The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/361)
-
Patent number: 5578624Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 26, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
-
Patent number: 5574032Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 12, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 5571803Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: December 22, 1995Date of Patent: November 5, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 5571828Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 5571814Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 5561128Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: October 1, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5559126Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5559235Abstract: The present invention relates to water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: 1) R.sup.1 and R.sup.2 represent independently, hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl;ii) R.sup.1 represents hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R.sup.2 represents --COR.sup.3,wherein:R.sup.3 represents hydrogen, lower alkyl, perhalo-lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy or lower alkoxy lower alkyl; oriii) R.sup.1 and R.sup.2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) ##STR2## wherein: Y represents O, S, SO, SO.sub.2, CH.sub.2 or NR.sup.4wherein:R.sup.Type: GrantFiled: June 10, 1994Date of Patent: September 24, 1996Assignee: Glaxo Wellcome Inc.Inventors: Michael J. Luzzio, Jeffrey M. Besterman, Michael G. Evans, Peter L. Myers
-
Patent number: 5559116Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5559117Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski
-
Patent number: 5550130Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: August 27, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5534633Abstract: Aminoketone-substituted coumarin sensitizers having tethered tertiary amino groups are described which have extremely good photosensitivity. The sensitizers of the instant invention have the formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent an alkyl group having 1 to 6 carbon atoms, and R.sub.3 and R.sub.4 each represent hydrogen; or at least one of R.sub.1 and R.sub.3 or R.sub.2 and R.sub.4 together represent an alkylene group having 2 to 4 carbon atoms,R.sub.5 represents an alkyl group having 1 to 6 carbon atoms or H,R.sub.6 represents an alkylene group having 1 to 6 carbon atoms, andR.sub.7 and R.sub.8 each independently represent an alkyl group having 1 to 6 carbon atoms, both of R.sub.7 and R.sub.8 taken together represent an alkylene group having 4 to 6 carbon atoms, or R.sub.5 or R.sub.6 taken together with R.sub.7 or R.sub.8 represent a five, six, or seven membered heterocyclic ring group.Type: GrantFiled: February 3, 1995Date of Patent: July 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: M. Zaki Ali
-
Patent number: 5527800Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: January 18, 1994Date of Patent: June 18, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
-
Patent number: 5525611Abstract: The invention provides lavendamycin analogs having the following formula: ##STR1## wherein X, Y and R.sup.1 through R.sup.9 are defined in the specification, and salts of these analogs. The invention also provides a method of making the lavendamycin analogs. The lavendamycin analogs have antitumor and antimicrobial activity.Type: GrantFiled: June 4, 1993Date of Patent: June 11, 1996Inventors: Mohammad Behforouz, Ronald L. Merriman
-
Patent number: 5521187Abstract: Novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: March 15, 1994Date of Patent: May 28, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
-
Patent number: 5516779Abstract: Compounds of the formula ##STR1## are inhibitors of 5 .alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: June 8, 1994Date of Patent: May 14, 1996Assignee: Merck & Co., Inc.Inventors: Derek Von Langen, Donald W. Graham, Richard L. Tolman
-
Patent number: 5516908Abstract: The present invention relates to novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifiuoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient.Type: GrantFiled: April 18, 1995Date of Patent: May 14, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Didier R. G. G. de Chaffoy de Courcelles
-
Patent number: 5500423Abstract: Novel 5,6-dihydro-4H-imidazo[4,5,1-ij]quinolines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: September 9, 1994Date of Patent: March 19, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Brian S. Freed
-
Patent number: 5484921Abstract: This invention relates to a method for the preparation of benzo[b]naphthyridines having the general formula (I) ##STR1## comprising: 1) condensation of an amine having the formula R'--NH--CH.sub.2 --CH.sub.2 --R" with a chlorofluoroquinoline of formula (II) ##STR2## 2) cyclization of the obtained fluoroquinoline of formula (IV) ##STR3## and; 3) oxidation of tetrahydro-1,2,3,4benzo[b]naphthyridine-1,8 of formula (V) ##STR4## is effected, and then, optionally, the ester obtained is transformed into an acid and optionally into a salt.Type: GrantFiled: April 8, 1994Date of Patent: January 16, 1996Assignee: Laboratoire Roger BellonInventors: Christophe Daubie, Jean-Jacques Legrand, Clive Pemberton
-
Patent number: 5468750Abstract: A compound of formula ##STR1## in which A represents S;R.sub.1 is selected from the group consisting of OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, phenyl, benzyl (C.sub.1 -C.sub.4)alkyl NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 ;R.sub.2 is selected from the group consisting of OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, and NZ.sub.1 Z.sub.2 ;R.sub.3 is selected from the group consisting of H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl, and benzyl;B is selected from the group consisting of phenyl; pyridyl; phenyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl or --NZ.sub.1 Z.sub.Type: GrantFiled: July 12, 1994Date of Patent: November 21, 1995Assignee: Elf SanofiInventors: Andre Bachy, Laurent Fraisse, Peter Keane, Etienne Mendes, Jean-Claude Vernieres, Jacques Simiand
-
Patent number: 5457098Abstract: There are disclosed preparation and compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl or taken together are a --CH.sub.2 -- group to form a cyclopropane ring.X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or alkyl,p and q are independently either 0 or 1;R.sup.3 is alkyl, alkenyl, cycloalkyl, alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 are hydrogen or alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl, or taken together with the nitrogen to form 4 to 8 atom heterocyclic group, ##STR3## optionally substituted with alkyl groups; Ar is aromaticR.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N--, --CH.dbd.N--, or --N.dbd.CH--,and n and m are 0, 1 or 2.Type: GrantFiled: January 28, 1994Date of Patent: October 10, 1995Assignee: Glaxo Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
-
Patent number: 5447937Abstract: Tetrahydrobenzothienopyridines of formula (I), ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.8 and R.sub.9 are as defined in the specification and pharmaceutical compositions containing such compounds are of use in treating anxiety, convulsion and sleep disorders.Type: GrantFiled: February 10, 1994Date of Patent: September 5, 1995Assignee: SmithKline Beecham p.l.c.Inventors: David T. Davies, Ian T. Forbes, Mervyn Thompson
-
Patent number: 5438062Abstract: Derivatives of benzo[5,6]cyclohepta pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.Type: GrantFiled: September 23, 1992Date of Patent: August 1, 1995Assignee: Schering CorporationInventors: John J. Piwinski, Ashit K. Ganguly, Michael J. Green, Frank J. Villani, Jesse Wong
-
Patent number: 5430032Abstract: Disclosed is a compound of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R is selected from the group consisting of: H, Cl, Br, F, and I; T represents C or N with the dotted line attached to T representing a double bond when T is C and being absent when T is N; and X represents O or S with the proviso that T is N when X is O.Also disclosed is a pharmaceutical composition comprising a compound of Formula I and a pharmaceutically acceptable carrier.Further disclosed is a method of treating asthma, allergy and/or inflammation comprising administering to a mammal in need of such treatment an anti-asthmatic, anti-allergic and/or an anti-inflammatory, respectively, effective amount of a compound of Formula I.Type: GrantFiled: January 21, 1994Date of Patent: July 4, 1995Assignee: Schering CorporationInventors: Jesse K. Wong, John J. Piwinski, Michael J. Green
-
Patent number: 5428043Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: October 29, 1992Date of Patent: June 27, 1995Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
-
Patent number: 5422351Abstract: Bis-benzo or benzopyrido piperidene, piperidylidene and piperazine compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof are disclosed, wherein Z represents --(C(R.sup.a).sub.2).sub.m --Y--(C(R.sup.a).sub.2).sub.n -- or ##STR2## The compounds of Formula I possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.Type: GrantFiled: December 14, 1992Date of Patent: June 6, 1995Assignee: Schering CorporationInventors: John J. Piwinski, Michael J. Green, Jesse Wong
