Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/219)
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Patent number: 5674867Abstract: The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt thereof as an active ingredient, and to novel indolocarbazole derivatives.Type: GrantFiled: May 18, 1994Date of Patent: October 7, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tatsuya Tamaoki, Yukimasa Shiotsu, Chikara Murakata, Shiro Akinaga, Masami Okabe, Yutaka Saito, Junichi Watanabe, Takako Shiraki
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Patent number: 5639750Abstract: The invention relates to the treatment fluid secretion caused by Cholera toxin that can be blocked through the administration of PAF antagonists BN 52021 and SR 27417.Type: GrantFiled: June 7, 1995Date of Patent: June 17, 1997Assignee: University of Virginia Patent FoundationInventors: Richard L. Guerrant, Guodong D. Fang, Manasses C. Fonteles
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Patent number: 5593988Abstract: A therapeutic agent for osteoporosis, comprising an azepine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof as an active ingredient, a method for treating osteoporosis comprising administering said compound and a use of said compound for the production of a therapeutic agent for osteoporosis. The compounds of the formula (I) have superior bone resorption-inhibitory activity and act to reduce the increased amount of calcium in blood serum, which is caused by bone resorption.Type: GrantFiled: August 2, 1994Date of Patent: January 14, 1997Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Japan Tobacco, Inc.Inventors: Tetsuya Tahara, Minoru Moriwaki, Kenji Chiba, Shunichi Manabe, Masanori Shindo, Takashi Nakagawa, Takeshi Nakamura
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Patent number: 5565449Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.Type: GrantFiled: May 26, 1995Date of Patent: October 15, 1996Assignee: Genentech, Inc.Inventors: Brent Blackburn, Peter Barker, Thomas Gadek, Robert McDowell, Lawrence McGee, Todd Somers, Rob Webb, Kirk Robarge
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Patent number: 5536717Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters X, Y, R.sub.1 and R.sub.2 are as defined in the specification which are useful as antidepressant and analgesic agents.Type: GrantFiled: November 22, 1993Date of Patent: July 16, 1996Assignee: Hoechst Marion Roussel Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5532233Abstract: The invention relates to new hetrazepines of general formula ##STR1## wherein A, Z, n, X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meanings given in the specification.The new compounds are intended for use in treating pathological conditions and diseases in which PAF (platelet activating factor) is implicated.Type: GrantFiled: September 8, 1994Date of Patent: July 2, 1996Assignee: Boehringer Ingelheim KGInventors: Karl H. Weber, Albrecht Harreus, Werner Stransky, Gerhard Walther, Jorge Casals-Stenzel, Gojko Muacevic, Hubert Heuer, Wolf-Dietrich Bechtel
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Patent number: 5492906Abstract: The invention relates to thieno-triazolo-diazepine derivatives of the formula: ##STR1## wherein Y stands for oxygen or sulphur and R stands for various substituents, to a preparation process of said compounds and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-asthmatic, anti-allergic and gastro-intestinal protectors.Type: GrantFiled: February 18, 1992Date of Patent: February 20, 1996Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Braquet, Andre Esanu, Jean-Pierre Laurent, Alain Rolland
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Patent number: 5482937Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are useful in the pharmaceutical field, especially in treating allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.Type: GrantFiled: October 6, 1994Date of Patent: January 9, 1996Assignee: Eisai Co., Ltd.Inventors: Kazuo Okano, Shuhei Miyazawa, Richard S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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Patent number: 5482936Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.Type: GrantFiled: January 12, 1995Date of Patent: January 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Kyle J. Lindstrom
