti, Maria Assunta Di Cesare
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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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Publication number: 20010029256Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: March 14, 2001Publication date: October 11, 2001Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6235730Abstract: 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases.Type: GrantFiled: October 26, 1999Date of Patent: May 22, 2001Assignee: Japan Tobacco, Inc.Inventors: Motohide Sato, Takeo Katsushima, Hajime Kinoshita
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Patent number: 6214820Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: April 10, 2001Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6121256Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R' 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.1 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.4 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: April 9, 1999Date of Patent: September 19, 2000Assignee: Institute of Medicinal Molecular Design, Inc.Inventor: Koichi Shudo
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Patent number: 6114329Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of a linear, cyclic or bicyclic, aromatic or aliphatic moiety containing a nitrogen atom;and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: January 26, 1998Date of Patent: September 5, 2000Assignee: SmithKline Beecham plcInventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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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: 5998409Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: June 2, 1995Date of Patent: December 7, 1999Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5965553Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, Alzheimer's agents or anti-acne agents.Type: GrantFiled: June 12, 1997Date of Patent: October 12, 1999Assignee: Pfizer Inc.Inventors: Andrew S. Bell, Ernest S. Hamanaka, Cheryl M. Hayward, Douglas A. Scully, Blanda Stammen
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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: 5852014Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: June 2, 1995Date of Patent: December 22, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5846968Abstract: 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: December 8, 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: 5834462Abstract: Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have each an antitumor action and are represented by the following general formula (I) and processes for producing the same are provided. These compounds have each an excellent antitumor activity.A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alky); and M represents a tricyclic structure selected from among the following ones; ##STR2## ?rings A and B represent each an unsaturated 5- or 6-membered ring; X represents N(R.sup.2), (wherein R.sup.2 represents hydrogen or lower alkyl), or NHCO;Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15);Z represents nitrogen or C(R.sup.Type: GrantFiled: March 23, 1995Date of Patent: November 10, 1998Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
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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: 5824676Abstract: 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 10, 1996Date of Patent: October 20, 1998Assignee: Allelix Biopharmaceuticals Inc.Inventors: Ashok Tehim, Jian-min Fu, Sumanas Rakhit
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Patent number: 5811420Abstract: Compounds of formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, unsubstituted lower alkyl or lower alkyl substituted by lower alkoxy or lower alkyl thio, or acyl which is unsubstituted or substituted by one or more of lower alkyl, lower alkyl substituted by halogen, and lower alkoxy;X is CO or CHOH;Y is CO or CH.sub.2 ; andZ is O or NH, and epimers and enantiomers thereof,or the physiologically usable salts thereof are useful as anti-tumor agents. They can be prepared by fermentation of Aspergillus sp. and, optionally, subsequent modification of functional groups.Type: GrantFiled: June 6, 1997Date of Patent: September 22, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Urvashi Hooda Dhingra, Haruyoshi Shirai, Yuki Takehana, Peter Michael Wovkulich, Nami Yabuki
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Patent number: 5780633Abstract: A new process for preparing a compound of the formula: ##STR1##Type: GrantFiled: May 6, 1996Date of Patent: July 14, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Satoshi Okada, Kozo Sawada, Akio Kuroda, Shinya Watanabe, Hirokazu Tanaka
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Patent number: 5773433Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3 to R.sup.10 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; R.sup.11 is hydrogen, C.sub.1-6 alkyl, or trifluoromethyl; R.sup.12 is hydrogen, C.Type: GrantFiled: April 25, 1997Date of Patent: June 30, 1998Assignee: Janssen Pharmaceutica, N.V.Inventors: Francisco Javier Fernandez-Gadea, Victor Karel Sipido, Jose Ignacio Andres-Gil, Theo Frans Meert
