Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Patent number: 5849921Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo?1,2-a!pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-?(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydroimidazo?1,2-a!pyridin-2-yl)-ben zimidazol-1-yl)-methyl!-biphenyl-2-carboxylic acid.Type: GrantFiled: June 2, 1995Date of Patent: December 15, 1998Assignee: Astra AktiebolagInventors: Robin Bernad Boar, Alan John Cross, Duncan Alastair Gray, Richard Alfred Green
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Patent number: 5847135Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: May 25, 1995Date of Patent: December 8, 1998Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
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Patent number: 5846988Abstract: Compounds useful as cytoprotective agents are disclosed. The compounds possess dual activity, containing a phenolic portion selected to have antioxidant or free radical scavenging properties and a thiazolidine-4-carboxylate portion selected for its potential to act as a cysteine prodrug.Type: GrantFiled: October 20, 1997Date of Patent: December 8, 1998Assignee: Alcon Laboratories, Inc.Inventor: Mark R. Hellberg
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Patent number: 5840739Abstract: Thiazoline acids and derivatives useful as chelators of trivalent metals in therapeutic applications have been prepared.Type: GrantFiled: March 29, 1996Date of Patent: November 24, 1998Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5837721Abstract: The disclosed invention is thifluzamide with an altered crystalline form, prepared by heat-melting and then cooling, and agricultural chemical compositions comprising such a thifluzamide as its effective ingredient.Type: GrantFiled: February 20, 1997Date of Patent: November 17, 1998Assignee: Rohm and Haas CompanyInventors: Norihito Hayakawa, Masatoshi Baba, Norihiro Suwa, Kazuhiro Yamagishi
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5827860Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Michael J. Costanzo, Bruce E. Maryanoff
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Patent number: 5827866Abstract: Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Michael J. Costanzo, Bruce E. Maryanoff
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Patent number: 5827859Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Siegfried Heinz Reich, Michael J. Rodriguez, John H. Tatlock
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Patent number: 5824688Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez
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Patent number: 5821250Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: October 13, 1998Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 5786515Abstract: A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.Type: GrantFiled: August 30, 1996Date of Patent: July 28, 1998Assignee: Merck & Co., Inc.Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
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Patent number: 5780638Abstract: 5-Hydroxymethylthiazole is prepared in an improved manner by reducing 5-formylthiazole using a borane compound. Particularly advantageous in this case is the use of 5-formylthiazole which has been obtained by reaction of a 2-halomalonaldehyde compound with thioformamide in the presence of less than 5% by weight of water (based on the reaction mixture).Type: GrantFiled: December 9, 1996Date of Patent: July 14, 1998Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Helmut Fiege
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Patent number: 5773455Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by one of the two following formulas: ##STR1## Each of the R groups is defined in the disclosure.Type: GrantFiled: June 28, 1996Date of Patent: June 30, 1998Assignee: Biomeasure, IncorporatedInventors: Zheng Xin Dong, Sun H. Kim
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Patent number: 5756534Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds of the formula: ##STR1## such as 3-isoquinolinecarboxamide,N-(,1-dimethylethyl)decahydro-2-?2-hydroxy-3-??2 -methyl-3-(methysulfonyl)-1-oxopropyl!amino!-4-phenylbutyl!-, ?3S-?2?2S*,3R*(R*)!,3.alpha.,4a.beta., 8 a.beta.!!- are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 31, 1995Date of Patent: May 26, 1998Assignee: Monsanto CompanyInventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
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Patent number: 5750543Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: May 12, 1998Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 5750706Abstract: The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.Type: GrantFiled: September 3, 1996Date of Patent: May 12, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Isabelle Huber, Fernand Schneider, Josef Stadlwieser, Sven Taylor