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Patent number: 5480881Abstract: The present invention is directed to the treatment of a disease caused by an amount of pathogenic LA-paf in lipoproteins and cells comprising administering to a subject requiring the treatment an effective amount of a paf-acether antagonist.Type: GrantFiled: August 11, 1993Date of Patent: January 2, 1996Inventor: Ruth Korth
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Patent number: 5470851Abstract: Thiazolidinecarboxylic acid amides having combined antiallergic and antiasthmatic activities with an antagonist activity against platelet Activating Factor and having the following general formula (I) ##STR1##Type: GrantFiled: September 30, 1993Date of Patent: November 28, 1995Assignee: Sankyo Company, LimitedInventors: Hiroshi Fukumi, Toshiaki Sakamoto, Mitsuo Sugiyama, Takeshi Yamaguchi, Takeshi Oshima, Fumitoshi Asai, Yasuteru Iijima
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Patent number: 5439905Abstract: Thienodiazepine compounds of the formula ##STR1## wherein each symbol is as defined in the specification, their pharmaceutically acceptable salts, and pharmaceutical compositions containing said compound.Since the compounds possess excellent antagonistic actions on cholecystokinin and gastrin, and exhibit potent and durable suppressive actions on pancreatic enzyme secretion and gastric acid secretion, they are useful as medicaments acting on the central nervous system and the peripheral nervous system, as well as prophylactic and therapeutic medicines for pancreatic disorders and gastrointestinal ulcers. Furthermore, they are expected to exhibit anti-dementia actions based on their antagonistic actions on cholecystokinin, and are useful as an anti-dementia.Type: GrantFiled: May 27, 1993Date of Patent: August 8, 1995Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Yoichi Naka, Keiichiro Haga, Masahiro Hosoya
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Patent number: 5438050Abstract: New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the inhibition of protein kinases, such as protein kinase C, for the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension, or for inflammatory processes, allergies, cancers, viral diseases, and certain degenerative damages of the central nervous system are disclosed.Type: GrantFiled: January 21, 1994Date of Patent: August 1, 1995Assignee: Godecke AktiengesellschaftInventors: Jurgen Kleinschroth, Johannes Hartenstein, Hubert Barth, Christoph Schachtele, Claus Rudolph, Gunter Weinheimer, Hartmut Osswald
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Patent number: 5438045Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OOO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.Type: GrantFiled: April 27, 1993Date of Patent: August 1, 1995Assignee: Eisai Co., Ltd.Inventors: Kazuo Okano, Shuhei Miyazawa, Richard S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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Patent number: 5436239Abstract: The invention relates to the treatment of antibiotic associated colitis, typically due to Clostridium difficile using the Platelet Activating Factor antagonists WEB 2170, SR 27417 or BN 52021, or the cyclooxygenase antagonist indomethacin. The PAF antagonists BN 52021 and SR 27417 and the cyclooxygenase antagonist indomethacin were effective in inhibiting the secretory effects caused by C. difficile Toxin A and by Cholera toxin.Type: GrantFiled: April 1, 1993Date of Patent: July 25, 1995Assignee: The University of Virginia Patent FoundationInventors: Richard L. Guerrant, Guodong Fang, Manasses C. Fonteles
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Patent number: 5407933Abstract: Compounds of formula (I): ##STR1## [wherein: A-- B is .dbd.C.dbd.CH--or a nitrogen atom; R.sup.1 is hydrogen, alkyl, aryl or aralkyl; and Z is alkylene] and pharmaceutically acceptable salts thereof are useful in the treatment and prevention of allergies and asthma.Type: GrantFiled: August 16, 1994Date of Patent: April 18, 1995Assignee: Sankyo Company, LimitedInventors: Hiroshi Fukumi, Toshiaki Sakamoto, Mitsuo Sugiyama, Yoshio Iizuka, Takeshi Yamaguchi
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Patent number: 5387585Abstract: The novel imidazodiazepine derivatives of the formula: ##STR1## wherein the substituents are as described in the specification, can be used for the control or prevention of epileptic seizures, anxiety, tension and excitation states, sleep disorders, schizophrenic symptoms, hepatic encephalopathy and senile dementia, as well as, in the partial or complete antagonization of undesired side-effects of substances acting on benzodiazepine receptors after over-dosage or after their use in intensive medicine and in anesthesia.Type: GrantFiled: November 15, 1993Date of Patent: February 7, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Rene Borer, Walter Gassner, Max Gerecke, Emilio Kyburz
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Patent number: 5382579Abstract: A triazolo-1,4-azepine compound of the below given formulas and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.Type: GrantFiled: August 26, 1991Date of Patent: January 17, 1995Assignee: Eisai Co., Ltd.Inventors: Kazuo Okano, Shuhei Miyazawa, Richard S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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Patent number: 5321023Abstract: This invention provides pyrido[4',3':2:3]indolo-[1,7-ab][1,5]benzodiazepines, pharmaceutical compositions containing these compounds, and methods of using these compounds to treat physiological or drug induced psychosis and/or dyskinesia.Type: GrantFiled: July 29, 1992Date of Patent: June 14, 1994Assignee: The Du Pont Merck Pharmaceutical Co.Inventor: Parthasarathi Rajagopalan
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Patent number: 5304553Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.Type: GrantFiled: May 28, 1993Date of Patent: April 19, 1994Assignee: Eisai Co., Ltd.Inventors: Kazuo Okano, Shuhei Miyazawa, Richar S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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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
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Patent number: 5240926Abstract: New substituted pyridyltriazines of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 have the meanings given in the description, and their use for combating pests.The compounds can be prepared by analogous processes, for example by reacting pyridylamidine hydrochloride with suitable methyl imidates or with suitable benzene-isothiocyanates, or by desulphurising mercapto-substituted pyridyltriazines or by reacting them with alcohols. The mercapto-substituted compounds are also new and can be prepared by analogous processes.Type: GrantFiled: August 21, 1992Date of Patent: August 31, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Dietmar Kuhnt, Heinz-Wilhelm Dehne, Stefan Dutzmann
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Patent number: 5240922Abstract: The present invention relates to a method of enhancing implantation of an embryo within the uterus of a female mammal. The method comprises administering an amount of a PAF antagonist, effective to enhance implantation, to the mammal. The invention also relates to a method of increasing the level of PAF around an embryo in the uterus of a female mammal by administering an amount of a PAF antagonist sufficient to inhibit PAF catabolism. Desirably the PAF antagonist is administered together with PAF or a homologue or analogue thereof. The invention also provides compositions comprising a PAF antagonist together with PAF or a homologue or analogue thereof, and a process for preparing the same.Type: GrantFiled: December 27, 1991Date of Patent: August 31, 1993Assignee: Northern Sydney Area Health ServiceInventor: Christopher O'Neill
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Patent number: 5238936Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.Type: GrantFiled: March 6, 1992Date of Patent: August 24, 1993Assignee: Adir et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre, Stephane Leonce
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Patent number: 5227378Abstract: The invention relates to compositions comprising combinations of a PAF antagonist and a LTD.sub.4 antagonist which combinations synergistically provide protection against allergic reactions such as antigen-induced death in mammals.In another aspect, the invention relates to the use of the referred to combinations in the treatment of allergic reactions.Type: GrantFiled: March 9, 1992Date of Patent: July 13, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Margaret O'Donnell, Ann Welton
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Patent number: 5221671Abstract: A triazolo-1,4-di-azepine compound of the below given formulas and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.Type: GrantFiled: October 17, 1991Date of Patent: June 22, 1993Assignee: Eisai Co., Ltd.Inventors: Kazuo Okano, Shuhei Miyazawa, Richard S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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Patent number: 5221672Abstract: The compound t-butyl (S)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][ 1,4]benzodiazepine-1-carboxylate of the formula ##STR1## can be used for the preparation of medicaments for the treatment of sleep disorders and also as a medicament for the treatment of sleep disorders.Type: GrantFiled: November 27, 1991Date of Patent: June 22, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Roman Amrein, Jean-Paul Laurent
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Patent number: 5206237Abstract: Pharmaceutical compositions containing benzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.Type: GrantFiled: May 14, 1991Date of Patent: April 27, 1993Assignee: Merck & Co., Inc.Inventors: Roger M. Freidinger, Mark G. Bock, Ben E. Evans
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Patent number: 5204342Abstract: Novel hydrogenated heterocyclic compounds, containing two nitrogen atoms, of the formula ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.5 and Rhd 7 are each, independently of the others, hydrogen or lower alkyl, m is 2 or 3, n is 1 or 2, and either R.sub.4 and R.sub.6 are each hydrogen or R.sub.4 and R.sub.6 together form an additional bond, in free form or in form of a salt, can be used as pharmaceutical active ingredients and can be manufactured in a manner known per se.Type: GrantFiled: March 31, 1992Date of Patent: April 20, 1993Assignee: Ciba-Geigy CorporationInventors: Wolfgang Frostl, Cesare Mondadori, Dietrich Strub, Armin Zust
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Patent number: 5180722Abstract: A camptothecin analog having the structure shown below: ##STR1## where Z is H or C.sub.1-8 alkyl and R is NO.sub.2, NH.sub.2, N.sub.3, hydrogen, halogen, COOH, OH, O--C.sub.1-3 alkyl, SH, S--C.sub.1-3 alkyl, CN, CH.sub.2 NH.sub.2, NH--C.sub.1-3 alkyl, CH.sub.2 --NH--C.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH--, or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S-- CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH.sub.2).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, CHO, C.sub.1-3 alkyl or NHCOCHR.sup.1 NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an .alpha.-amino acid and R.sup.2 and R.sup.3, independently are hydrogen or a lower alkyl group or R.sup.Type: GrantFiled: September 13, 1990Date of Patent: January 19, 1993Assignee: Research Triangle InstituteInventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
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Patent number: 5166202Abstract: Midazolam and its pharmaceutically acceptable salts are useful in the treatment of panic disorder, panic attacks and the prevention of panic attacks.Type: GrantFiled: December 13, 1991Date of Patent: November 24, 1992Assignee: Trustees of the University of PennsylvaniaInventor: Edward E. Schweizer
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Patent number: 5147872Abstract: Methods and means for treating psoriasis, as well as Crohn's disease and other HLA-related disorders, to abate their symptoms, with a pharmaceutical diazepine having a component triazolo ring. HLA-related disorders amenable to such treatment include (i) persistent eruptive, granular, or ulcerative conditions of the skin, mouth, or gastrointestinal tract; and (ii) dibilitating inflammatory conditions of the circulatory, muscular, and nervous systems. This treatment alleviates abnormality or unbalance of patients' immune systems, such as an overabundance of natural killer cells and/or an abnormality of helper T-cell/suppressor T-cell ratio, and alleviates the self-cannibilism of the Koebner phenomenon, when present. Triazolobenzodiazepines, such as alprazolam or triazolam, and triazolothienodiazepines, such as etizolam, are examples of preferred treating compositions.Type: GrantFiled: June 19, 1990Date of Patent: September 15, 1992Inventor: Daniel H. Golwyn
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Patent number: 5106845Abstract: The present invention is directed to a new class of cyclic guanidines of the formula: ##STR1## in which Q is represented by a substituent selected from the group consisting of (CH.sub.2).sub.n in which n is an integer from 2-10, ##STR2## A is a substituent selected from the group consisting of --NH--(CH.sub.2).sub.m in which m is an integer from 0-5, a piperidino substituent, or a piperazino substituent; both Ar and Ar.sub.1 are each independently represented by a phenyl ring, each of which may be optionally substituted with up to 3 substituents, each selected from the group consisting of halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and trifluoromethyl; and R is represented by either hydrogen or a C.sub.1-4 alkyl; R.sub.1 is represented by hydrogen or a C.sub.1-4 alkyl; the optional isomers and tautomers thereof; and the pharmaceutically acceptable acid addition salts thereof, and their use as calcium antagonists.Type: GrantFiled: January 10, 1990Date of Patent: April 21, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, Hsien C. Cheng, John M. Kane