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Patent number: 5719140Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: November 7, 1994Date of Patent: February 17, 1998Assignee: G.D. Searle & Co.Inventors: Nizal Samuel Chandrakumar, Timothy Joseph Hagen, Barnett Sylvain Pitzele, Sofya Tsymbalov, E. Ann Hallinan
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Patent number: 5705498Abstract: 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: GrantFiled: May 4, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plc.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5661146Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: May 18, 1995Date of Patent: August 26, 1997Assignee: G.D. Searle & Co.Inventors: Nizal Samuel Chandrakumar, Donald Willis Hansen, Jr., Karen Berenice Peterson, Barnett Sylvain Pitzele
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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: 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: 5576315Abstract: The present invention provides dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: August 1, 1995Date of Patent: November 19, 1996Assignee: G.D. Searle & Co.Inventors: E. Ann Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Jean-Pierre Van Hoeck, Albert C. Lee
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Patent number: 5538965Abstract: 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: December 12, 1994Date of Patent: July 23, 1996Assignee: Allelix Biopharmaceuticals Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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Patent number: 5512561Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for the treatment of prostaglandin E.sub.2 -mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin E.sub.2 -mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: March 10, 1995Date of Patent: April 30, 1996Assignee: G. D. Searle & Co.Inventors: Nizal S. Chandrakumar, Horng-Chih Huang, Richard A. Mueller
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Patent number: 5512563Abstract: 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: June 13, 1994Date of Patent: April 30, 1996Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Fuk-Wah Sum, Xuemei Du
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Patent number: 5508277Abstract: Novel bicyclic pyrimidine compounds for use as drugs and having formula (I). Said novel compounds and physiologically tolerable salts thereof may be used in therapeutics, particularly for suppressing tumour cell resistance to antineoplastic agents.Type: GrantFiled: August 10, 1994Date of Patent: April 16, 1996Assignee: Adir Et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre
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Patent number: 5504077Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: February 22, 1995Date of Patent: April 2, 1996Assignee: G. D. Searle & Co.Inventors: Joe T. Collins, Donald W. Hansen, Jr., Karen H. Peterson, Barnett S. Pitzele, David B. Reitz
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Patent number: 5464830Abstract: The present invention provides dibenzoxazepine compounds, of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: August 24, 1994Date of Patent: November 7, 1995Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Albert C. Lee, Jean-Pierre Van Hoeck
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Patent number: 5461047Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: May 18, 1994Date of Patent: October 24, 1995Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Karen B. Peterson
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Patent number: 5461046Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: September 24, 1993Date of Patent: October 24, 1995Assignee: G. D. Searle & Co.Inventors: Robert K. Husa, Michael F. Rafferty, Timothy J. Hagen, E. Ann Hallinan
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Patent number: 5449675Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: June 9, 1994Date of Patent: September 12, 1995Assignee: G. D. Searle & Co.Inventors: Nizal S. Chandrakumar, Donald W. Hansen, Jr., Karen B. Peterson, Barnett S. Pitzele
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Patent number: 5449673Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: January 10, 1994Date of Patent: September 12, 1995Assignee: G. D. Searle & Co.Inventors: Nizal S. Chandrakumar, Timothy J. Hagen, E. Ann Hallinan, Robert K. Husa
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Patent number: 5449674Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: March 3, 1994Date of Patent: September 12, 1995Assignee: G. D. Searle & Co.Inventors: Timothy J. Hagen, Nizal S. Chandrakumar, E. Ann Hallinan, Shashidhar N. Rao, Barnett S. Pitzele
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Patent number: 5441950Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: June 9, 1994Date of Patent: August 15, 1995Assignee: G. D. Searle & Co.Inventors: Joe T. Collins, Donald W. Hansen, Jr., Karen B. Peterson, Barnett S. Pitzele, David B. Reitz
