Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/366)
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Patent number: 6127387Abstract: The application concerns a method of identifying compounds that can be used to inhibit undesired human CD4.sup.+ T cell immune responses by identifying compounds that block the interaction of CD4 and class II MHC gene products and a method of treatment which comprises administering such an identified compound. The compounds that inhibit undesired human CD4.sup.+ T cell immune responses can be used to treat disease such as multiple sclerosis and to prevent graft rejection and graft versus host disease. More specifically, the application concerns compounds having molecular weights between about 500 and 150 that bind to the GFCC'C" portion of the D1 domain of human CD4 lymphocyte cell surface antigen.Type: GrantFiled: December 9, 1997Date of Patent: October 3, 2000Assignee: Thomas Jefferson UniversityInventors: Ziwei Huang, Robert Korngold
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Patent number: 6124331Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: June 30, 1999Date of Patent: September 26, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, Wai C. Wong, Stewart A. Noble
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Patent number: 6124277Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 11, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 6107318Abstract: A compound of Formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein n is an integer between 2 and 6 and R.sub.1 is a methyl group or a group ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, methoxy, methylsulfonyl, or one of R.sub.2, R.sub.3 and R.sub.4 together with another one of the three substituents forms a --O--CH.sub.2 --O-- bridge. The asterisk marks an asymmetric carbon atom.Type: GrantFiled: December 6, 1999Date of Patent: August 22, 2000Assignee: Zambon Group S.p.A.Inventors: Felice Pocchiari, Claudio Masotto, Paolo Cavalleri, Stefania Montanari, Francesco Santangelo
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Patent number: 6090833Abstract: Polycyclic dihydrothiazoles, processes for their preparation, and their pharmaceutical uses are provided. Preferred compounds are represented by the formula I ##STR1## wherein the radicals may have various meanings. The compounds are particularly useful as anorectics.Type: GrantFiled: September 29, 1999Date of Patent: July 18, 2000Assignee: Aventis Pharma Deutschand GmbHInventors: Gerhard Jaehne, Heiner Glombik, Karl Geisen, Martin Bickel
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Patent number: 6080771Abstract: DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents CO(CR.sup.4A R.sup.4B).sub.n1 (O(CH.sub.2).sub.p1).sub.n2 OR.sup.5 {wherein n1 represents an integer of 1 or 2; R.sup.4A and R.sup.4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R.sup.Type: GrantFiled: August 13, 1998Date of Patent: June 27, 2000Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yutaka Kanda, Hitoshi Arai, Hiroyuki Yamaguchi, Tadashi Ashizawa, Shun-ichi Ikeda, Chikara Murakata, Tatsuya Tamaoki
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Patent number: 6066658Abstract: A compound represented by the formula: ##STR1## wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R.sup.1 represents an optionally substituted hydrocarbon group; R.sup.2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.Type: GrantFiled: February 19, 1999Date of Patent: May 23, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Tsuneo Oda, Masatoshi Hazama, Shigehisa Taketomi
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Patent number: 6057318Abstract: The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N;Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene;Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.Type: GrantFiled: May 20, 1998Date of Patent: May 2, 2000Assignee: SanofiInventors: Andre Bernat, Jean-Marc Herbert, Gerard Valette
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Patent number: 6040451Abstract: This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: June 30, 1999Date of Patent: March 21, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Yoon T. Jeon, Charles Gluchowski
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Patent number: 5990111Abstract: This invention relates to the use of aldose reductase inhibitors in the treatment, prevention or reversal of diabetic cardiomyopathy in a human subject.Type: GrantFiled: May 1, 1998Date of Patent: November 23, 1999Assignee: Pfizer Inc.Inventor: Brian F. Johnson
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Patent number: 5981558Abstract: DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4, or the like; R.sup.2 represents hydrogen or COR.sup.6 ; R.sup.3 represents --CH.sub.2 OCOR.sup.7, phthalimidomethyl, or the like; and W represents oxygen or NR.sup.8 (wherein R.sup.8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).Type: GrantFiled: August 13, 1998Date of Patent: November 9, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hitoshi Arai, Yutaka Kanda, Hiroyuki Yamaguchi, Tadashi Ashizawa, Chikara Murakata, Shun-ichi Ikeda, Tatsuya Tamaoki