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Patent number: 5747518Abstract: The substituted thiophene derivative of the invention which is represented by the general formula (1) has a broad disease spectrum for a pathogenic fungus of various crops, exhibits an excellent controlling effect on disease such as gray mold, powdery mildew and rust in particular, and is also effective for a resistant fungus of conventional fungicides which has become a serious problem, and consequently is useful for an agricultural and horticultural fungicide.Type: GrantFiled: April 3, 1996Date of Patent: May 5, 1998Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Yukihiro Yoshikawa, Kanji Tomiya, Hiroyuki Katsuta, Hideo Kawashima, Osamu Takahashi, Shunichi Inami, Yuji Yanase, Junro Kishi, Hitoshi Shimotori, Naofumi Tomura
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Patent number: 5733882Abstract: The present invention provides compounds, more particularly dipeptide analogs, which bind to retroviral proteases. These compounds are inhibitors of retroviral proteases and are useful for treating diseases related to infection by retroviruses.Type: GrantFiled: February 28, 1995Date of Patent: March 31, 1998Assignee: SmithKline Beecham CorporationInventors: Thomas Joseph Carr, Peter Lawrence DeMarsh, Geoffrey Bainbridge Dreyer, Ashley Edward Fenwick
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Patent number: 5693310Abstract: Compounds of general Formula I ##STR1## wherein R.sup.3 is a saturated, unsaturated, straight- or branched-chain or cyclic aliphatic hydrocarbon residue of up to 16 carbon atoms or, if R.sup.4 is a hydrogen atom, a cycloalkyl group or an aryl or aralkyl group optionally substituted by one or several C.sub.1 -C.sub.6 -dialkylamino groups or by one or several C.sub.1 -C.sub.6 -alkoxy groups,R.sup.4 is a hydrogen atom, a saturated, unsaturated, straight- or branched-chain or cyclic hydrocarbon residue of up to 16 carbon atoms, orR.sup.3 and R.sup.4 jointly mean a saturated or unsaturated 5- or 6-membered ring optionally substituted or containing an O, S, N atom or oxo substituent, and Y is COOX or CONR.sub.3 R.sub.4,are valuable complexing agents, complexes or complex salts, e.g., for use as NMR or X-ray diagnostic image-enhancement agents or radioactive diagnostic agents.Type: GrantFiled: November 19, 1990Date of Patent: December 2, 1997Assignee: Schering AktiengesellschaftInventors: Heinz Gries, Bernd Raduechel, Hans-Joachim Weinmann, Wolfgang Muetzel, Ulrich Speck
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Patent number: 5691366Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5691359Abstract: Heterocyclylcarbonyl substituted benzofuranyl- and thiophenyl-alkanecarboxylic acid derivatives are prepared by reacting appropriately substituted hydroxybenzene butanoic acid esters with heterocyclic ketones. The inventive compounds can be used for the preparation of medicaments, particularly of medicaments for the treatment and prevention of acute and chronic inflammatory processes.Type: GrantFiled: May 23, 1995Date of Patent: November 25, 1997Assignee: Bayer AktiengesellschaftInventors: Rudiger Fischer, Gabriele Braunlich, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Mary F. Fitzgerald
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Patent number: 5686622Abstract: Thiazolidine derivatives of formula (I), in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification. The invention also concerns the salts of these derivatives, the preparation thereof and drugs containing same.Type: GrantFiled: December 19, 1996Date of Patent: November 11, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Marc Capet, Marie-Christine Dubroeucq, Claude Guyon, Franco Manfre
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Patent number: 5686435Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.Type: GrantFiled: December 7, 1995Date of Patent: November 11, 1997Assignee: Research Institute for Medicine and ChemistryInventors: Robert Henry Hesse, Gaddam Subba Reddy, Sundara Katugam Srinivasasetty Setty
