The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
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Patent number: 6369232Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: August 8, 2001Date of Patent: April 9, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Achyutharao Sidduri
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6353111Abstract: 2,3-Di-substituted trans olefinic N-heteroaromatic or urido propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: December 1, 2000Date of Patent: March 5, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Ramakanth Sarabu, Achyutharao Sidduri
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Patent number: 6323315Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.Type: GrantFiled: March 31, 2000Date of Patent: November 27, 2001Assignees: BASF Aktiengesellschaft, Arizona Board of RegentsInventors: George R. Pettit, Jayaram K. Srirangam, Michael D. Williams, Kieran P. M. Durkin, Teresa Barlozzari, Andreas Kling, Bernd Janssen, Andreas Haupt
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Patent number: 6320050Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: March 15, 2000Date of Patent: November 20, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Ramakanth Sarabu
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Patent number: 6313305Abstract: A compound having the formula selected from the group consisting of wherein either R3p and R4p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R2p is selected from the group consisting of —CN, —F, Br and I and R1p and R5p are hydrogen or R5p is —F and R1p and R2p are hydrogen or R1p and R2p are F and R5p is hydrogen, or R4p and R5p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R3p is selected from the group consisting of F and —CN and R1p and R2p are hydrogen, R8 is hydrogen or an amine protective group and R10 is the remainder in which the hydroxy or amino are protected wherein R′1 is selected from the group consisting of alkyl of 1 to 4 carbon atoms, —CN, carboxy and alkoxy carbonyl of 1 to 4 carbon atoms.Type: GrantFiled: July 21, 1997Date of Patent: November 6, 2001Assignee: Hoechst Marion RousselInventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin d'Ambrieres, Daniel Humbert, Christophe Dini
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Patent number: 6306871Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: September 19, 2000Date of Patent: October 23, 2001Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6294674Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds. wherein Q is an un-natural amino acid. More particurlarly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthiritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: March 2, 1999Date of Patent: September 25, 2001Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 6288061Abstract: The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 21, 2000Date of Patent: September 11, 2001Assignee: Welfide CorporationInventors: Hiroyuki Sueoka, Jouji Yasuoka, Akira Nishiyama, Masatoshi Kiuchi, Katsuya Yamamoto, Kunio Sugahara, Syuji Ehara, Kei Sakata
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Patent number: 6239152Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.Type: GrantFiled: January 22, 1999Date of Patent: May 29, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
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Patent number: 6228871Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases and conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.Type: GrantFiled: June 29, 1999Date of Patent: May 8, 2001Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, Randall W. Hungate, William F. Hoffman, William R. Huckle, Richard L. Kendall, Kenneth A. Thomas, Jr.
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Patent number: 6225323Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: August 11, 1998Date of Patent: May 1, 2001Assignee: Joseph KoziakInventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6197970Abstract: The present invention is directed to a process for producing 2-hydroxybenzamide derivatives (2) or (5) according to either one of the following reaction schemes.Type: GrantFiled: December 23, 1999Date of Patent: March 6, 2001Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masaaki Nagasawa, Hiroyasu Nishioka, Takanori Suzuki, Eiichi Nagano, Katsuyuki Ishii, Ryu Nakao
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Patent number: 6191150Abstract: A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5 and R6 are as described in the specification, or a pharmaceutically acceptable salt, solvate, biohydrolyzable ester, biohydrolyzable amide, affinity reagent, or prodrug thereof.Type: GrantFiled: August 25, 1999Date of Patent: February 20, 2001Assignee: Glaxo Wellcome Inc.Inventors: Robert Carl Andrews, Marc Werner Andersen, Dulce Garrido Bubacz, Joseph Howing Chan, David John Cowan, Michael David Gaul, Daryl Lynn McDougald, David Lee Musso, Michael Howard Rabinowitz, Jennifer Badiang Stanford, Robert William Wiethe
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Patent number: 6169089Abstract: The current invention discloses aminotetrazole derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 12, 1999Date of Patent: January 2, 2001Assignee: G. D. Searle & CompanyInventors: E. Ann Hallinan, Donald W. Hansen, Jr., Sofya Tsymbalov
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Patent number: 6165943Abstract: Thiazolimine derivatives of the formula I ##STR1## where: X and Y independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl;Z is hydrogen; C.sub.l -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl, C.sub.2 -C.sub.8 -alkynyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.8 -alkylthio, it being possible for these groups to be substituted by one to five halogen or C.sub.1 -C.sub.4 -alkoxy; aryl, hetaryl, benzyl, it being possible for these groups to be substituted by C.sub.l -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.l -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, halogen, nitro or cyano; or one of the groups below: ##STR2## R.sup.1 and R.sup.2 are each hydrogen, halogen; C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl, it being possible for these groups to be substituted by one to five halogens or by C.sub.1 -C.sub.4 -alkoxy;n is 1 or 2;m is 0, 1 or 2R.sup.3 -R.sup.Type: GrantFiled: September 21, 1999Date of Patent: December 26, 2000Assignee: BASF AktiengesellschaftInventors: Guido Mayer, Martina Otten, Uwe Kardorff, Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Joachim Rheinheimer, Matthias Witschel, Roland Gotz, Michael Rack, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 6162823Abstract: The present invention provides compounds having the of the formula I: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: March 12, 1997Date of Patent: December 19, 2000Assignee: G.D. Searle & Co.Inventors: Thomas Dale Penning, Stella Siu-tzyy Yu, James Malecha, Chi-Dean Liang, Mark Andrew Russell
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Patent number: 6159973Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2).sub.a --(X.sub.1).sub.b --Q.sub.1 --Q.sub.2 --C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radicalor one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 --R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2,their preparation process and their use as pesticides.Type: GrantFiled: July 21, 1999Date of Patent: December 12, 2000Assignee: Hoechst Schering Agrevo S.A.Inventors: Jacques Demassey, Michel Gohar, Christian Wehrey
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Patent number: 6140330Abstract: A thiazole compound of the formula: ##STR1## wherein T is lower alkylene; u is 0 or 1; R.sup.1 and R.sup.2 are the same or different and are each H, or lower alkyl, etc.; R.sup.3 is ##STR2## R.sup.4 is H or lower alkanoyloxy-lower alkyl, which shows inhibitory activity on protein kinase C (PKC, Ca.sup.2+ /phospholipid-depending serine/threonine protein phosphatase), and are useful as a protein kinase C inhibitor.Type: GrantFiled: March 24, 1998Date of Patent: October 31, 2000Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Toyoki Mori, Michiaki Tominaga, Fujio Tabusa, Kazuyoshi Nagami, Kaoru Abe, Kenji Nakaya, Isao Takemura, Tomoichi Shinohara, Yoshihisa Tanada, Takahito Yamauchi
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Patent number: 6124455Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: January 25, 2000Date of Patent: September 26, 2000Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6121301Abstract: The present invention relates to a substituted benzoylaminothiazole derivative represented by the following formula (I): ##STR1## wherein X represents an imino group which may be substituted by a lower alkyl group, or an oxygen atom, R.sup.1 represents a cyano group, a lower alkoxycarbonyl group, a lower alkoxycarbonylamino group, a lower alkylsulfonylamino group, a lower alkanoyl or lower alkylsulfonyl group which may be substituted by a halogen atom, a 1-ureido group, a halo-substituted lower alkyl group or a 2-pyrrolylimino group, R.sup.2 and R.sup.3 are the same or different and each independently represents a hydrogen atom or a lower alkyl group and m stands for an integer of 2 to 4, or a salt thereof; and a medicament comprising the compound as an effective ingredient. The compound of the invention is useful as a preventive and therapeutic agent for epigastric dyscomfort, nausea, vomiting, heartburn, anorexia, bellyache, abdominal flatulence, chronic gastritis or the like.Type: GrantFiled: April 21, 1999Date of Patent: September 19, 2000Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masaaki Nagasawa, Kenji Sato, Tadashi Kurimoto, Shigeru Ueki
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Patent number: 6114365Abstract: 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): ##STR1## where R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein, or pharmaceutically acceptable salts thereof, are useful in, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.Type: GrantFiled: August 12, 1999Date of Patent: September 5, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Pevarello, Raffaella Amici, Manuela Villa, Barbara Salom, Anna Vulpetti, Mario Varasi
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Patent number: 6100282Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.Type: GrantFiled: December 22, 1998Date of Patent: August 8, 2000Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Patent number: 6096898Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.Type: GrantFiled: October 22, 1999Date of Patent: August 1, 2000Assignee: Dow AgroSciences LLCInventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
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Patent number: 6048883Abstract: This invention provides compounds of formula (I):A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --Y.R.sup.2(I)or a tautomeric form thereof or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein A.sup.1, A.sup.2, A.sup.3, R.sup.2, X, Y and n are as defined herein; pharmaceutical composition comprising such compounds and the use of such a compounds for treating hyperglycemia.Type: GrantFiled: March 9, 1995Date of Patent: April 11, 2000Assignee: SmithKline Beecham p.l.c.Inventors: David Haigh, John Thomas Sime
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Patent number: 6048884Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. ##STR1## (The symbols in the formula have the following meanings. (whereinA: heteroarylene;X: bond, O, S, --NR.sup.5 --, --NR.sup.5 CO--, --NR.sup.5 CONH--, --NR.sup.5 SO.sub.2 -- or --NR.sup.5 C(.dbd.NH)NH--;R.sup.1 : --H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl;R.sup.2a, R.sup.2b : --H or -lower alkyl, which may be the same or different;R.sup.3 : --H or -lower alkyl;R.sup.4a, R.sup.4b : --H or --OH, which may be the same different, or R.sup.4a and R.sup.4b are taken together to form .dbd.O or .dbd.N.about.O-lower alkyl; andR.sup.5 : --H or -lower alkyl.Type: GrantFiled: May 7, 1999Date of Patent: April 11, 2000Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Tatsuya Maruyama, Kenichi Onda, Masahiko Hayakawa, Takumi Takahashi, Takayuki Suzuki, Tetsuo Matsui
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Patent number: 6017956Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.Type: GrantFiled: March 25, 1998Date of Patent: January 25, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5981557Abstract: The present invention relates to an aminothiazole derivative represented by the following formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represents a hydrogen atom, a hydroxy group, a lower alkyl group, a lower alkoxy group or the like; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a halogen atom or a lower alkyl group; m stands for an integer of 0 to 4, A represents a substituted amino group, a substituted imino group, a heterocyclic group or the like; and B stands for an imino group or an oxygen atom, a medicament containing it and an intermediate for the preparation of said compound. The compound has strong restoration effects on dysmotility in the gastrointestinal tract and at the same time has high safety so that it is useful as an excellent gastroprokinetic.Type: GrantFiled: November 18, 1997Date of Patent: November 9, 1999Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masaaki Nagasawa, Masakazu Murata, Hiroyasu Nishioka, Tadashi Kurimoto, Shigeru Ueki, Osamu Kitagawa
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Patent number: 5932606Abstract: A compound which inhibits human thrombin and where has the structure and pharmaceutically acceptable salts thereof, wherein such as ##STR1## which are useful for inhibiting formation of blood platelet aggregates in blood in a mammal.Type: GrantFiled: March 20, 1998Date of Patent: August 3, 1999Assignee: Merck & Co., Inc.Inventors: Richard C. A. Isaacs, Adel M. Naylor-Olsen, Bruce D. Dorsey, Christina L. Newton
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Patent number: 5922881Abstract: The invention relates to novel heterocyclic imino derivatives, several processes for their preparation and their use for controlling pests.Type: GrantFiled: November 27, 1996Date of Patent: July 13, 1999Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Thomas Seitz, Ralf Tiemann, Heinz-Wilhelm Dehne, Klaus Stenzel
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Patent number: 5919787Abstract: The current invention discloses aminotetrazole derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: October 5, 1998Date of Patent: July 6, 1999Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Donald W. Hansen, Jr., Sofya Tsymbalov
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Patent number: 5919940Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.Type: GrantFiled: October 16, 1998Date of Patent: July 6, 1999Assignee: British Biotech Pharmaceuticals LimitedInventor: Fionna Mitchell Martin
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Patent number: 5854251Abstract: Aminotetrazole derivatives of the formula (I) wherein the variables are as defined in the disclosure are useful as nitric oxide synthase inhibitors.Type: GrantFiled: April 30, 1997Date of Patent: December 29, 1998Assignee: G. D. Searle & Co.Inventors: Ann E. Hallinan, Donald W. Hansen, Jr., Sofya Tsymbalov
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Patent number: 5849747Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.Type: GrantFiled: March 15, 1996Date of Patent: December 15, 1998Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5847156Abstract: 1,4-Diketopyrrolopyrroles of the formula ##STR1## in which A and B independently of one another are a group of the formula ##STR2## R.sub.1 is a long-chain radical containing a reactive group capable of polymerization, and R.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR3## or R.sub.1. The novel diketopyrrolopyrroles are suitable for preparing coloured polymers with unexpectedly advantageous colour effects.Type: GrantFiled: January 29, 1997Date of Patent: December 8, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Sameer Hosam Eldin, Abul Iqbal
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Patent number: 5723462Abstract: Disclosed are compounds of formula I: ##STR1## wherein R.sub.8 and R.sub.9 independently represent hydrogen or organic substituents;W represents optionally substituted thiazolyl or quinoxalinyl;X is hydrogen, hydroxy or lower alkyl; andT is hydrogen, halogen, hydroxy, nitro, amino or alkyl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptor. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: April 26, 1996Date of Patent: March 3, 1998Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Patent number: 5712270Abstract: This invention relates to methods of treating neurological illnesses related to acetylcholine deficiency in the CNS including memory loss attending senility, Parkinson's disease, Down's syndrome or senile pugilistica by administering a therapeutically effective compound of the formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl, halo, perhaloalkyl, hydroxy, alkoxy, aryl or arylalkyl; n is an integer from 0-5; R is azabicyclo?2.2.2!octyl or azabicyclo?2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy, halo or perhaloalkyl; N-(pyridyl)piperazinyl; N-(pyrimidinyl)piperazinyl; or 3-azabicyclo-?3.2.2!non-3-yl; X is oxygen or NH; n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 30, 1996Date of Patent: January 27, 1998Assignee: American Home Products CorporationInventor: Annmarie L. Sabb
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Patent number: 5688821Abstract: This invention relates to compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are both hydrogen or R.sup.1 and R.sup.2 form a bond;m=1 and n=3 and p=6,or m=3, 5 or 7 and n=1 and p=6,or m=4 and n=2 and p=6 or 8,and the E (trans) and Z (cis) isomers when R.sup.1 =R.sup.2 =H;and the basic addition salts thereof which are inhibitors of phospholipase A.sub.2 and are thus useful agents in the treatment of inflammatory diseases where arachidonic acid metabolic products are implicated, such as rheumatoid arthritis, inflammatory bowel diseases such as ulcerative colitis, atopic dermatitis conditions such as psoriasis and immediate hypersensitivity reactions such as allergic bronchial asthma and allergic rhinitis; and as gastric cytoprotective agents.Type: GrantFiled: December 20, 1996Date of Patent: November 18, 1997Assignee: American Home Products CorporationInventor: Kenneth Lewis Kees
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Patent number: 5688959Abstract: Color photographic motion picture elements adapted to form a multicolor photographic dye image and an integral, infrared-absorbing, dye sound track and comprising 1-hydroxy-2-N-(5-alkyl-thiazol-2-yl)-naphthamide couplers that are capable of forming quinone imine dyes absorbing infrared radiation in the spectral range from about 600 to about 1000 nm by reaction with an oxidized aromatic primary amino developing agent, the thiazol-2-yl group of said naphthamide couplers bearing a 4-para-C.sub.1 -C.sub.4 alkoxyphenyl group or a 4-para-C.sub.1 -C.sub.4 alkylphenyl group, the hydrogen atoms of said C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkyl being unsubstituted or at least one of them having been substituted by a halogen atom.Type: GrantFiled: May 6, 1991Date of Patent: November 18, 1997Assignee: Agfa-Gevaert, N.V.Inventors: Henri Fran.cedilla.ois Olbrechts, Raphael Karel Van Poucke, Christian Charles Van den Sande
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Patent number: 5684008Abstract: The current invention discloses aminotetrazole derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: November 9, 1994Date of Patent: November 4, 1997Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Donald W. Hansen, Jr., Sofya Tsymbalov
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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: 5672712Abstract: Object: To provide compounds useful as inhibitors of blood platelet aggregation for intravenous administration.Constitution: A thiazoline derivative represented by the formula: ##STR1## ?wherein R.sup.1 is a hydroxyl group, an alkoxy group, a cycloalkoxy group or a group represented by the formula: R.sup.4 NH-- (wherein R.sup.4 is a cycloalkyl group), R.sup.2 is an alkyl group, a cycloalkyl group or a phenylalkyl group, R.sup.3 is a hydrogen atom or an alkyl group, and n is an integer of 2 to 9! or a salt thereof.Type: GrantFiled: December 12, 1996Date of Patent: September 30, 1997Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Akira Manaka, Keiko Takahashi, Yutaka Kawashima, Katsuo Hatayama
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Patent number: 5668128Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sub.1 and Q are independently an optionally esterified or amidated carboxyl group; R.sub.2 is hydrogen, an acyl group or an optionally substituted hydrocarbon residue; X is a divalent hydrocarbon residue which may be substituted; or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as agents for inhibiting thiol protease.Type: GrantFiled: September 5, 1995Date of Patent: September 16, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigetoshi Tsubotani, Masayuki Takizawa, Mikio Shirasaki, Junji Mizoguchi, Yoshiaki Shimizu
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Patent number: 5663185Abstract: Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1alkyl, alkoxy, alkylaminoR.sup.2alkyl;Aa direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofBhydrogen, halogen,alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylUCH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;Xhydrogen, cyano, nitro, halogen,alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof,amino which may bear one or two of the abovementioned groups;m1 or 2,Yoxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.Type: GrantFiled: March 20, 1995Date of Patent: September 2, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Horst Wingert, Hartmann Koenig, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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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: 5648497Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.Type: GrantFiled: March 24, 1995Date of Patent: July 15, 1997Assignee: Abbott LaboraotriesInventors: Dale J. Kempf, Daniel W. Norbeck, Lynn M. Codacovi, Hing L. Sham, Steven J. Wittenberger
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Patent number: 5627198Abstract: The invention relates to heterocyclic amides of the formula ##STR1## in which the radicals A, Z, A.sub.1, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, to a process for the preparation of these amides and to their use as active substances for the curing and amelioration of disorders and diseases which can be treated by exerting influence on potassium channels.Type: GrantFiled: December 4, 1995Date of Patent: May 6, 1997Assignee: Hafslund Nycomed Pharma AktiengesellschaftInventors: Peter Esch, Robertson Towart, Franz Rovenszky
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Patent number: 5554634Abstract: Disclosed herein are compounds of the formula:A'--N(R.sup.1')c(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A' is HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1' is R.sup.7 R.sup.8 NC(O)CH.sub.2 wherein R.sup.7 hydrogen or lower alkyl and R.sup.8 is lower alkyl; R.sup.2 is, for example, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.Type: GrantFiled: May 1, 1995Date of Patent: September 10, 1996Assignee: Bio-Mega Boehringer Ingelheim Research Inc.Inventors: Paul C. Anderson, Teddy Halmos, Grace L. Jung, Marc-Andr e Poupart, Bruno Simoneau
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Patent number: 5538991Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 14, 1994Date of Patent: July 23, 1996Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee
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Patent number: RE37094Abstract: Compounds of formula in which R1 represents H, an alkyl or a substituted alkyl, R2 represents H or alkyl and R3 represents an optionally substituted cycloalkyl or an optionally substituted aromatic group, which can be a phenyl or a heterocyclic group comprising one or more hetero-atoms chosen from O, S and N, or R2 and R3 considered together represent the group which is optionally substituted on the phenyl ring, and Z represents a heterocycle comprising one or more heteroatoms chosen from O, S and N, fused with an aromatic ring which can comprise a hetero-atom and can be substituted, the said heterocycle being optionally substituted on N, when it comprises such an atom, by an alkyl or a substituted alkyl group, and the salts of these compounds with acids or bases. Use of these compounds as medicaments. No figure.Type: GrantFiled: September 11, 1995Date of Patent: March 13, 2001Assignee: SanofiInventors: Daniel Fréhel, Danielle Gully, Gérard Valette, Jean-Pierre Bras