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Patent number: 5410046Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.Type: GrantFiled: May 11, 1993Date of Patent: April 25, 1995Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Robert M. Wallis
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Patent number: 5395932Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## wherein X is oxygen, sulfur ##STR2## A is --CH.sub.2 -- or ##STR3## E and F may be --CH, oxygen, nitrogen or sulfur, and may not be the same; G is oxygen, nitrogen or sulfur; with the proviso that when G is oxygen or sulfur, one of E or F is nitrogen, which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: April 30, 1993Date of Patent: March 7, 1995Assignee: G. D. Searle & Co.Inventors: Nizal S. Chandrakumar, Timothy J. Hagen, Barnett S. Pitzele, Sofya Tsymbalov, E. Ann Hallinan
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Patent number: 5378840Abstract: The present invention provides dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: August 24, 1993Date of Patent: January 3, 1995Assignee: G. D. Searle & Co.Inventors: Albert C. Lee, E. Ann Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Jean-Pierre Van Hoeck
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Patent number: 5354747Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: June 16, 1993Date of Patent: October 11, 1994Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Karen B. Peterson
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Patent number: 5354746Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: June 1, 1993Date of Patent: October 11, 1994Assignee: G. D. Searle & Co.Inventors: Nizal S. Chandrakumar, Barnett S. Pitzele
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Patent number: 5329006Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.Type: GrantFiled: September 6, 1991Date of Patent: July 12, 1994Assignee: Ciba-Geigy CorporationInventors: Hans Baumann, Ian J. Fletcher
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Patent number: 5324722Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: May 7, 1993Date of Patent: June 28, 1994Assignee: G. D. Searle & Co.Inventors: Timothy J. Hagen, Michael Clare, Michael F. Rafferty, E. Ann Hallinan
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Patent number: 5304644Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: April 15, 1992Date of Patent: April 19, 1994Assignee: G. D. Searle & Co.Inventors: Robert K. Husa, Michael F. Rafferty, Timothy J. Hagen, E. Ann Hallinan
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Patent number: 5288719Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a 2-, 3-, 8- and/or 10-substituted dibenzoxazepine compound having a structure of the formula: ##STR1## or a pharmaceutically-acceptable salt thereof, wherein: X is --NH-- or --CH.sub.2 --;Y is(1) --CH.sub.2 -- when X is --NH--, and(2) --NH-- when X is --CH.sub.2 --;R.sup.1 is hydrogen, halogen or --OR.sup.4 ;R.sup.4 is hydrogen, alkyl or ##STR2## Z is oxygen, sulfur, --SO--, --SO.sub.2 -- or --NR.sup.5 --; R.sup.5 is hydrogen or t-butyloxycarbonyl;R.sup.2 is hydrogen, halogen or trifluoromethyl;R.sup.3 is hydrogen, halogen, aryl, heteroaryl in which the heteroatoms are selected from oxygen, nitrogen and/or sulfur, or --NR.sup.6 R.sup.7 ;R.sup.6 and R.sup.7 are each independently hydrogen or alkyl;R.sup.8 is alkyl, aryl or ##STR3## R.sup.9 and R.sup.Type: GrantFiled: January 21, 1993Date of Patent: February 22, 1994Assignee: G. D. Searle & Co.Inventors: Robert K. Husa, Timothy J. Hagen, E. A. Hallinan
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Patent number: 5286722Abstract: The invention relates to tetrahydropyridinyldibenzazepine derivatives of the formula I ##STR1## wherein R.sub.1 is a substituent selected from the group consisting of hydrogen, halogen, and lower alkyl;R.sub.2 is selected from hydrogen, and unsubstituted or hydroxy substituted lower alkyl or lower alkenyl;X is O, S, or CH.sub.2 ;Y is HC.dbd.CH or S;or a pharmaceutically acceptable salt thereof.These compounds are dopamine antagonists and are therefore useful for the treatment of psychotic disorders such as schizophrenia, schizophreniform disorder, delusional disorder, acute manic states, senile and presenile psychotic states, toxic psychoses, psychoactive-substance induced psychoses, symptoms of severe restlessness, hyperexcitability and anxiety, motor disorders, among which Tourette's disorder and Huntington's chorea, nausea and vomiting, hiccup and dizziness.Type: GrantFiled: November 25, 1992Date of Patent: February 15, 1994Assignee: Akzo N.V.Inventors: James Cairns, Samuel G. Gibson, Duncan R. Rae
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Patent number: 5281590Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a compound of Formula I: ##STR1##Type: GrantFiled: September 2, 1992Date of Patent: January 25, 1994Assignee: G. D. Searle & Co.Inventors: Robert K. Husa, E. Ann Hallinan, Marc Herin, Michel Lesne