-
Patent number: 5420132Abstract: A compound of formula (I): ##STR1## wherein: X represents O, S or H.sub.2,R and R' each represents hydrogen or together form a bond,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description.useful in the treatment or prevention of disorders involving oxidative processes.Type: GrantFiled: May 6, 1994Date of Patent: May 30, 1995Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Valerie Thiery, Gerard Adam, Jean-Guy Bizot-Espiard, Bruno Pfeiffer, Pierre Renard
-
Patent number: 5418238Abstract: A compound of formula (I): ##STR1## wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.7 cycloalkyl or a C.sub.6 -C.sub.10 cycloalkylalkyl group, aryl or a C.sub.7 -C.sub.10 arylalkyl group, or a C.sub.6 -C.sub.10 heterocyclylalkyl group;R.sub.3 is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aryl or a C.sub.7 -C.sub.10 arylalkyl group;Z is a C.sub.1 -C.sub.6 alkyl group, an --OR.sub.5 group wherein R.sub.5 is a C.sub.1 -C.sub.6 alkyl group, ##STR2## group wherein each of R.sub.6 and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl or R.sub.6 and R.sub.7 taken together with the nitrogen to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring; and the symbol represents a single or a double bond, is a testosterone 68 5.alpha.Type: GrantFiled: July 29, 1993Date of Patent: May 23, 1995Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Achille Panzeri, Marcella Nesi, Enrico di Salle
-
Patent number: 5416087Abstract: Bis-benzo cyclohepta piperidine, piperidylidene and piperazine compounds of the general formula, ##STR1## and pharmaceutically acceptable salts thereof are disclosed, which possess anti-allergic and/or anti-inflammatory activity. Methods for preparing and using the compounds are also described.Type: GrantFiled: April 7, 1993Date of Patent: May 16, 1995Inventors: Jesse K. Wong, John J. Piwinski, Michael J. Green
-
Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
-
Patent number: 5360799Abstract: Compounds of formula ##STR1## in which R.sub.1 represents OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, benzyl, phenyl, (C.sub.1 -C.sub.4)alkylNZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; R.sub.2 represents OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio or NZ.sub.1 Z.sub.2 ; R.sub.3 represents H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl or benzyl; A represents N and R represents H or (C.sub.1 -C.sub.4)alkyl which can be substituted by phenyl or NZ.sub.1 Z.sub.2 ; B represents phenyl which is coupled to the pyridyl ring and is optionally substituted by one or more groups chosen from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; and Z.sub.1 and Z.sub.2 represent, independently of each other, H, (C.sub.1 -C.sub.6) alkyl, formyl or benzyl, or they form with the nitrogen atom to which they are attached an optionally substituted saturated heterocycle and their salts.Type: GrantFiled: August 19, 1993Date of Patent: November 1, 1994Assignee: Elf SanofiInventors: Andre Bachy, Laurent Fraisse, Peter Keane, Etienne Mendes, Jean-Claude Vernieres, Jacques Simiand
-
Patent number: 5350750Abstract: .beta.-carboline-3-hydroxyalkylcarboxylic acid ester derivatives of formula I ##STR1## in which R.sup.A, n, R.sup.4 and R.sup.3, have the meaning indicated in the claims, as well as their production and their use in pharmaceutical agents are described.Type: GrantFiled: March 1, 1993Date of Patent: September 27, 1994Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Martin Kruger, Dieter Seidelmann, Ralph Schmiechen, Werner Krause, Herbert Schneider, Lechoslaw Turski
-
Patent number: 5344830Abstract: Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: December 10, 1992Date of Patent: September 6, 1994Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
-
Patent number: 5342947Abstract: The present invention relates to the synthesis of water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: n represents the integer 1 or 2;R.sup.1 represents independently, hydrogen, lower alkyl, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; andR.sup.2 represents hydrogen andthe pharmaceutically acceptable salts thereof.Type: GrantFiled: October 9, 1992Date of Patent: August 30, 1994Assignee: Glaxo Inc.Inventors: Karen Lackey, Daniel D. Sternbach
-