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Patent number: 5684198Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.Type: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5684002Abstract: A compound having the structure: ##STR1## wherein (a) W is --C(X')--NRR' or --NR--C(X')R';(b) X and X' are independently O or S;(c) each Y is independently hydrogen or straight, branched or cyclic alkanyl having from 1 to about 3 carbon atoms, or the two Y's are bonded to form an alkanyl ring having from 3 to about 7 carbon atoms;(d) Z is unsubstituted branched or cyclic alkyl, or unsubstituted or alkanyl-substituted phenyl or benzyl, Z having from 3 to about 10 atoms other than hydrogen;(e) R and R' are each independently selected from hydrogen, hydroxy straight, branched or substituted alkyl having from 1 to about 6 carbon atoms, and cyclic alkyl having from 3 to about 7 carbon atoms; unsubstituted or substituted aryl, heteroaryl or heterocyclic groups; or R and R' are bonded together to form a ring having from from 3 to about 8 atoms wherein about 1 to about 4 atoms may be heteroatoms;pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: June 7, 1995Date of Patent: November 4, 1997Assignee: The Procter & Gamble CompanyInventors: Michael Wiard Scherz, John Michael Janusz
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Patent number: 5677320Abstract: Compounds of Formula 1 ##STR1## wherein the symbols are as defined in the specification, have retinoid like biological activity.Type: GrantFiled: January 9, 1997Date of Patent: October 14, 1997Assignee: AllerganInventor: Roshantha A. Chandraratna
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Patent number: 5675024Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: November 22, 1995Date of Patent: October 7, 1997Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5663200Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.Type: GrantFiled: October 19, 1995Date of Patent: September 2, 1997Assignee: Ciba-Geigy CorporationInventors: Guido Bold, Hans-Georg Capraro, Alexander Fassler, Marc Lang, Shripad Subray Bhagwat, Satish Chandra Khanna, Janis Karlis Lazdins, Jurgen Mestan
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Patent number: 5661167Abstract: The present invention relates to compounds of formula 1, ##STR1## including all of its stereoisomers, compositions, and processes for preparation of the same. The compounds of the present invention are also useful in their pharmacological activities as they directly act as inhibitors of prolyl endopeptidase and thereby provide a methods for memory enhancement, preventing or slowing the affects of amnesia or memory deficits.Type: GrantFiled: December 2, 1996Date of Patent: August 26, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Norton P. Peet, Shujaath Mehdi, Joseph P. Burkhart
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Patent number: 5656637Abstract: A novel thiazole derivative represented by general formula (I), which has a selected agonistic activity for 5-HT.sub.3 receptor, a pharmaceutical composition thereof, and a process for producing the same. In the said formula, R.sup.1 represents hydrogen or lower alkoxy; R.sup.2 and R.sup.3 are such that R.sup.2 represents hydrogen and R.sup.3 represents a group, --Y--Het, wherein Y represents a single bond or lower alkylene and Het represents a nitrogenous heterocyclic group, or alternatively R.sup.2 and R.sup.3 are combined together to form a group, --(CH.sub.2).sub.m --NR.sup.4 --(CH.sub.2).sub.n --, wherein m and n are each 1 or 2 and R.sup.4 represents lower alkyl; and X represents --NH--, --NHC(.dbd.O)NH--, --C(.dbd.O)NH-- or --NHC(.dbd.O)--.Type: GrantFiled: November 3, 1994Date of Patent: August 12, 1997Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Mitsuaki Ohta, Isao Yanagisawa, Keiji Miyata
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Patent number: 5656657Abstract: 3-amino-5-carbonylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.Type: GrantFiled: May 30, 1995Date of Patent: August 12, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5639772Abstract: 3-amino-5-aryl- and 5-heteroarylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.Type: GrantFiled: May 30, 1995Date of Patent: June 17, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5637602Abstract: This invention relates to a compound of formula (I), their salts, the preparation thereof and drugs containing same. The compounds of formula (I) have interesting pharmacological properties. Said compounds have a high affinity for chloecystokinin (CCK) and gastrin receptors and are therefore useful in the treatment and prevention of CCK and gastrin-related disorders affecting the nervous system and gastrointestinal tract.Type: GrantFiled: June 7, 1995Date of Patent: June 10, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Marc Capet, Marie-Christine Dubroeucq, Franco Manfre, Jean-Paul Martin
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Patent number: 5633270Abstract: Derivatives of formula (I), their salts, the preparation of said derivatives and drugs containing same. The compounds of formula (I) have interesting pharmacological properties.Type: GrantFiled: June 6, 1995Date of Patent: May 27, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Marie-Christine Dubroeucq, Franco Manfre
