Chalcogen Bonded Directly To The Tricyclo-carbocyclic Ring System Patents (Class 546/204)
-
Patent number: 6288123Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: September 11, 2001Assignee: Cambridge NeuroSciences, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
-
Patent number: 6239148Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: April 6, 1998Date of Patent: May 29, 2001Assignee: Novo Nordisk A/SInventors: Florenzio Zaragossa Dörwald, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh Jørgensen, Uffe Bang Olsen, Henrik Sune Andersen, Svend Treppendahl, Polivka Zdenék, Silhánková Alexandra, Sindelár Karel
-
Patent number: 6174924Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: January 16, 2001Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
-
Patent number: 6172085Abstract: A compound of the formula: wherein R1 and R2 each represents hydrogen, lower alkyl which may be substituted or acyl; R3, R4 and R5 each represents lower alkyl which may be substituted or lower alkoxy which may be substituted or R4 and R5 taken together represent a 5- or 6-membered carbocyclic group; R6 represents lower alkyl; Ar represents an aromatic group which may be substituted; ring A represents a 5- to 8-membered nitrogen-containing heterocyclic ring which may be substituted; X represents lower alkylene which may be substituted; Y represents carbon or nitrogen; Za represents CH2, COCH2, OCH2, SCH2, NHCH2, etc.; Zb represents a bond or a divalent aliphatic hydrocarbon group which may be substituted and may contain O, N or S; and m represents an integer of 1 to 3, or a salt thereof is useful for a pharmaceutical composition for modulating sodium channel.Type: GrantFiled: February 8, 1999Date of Patent: January 9, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Tadatoshi Hashimoto, Kohji Fukatsu
-
Patent number: 6143791Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 7, 1995Date of Patent: November 7, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Hu Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
-
Patent number: 6140338Abstract: The present invention relates to a compound of the general formula: ##STR1## wherein each of R.sup.1 and R.sup.2 which may be the same or different, is e.g. a hydrogen atom, a halogen atom or a lower alkyl group, X is an oxygen atom, a sulfur atom or CH, Y is CH or a nitrogen atom, and A is e.g. a 1-substituted-4-piperidinyl group, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable anion-exchange product thereof or a hydrate thereof. The compounds of the present invention have chemokine receptor antagonism, and thus they are useful as treating agents for various diseases relating to chemokine, such as acute inflammatory diseases, chronic inflammatory diseases, acquired immune deficiency syndrome, cancer, ischemic reflow disorder and/or arteriosclerosis.Type: GrantFiled: January 29, 1999Date of Patent: October 31, 2000Assignee: Banyu Pharmaceutical, Co., Ltd.Inventors: Akira Naya, Yufu Owada, Toshihiko Saeki, Kenji Ohwaki, Yoshikazu Iwasawa
-
Patent number: 6121281Abstract: Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is vinyl or ethyl; and R.sup.2 is a group R.sup.3, R.sup.4 CH.sub.2 --, or R.sup.5 R.sup.6 C.dbd.CH--; wherein each of R.sup.3 and R.sup.4 is an azabicyclic ring system or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.Type: GrantFiled: January 29, 1999Date of Patent: September 19, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Andrew Kenneth Takle, Eric Hunt, Antoinette Naylor
-
Patent number: 6100253Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: August 17, 1999Date of Patent: August 8, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
-
Patent number: 6040318Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: June 17, 1998Date of Patent: March 21, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
-
Patent number: 6015900Abstract: Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents; A is an optionally substituted alkylene; R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents; R.sub.5 is hydrogen or lower alkyl; R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members; Z is nitrogen or carbon; and W is optionally susbtituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: November 23, 1998Date of Patent: January 18, 2000Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
-
Patent number: 6004959Abstract: The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).Type: GrantFiled: April 18, 1997Date of Patent: December 21, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Winton D. Jones, Fred L. Ciske, Robert J. Dinerstein, Keith A. Diekema
-
Patent number: 5968954Abstract: New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are as defined in the description, in the form of a racemic mixture and in the form of optical isomers, and physiologically-tolerable acid addition salts thereof. The products of the invention are useful as medicaments and exhibit selective binding affinity for the 5HT.sub.1B receptors.Type: GrantFiled: February 26, 1998Date of Patent: October 19, 1999Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert
-
Patent number: 5955632Abstract: New seco-D steroid derivatives, processes for their preparation and pharmaceutical compositions are provided, which are active on the cardiovascular system.Type: GrantFiled: July 10, 1997Date of Patent: September 21, 1999Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Mauro Gobbini, Sergio De Munari, Giorgio Fedrizzi, Patrizia Ferrari, Piero Melloni, Marco Santagostino, Marco Torri
-
Patent number: 5935951Abstract: The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of ##STR1## formula (I), in which R.sub.1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; R.sub.2 is cycloalkyl or a phenyl or naphthyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; R.sub.3 and R.sub.4 together are lower alkylene or aza-, oxa- or thia-lower alkylene; or R.sub.3 is lower alkyl, lower alkoxy-lower alky, di-lower alkylamino-lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); and R.sub.4 is hydrogen, lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); R.sub.Type: GrantFiled: March 5, 1997Date of Patent: August 10, 1999Assignee: Novartis Finance CorporationInventors: Silvio Ofner, Siem Jacob Veenstra
