Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/376)
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Patent number: 5650412Abstract: Compounds of formula ##STR1## are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 26, 1995Date of Patent: July 22, 1997Assignee: Merck & Co., Inc.Inventors: Byeong Moon Kim, Joseph P. Vacca
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Patent number: 5650456Abstract: This invention relates to coumarin derivatives of formula (I) ##STR1## where Z represents OR.sup.3 or NR.sup.4 R.sup.5,to their preparation, and to their use for the production of polymers with luminophors on their side chains.Type: GrantFiled: February 9, 1996Date of Patent: July 22, 1997Assignee: Bayer AktiengesellschaftInventors: Chen Yun, Rolf Wehrmann, Burkhard Kohler
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Patent number: 5646149Abstract: Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the compounds and corresponding pharmaceutical compositions are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, George Barnes, Robert J. Collier, Jr.
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Patent number: 5637583Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: September 27, 1994Date of Patent: June 10, 1997Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 5637703Abstract: The invention concerns chemical compounds, derivatives of genistein, which exhibit pronounced immunosuppressant and antitumor activity. In particular, the invention concerns compounds having general formula 1, where R.sup.1, R.sup.2, R.sup.3 are the same or different, R.sup.1 denotes hydrogen or alkyl, R.sup.2 and R.sup.3 are the same or different and denote hydrogen, alkyl or aryl, or R.sup.2 and R.sup.3 are taken together with the nitrogen to which they are connected to form a heterocycle ring.Type: GrantFiled: August 13, 1996Date of Patent: June 10, 1997Assignee: Drug InstituteInventors: Aleksander P. Mazurek, Krzysztof Biniecki, Lech Kozerski
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Patent number: 5618938Abstract: Compounds of the formula ##STR1## and their salts with mineral or organic acids are useful as neurokinin receptor antagonists. Methods of preparing the compounds, especially pure STEREO ISOMERS thereof, are provided.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5614524Abstract: A class of substituted piperazine derivatives of formula I ##STR1## are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated conditions, for which a selective agonist of these receptors is indicated.Type: GrantFiled: May 19, 1995Date of Patent: March 25, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: V. G. Matassa, L. J. Street, A. J. Reeve
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Patent number: 5607937Abstract: The present invention relates to D,L-, L- and D-phenylalanine piperazides of formula (I) defined in claim 1 that inhibit blood coagulation, and thrombin and/or trypsin, respectively. The compounds are extraordinarily absorbable after oral, intraduodenal and in particular rectal administration and show only a low toxicity.Type: GrantFiled: January 5, 1995Date of Patent: March 4, 1997Assignee: Pentapharm AGInventors: Joerg Stuerzebecher, Helmut Vieweg, Peter Wikstroem, Christoph Adler
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Patent number: 5607939Abstract: The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.Type: GrantFiled: April 25, 1995Date of Patent: March 4, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
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Patent number: 5605896Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: August 31, 1994Date of Patent: February 25, 1997Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5580863Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: May 13, 1994Date of Patent: December 3, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5565457Abstract: The compounds are N-(2,3,4-trimethoxybenzyl)piperazines N'-substituted by a radical containing a sulfonamide group, and pharmaceutically tolerable salts thereof, useful for treating myocardial ischaemic pathologies, cerebral vascular accident and manifestations of deficiency associated with chronic cerebral circulatory disorders.A compound disclosed is : N-benzyl-N-{3,3-dimethyl-4-[4-(2,3,4-trimethoxybenzyl) piperazin-1-yl]butyl}-(isoquinolin-5-yl)sulfonamide and its fumarate.Type: GrantFiled: February 23, 1995Date of Patent: October 15, 1996Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Jean-Paul Vilaine, Nicole Villeneuve, Jean-Pierre Iliou, Jean-Pierre Bidouard
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Patent number: 5563141Abstract: A compound of the general formula(M.sup.1).sub.n --Q--(M.sup.2).sub.1-n --L--A Iwherein:n is 0 or 1;M.sup.1 is an amino group;Q is an aromatic heterocyclic group containing a basic nitrogen atom;M.sup.2 is an imino group;L is a template group; andA is an acidic group, or an ester or amide derivative thereof, or a sulphonamide group;and pharmaceutically acceptable salts and pro-drugs thereof, for use in the treatment of a disease in which platelet aggregation mediated by the binding of adhesion molecules to GPIIb-IIIa is involved. Novel compounds are also disclosed.Type: GrantFiled: March 28, 1994Date of Patent: October 8, 1996Assignee: Zeneca LimitedInventors: Michael G. Wayne, Michael J. Smithers, John W. Rayner, Alan W. Faull, Robert J. Pearce, Andrew G. Brewster, Richard E. Shute, Stuart D. Mills, Peter W. R. Caulkett