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Patent number: 5955485Abstract: The present invention is concerned with the method of using a 2,3-dihydro-imidazo?2,1-b!benzothiazole derivative for the manufacture of a medicament for the therapeutic or prophylactic treatment of humans suffering from ageing of, or degenerative diseases of the nervous and vascular system which are associated with oxidative stress.Type: GrantFiled: August 12, 1997Date of Patent: September 21, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Joris De Brabander, Anne Simone Josephine Lesage, Josepha Eduarda Maria Francisca Leysen
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Patent number: 5955484Abstract: Plant-protecting active ingredient mixtures having synergistically enhanced action, wherein component I is a compound having plant-immunising action of formula I ##STR1## wherein Z is CN, COOH or a salt thereof, CO--OC.sub.1 -C.sub.4 alkyl or CO--SC.sub.1 -C.sub.4 alkyl;and wherein component II is a compound selected from the groupA) 4-?3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)acryloyl!morpholine ("dimethomorph");B) 5-methyl-1,2,4-triazolo?3,4-b!?1,3!benzothiazole ("tricyclazole"); andC) 3-allyloxy-1,2-benzothiazole-1,1-dioxide ("probenazole").Type: GrantFiled: April 28, 1998Date of Patent: September 21, 1999Assignee: Novartis Finance CorporationInventor: Wilhelm Ruess
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Patent number: 5952354Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.Type: GrantFiled: July 21, 1993Date of Patent: September 14, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
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Patent number: 5948804Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: September 5, 1997Date of Patent: September 7, 1999Assignee: Synaptic Pharmaceutical CorporationInventors: Yoon T. Jeon, Charles Gluchowski
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Patent number: 5925657Abstract: Disclosed herein are methods for reducing or preventing cytokine production associated with an inflammatory response, involving administering to a mammal a therapeutically-effective amount of a thiazolidinedione PPAR.gamma. agonist.Type: GrantFiled: June 18, 1997Date of Patent: July 20, 1999Assignee: The General Hospital CorporationInventors: Brian Seed, Chengyu Jiang
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Patent number: 5919799Abstract: An imidazothiazole compound having the formula (A): ##STR1## wherein R.sub.1 is a phenyl or napthyl which may have a substituent, R.sub.2 is an acyl, and the two bonds at dotted line portions may or may not exist simultaneously, or a pharmacologically acceptable salt thereof and an agent for overcoming resistance to an anti-neoplastic agent or an enhancer for the effect of an anti-neoplastic agent comprising said compound or a pharmacologically acceptable salt thereof as an active ingredient.Type: GrantFiled: September 9, 1997Date of Patent: July 6, 1999Assignee: Nikken Chemicals Co., Ltd.Inventors: Shigeyuki Tasaka, Akira Kiue
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Patent number: 5866595Abstract: According to the present invention, compounds selected from the thiozole class of organic molecules are employed as antagonists for receptor-operated ion channels (ROICs) useful in the treatment of a variety of disease states in which ROICs are implicated. ROICs of particular interest are receptor-operated calcium channels (ROCCs). Compounds of particular interest with respect to the subject invention are compounds of the thiazolidinedione class of organic molecules, more particularly ciglitazone. Disease states in which particular utility is expected include vasculoproliferative diseases such as atherosclerosis, restenosis following angioplasty, and other conditions in which PDGF is known to play a role. The utility of the present invention with respect to further studies on the operation of ROICs and ROCCs and their role in disease will be apparent to those of skill in the art.Type: GrantFiled: November 10, 1994Date of Patent: February 2, 1999Assignee: The Regents of The University of CaliforniaInventors: Harrihar A. Pershadsingh, Theodore W. Kurtz
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Patent number: 5861424Abstract: A pharmaceutical composition for treatment of cancer in a mammal comprising:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formulas (1) to (6) ##STR1## wherein X.sub.1 is O, S, Se, or >N--R.sub.14, ##STR2## X.sub.2 is O, S, Se, >N--R.sub.15, X.sub.3 is O, S, Se, ##STR3## X.sub.4 is >N--R.sub.19, or Y.sub.1 is O, S, Se, or >N--R.sub.18 ;Z.sub.1 represents an atomic group necessary to form a saturated or unsaturated 5- or 6-membered ring which may be substituted or may have another ring fused therewith;Z.sub.2 is a naphthalene ring, an anthracene ring or a phenanthrene ring which may be substituted; in combination with(B) a pharmaceutically acceptable carrier or diluent; and a method for treatment of cancer comprising administering the above pharmaceutical composition to a host afflicted with cancer.Type: GrantFiled: June 7, 1995Date of Patent: January 19, 1999Assignees: Dana Farber Cancer Institute, Fuji Photo Film Co., Ltd.Inventors: Lan Bo Chen, Tadao Shishido
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Patent number: 5852014Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: June 2, 1995Date of Patent: December 22, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5834499Abstract: A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms;one of L.sub.1 or L.sub.Type: GrantFiled: August 26, 1996Date of Patent: November 10, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Iwaoka, Hideki Anan, Naoki Imanishi, Kenichi Kazuta, Hiroyuki Koshio, Takeshi Suzuki, Hirotsune Itahana, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
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Patent number: 5705498Abstract: Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl;A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms;R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl;R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy;R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy,Y is O or NH, or CO--Y together are a heterocyclic bioisostere;Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; andR.sub.6 is hydrogen or C.Type: GrantFiled: May 4, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plc.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5705509Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5698574Abstract: The present invention relates to 5-membered heteroaryl-oxazolidinones, to processes for their preparation and to their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: July 17, 1995Date of Patent: December 16, 1997Assignee: Bayer AktiengesellschaftInventors: Bernd Riedl, Dieter Habich, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus Dieter Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
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Patent number: 5686459Abstract: Novel dioxopyrrolo-pyrrole derivatives of the formula ##STR1## as well as hydrates or solvates thereof, which inhibit thrombin-induced or Factor Xa-induced platelet aggregation and fibrinogen clotting in blood plasma. The derivatives can be manufactured from the corresponding maleimides which are N-substituted by .alpha.-amino carboxylic acids of the formula HN(R.sup.2)CH(R.sup.4)COOH, or functional derivatives thereof; and ketones or aldehydes of the formula R.sup.5 C(O)R.sup.6.Type: GrantFiled: February 26, 1996Date of Patent: November 11, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Francois Diederich, Ulrike Obst, Sabine Wallbaum, Lutz Weber
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Patent number: 5677321Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: February 29, 1996Date of Patent: October 14, 1997Assignee: Synaptic Pharmaceutical CorporationInventors: Yoon T. Jeon, Charles Gluchowski
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Patent number: 5670530Abstract: An anti-cancer composition comprising a rhodacyanine compound and cyclodextrin or derivative thereof, wherein said rhodacyanine compound is selected from the group consisting of compounds represented by the following Formula (I), the cation moiety of which has a log P value of 4.5-12: ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, each represents O, S, Se, ##STR2## Y.sub.1 represents O, S, Se, or ##STR3## R.sub.1 and R.sub.3, which may be the same or different, each represents an alkyl group;R.sub.2 represents an alkyl group, an aryl group or a heterocyclic group;Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;L.sub.1, L.sub.2 and L.sub.3, which may be the same or different, each represents a methine group or nitrogen atom and L.sub.1 and R.sub.3 may combine and form a 5- or 6-membered ring;R.sub.4 and R.sub.5, which may be the same or different, each represents an alkyl group;R.sub.6 and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: September 23, 1997Assignees: Fuji Photo Film Co., Ltd., Dana Farber Cancer InstituteInventors: Lan Bo Chen, Tadao Shishido
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Patent number: 5643926Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.Type: GrantFiled: January 19, 1994Date of Patent: July 1, 1997Assignee: Eli Lilly and CompanyInventors: Raymond F. Brown, J. Jeffry Howbert, Karen L. Lobb, David A. Neel, Jon K. Reel, Beverley Greenwood
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Patent number: 5637603Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.Type: GrantFiled: April 25, 1995Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
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Patent number: 5618831Abstract: A pharmaceutical composition for treatment of cancer in an animal comprising:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formula (I). ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, each represents an alkyl group or an aryl group;L.sub.1 and L.sub.2 each represents a methine group or a substituted methine group;X represents a pharmaceutically acceptable anion;k represents a number necessary for electrical charge balance;n represents 0 or 1; and(B) a pharmaceutically acceptable carrier or diluent.Type: GrantFiled: May 16, 1994Date of Patent: April 8, 1997Assignees: Fuji Photo Film Co., Ltd., Dana Farber Cancer InstituteInventors: Tadao Shishido, Masayuki Kawakami, Akihiko Ikegawa, Toshinao Ukai, Keizo Koya, Lan B. Chen
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Patent number: 5604224Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: May 30, 1995Date of Patent: February 18, 1997Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5599825Abstract: There are provided methine compounds having the following structure and their analogs, with a high solubility and are usefull as an active ingredient for pharmaceutical composition for treatment of cancer: ##STR1##Type: GrantFiled: April 12, 1995Date of Patent: February 4, 1997Assignee: Fuji Photo Film Co., Ltd.Inventors: Noriaki Tatsuta, Akihiko Okegawa, Masayuki Kawakami, Keizo Koya
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Patent number: 5585091Abstract: Compounds which, per molecule, contain at least 2 benzazolyl groups are outstandingly suitable as UV absorbers for sunscreen compositions.Type: GrantFiled: February 22, 1995Date of Patent: December 17, 1996Assignee: Haarmann & Reimer GmbHInventors: Ralf Pelzer, Roland Langner, Horst Surburg, Horst Sommer, Alfred Krempel, Rudolf Hopp
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5565479Abstract: Condensed thiazole derivatives useful as 5-HT.sub.3 receptor agonists are provided and can be represented by the following formula (I) or a pharmaceutically acceptable salt thereof, a process for the production thereof and a pharmaceutical composition thereof: ##STR1## wherein R, A, L.sub.1, L.sub.2, L, and R.sup.1 -R.sup.Type: GrantFiled: April 28, 1995Date of Patent: October 15, 1996Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Iwaoka, Hiroyuki Koshio, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
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Patent number: 5556855Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.Type: GrantFiled: December 29, 1994Date of Patent: September 17, 1996Assignee: Pharmacia ABInventors: Hubert Agback, Leif Ahrgren, Thomas Berglindh, Martin Haraldsson, G oran Smedeg.ang.rd, Lars-Inge Olsson
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Patent number: 5512564Abstract: The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I ##STR1## in which HET represents a heterocyclic ring with 3-7 ring atoms which can be substituted by one, two or three residues R.sup.1 which can be the same or different,Y represents an oxygen or sulphur atom, or a SO or SO.sub.2 group,X can be an oxygen or sulphur atom,R denotes an aliphatic residue with 1-9 C-atoms which can be substituted by phenyl or denotes a phenyl ring or a carbocyclic ring with 7-15 C atoms or a heterocyclic ring system each having 5 or 6 ring atoms,in which the aforementioned phenyl rings, carbocyclic rings or heterocyclic ring system can be substituted once or several times, if desired, and R1-R5 denote hydrogen or an aliphatic residue, as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts.Type: GrantFiled: March 4, 1994Date of Patent: April 30, 1996Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Herbert Leinert, Alfred Mertens
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Patent number: 5506243Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.Type: GrantFiled: April 28, 1994Date of Patent: April 9, 1996Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
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Patent number: 5449681Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.Type: GrantFiled: November 22, 1993Date of Patent: September 12, 1995Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
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2-thienylimidazo[2,1-.beta.]benzothiazole-3-acetic acid derivatives, their preparation and their use
Patent number: 5418248Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydroxy group, a C.sub.1 -C.sub.4 alkoxy group or an amino group of general formula --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 each represent, independently of each other, a hydrogen atom, a straight or branched C.sub.1 -C.sub.4 alkyl group, an allyl group or a methoxyethyl group, or alternatively --NR.sub.4 R.sub.5 represents a heterocycle containing 3 to 6 carbon atoms,Y represents a thienyl group optionally substituted by an alkyl group, andX represents a hydrogen or halogen atom,are useful as anticonvulsants and auxiolytics.Type: GrantFiled: December 29, 1993Date of Patent: May 23, 1995Assignee: SynthelaboInventors: Mireille Sevrin, Claude Morel, Michel Mangane, Pascal George -
Patent number: 5397794Abstract: The present invention concerns the use of compounds of the general formula I ##STR1## for the preparation of medicaments for the treatment of viral or retroviral infections, whereby R signifies a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical with 1-7 carbon atoms, which can possibly be substituted by phenyl, or a phenyl ring which can possibly be substituted one or more times by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl, trifluoromethyl, methylsulphonyl or halogen, such as fluorine, chlorine or bromine, n stands for the numbers 0, 1 or 2, as well as of their pharmacologically compatible salts or tautomers.Type: GrantFiled: July 20, 1993Date of Patent: March 14, 1995Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Alfred Mertens, Herbert Leinert, Ulrike Leser, Bernhard Konig, Hans Seidel
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Patent number: 5378706Abstract: The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: - R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group or an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pydridino group.Type: GrantFiled: May 28, 1993Date of Patent: January 3, 1995Assignee: SanofiInventors: Kathleen Biziere, Dominique Olliero, Paul Worms
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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: 5294629Abstract: A novel benzothiazole or benzimidazole derivative represented by formula (I) ##STR1## wherein X represents a sulfur atom or a NH group; R.sup.1 represents a hydrogen atom, a lower alkoxy group, a chlorine atom, a bromine atom or an iodine atom; R.sup.2 represents a hydrogen atom a substituted or unsubstituted lower alkyl group, a vinyl group, an aryl group or an acyl group; m is an integer of 1, 2 or 3; and n is an integer of 0, 1 or 2, which shows an excellent acid secretion suppressing effect and gastric mucosa protecting effect, and an antiulcer agent containing the same as an active ingredient.Type: GrantFiled: March 25, 1993Date of Patent: March 15, 1994Assignee: Meiji Seika Kaisha, Ltd.Inventors: Tomoya Machinami, Kazue Yasufuku, Seiji Shibahara, Fumiya Hirano, Yasukatsu Yuda, Motohiro Nishio, Yuji Matsuhashi, Takashi Tsuruoka, Kiyoaki Katano, Shigeharu Inoye
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Patent number: 5217987Abstract: Mazindol and other nonreinforcing dopamine uptake inhibitors are effective to lessen craving for abused substances.Type: GrantFiled: February 5, 1990Date of Patent: June 8, 1993Inventor: Stephen P. Berger
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Patent number: 5217984Abstract: 1-Phenyl substituted-1H,3H-thiazole [3,4-a] benzimidazoles are prepared by reaction of o.phenilendiamine with a substituted benzaldehyde and with 2-mercaptoacetic acid. The new compounds are antiviral products.Type: GrantFiled: July 25, 1991Date of Patent: June 8, 1993Inventors: Pietro Monforte, Anna M. Monforte, Maria Zappala, Giovanni Romeo, Silvana Grasso, Alba Chimirri
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5007953Abstract: Methods of using comminuted Alder bark as a stimulator of seed germination and growth media comprising comminuted Alder bark are disclosed. Also disclosed are seed treatment dusts comprising an active ingredient, a diluent material and comminuted Alder bark and methods of using these dusts. The active ingredients include fungicides, insecticides and other pesticides. The diluent materials used include clays and talcs.Type: GrantFiled: December 22, 1988Date of Patent: April 16, 1991Assignee: Snake River Chemicals, Inc.Inventor: Charles C. Chollet
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Patent number: 4981864Abstract: The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## or R.sub.1 is a 5 or 6 membered heterocycle or when X is a valency bond R.sub.1 is also H, OH, mercapto, amino, alkyl, alkenyl, alkynyl, haloalkyl, alkylthio, formylaminoalkyl, pyridylcarbonylamino, cycloalkyl, or cycloalkenyl, alkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl or hydroxyalkyl of claim 1 or 2 for the preparation of pharmaceutical compositions with an erythrocyte aggregation inhibition action useful, for example, in states of shock or circulatory disturbance.Type: GrantFiled: November 30, 1988Date of Patent: January 1, 1991Assignee: Boehringer Mannehim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Jens-Peter Hoelck, Erwin Boehm, Ulrich Martin
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Patent number: 4978671Abstract: The invention relates to novel thieno-(3',4'-4,5)imidazo(2,1-b)thiazole derivatives of the formula ##STR1## in which R.sub.1 denotes hydrogen, halogen or CF.sub.3 andR.sub.2 denotes hydrogen or C.sub.1 -C.sub.4 alkyl and, in the case in which R.sub.2 denotes hydrogen, their pharmaceutically utilizable salts, a process for the preparation of these compounds and their use for the treatment of cancer or rheumatoid arthritis caused by a defective immune system.Type: GrantFiled: August 30, 1989Date of Patent: December 18, 1990Assignee: Chemisch Pharmazeutische Forschungsgesellschaft m.b.H.Inventors: Dieter Binder, Franz Rovenszky, Hubert P. Ferber