Patent number: 5332740Abstract: Novel DC-89 derivatives represented by general formula (I): ##STR1## wherein X represents Cl or Br; R.sup.1 represents hydrogen, CONR.sup.2 R.sup.3 (in which R.sup.2 and R.sup.3 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl group), ##STR2## (in which n represents an integer of 4 to 7), ##STR3## (in which R.sup.4 represents oxygen, N--CH.sub.3 or N--CH.sub.2 CH.sub.2 NH.sub.2), ##STR4## (in which R.sup.5 R.sup.6 and R.sup.7 independently represent a straight-chain or branched alkyl group having 1 to 4 carbon atoms); and ##STR5## (in which Y represents hydrogen or CO.sub.2 CH.sub.3); provided that when R.sup.1 is hydrogen, CONR.sup.2 R.sup.3 or SiR.sup.5 R.sup.6 R.sup.7, ##STR6## and pharmaceutically acceptable salts thereof have an excellent anti-tumor activity and are expected to be useful as anti-tumor compositions.Type: GrantFiled: April 13, 1993Date of Patent: July 26, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiromitsu Saito, Satoru Nagamura, Akira Asai, Eiji Kobayashi, Katsushige Gomi
-
Patent number: 5324725Abstract: Pharmacologically active compounds having anti-allergic properties corresponding to the formula I ##STR1## which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.Type: GrantFiled: August 21, 1992Date of Patent: June 28, 1994Assignee: Kali-Chemie Pharma GmbHInventors: Daniel Jasserand, Dominique Paris, Patrice Demonchaux, Michel Cottin, Francois Floc'H, Pierre Dupassieux, Richard White
-
Patent number: 5304554Abstract: Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensinBACKGROUND OF THE INVENTIONThe United States government has rights in this invention as a result of a grant from the NIAID of the National Institute of Health, Bethesda, Md.Type: GrantFiled: March 11, 1992Date of Patent: April 19, 1994Assignees: Emory University, Georgia State University Research FoundationInventors: Lucjan Strekowski, Roman L. Wydra, Steven E. Patterson, Raymond F. Schinazi
-
Patent number: 5304558Abstract: Novel diphenylmethyl piperazine derivatives of this invention have a chemical structure represented by the following Formula [I]: ##STR1## wherein R represents ##STR2## The compounds have an effect of inhibiting the overcontraction and overextension of the myocardium without being accompanied by a myocardium-inhibiting effect. By using the novel diphenylmethyl piperazine derivatives as an effective ingredient, it is possible to obtain a myocardial necrosis inhibitor which can protect against myocardial necrosis, and a drug for the treatment and prevention of acute myocardial infarction.Type: GrantFiled: March 2, 1993Date of Patent: April 19, 1994Assignee: Kirin Brewery Co., Ltd.Inventors: Noboru Kaneko, Makoto Takeishi, Tatsushi Oosawa, Kouji Akimoto, Hideo Oota, Tatsuo Nakajima
-
Patent number: 5302589Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.Type: GrantFiled: August 7, 1992Date of Patent: April 12, 1994Assignee: Glaxo, Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
-
Patent number: 5292726Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: May 19, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Sander G. Mills, Mu T. Wu
-
Patent number: 5273975Abstract: Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C.dbd.O, C.dbd.S, C-SCH.sub.3, C.dbd.NH, C-NH.sub.2, C-NHCH.sub.3, C--NHCOOCH.sub.3, or C--NHCN. B is CH.sub.2, CH, C.dbd.O, N, NH or N--CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C.dbd.O, O, N, NH or N--CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.Type: GrantFiled: December 6, 1991Date of Patent: December 28, 1993Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Richard F. Heier, Jeanette K. Morris
-
Patent number: 5237065Abstract: Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.Type: GrantFiled: February 4, 1992Date of Patent: August 17, 1993Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
-
Patent number: 5237061Abstract: A process for preparing compounds of the formula ##STR1## which comprises reacting an imidazolide of the formula ##STR2## with an amine of the formula NHR.sub.4 R.sub.5 in the presence of a Grignard reagent to form a compound of formula I or reacting an imidazolide of formula II with a compound of the formula R.sub.6 Mgx to form a compound of formula I.Type: GrantFiled: October 31, 1988Date of Patent: August 17, 1993Assignee: Merck & Co., Inc.Inventors: Apurba Bhattacharya, Ulf H. Dolling, Joseph S. Amato, John M. Williams
-
Patent number: 5229387Abstract: Compounds of the formula ##STR1## wherein: m is an integer of 1-6;n is an integer of 1 or 2;X and Y are independently hydrogen; hydroxy; lower alkyl; lower alkoxy; or halo; or X and Y when adjacent and taken together are methylenedioxy or ethylene-1,2-dioxy;R is ##STR2## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or halo; and ##STR3## and pharmaceutically acceptable acid addition salts thereof. The compounds and salts exhibit useful pharmacological properties, including selective .alpha..sub.2 -adrenoceptor antagonist properties and 5-HT.sub.1A receptor partial agonist properties, and are particularly useful for the treatment of sexual dysfunction, depression and anxiety.Type: GrantFiled: September 20, 1991Date of Patent: July 20, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, Brian H. Vickery, Mike Spedding
-
Patent number: 5229511Abstract: This invention pertains to novel 3-substituted-aminomethyl-3-substituted-oxy-17a-methyl-17a-lower-alkyl-17a -aza-D-homo-5-alpha-androstane compounds useful as muscle relaxants, methods for preparing such compounds, and method for administering muscle relaxation, wherein the novel compounds are represented the general formula: ##STR1## including optical active isomeric forms, and pharmaceutically acceptable acid addition salts thereof, wherein:R is a selected from the group consisting of hydrogen, lower-alkyl, lower-alkyl carbonyl, and di(lower-alkyl)amino carbonyl:R.sup.1 is selected from the group consisting of: di(lower-alkyl)substituted amino; lower-cycloalkyl lower-alkyl, lower-alkyl substituted amino;, -piperidinyl; 1-pyrrolidinyl; 1-hexamethyleneimino; 4-morpholinyl; 1-piperazinyl, 1-(4-methylpiperazinyl), tri(lower-alkyl)substituted amino, 1-(1-methylpiperidinyl); 1-(1-methylpyrrolidinyl); and 1-(4,4-dimethylpiperazinyl), each lower-alkyl group having from 1 to 6 carbon atoms;R.sub.Type: GrantFiled: June 8, 1992Date of Patent: July 20, 1993Assignee: Anaquest, Inc.Inventor: Roger S. Chen
-
Patent number: 5227380Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show antileukemic and anti-tumor activity.Type: GrantFiled: December 31, 1990Date of Patent: July 13, 1993Assignee: Research Triangle InstituteInventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
-
Patent number: 5215989Abstract: Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members, X and Y are bridging groups, Q is a nitrogen containing heterocycle, R.sup.2 and R.sup.3 are H, substituted or unsubtituted C.sub.1-3 alkyl, C.sub.1-3 alkoxy, N(R).sub.2, halogen, CF.sub.3 or R.sup.5 and R.sup.1 is H or an aryl group.Type: GrantFiled: July 15, 1991Date of Patent: June 1, 1993Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
-
Patent number: 5210194Abstract: Ergoline derivatives of the formula I: ##STR1## wherein R represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 represents hydrogen, chlorine, bromine or methyl; either R.sub.2 and R.sub.3 both represent hydrogen or together represent a chemical bond; R.sub.4 represents a C.sub.1 -C.sub.4 hydrocarbon group; each of R.sub.5, R.sub.6, R.sub.8 and R.sub.9 independently represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.7 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or C.sub.3 -C.sub.7 cycloalkyl and n is 0, 1 or 2; are prepared by reaction between compounds of the formulae II and III: ##STR2## and subsequent cyclization of the resultant compounds. The compounds of the formula I are known useful anxiolytic, antipsychotic and anti-parkinson agents.Type: GrantFiled: September 25, 1991Date of Patent: May 11, 1993Assignee: Farmitalia Carlo Erba S.r.l. An Italian Body CorporateInventors: Sergio Mantegani, Gabriella Traquandi, Tiziano Bandiera, Enzo Brambilla
-
Patent number: 5208237Abstract: A novel series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, (CH.sub.2).sub.m R.sup.3 ; benzoxazol-2yl, or benzothiazol2-yl;R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.Type: GrantFiled: April 3, 1992Date of Patent: May 4, 1993Assignee: Bristol-Meyers Squibb CompanyInventors: Piyasena Hewawasam, Nicholas A. Meanwell
-
Patent number: 5196428Abstract: A novel series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## Wherein R is H, or C.sub.1 -C.sub.4 lower alkyl;X is OR.sup.1, NR.sup.2 R.sup.3, or ##STR2## Z is O, NH, N(CH.sub.2).sub.m R.sup.5 or CHR.sup.6 ; R.sup.1 is C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.3 is H, C.sub.1 -C.sub.4 lower alkyl, or C.sub.4 -C.sub.8 cycloalkyl;R.sup.5 is C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, 2-pyranyl, 2-thienyl, 3-thienyl, piperidinyl-N-CH, N-2-pyridyl, N-2-pyrimidinyl, or substituted or unsubstituted phenyl wherein the substituent is halogen;R.sup.6 is H, 1-piperidinyl, or phenylmethyl;m is an integer of 1-3; andn is an integer of 1.5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasm.Type: GrantFiled: April 3, 1992Date of Patent: March 23, 1993Assignee: Bristol-Myers Squibb CompanyInventor: Nicholas A. Meanwell