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Patent number: 5550129Abstract: Described are 2H-1-benzopyran-2-ones (coumarin derivates) of general formula (I), ##STR1## wherein R.sup.1 is a hydroxyl group, a lower-alkoxy group, a cycloalkoxy group with 4 to 6 C-atoms or the alkyl- or arylsulphonyloxy group R.sup.6 --SO.sub.2 O--;R.sup.2 and R.sup.3, independently of each other, are hydrogen atoms, hydroxyl groups, lower-alkoxy groups or cycloalkoxy groups with 4 to 6 C-atoms;R.sup.4 is a hydrogen atom, a lower-alkyl group with 1 to 4 C-atoms or a phenyl group;Y is a nitrogen atom, a CH group or a COH group;R.sup.5 is a phenyl, naphtyl, pyridinyl or pyrimidinyl group which may optionally be substituted by one or two C.sub.1 -C.sub.5 alkyl groups, by one or two halogen atoms, by a halogen and C.sub.1 -C.sub.5 alkyl together, by perfluoroalkyl with 1 to 3 C-atoms, by C.sub.1 -C.sub.5 alkoxy, by hydroxy, by methylenedioxy or by nitro;R.sup.6 is a lower-alkyl group, a cycloalkyl group with 4 to 6 C-atoms or a phenyl group which may optionally be substituted by one or two C.sub.1 -C.sub.Type: GrantFiled: April 5, 1995Date of Patent: August 27, 1996Assignee: Willmar Schwabe GmbH & Co.Inventors: Michael N oldner, Shyam S. Chatterjee, Hermann Hauer
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Patent number: 5541323Abstract: Anhydride compounds which contain at least one rodlike mesogenic moiety and at least two anhydride groups per molecule, wherein each of said aromatic anhydride groups is linked to the mesogen via an ester linkage are prepared. These anhydride compounds are useful in curing epoxy resins to provide the cured products with one or more improved properties.Type: GrantFiled: January 18, 1995Date of Patent: July 30, 1996Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5539112Abstract: 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.Type: GrantFiled: June 5, 1995Date of Patent: July 23, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Akama, Shun-ichi Ikeda, Yasushi Shida, Masaji Kasai, Hiroyuki Ishida, Uichiro Kimura, Katsushige Gomi, Hiromitsu Saito, Kimihisa Ueno
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Patent number: 5536833Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.Type: GrantFiled: May 26, 1995Date of Patent: July 16, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas C. Sedergran, Nachimuthu Soundararajan
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Patent number: 5519023Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and Z are as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base and medicaments containing the same, useful in the treatment and prevention of stress, anxiety, and related ailments.Type: GrantFiled: July 2, 1993Date of Patent: May 21, 1996Assignee: Adir et CompagnieInventors: Marc Payard, Genevieve Baziard-Mouysset, Gilbert De Saqui-Sannes, Beatrice Guardiola, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
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Patent number: 5500425Abstract: Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.Type: GrantFiled: September 9, 1994Date of Patent: March 19, 1996Assignee: Aktiebolaget AstraInventors: Lars-Gunnar Larsson, Lucy A. Renyl, Svante B. Ross, Daniel D. Sohn, Seth-Olov Thorberg
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Patent number: 5496853Abstract: Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R.sub.1, R.sub.2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.Type: GrantFiled: April 26, 1995Date of Patent: March 5, 1996Assignee: Teijin LimitedInventors: Tatsuki Shiota, Takumi Takeyasu, Kenichiro Kataoka, Tsutomu Mochizuki, Hirofumi Tanabe, Mikio Ota, Masatoshi Kano, Hisao Yamaguchi
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Patent number: 5474994Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: May 26, 1993Date of Patent: December 12, 1995Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5472962Abstract: A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial cancer, endometriosis, mastopathy, etc.This compound is characterized in that the 2-position (the substituent R.sup.2) of the benzothiophene nucleus is substituted by a halogen atom; a lower alkyl group; or a cycloalkyl or cycloalkenyl group optionally substituted by a lower alkyl group, a hydroxyl group, acyloxy group or an oxo group.Type: GrantFiled: May 13, 1994Date of Patent: December 5, 1995Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Naoyuki Koizumi, Shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Teruaki Matsui, Mamoru Mieda, Hiroo Takahashi, Tomoyuki Saito, Kenyu Shibata
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Patent number: 5464834Abstract: New N-substituted N'-heterobicyclic piperazines corresponding to the general formula I: ##STR1## wherein: R represents: ##STR2## D represents a single bond, except when R represents naphthyl, or a hydrocarbon chain having 1 to 8 carbon atoms inclusive which is straight-chain or branched by a gem-dimethyl; andA-B represents: --(CH.sub.2).sub.2 --O--, --(CH.sub.2).sub.3 --O--, or --CO--CH.dbd.CH--,as well as their possible stereoisomers, epimers, and pharmaceutically-acceptable acid addition salts thereof; and medicinal products containing the same, useful in the treatment of a disorder requiring a 5-HT.sub.1A receptor antagonist.Type: GrantFiled: June 11, 1993Date of Patent: November 7, 1995Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Jean-Michel Rivet
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Patent number: 5457103Abstract: Compounds of the general formula (I): ##STR1## in which R represents: a hydrogen atom, ora radical --OR'in which R' is as defined in the description.Type: GrantFiled: August 18, 1993Date of Patent: October 10, 1995Assignee: Adir et CompagnieInventors: Yves Rolland, Guy Lewin, Jean-Paul Vilaine, Albert Lenaers, Catherine Thollon
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Patent number: 5440048Abstract: Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 5, 1994Date of Patent: August 8, 1995Assignee: Hoechst-Roussel Pharmaceuticals IncInventors: Helen H. Ong, Nicholas J. Hrib, Joseph Perez, John G. Jurcak
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Patent number: 5430033Abstract: Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formula R is hydrogen or one or two lower alkyl groups, R.sup.1 is a mono of bicyclic aryl or heteroaryl radical, R.sup.2 is aryl and A is a C.sub.2-5 alkylene chain optionally substituted by lower alkyl.Type: GrantFiled: April 22, 1994Date of Patent: July 4, 1995Assignee: John Wyeth & Brother Ltd.Inventors: Ian A. Cliffe, Anderson D. Ifill, Howard L. Mansell, Terence J. Ward, Alan C. White
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Patent number: 5428038Abstract: Novel 2H-1-benzopyran-2-ones (coumarin derivatives) of the general formula (I) are provided: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and Y are defined as in the specification, and the addition compounds thereof with physiologically compatible acids, intermediates and methods for the preparation thereof. The coumarin compounds possess a neuroprotective and anti-allergic action.Type: GrantFiled: October 8, 1993Date of Patent: June 27, 1995Assignee: Dr. Willmar Schwabe GmbH & Co.Inventors: Shyam S. Chatterjee, Michael Noldner, Hermann Hauer, Egon Koch
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Patent number: 5424313Abstract: The invention relates to new compositions with pyschotropic activity which comprise a compound of formula 1 of the formula sheet as the active substance. The compounds of formula 1 are for the greater part new compounds. The invention therefore also relates to these new compounds and to the preparation thereof in a manner known for the synthesis of analogous compounds.Type: GrantFiled: October 12, 1993Date of Patent: June 13, 1995Assignee: Duphar International Research B.V.Inventors: Jan Hartog, Berend Olivier, Ineke Van Wijngaarden, Cornelis G. Kruse, Johannes A. M. Van Der Heyden, Dirkje A. Van Dalen-Van Der AA
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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
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Patent number: 5412117Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents =O, =S, =N-Z (Z represents a lower alkyl group, etc.), or =CHNO.sub.2 ; Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 each represent a hydrogen atom, a lower alkyl group, etc., are disclosed. The benzopyran derivatives exhibit K.sup.+ channel activating activities and are widely applicable as antiasthmatics, antiepileptics, and the like.Type: GrantFiled: January 26, 1993Date of Patent: May 2, 1995Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hiroyuki Nabata
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Patent number: 5395834Abstract: A compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and n are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal product containing the same for treating a mammal afflicted with a disorder connected with peroxydation processes and biosynthesis of eicosanoids.Type: GrantFiled: April 11, 1994Date of Patent: March 7, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Jean-Paul Babingui, Sylvie Robert-Piessard, Pierre Renard, Daniel-Henri Caignard, Jean-Francois Renaud de la Faverie, Gerard Adam
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Patent number: 5395835Abstract: Naphthalamides are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as antipsychotic agents and as agents for the treatment of disorders which respond to dopaminergic blockade including psychotic depression, substance abuse, and compulsive disorders.Type: GrantFiled: March 24, 1994Date of Patent: March 7, 1995Assignee: Warner-Lambert CompanyInventors: Shelly A. Glase, Suzanne R. Kesten, Lawrence D. Wise, Jonathan Wright
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Patent number: 5393775Abstract: A compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and n are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same for treating a mammal afflicted with a disorder connected with peroxydation processes and biosynthesis of eicosanoids.Type: GrantFiled: September 7, 1993Date of Patent: February 28, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Jean-Paul Babingui, Sylvie Robert-Piessard, Pierre Renard, Daniel-henri Caignard, jean-Francois Renaud de la Faverle, Gerard Adam
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Patent number: 5389668Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.Type: GrantFiled: January 12, 1994Date of Patent: February 14, 1995Assignee: Adir Et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
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Patent number: 5385930Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.Type: GrantFiled: January 14, 1994Date of Patent: January 31, 1995Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
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Patent number: 5376681Abstract: A novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3 R.sup.4 and R.sup.5 are an optionally acylated hydroxyl optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial schleosis, hepatopathy, cerebrovascular diseases and the like.Type: GrantFiled: October 30, 1991Date of Patent: December 27, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Shigenori Ohkawa, Takayuki Doi
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Patent number: 5338735Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.Type: GrantFiled: August 12, 1993Date of Patent: August 16, 1994Assignee: Lilly Industries LimitedInventors: John Fairhurst, David E. Tupper
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Patent number: 5334715Abstract: Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: February 1, 1993Date of Patent: August 2, 1994Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Nicholas J. Hrib, Joseph Perez, John G. Jurcak
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Patent number: 5332743Abstract: Compounds of the general formula I: ##STR1## are disclosed as potent antipsychotic agents. Novel methods of use and intermediates used to make the compounds of formula I are also disclosed.Type: GrantFiled: June 12, 1992Date of Patent: July 26, 1994Assignee: McNeilab, Inc.Inventors: Ellen W. Baxter, Allen B. Reitz
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Patent number: 5322943Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: August 26, 1991Date of Patent: June 21, 1994Assignee: The Upjohn CompanyInventors: John M. McCall, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5317020Abstract: Aromatic amine derivatives of the general formula (I) ##STR1## or salts of the derivatives with mineral or organic acids are useful as neurokinin receptor antagonists.Type: GrantFiled: November 5, 1990Date of Patent: May 31, 1994Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5314889Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).Type: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
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Patent number: 5300522Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen. acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.5 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: August 18, 1992Date of Patent: April 5, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5283246Abstract: The compounds are substituted trimetazidine useful for the treatment of ischaemic pathologies and peripheral vascular pathology.A compound disclosed is 4-(2,3,4-trimethoxybenzyl)-1-[3-(4-hydroxy-2,3,5-trimethylphenoxy)propyl]p iperazine.Type: GrantFiled: September 17, 1992Date of Patent: February 1, 1994Assignee: Adir et CompagnieInventors: Gilbert Regnier, Jean-Paul Vilaine, Nicole Villeneuve, Jean-Pierre Bidouard, Jean-Pierre Iliou, Albert Lenaers
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Patent number: 5280024Abstract: Compounds of the general formula (I): ##STR1## in which R represents: a hydrogen atom, ora radical --OR'in which R' is as defined in the description.Type: GrantFiled: March 25, 1993Date of Patent: January 18, 1994Assignee: Adir et CompagnieInventors: Yves Bolland, Guy Lewin, Jean-Paul Vilaine, Lenaers Albert, Catherine Thollon
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Patent number: 5278174Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.Type: GrantFiled: May 17, 1991Date of Patent: January 11, 1994Assignee: Scios Nova, Inc.Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
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Patent number: 5276168Abstract: A new method for the treatment of ischemic conditions and arrhythmia is disclosed. The method uses compounds of the formula ##STR1## wherein A can be --CH.sub.2 --, --O--, --NR.sub.9 --, --S--, --SO--, --SO.sub.2 --; X can be oxygen or sulfur; Y can be --NR.sub.8, --O--, --S--, --CH.sub.2 -- and the R groups are as defined herein. Novel compounds within the definition of formula I are also disclosed.Type: GrantFiled: June 19, 1992Date of Patent: January 4, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5270312Abstract: Substituted piperazines and derivatives of Formula I ##STR1## are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: October 24, 1991Date of Patent: December 14, 1993Assignee: Warner-Lambert CompanyInventors: Shelly Glase, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
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Patent number: 5268477Abstract: The claimed invention is to triazin-2-yl and triazin-3-yl piperazines which are useful intermediates in the preparation of amino substituted steroid (XI) which are useful pharmaceutical agents.Type: GrantFiled: November 19, 1992Date of Patent: December 7, 1993Assignee: The Upjohn CompanyInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
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Patent number: RE35053Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: October 9, 1992Date of Patent: October 10, 1995Assignee: The Upjohn CompanyInventors: John M. McCall, E. Jon Jacobsen