Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos (e.g., 3-azabicyclo-(3.2.2)nonanes, Etc.) Patents (Class 540/582)
  • Patent number: 5696129
    Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in treatment of gastrointestinal disorders, cardiovasular disorders and CNS disorders.
    Type: Grant
    Filed: March 29, 1995
    Date of Patent: December 9, 1997
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Francis David King, Laramie Mary Gaster, Paul Adrian Wyman, Graham Francis Joiner
  • Patent number: 5658902
    Abstract: Novel quinazoline inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin and in controlling hypertension, myocardial infarction and ischemia, metabolic, endocrinological, and neurological disorders, congestive heart failure, endotoxic and hemorrhagic shock, septic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, cyclosporin-A induced nephrotoxicity, angina, gastric mucosal damage, ischemic bowel disease, cancer, pulmonary hypertension, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, cerebral ischemia and vasospasm, and diabetes.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: August 19, 1997
    Assignee: Warner-Lambert Company
    Inventors: Kyunghye Ahn, Xue-Min Cheng, Annette Marian Doherty, Edward Faith Elslager, Brian Kornberg, Chitase Lee, Daniele Leonard, Sham Nikam, Leslie Morton Werbel
  • Patent number: 5646154
    Abstract: Quinazoline compounds represented by general formula (1) or (2) possess an activity of significantly inhibiting the production or secretion of a tumor necrosis factor and are useful as drugs for the treatment of diseases wherein a tumor necrosis factor is considered to be involved in causing those diseases: ##STR1## wherein R.sup.1 through R.sup.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: July 8, 1997
    Assignee: Sumitomo Pharmaceuticals Co., Ltd.
    Inventors: Kenji Irie, Yutaka Ueda, Norio Fujiwara
  • Patent number: 5563148
    Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: October 8, 1996
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
  • Patent number: 5552412
    Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
    Type: Grant
    Filed: January 9, 1995
    Date of Patent: September 3, 1996
    Assignee: Pfizer Inc
    Inventors: Kimberly O. Cameron, Paul A. Dasilva Jardine, Robert L. Rosati
  • Patent number: 5538985
    Abstract: Antipsychotics and ischemic cerebral disease therapeutics comprising as an effective ingredient a compound represented by the following formula (1) or (2): ##STR1## or a salt thereof. These drugs do not induce extrapyramidal side effects.
    Type: Grant
    Filed: January 24, 1995
    Date of Patent: July 23, 1996
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Hajime Iizuka, Takahisa Oguchi, Yoji Aoki, Norio Ohto, Kazutoshi Horikomi, Takaichi Miwa, Takeshi Kamioka, Shoji Kawashima
  • Patent number: 5523299
    Abstract: Compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonyl, trifluoromethylsulphonyl; optionally substituted arylsulphonyl, optionally substituted heteroarylsulphonyl, optionally substituted aralkylsulphonyl, optionally substituted heteroaralkylsulphonyl, nitro, cyano, amino, mono- or di-alkylamino, trifluoromethyl, trifluoromethoxy, hydroxyl, hydroxyalkyl, C.sub.1-4 alkylthio, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, alkylaminosulphonyl or dialkylaminosulphonyl; or R.sup.1 and R.sup.2 together form a linking chain-(CH.sub.2).sub.m Op (wherein m is 2 to 4 and p is zero or 1) which chain may be optionally substituted by one or two C.sub.1-4 alkyl groups; and Y represents a group selected from (a) or (b) wherein R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.
    Type: Grant
    Filed: February 3, 1995
    Date of Patent: June 4, 1996
    Assignee: SmithKline Beecham PLC
    Inventors: Geoffrey Stemp, Michael S. Hadley, David J. Nash, Christopher N. Johnson
  • Patent number: 5512579
    Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl. etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: April 30, 1996
    Assignee: Eisai Co., Ltd.
    Inventors: Shuhei Miyazawa, Yorohisa Hoshino, Hisashi Shibata, Kazuo Hirota, Takaaki Kameyama, Shinya Abe, Takashi Yamanaka
  • Patent number: 5498614
    Abstract: The invention relates to bridged aza-bicyclic derivatives of formula (I). These compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. Also disclosed are intermediates used in the synthesis of compound of formula (I).