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Patent number: 5633375Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.Type: GrantFiled: June 7, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
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Patent number: 5614520Abstract: Pharmaceutical compositions for treating gout or hyperuricemia and containing a new categorized compound, i.e. 2-arylthiazole derivatives, as an active ingredient, are provided. The 2-arylthiazole derivatives in the present invention are represented by the following formula (I): ##STR1## wherein Ar is an unsubstituted or substituted pyridyl, thienyl, furyl, naphthyl or phenyl group;X is a hydrogen atom, alkyl group or carboxyl group which may be protected, andY is a hydrogen atom, alkyl group, or a hydroxyl or carbonyl group which may be protected.Furthermore, novel compounds included in the 2-arylthiazole derivatives and pharmaceutically acceptable salts thereof are provided.Type: GrantFiled: January 30, 1995Date of Patent: March 25, 1997Assignee: Teijin LimitedInventors: Shiro Kondo, Hisashi Fukushima, Masaichi Hasegawa, Masahiro Tsuchimoto, Ikuo Nagata, Yoshio Osada, Keiji Komoriya, Hisao Yamaguchi
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Patent number: 5610144Abstract: This invention relates to compositions of formula: ##STR1## and their salts, their preparation and the medicaments containing them.Type: GrantFiled: June 27, 1994Date of Patent: March 11, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Marc Capet, Claude Cotrel, Claude Guyon, Michel Joannic, Franco Manfre, G erard Roussel, Marie-Christine Dubroeuco, Michel Cheve, Gilles Dutruc-Rosset
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Patent number: 5608062Abstract: A process is described for preparing trifluoromethyl ketones of the formula I ##STR1## where R has the given meanings, wherein an alcohol of the formula II ##STR2## is reacted with a compound of the formula IVYO.sub.n H (IV)where n has the given meaning.Type: GrantFiled: September 21, 1994Date of Patent: March 4, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Uwe D oller, Bernd Scharbert, Laurent Weisse
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Patent number: 5591758Abstract: Organic nitrates, processes for their preparation and their use in the treatment of vascular diseases and in particular in the treatment of angina.The said nitrates correspond to the following formula I:R--CO--(A).sub.n --Y--B (I)in which:R represents, in particular, a sulphur-containing radical and a sulphur-containing amino acid residue; A represents, in particular, a CH.sub.2 group or a substituted amino acid; n is 0 or 1 or greater than 1; Y represents an oxygen atom or an NH group and B represents, in particular, a 1,4:3,6-dianhydro hexitol mononitrate radical, an itol nitrate radical or an inositol radical.The said organic nitrates are prepared by reacting:I. either a thio acid of the type R--COOH, in which R has the same meaning as above, with a derivative of formula II: (A).sub.n --Y--B, in which A, Y, B and n have the same meaning as above,II. or a derivative of formula III: R--CO--(A).sub.Type: GrantFiled: May 4, 1993Date of Patent: January 7, 1997Assignee: Laboratoires Hoechst, SAInventors: Jean-Pierre Nallet, Jacques Dreux, Alain Berdeaux, Vincent Richard, Piero Martorana, Helmut Bohn
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Patent number: 5585486Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is (CR.sub.5 R.sub.6).sub.n, (CR.sub.5 R.sub.6).sub.n,-aryl, (CR.sub.5 R.sub.6).sub.n -heteroaryl, X-(CR.sub.5 R.sub.6).sub.n, X-(CR.sub.5 R.sub.6).sub.n -aryl or X-(CR.sub.5 R.sub.6).sub.n -heteroaryl wherein aryl and heteroaryl may be optionally substituted;X is 0 or NR.sub.5 ;R.sub.5 and R.sub.6 are independently H or lower alkyl;R.sub.2 is H, halo, lower alkyl or (CR.sub.5 R.sub.6).sub.n -aryl;R.sub.3 and R.sub.4 are independently H or alkyl;A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine;Z is CH.sub.2 or O; andn is 0-4;pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta.Type: GrantFiled: May 12, 1995Date of Patent: December 17, 1996Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Todd L. Graybill, Gary J. Speier, Catherine P. Prouty, Stanley J. Schmidt