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Patent number: 5070086Abstract: Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of hyperproliferative skin disease are disclosed.Type: GrantFiled: June 15, 1990Date of Patent: December 3, 1991Assignee: Schering CorporationInventor: Richard Friary
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Patent number: 5057514Abstract: 1. A compound having the formula (I): ##STR1## wherein A is --CH.sub.2 --, --O--, or --S--; R.sup.1 is CH.sub.3 or OCH.sub.3 ; R.sup.2 is hydroxy of carboxy which may be optionally esterized or amidated; R.sup.3 is H or a lower alkyl; and n is 0 or an integer of 1 to 6 or a pharmaceutically acceptable sale thereof.Type: GrantFiled: December 20, 1988Date of Patent: October 15, 1991Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kenji Suzuki, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
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Patent number: 5049560Abstract: This invention relates to thieno-triazolo-diazepine derivatives of the formula ##STR1## wherein R represents various substituents, to a preparation process of these compounds consisting in reacting the thieno-triazolo-diazepine compound of the formula ##STR2## on RSO.sub.2 Cl and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-PAF and anti-ischemic agents.Type: GrantFiled: March 20, 1990Date of Patent: September 17, 1991Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Andre Esanu, Pierre Braquet, Christiane Martin, Jean-Pierre Laurent
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Patent number: 5049559Abstract: The invention relates to thieno-triazolo-diazepine derivatives of the formula ##STR1## wherein Y stands for oxygen or sulphur and R stands for various substituents, to a preparation process of said compounds and to therapeutic compositions containing the same. The compounds are particularly interesting in the treatment of ischemia.Type: GrantFiled: May 11, 1990Date of Patent: September 17, 1991Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Braquet, Andre Esanu, Jean-Pierre Laurent, Jacques Pommier
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Patent number: 5010092Abstract: Drug treatment therapies and kits for use therewith are disclosed. They involve the use of methimazole and/or its pro-drug carbimazole to reduce nephrotoxic effects of chemical exposure. In one embodiment, a patient receives cisplatin and then is treated with methimazole. The time delay in providing methimazole prevents the methimazole from being substantially expelled by the kidney prior to cisplatin reaching the kidney.Type: GrantFiled: December 22, 1989Date of Patent: April 23, 1991Assignee: Wisconsin Alumni Research FoundationInventor: Adnan A. Elfarra
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Patent number: 5008263Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.Type: GrantFiled: March 20, 1990Date of Patent: April 16, 1991Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael J. Fray
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Patent number: 5008262Abstract: The instant invention is drawn to the use of clomipramine for treating trichotillomania and onchyphagia.Type: GrantFiled: April 19, 1988Date of Patent: April 16, 1991Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Susan E. Swedo, Judith L. Rapoport, Henrietta L. Leonard
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Patent number: 4997831Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.Type: GrantFiled: August 31, 1989Date of Patent: March 5, 1991Assignee: Glaxo Group LimitedInventors: David E. Bays, Ian H. Coates, Alexander W. Oxford, Peter C. North
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Patent number: 4997832Abstract: Disclosed are the compounds of formula I ##STR1## wherein R.sub.1 -R.sub.3 represent hy drogen or lower alkyl; m represents the integer 2 or 3; n represents the integer 1 or 2; Het represents a pyrrole or imidazole ring bonded at any two adjacent positions and optionally substituted by one or two of lower alkyl; and pharmaceutically acceptable salts of compounds of formula I wherein Het represents optionally substituted imidazole; their methods of preparation; pharmaceutical compositions thereof, and their use for treating cognitive disorders in mammals.Type: GrantFiled: October 24, 1989Date of Patent: March 5, 1991Assignee: Ciba-Geigy CorporationInventor: Jan W. F. Wasley
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Patent number: 4985423Abstract: The invention relates to a group of new 1,4-diazepine derivatives of the formula ##STR1## wherein A represents a group of the formulae 2-10 ##STR2## These compounds have a strong anti-ulcer activity after oral administration.Type: GrantFiled: July 3, 1989Date of Patent: January 15, 1991Assignee: Duphar International Research B.V.Inventors: Jacobus A. J. den Hartog, Herman H. van Stuivenberg, Ineke van Wijngaarden
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Patent number: 4983601Abstract: Novel benzo[b]pyrrolo[3,2,1-jk]benzodiazepines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing the compounds or compositions thereof are disclosed.Type: GrantFiled: August 7, 1989Date of Patent: January 8, 1991Assignee: Hoechst-Roussel Pharmaceutical Inc.Inventors: Edward J. Glamkowski, Barbara E. Kurys
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Patent number: 4960770Abstract: A thienotriazolodiazepine compound of the formula: ##STR1## wherein Ar is phenyl, pyridyl, substituted phenyl or substituted pyridyl; R.sup.1 and R.sup.3 are the same or different and each is hydrogen, alkyl having 1 to 4 carbon atoms; R.sup.2 is hydrogen, alkyl having 1 to 4 carbon atoms or trifluoromethyl; R.sup.4 is straight or branched chain alkyl, alkenyl or alkynyl having 6 to 18 carbon atoms, or a thienodiazepine compound of the formula: ##STR2## wherein Ar, R.sup.1, R.sup.2 and R.sup.4 are as defined above, and pharmaceutically acceptable acid addition salt thereof.These compounds are useful as drugs for the treatment of circulatory diseases and various PAF-induced diseases. The compound (II) is also useful as an intermediate for preparing the compound (I).Type: GrantFiled: January 11, 1989Date of Patent: October 2, 1990Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Minoru Moriwaki, Masao Abe, Hiroshi Mikashima, Tetsuya Tahara
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Patent number: 4950664Abstract: Nasal administration of benzodiazepines is described as providing improved therapeutic effects as compared to conventional delivery techniques. The compositions comprise a benzodiazepine hypnotic in a pharmaceutically acceptable nasal carrier.Type: GrantFiled: September 16, 1988Date of Patent: August 21, 1990Assignee: Rugby-Darby Group Companies, Inc.Inventor: Arthur H. Goldberg
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Patent number: 4929615Abstract: Novel 7H-benzo[b]pyrazino[1,2-d]pyrrolo[3,2,1-jk][1,4]benzodiazepines, processes for the preparation thereof, and a method of treating depression utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: June 12, 1989Date of Patent: May 29, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Barbara E. Kurys
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Patent number: 4914095Abstract: A compound of the formula ##STR1## is useful to treat psychotic disorders in humans, especially schizophrenia, and to prevent exacerbations thereof. The compound can be used as a single therapeutic agent or in combination with neuroleptics such as haloperidol.Type: GrantFiled: January 13, 1989Date of Patent: April 3, 1990Assignee: Hoffmann-La Roche Inc.Inventor: Walter Merz
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Patent number: 4908361Abstract: Novel Tetrahydroisoquino[2,1-c][1,3]benzodiazepines are disclosed having the formula ##STR1## where X and Y are each independently hydrogen, halogen, loweralkyl, loweralkoxy or --CF.sub.3, and R is hydrogen or loweralkyl, and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility in enhancing memory.Type: GrantFiled: April 28, 1989Date of Patent: March 13, 1990Assignee: Hoechst-Roussel IncorporatedInventors: Lawrence L. Martin, Richard C. Allen
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Patent number: 4897392Abstract: There are disclosed compounds having the formula ##STR1## where X is H, halogen, --OH,--OCH.sub.3,--NO.sub.2 or --CF.sub.3 ; Y is H, Cl or Br; Z is H, halogen, --OH or --OCH.sub.3 ; and R is H, loweralkyl, --CH.sub.2 OH or diloweralkylaminomethyl, which compounds are useful as analgesic agents.Type: GrantFiled: July 3, 1989Date of Patent: January 30, 1990Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: John J. Tegeler, Eileen M. Gardenhire, Grover C. Helsley