-
Patent number: 5932734Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: August 7, 1997Date of Patent: August 3, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
-
Patent number: 5922879Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy; --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1 R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.Type: GrantFiled: December 22, 1997Date of Patent: July 13, 1999Assignee: Neurogen CorporationInventors: Xi Chen, Jan William Francis Wasley
-
Patent number: 5883257Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: December 19, 1997Date of Patent: March 16, 1999Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
-
Patent number: 5834459Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O);Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which D4 receptor stimulation is implicated, such as schizophrenia, is also described.Type: GrantFiled: April 1, 1996Date of Patent: November 10, 1998Assignee: Allelix Biopharmaceuticals Inc.Inventor: Jian-Min Fu
-
Patent number: 5739135Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.Type: GrantFiled: June 6, 1995Date of Patent: April 14, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino
-
Patent number: 5716949Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 28, 1996Date of Patent: February 10, 1998Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen
-
Patent number: 5712292Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: October 18, 1995Date of Patent: January 27, 1998Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
-
Patent number: 5693649Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: October 18, 1995Date of Patent: December 2, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
-
Patent number: 5688788Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 18, 1995Date of Patent: November 18, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
-
Patent number: 5686586Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis.In the formula, X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.Type: GrantFiled: October 4, 1996Date of Patent: November 11, 1997Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
-
Patent number: 5668129Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 27, 1996Date of Patent: September 16, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
-
Patent number: 5659033Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl.Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: September 13, 1995Date of Patent: August 19, 1997Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
-
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
-
Patent number: 5523387Abstract: This invention relates to dyes in salt form which are useful for mass dyeing of synthetic polymers. In particular, this invention relates to ammonium or immonium salt-containing dyes that display good polymer affinity, and the methods for using those dyes to color polymeric substrates.Type: GrantFiled: June 14, 1994Date of Patent: June 4, 1996Assignee: Sandoz Ltd.Inventors: Jurgen Goldmann, Bansi L. Kaul
-
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
-
Patent number: 5436243Abstract: Potentiating agents inhibit the development of multidrug resistance, reduce drug-resistance in drug-resistant tumors, or sensitize tumors to antineoplastic drugs, thereby potentiating the effect of antineoplastic agents. The potentiating agents are aminoanthraquinones, preferably 1,4-bis(N-substituted) amino anthraquinones, and pharmaceutically acceptable salts thereof.Type: GrantFiled: November 17, 1993Date of Patent: July 25, 1995Assignees: Research Triangle Institute Duke University, Pharmaceuticals CorporationInventors: Clifford W. Sachs, Robert L. Fine, Lawrence M Ballas, R. Ivy Carroll, Robert Bell
-
Patent number: 5428043Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: October 29, 1992Date of Patent: June 27, 1995Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
-
Patent number: 5424318Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes anthraquinone, X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR5## (in all the above formulas, n is an integer of 1 through 7 and R.sup.3 represents a lower alkyl group or a benzyl group), a group of the formula ##STR6## a group of the formula ##STR7## a group of the formula --O--CH.sub.2 CH.sub.2 CH.dbd.Type: GrantFiled: January 5, 1994Date of Patent: June 13, 1995Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
-
Patent number: 5418235Abstract: Aminoalkyl-substituted 5-mercaptothiazoles of the formula ##STR1## where R.sup.1, n and A have the meanings stated in the description, and the preparation thereof are described.The compounds are suitable for controlling diseases.Type: GrantFiled: December 13, 1993Date of Patent: May 23, 1995Assignee: BASF AktiengesellschaftInventors: Beatrice Rendenbach-Mueller, Liliane Unger, Hans-Juergen Teschendorf
-
Patent number: 5393890Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.Type: GrantFiled: July 1, 1994Date of Patent: February 28, 1995Assignee: Ajinomoto Co., Inc.Inventors: Masataka Syoji, Kozo Toyota, Chikahiko Eguchi, Ryoto Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura
-
Patent number: 5348965Abstract: The invention relates to therapeutically active azaheterocyclic compounds and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.Type: GrantFiled: May 14, 1992Date of Patent: September 20, 1994Assignee: Novo Nordisk A/SInventors: Knud E. Andersen, Lars J. S. Knutsen, Per O. Sorensen, Behrend F. Lundt, Jesper Lau, Hans Petersen
-