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Patent number: 5580999Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, -N(alkoxycarbonyl)-,-N(acyl)- or --S--or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: May 12, 1995Date of Patent: December 3, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5571920Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: January 26, 1996Date of Patent: November 5, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5567671Abstract: The present invention relates to 1-H-3-phenyl-5-cyloalkylpyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents optionally substituted cycloalkyl andB represents hydrogen or optionally substituted alkyl,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## These compounds possess herbicidal and pesticidal activity.Type: GrantFiled: February 22, 1994Date of Patent: October 22, 1996Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Ulrike Wachendorff-Neumann
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Patent number: 5554581Abstract: The present invention relates to 3,4,5,6-tetrahydrophthalamide derivatives and 3,4,5,6-tetrahydroisophthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof.More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetrahydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): ##STR1## These tetrahydrophthalamide derivatives and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment.Type: GrantFiled: May 25, 1995Date of Patent: September 10, 1996Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.Inventors: Kenji Hirai, Tomoko Matsukawa, Tomoyuki Yano, Emiko Ejiri, Kiyomi Aizawa, Koichi Shikakura, Tomoko Yoshii, Sadayuki Ugai, Osamu Yamada, Shigeki Kishi
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Patent number: 5550248Abstract: Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: C.sub.m H.sub.p is an alkylene chain wherein m is 0, 1, 2, or 3 and p=(2.times.m)-1, except that when m is 0, p is also 0;n is 0, 1, 2 or 3;R is CO.sub.2 R', CH.sub.2 OH, CONHSO.sub.2 R.sup.3, CONHR.sup.4, or --CH.sub.2 --5--tetrazolyl;R' is hydrogen, alkyl, or alkali metal;X is O or NH;Y is --O--, a single bond or vinylene, except that Y cannot be --O-- when n is 0;and the remaining symbols are as defined in the specification.Type: GrantFiled: November 29, 1990Date of Patent: August 27, 1996Assignee: E.R. Squibb & Sons, Inc.Inventor: Raj N. Misra
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Patent number: 5547978Abstract: The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,R.sup.2 represents a heterocyclic compound selected from the group consisting of 2-thiazole, 2-oxazole, 2-imidazole, 2-pyrrole, 2-thiophene, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 2-indole, 2-thiazolo[5,4-b]pyridine, 2-oxazolo[4,5-b]pyridine, 2-imidazo[4,5-b]pyridine, 5-thiazole, 2-thiazoline, 2-pyridine, 3-pyridine, 5-pyrimidine, 2-pyrazine, 2-triazole or 2-pyrazole wherein the heterocyclic compound may be unsubstituted or substituted independently with R.sup.4 or R.sup.5 wherein R.sup.4 and R.sup.5 are H, C.sub.1-5 alkyl, aryl or R.sup.4 and R.sup.Type: GrantFiled: November 23, 1994Date of Patent: August 20, 1996Assignee: Meiji Seika Kaisha, Ltd.Inventors: Burton G. Christensen, Takashi Egawa, Yasuyuki Ichimaru, Shokichi Ohuchi, Tsuneo Okonogi, Arthur A. Patchett, Seiji Shibahara, Seiji Tsutsumni
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Patent number: 5536723Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: October 6, 1994Date of Patent: July 16, 1996Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5536737Abstract: Compounds of the formula ##STR1## wherein R is a hydrogen atom or an acyl; U is --O--, --CHR.sup.1 -- or --NR.sup.2 -- wherein R.sup.1 is a hydrogen atom or a hetero ring, and R.sup.2 is a hydrogen atom or a lower alkoxycarbonyl lower alkyl; V is --O--, --S--, --CHR.sup.3 -- or --NR.sup.4 -- wherein R.sup.3 is a hydrogen atom or a lower alkoxycarbonyl, and R.sup.4 is a hydrogen atom, a lower alkyl or an acyl; W is methyl, a hetero ring or optionally substituted phenyl; X and Y are the same or different and each is --CH.sub.2 -- or --S--; m is an integer of 0 to 6; and n is an integer of 1 to 4, and pharmaceutically acceptable salts thereof.The compounds of the present invention have specifically strong inhibitory activity against prolyl endopeptidase, and suppress decomposition and inactivation of TRH, substance P, neurotensin, vasopressin and the like. Accordingly, the compounds can be used for the prophylaxis and/or treatment of dementia and amnesia including Alzheimer's disease.Type: GrantFiled: May 24, 1995Date of Patent: July 16, 1996Assignee: Japan Tobacco Inc.Inventors: Koji Kobayashi, Minoru Akamatsu, Shinji Yata, Hiroyuki Abe, Katsuo Toide, Motohiro Kogayu, Itsuo Uchida
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Patent number: 5527829Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: May 23, 1994Date of Patent: June 18, 1996Assignee: Agouron Pharmaceuticals, Inc.Inventor: Vincent J. Kalish