    Type: Grant
    Filed: November 7, 1994
    Date of Patent: March 12, 1996
    Assignee: Pfizer Inc.
    Inventor: Manoj C. Desai
  • Patent number: 5414009
    Abstract: The present invention relates to compounds ##STR1## where G is ##STR2## and Z is oxygen or sulfur and the remaining variables are as defined in the Specification. The compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.
    Type: Grant
    Filed: January 4, 1993
    Date of Patent: May 9, 1995
    Assignee: Novo Nordisk A/S
    Inventors: Preben H. Olesen, Per Sauerberg
  • Patent number: 5364863
    Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
    Type: Grant
    Filed: April 26, 1993
    Date of Patent: November 15, 1994
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
  • Patent number: 5352685
    Abstract: The thieno[3.2-b]pyridine derivative of the present invention promote the gastric emptying in male ddy mice and the gastric contraction in dogs sutured with a strain-gauge transducer. It is believed that the derivatives have the action to enhance gastric motor action and gastric emptying. Therefore, the compound of the present invention are effective for the prevention and therapeutical treatment of the symptoms caused by gastric hypanakinesis, such as heartburn, abdominal distension feeling, anorexia, unpleasant feeling on upper abdomen, abdominalgia, nausea, vomiting, etc. caused by the underlying diseases such as acute and chronic gastritis, stomach and duodenum ulcer, gastroneurosis, gastroptosis, etc. The present invention also encompasses a pharmaceutical composition containing as the effective ingredient a compound of the present invention, and a method for producing the same.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: October 4, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Akira Maruyama, Shigeru Ogawa, Satoshi Yamazaki, Akihiro Tobe
  • Patent number: 5260293
    Abstract: The present invention provides pyrazines, pyridazines or pyrimidines, or salts or prodrugs thereof, substituted on one of the ring carbon atoms thereof with a non-aromatic azacyclic or azabicyclic ring system; and independently substituted on each of the other ring carbon atoms with a substituent of low lipophilicity or a hydrocarbon substituent; which compounds stimulate central muscarinic acetylcholine receptors and therefore are useful in the treatment of neurological and mental illnesses.
    Type: Grant
    Filed: October 10, 1991
    Date of Patent: November 9, 1993
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Leslie J. Street, John Saunders
  • Patent number: 5223625
    Abstract: The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: June 29, 1993
    Assignee: Duphar International Research B.V.
    Inventors: Ineke Van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters
  • Patent number: 5219849
    Abstract: A class of pyrazine, pyrimidine and pyridazine derivatives, substituted by a non-aromatic azabicyclic ring system and optionally by up to two further substituents, is of use in the preparation of medicaments, especially formulations adapted for topical administration to the eye, suitable for the treatment of glaucoma and/or for reducing intraocular pressure.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: June 15, 1993
    Assignee: Merck Sharp & Dohme
    Inventors: Victor Lotti, Graham A. Showell
  • Patent number: 5110828
    Abstract: Novel compounds of formula (I), a process for their preparation, and their use as pharmaceutical agents are described: ##STR1## wherein R.sub.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is hydrogen or C.sub.1-4 alkyl, subject to the proviso that when R.sub.2 is a group OCOR.sub.5 or a group NHR.sub.6, R.sub.3 is C.sub.1-4 alkyl.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: May 5, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Steven M. Bromidge, Michael S. Hadley, Barry S. Orlek
  • Patent number: 5106843
    Abstract: Aryl ureas and carbamic acid derivatives of formulaA--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including 3,5-dichlorophenylW is O or SY is NH or O andB is a specified saturated azacyclic ring, e.g. tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.
    Type: Grant
    Filed: December 19, 1989
    Date of Patent: April 21, 1992
    Assignee: American Home Products Corporation
    Inventors: Terence J. Ward, Janet C. White
  • Patent number: 5049556
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.
    Type: Grant
    Filed: August 2, 1989
    Date of Patent: September 17, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Karen A. Joiner
  • Patent number: 4988706
    Abstract: Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described: ##STR1## in which X represents a group ##STR2## wherein one of Y and Z represents nitrogen and the other represents CR where R is selected from halogen, CN, OR.sup.1, SR.sup.1, N(R.sup.1).sub.2, NHR.sup.1, NHCOR.sup.1, NHCOOCH.sub.3, NHCOOC.sub.2 H.sub.5, NHOR.sup.1, NHNH.sub.2, COR.sup.1, COR.sup.2, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or C.sub.1-2 alkyl substituted with OR.sup.1, N(R.sup.1).sub.2, SR.sup.1, CO.sub.2 R.sup.1, CON(R.sup.1).sub.2 or one or two halogen atoms, in which R.sup.1 is hydrogen or C.sub.1-2 alkyl and R.sup.2 is OR.sup.1, NH.sub.2 or NHR.sup.1 ; and each of p and q independently represents an integer of 2 to 4.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: January 29, 1991
    Assignee: Beecham Group P.L.C.
    Inventors: Michael S. Hadley, Barry S. Orlek, Paul A. Wyman, Harry J. Wadsworth
  • Patent number: 4988691
    Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2 and Y have the meanings indicated in the description), a process for the preparation thereof and pharmaceutical compositions containing them as active ingredient are described.Compounds of formula I exhibit anto-serotonin activity.
    Type: Grant
    Filed: January 8, 1990
    Date of Patent: January 29, 1991
    Assignee: Zambon Group S.p.A.
    Inventors: Giancarlo Benelli, Angelo Carenzi, Dario Chiarino, Mario Fantucci
  • Patent number: 4983600
    Abstract: Aroyl ureas and carbamic acid derivatives of formulaA--CO--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including optionally substituted phenylW is O or SY is NH or S andB is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.
    Type: Grant
    Filed: October 16, 1989
    Date of Patent: January 8, 1991
    Assignee: John Wyeth & Brother Limited
    Inventors: Terence J. Ward, Janet C. White, Gerald Bradley
  • Patent number: 4971975
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents R.sub.1 OOC-- in which R.sub.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl; R.sub.2 O-- in which R.sub.2 is C.sub.1-2 alkyl, C.sub.1-2 alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups;a group ##STR2## in which Y represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-2 alkyl group, Y being optionally C-substituted by a methyl group; or a group ##STR3## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.3 and the other is nitrogen or CR.sub.4 where R.sub.3 and R.sub.4 are independently selected from hydrogen and methyl; and each of p and q independently represents an integer of 2 to 4.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: November 20, 1990
    Assignee: Beecham Group plc
    Inventors: Michael S. Hadley, Paul A. Wyman, Barry S. Orlek
  • Patent number: 4937239
    Abstract: Novel 1-azabicycloalkane- and alkene-oximes (Ia) and 8-azabicyclo[3.2.1]octane- and octene-oximes (Ib) are provided, these compounds being useful as agents for treating pain or for treating the symptoms of senile cognitive decline. Also provided are pharmaceutical compositions containing the compounds and methods of treatment using the compounds in dosage form.
    Type: Grant
    Filed: February 13, 1989
    Date of Patent: June 26, 1990
    Assignee: Warner-Lambert Company
    Inventors: David J. Lauffer, Walter H. Moos, Hasile Tecle
  • Patent number: 4921982
    Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.
    Type: Grant
    Filed: June 14, 1989
    Date of Patent: May 1, 1990
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
  • Patent number: 4883874
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen;either R.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylithio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.
    Type: Grant
    Filed: February 8, 1989
    Date of Patent: November 28, 1989
    Assignee: Beecham Group plc. of Beecham House
    Inventors: Francis D. King, Michael S. Hadley, Roger T. Martin
  • Patent number: 4826839
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen; either R.sub.1 is C.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O) n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.
    Type: Grant
    Filed: July 17, 1986
    Date of Patent: May 2, 1989
    Assignee: Beecham Group p.l.c.
    Inventors: Francis D. King, Michael S. Hadley, Roger T. Martin
  • Patent number: 4826838
    Abstract: Carbocyclic and heterocyclic carbonylmethylene- and carbonylmethylpiperidines and -pyrrolidines are serotonin antagonists.
    Type: Grant
    Filed: July 7, 1987
    Date of Patent: May 2, 1989
    Assignee: Sandoz Ltd.
    Inventors: Brian P. Richardson, Rudolf K. A. Giger, Gunter Engel, Roland Furler
  • Patent number: 4822795
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;X is N or CR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1-6 alkoxy;Y is N or CR.sub.4 wherein R.sub.4 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;R.sub.1 and R.sub.2 are independently selected from hydrogen, or halogen;Z is a group of formula (a), (b) or (c): ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; andR.sub.5 or R.sub.
    Type: Grant
    Filed: July 27, 1987
    Date of Patent: April 18, 1989
    Assignee: Beecham Gropup p.l.c.
    Inventor: Francis D. King
  • Patent number: 4808588
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: February 28, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Francis D. King
  • Patent number: 4803199
    Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: February 7, 1989
    Inventors: Peter Donatsch, Gunter Engel, Bruno Hugi, Brian P. Richardson, Paul A. Stadler, deceased, by Hildegard R. Stadler, heir, by Brigitte M. Stadler, heir, by Sigrid A. Stadler, heir, by Gerald Breuleux, legal representative
  • Patent number: 4798829
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 1, 2, or 3; and m and p are independently 1 or 2 such that m+n+p.gtoreq.4;X is NH; or O when Ar is of formula (a) and R.sub.4 is hydrogen or when Ar is a heteroaromatic group which may be substituted;R.sub.1, R.sub.2 and R.sub.3 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: ##STR2## wherein either R.sub.4 is C.sub.1-6 alkoxy and one of R.sub.5, R.sub.6, and R.sub.7 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkyl or phenyl C.sub.
    Type: Grant
    Filed: August 14, 1986
    Date of Patent: January 17, 1989
    Assignee: Beecham Group plc.
    Inventors: Francis D. King, Karen A. Joiner
  • Patent number: 4797387
    Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X is a moiety capable of hydrogen bonding to the NH group depicted in formula (I);R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, carboxy, C.sub.1-6 alkoxycarbonyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.4-5 polymethylene; andZ is a group of formula (a), (b) or (c) ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; and R.sub.3 or R.sub.4 is C.sub.1-7 alkyl, C.sub.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: January 10, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Francis D. King
  • Patent number: 4789673
    Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: December 6, 1988
    Inventors: Peter Donatsch, Gunter Engel, Bruno Hugi, Brian P. Richardson, Hildegard R. Stadler, Brigitte M. Stadler, Sigrid A. Stadler, Gerald Breuleux
  • Patent number: 4788184
    Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.
    Type: Grant
    Filed: November 13, 1987
    Date of Patent: November 29, 1988
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4775668
    Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically aceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.
    Type: Grant
    Filed: August 19, 1986
    Date of Patent: October 4, 1988
    Assignee: Pfizer Inc.
    Inventors: Martin R. Jefson, Paul R. McGuirk
  • Patent number: 4697019
    Abstract: A compound of formula (XXII): ##STR1## or a compound of formula (XXIII): ##STR2## wherein in formula (XXIII), j.sup.1 -1 is 1 to 4; and Q.sub.6 and Q.sub.7 are on the same carbon atom; and wherein, in formulae (XXII) and (XXIII), Q.sub.6 is NH.sub.2 and Q.sub.7 is H, and either p is 0 to 2 and q is 1; or p is 1 and q is 0 to 3; and one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl --C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen; and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl.
    Type: Grant
    Filed: March 21, 1986
    Date of Patent: September 29, 1987
    Assignee: Beecham Group p.l.c.
    Inventor: Francis D. King
  • Patent number: 4612319
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, or N-oxide thereof, or a solvate of any of the foregoing: ##STR1## wherein p is 0 to 2; q is 0 to 3; j is 0 to 4;one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl; andA is of formula (II): ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are each independently selected from hydrogen, halogen, CF.sub.3 C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 carboxylic acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: April 12, 1983
    Date of Patent: September 16, 1986
    Assignee: Beecham Group p.l.c.
    Inventor: Francis D. King