Patent number: 5344835Abstract: According to the invention there is provided a compound of formula (I): R.sup.1 --O(CH.sub.2).sub.m A(CH.sub.2).sub.n XR or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is a group of formula (a or b) where Z is --(CH.sub.2).sub.2-, --CH.dbd.CH--, --CH.sub.2 --S-- or --CH.sub.2 --O--; R is a group of formula (c, d or Het) and A is a group of formula (e, f or g) in which the N atom is attached to the group (CH.sub.2)n; m is 1 or 2; n is an integer of from 1 to 4; p is 1, 2 or 3; R.sup.2 and R.sup.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy-(C.sub.1 -C.sub.4 alkyl), hydroxy, C.sub.1 -C.sub.4 alkoxy, halo, trifluoromethyl, nitro, cyano, sulphamoyl, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), carboxy, --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), --CH.sub.2).sub.q CONR.sup.4 R.sup.5, -- (CH.sub.2).sub.q OCONR.sup.4 R.sup.5, --CH.sub.2).sub.q NR.sup.6 R.sup.7 or --NHSO.sub.2 NH.sub.2 in which R.sup.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.Type: GrantFiled: July 2, 1992Date of Patent: September 6, 1994Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross
-
Patent number: 5302602Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: May 18, 1992Date of Patent: April 12, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
-
Patent number: 5276053Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
-
Patent number: 5250681Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.Type: GrantFiled: February 15, 1991Date of Patent: October 5, 1993Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura
-
Patent number: 5237059Abstract: A compound capable of generating an acid by light irradiation selected from the group consisting of oxime sulfonic acid esters of formula (I): ##STR1## wherein R.sup.1 is an alkyl group, each of R.sup.2 and R.sup.3 is selected from the group consisting of a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group and a cyano group, and R.sup.2 and R.sup.3 may optionally combine to form a ring; and N-hydroxyimidesulfonic acid esters of formula (II): ##STR2## wherein R.sup.1 is an alkyl group, and A is a group selected from the group consisting of a substituted or unsubstituted arylene group, a substituted or unsubstituted alkylene group and a substituted or unsubstituted alkenylene group, wherein the compound capable of generating an acid by light irradiation is useful as an image-forming materials, etc. and has high reactivity to light of from the near ultraviolet region to the visible region.Type: GrantFiled: March 20, 1992Date of Patent: August 17, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Kan Wakamatsu, Yuichi Wakata
-
Patent number: 5189065Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.Type: GrantFiled: October 17, 1991Date of Patent: February 23, 1993Assignee: Roussel UclafInventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
-
Patent number: 5180736Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
-
Cyclophanes, pharmaceutical compositions containing these compounds and processes for preparing them
Patent number: 5147882Abstract: Cyclophanes of the general formula ##STR1## wherein X.sub.1, X.sub.2, A, R and R.sub.1 to R.sub.4 are as defined herein, the enantiomers, diastereomers and addition salts thereof and, more particularly, for pharmaceutical use, the physiologically acceptable addition salts thereof, which have pharmacological properties such as lowering blood pressure, dilating the coronary blood vessels and a mild heart rate lowering activity, pharmaceutical compositions which contain these compounds and processes for preparing them.Type: GrantFiled: March 28, 1991Date of Patent: September 15, 1992Assignee: Karl Thomae GmbHInventors: Manfred Psiorz, Volker Trach -
Patent number: 5143922Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 20, 1990Date of Patent: September 1, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
-
Patent number: 5132313Abstract: The present invention relates to novel NMDA receptor antagonists and methods for their use. The present invention also provided pharmaceutical compositions comprising such NMDA receptor antagonists.Type: GrantFiled: October 26, 1989Date of Patent: July 21, 1992Assignee: University of PittsburghInventors: Alan P. Kozikowski, Yuan-Ping Pang
-
Patent number: 5116958Abstract: Disperse dyes, which produce dyeings of excellent thermomigration fastness, consisting of a chromophore and a lactam or oxime radical which detaches on heating to leave an isocyanate or isothiocyanate group, which reacts with a suitable group in the environment. The disclosed dyes are described by the formula ##STR1## where F is the radical of a dye which is free of water-solubilizing groups,B is a bridge member or a direct bond,Z is O or S andV is the radical of a group H--V, where H--V is an oxime of the formula ##STR2## or a lactam of the formula ##STR3## in which R.sup.1 and R.sup.2 are each independently of the other substituted or unsubstituted alkyl or aryl, orR.sup.1 and R.sup.2 together with the carbon atom linking them form a cycloaliphatic ring,R is hydrogen or alkyl andn is an integer from 4 to 11.Type: GrantFiled: January 5, 1990Date of Patent: May 26, 1992Assignee: Ciba-Geigy CorporationInventors: Peter Liechti, Martin Trottmann
-
Patent number: 5106856Abstract: There are disclosed various compounds of the formula below, ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy or nitro;Y is hydrogen or loweralkoxy; or alternatively, X and Y combined together form the group --OCH.sub.2 O-- in which case the positions of X and Y on the benzene ring moiety must be adjacent to each other;and Z is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen or nitro;which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Type: GrantFiled: June 7, 1991Date of Patent: April 21, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
-
Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
-
Patent number: 5089505Abstract: A series of novel 1-(phenethyl) and 1-(1-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone. The most preferred compound is (3R)-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)piperidine. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: July 6, 1989Date of Patent: February 18, 1992Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Robert M. Wallis
-
Patent number: 5089506Abstract: Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl wherein each of R.sup.12 and R.sup.Type: GrantFiled: April 30, 1990Date of Patent: February 18, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng