Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
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Patent number: 7186730Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: GrantFiled: May 24, 2002Date of Patent: March 6, 2007Assignee: SmithKline Beecham p.l.c.Inventors: Catherine Genevieve Yvette Dartois, Roger Edward Markwell, Guy Marguerite Marie Gerard Nadler, Neil David Pearson
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Patent number: 7141564Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: GrantFiled: May 24, 2002Date of Patent: November 28, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
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Patent number: 7125868Abstract: The present invention is related to a type of thienothiazine compounds having molecular structure of formula (1) and their pharmaceutically acceptable salts or solvates.Type: GrantFiled: December 24, 2003Date of Patent: October 24, 2006Inventor: Jing Li
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Patent number: 7112582Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is S.Type: GrantFiled: May 1, 2003Date of Patent: September 26, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo dos Santos, Fuk-Wah Sum, Yang-I Lin
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Patent number: 7087626Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.Type: GrantFiled: May 13, 2002Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Todd Vincent DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Jr., Hong-Yu Li, William Thomas McMillen, Shawn Christopher Miller, Jason Scott Sawyer, Edward C. R. Smith, Jonathan Michael Yingling
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Patent number: 7064122Abstract: The subject invention features compounds having the structure: wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1-C15 alkyl, C1-C8 alkylaryl, —C(O)OR4, —C(O)NR4R5, —CR6R6?OR4, —CR6R6?OC(O)R4, —CR6R6?OC(O)NHR7, —C(O)NR10R11, —C(O)NR8R9NR8R9, —N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1—C30 alkyl or branched C3-C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, —CH2-aryl, aryl —C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6? are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstitutedType: GrantFiled: December 20, 2002Date of Patent: June 20, 2006Assignee: OSI Pharmaceuticals, Inc.Inventors: David Witter, Arlindo Castelhano
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Patent number: 7057036Abstract: A pyrrolesulfonamide derivative having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C? or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C?; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group.Type: GrantFiled: July 10, 2003Date of Patent: June 6, 2006Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 7049437Abstract: The present invention provides a process of a compound of the formula (I): wherein R is heteroaryl or the like, ring A is a heteroalicyclic group or the like comprising reacting a compound of the formula (II): wherein Hal is halogen and the other symbols are the same as the above, in the presence of a sulfinic acid salt and further in the presence of an acid or a salt with an organic base, and a novel crystal form of 2-(3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine phosphate monohydrate.Type: GrantFiled: March 29, 2001Date of Patent: May 23, 2006Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Matsubara, Takashi Ohya, Masaaki Uenaka
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Patent number: 7049312Abstract: Q is —N=or CR2 X is S, O or NOR3 Y is —O—, —S—, —SO— or —SO2— R and R1 are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl group R2 is H or a substituent R3 is H, or —C(O)R4 R4 is a substituted or unsubstituted aliphatic or aromatic group n is an integer from 0 to 1 Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.Type: GrantFiled: June 2, 2000Date of Patent: May 23, 2006Assignee: Abbott GmbH & Co. KGInventors: Paul Rafferty, David Calderwood, Lee Arnold, Beatriz Gonzalez Pascual, Jose L. Ortego Martinez, Maria J. Perez de Vega, Isabel Fernandez
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Patent number: 7026313Abstract: The present invention provides 2-thia-1,6,8-triaza-naphthalene-2,2-dioxide inhibitors of cyclin-dependent kinases, uses thereof and pharmaceutical compositions thereof. These compounds are useful for treating cell proliferative disorders, such as cancer, atherosclerosis, and restenosis. These compounds are potent inhibitors of kinases such as cyclin-dependent (cdks) and growth factor-mediated kinases.Type: GrantFiled: January 21, 2003Date of Patent: April 11, 2006Assignee: Warner-Lambert CompanyInventor: Joseph Thomas Repine
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Patent number: 6960579Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.Type: GrantFiled: May 10, 1999Date of Patent: November 1, 2005Assignee: Alcon Manufacturing, Ltd.Inventors: Jesse A. May, Thomas R. Dean, Najam A. Sharif, Hwang-Hsing Chen
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Patent number: 6953801Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: May 21, 2002Date of Patent: October 11, 2005Assignee: Neurogen CorporationInventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
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Patent number: 6943158Abstract: Compounds of formula I are p38 inhibitors: or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen or alkyl; R2 alkyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkyl, cyanoalkyl, heterocyclyl, heterocyclylalkyl, or —Y1—C(O)—Y2—R11 (where Y1 and Y2 are independently either absent or an alkylene group and R11 is hydrogen, alkyl, haloalkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino); R3 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterosubstituted cycloalkyl, heterocyclyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(?O)—R4 (where R4 is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino), or acyl; Ar1 is aryl; X1 is O, NR5 or S, where R5 is hydrogen or alkyl; and X2 is a bond, O, NR6, S or CH2, where R6 is hydrogen or alkyl.Type: GrantFiled: November 18, 2003Date of Patent: September 13, 2005Assignees: Roche Palo Alto LLC, Hoffmann-La Roche Inc.Inventors: Jian Jeffrey Chen, Kin-Chun Thomas Luk
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Patent number: 6939870Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.Type: GrantFiled: August 29, 2003Date of Patent: September 6, 2005Assignee: WyethInventors: Aranapakam M. Venkatesan, Jamie M. Davis, Yansong Gu
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Patent number: 6867211Abstract: The present invention relates to 4-pyridyl- and 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1: in which the variables have the meanings indicated in the description. The compounds according to the invention have immunomodulating and/or cytokine release-inhibiting action and are therefore utilizable for the treatment of disorders which are connected with a disturbance of the immune system.Type: GrantFiled: January 31, 2001Date of Patent: March 15, 2005Assignee: Merckle GmbHInventors: Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
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Publication number: 20040209871Abstract: Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.Type: ApplicationFiled: November 21, 2003Publication date: October 21, 2004Applicants: Tularik Inc., Japan Tobacco Inc.Inventors: Brian M. Fox, Noboru Furukawa, Xiaolin Hao, Kiyosei Iio, Takashi Inaba, Simon M. Jackson, Frank Kayser, Marc Labelle, Kexue Li, Takuya Matsui, Dustin L. McMinn, Nobuya Ogawa, Steven M. Rubenstein, Shoichi Sagawa, Kazuyuki Sugimoto, Masahiro Suzuki, Masahiro Tanaka, Guosen Ye, Atsuhito Yoshida, Jian Zhang
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Publication number: 20040180838Abstract: The use of bicyclic carbohydrates for the treatment of parasite infections is described. Different bicyclic carbohydrates have been tested in vitro against a number of protozoa. These compounds also have been screened against viruses, tumors, bacteria and fungi. Compound A1, a thiophenyl-containing bicyclic carbohydrate possessed significant activity against Trypanosoma brucei rhodiense, a parasite that causes the lethal sleeping sickness. Compound A2 and Compound A3, bicyclic carbohydrates with halogen containing aryl groups, possessed significant activity against Leishmania donovani, a parasite that causes leishmaniasis. Bicyclic carbohydrates in general, and Compound A1, Compound A2 and Compound A3 more specifically, could be possible treatments for the sleeping sickness and leishmaniasis in the future.Type: ApplicationFiled: January 7, 2004Publication date: September 16, 2004Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Bart Ruttens
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Publication number: 20040157835Abstract: The present invention is related to a type of thienothiazine compounds having molecular structure of formula (1) and their pharmaceutically acceptable salts or solvates. The present invention is also related to the method of producing the formula (1) compound, an anti-inflammatory and analgesic pharmaceutical composition containing the formula (1) compound, and the method of using the formula (1) compound to prepare anti-inflammatory and analgesic medicine.Type: ApplicationFiled: December 24, 2003Publication date: August 12, 2004Inventor: Jing Li
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Publication number: 20040127705Abstract: A pyrrolesulfonamide derivative having the following formula (I): 1Type: ApplicationFiled: July 10, 2003Publication date: July 1, 2004Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6747023Abstract: Described in the present invention are a sulfonyl derivative represented by the following formula (I): Q1—Q2—T1—Q3—SO2—QA (I) [wherein Q1 represents a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group, 5- or 6-membered heterocyclic group, dicyclic fused ring or tricyclic fused ring group which may have a substituent; Q2 represents a single bond, an oxygen atom, a sulfur atom, a linear or branched C1-6 alkylene group or the like; QA represents an arylalkenyl group which may have a substituent or a heteroarylalkenyl group which may have a substituent; and T1 represents a carbonyl group or the like] and a medicament comprising the same. The compound has strong FXa inhibitory action, provides prompt, sufficient and long-lasting anti-thrombus effects when orally administered, and has low side effects and is therefore useful as an excellent anticoagulant.Type: GrantFiled: February 12, 2001Date of Patent: June 8, 2004Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Syozo Kobayashi, Satoshi Komoriya, Noriyasu Haginoya, Masanori Suzuki, Toshiharu Yoshino, Takayasu Nagahara, Tsutomu Nagata, Haruhiko Horino, Masayuki Ito, Akiyoshi Mochizuki
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Publication number: 20040106604Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors. The disclosed invention relates to compounds of the structure (I) wherein (I) is a four, five, or six membered saturated ring and X is C, O or S.Type: ApplicationFiled: November 6, 2003Publication date: June 3, 2004Inventors: Douglas Beight, Todd DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Hong-Yu Li, William McMillen, Shawn Christopher Miller, Jason Sawyer, Edward C.R. Smith, Jonathan Michael Yingling
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Publication number: 20040087580Abstract: The present invention relates to new 4-hydroxy-2H-thieno[2,3-e]-1,2-thiazine-3-carboxamide-1,1-dioxides of general formula 1Type: ApplicationFiled: July 21, 2003Publication date: May 6, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Guenter Trummlitz, Wolfhard Engel, Wolfgang Eberlein, Guenther Engelhardt, Joanne Van Ryn
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Patent number: 6727258Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: March 19, 2001Date of Patent: April 27, 2004Assignee: King Pharmaceutical Research & Development, Inc.Inventor: Pier Giovanni Baraldi
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Publication number: 20040063580Abstract: The present invention provides a bicyclic triazolone derivative represented by the formula:Type: ApplicationFiled: June 26, 2003Publication date: April 1, 2004Inventors: Takashi Kuragano, Yasushi Tanaka
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Patent number: 6713477Abstract: A hydroxamic acid derivative represented by formula (1) or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which has a matrix metalo-proteinase inhibitor.Type: GrantFiled: November 9, 2001Date of Patent: March 30, 2004Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Gerard Robert Scarlato, Sara Sabina Hadida Ruah, Tamiki Nishimura, Masashi Nakatsuka, Fumio Samizo, Yumiko Kamikawa, Hitoshi Houtigai
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Publication number: 20030195199Abstract: The subject invention features compounds having the structure: 1Type: ApplicationFiled: December 20, 2002Publication date: October 16, 2003Inventors: David Witter, Arlindo Castelhano
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Publication number: 20030186973Abstract: The present invention provides 2-thia-1,6,8-triaza-naphthalene-2,2-dioxide inhibitors of cyclin-dependent kinases, uses thereof and pharmaceutical compositions thereof.Type: ApplicationFiled: January 21, 2003Publication date: October 2, 2003Inventor: Joseph Thomas Repine
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Publication number: 20030153558Abstract: The present invention relates to 4-pyridyl- und 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1 1Type: ApplicationFiled: November 5, 2002Publication date: August 14, 2003Inventors: Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
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Patent number: 6600035Abstract: Compounds of formula (I) in which: R1 is hydrogen or an organic substituent group; R2 is a fused bicyclic heterocyclic ring system of general formula (a) wherein R4 and R5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is 0, 1 or 2; and R3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol ═/═ indicates that the double bond may be in either the E or Z configuration.Type: GrantFiled: May 24, 1995Date of Patent: July 29, 2003Assignee: SMithKline Beecham p.l.c.Inventors: Nigel John Perryman Broom, Frank Peter Harrington
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Publication number: 20030109520Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: ApplicationFiled: October 22, 2002Publication date: June 12, 2003Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Publication number: 20030105085Abstract: Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: ApplicationFiled: February 27, 2002Publication date: June 5, 2003Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6562811Abstract: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di(C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33, or —NR34R35; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 18, 2001Date of Patent: May 13, 2003Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Publication number: 20030064962Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): 1Type: ApplicationFiled: December 12, 2001Publication date: April 3, 2003Inventors: Peter William Glunz, Brent Dale Douty, Wei Han
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Publication number: 20030055049Abstract: The invention relates to compounds of the formula 1 1Type: ApplicationFiled: August 22, 2002Publication date: March 20, 2003Applicant: Pfizer Inc.Inventors: John Charles Kath, Norma Jacqueline Tom, Eric David Cox, Samit Kumar Bhattacharya
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Patent number: 6528513Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.Type: GrantFiled: December 15, 2000Date of Patent: March 4, 2003Assignee: Tularik INCInventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
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Publication number: 20030018023Abstract: The present application describes 5-6 or 5-7 heterobicyclics of Formula I: 1Type: ApplicationFiled: March 25, 2002Publication date: January 23, 2003Inventors: Donald Joseph Philip Pinto, Renhua Li
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Publication number: 20020137928Abstract: A pyrrolesulfonamide compound having the following 1Type: ApplicationFiled: August 28, 2001Publication date: September 26, 2002Applicant: SUNTORY LIMITEDInventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6432945Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: March 30, 2001Date of Patent: August 13, 2002Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Publication number: 20020045622Abstract: This invention is directed to compounds of the formula 1Type: ApplicationFiled: November 21, 2001Publication date: April 18, 2002Inventor: Philip A. Carpino
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Publication number: 20020042415Abstract: This invention is directed to compounds of the formula 1Type: ApplicationFiled: March 30, 2001Publication date: April 11, 2002Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Publication number: 20020040017Abstract: A pyrrolesulfonamide derivative having the following formula (I): 1Type: ApplicationFiled: June 4, 2001Publication date: April 4, 2002Applicant: SUNTORY LIMITEDInventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6348457Abstract: The invention is concerned with novel compounds of the formula the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein X is oxygen or sulphur; R1 is hydrogen or halo; R2 is hydrogen, C1-4alkyl, phenylmethyl or halophenylmethyl; Alk is C1-4alkanediyl; —Z—A— is a bivalent radical selected from the group consisting of —S—CH2—CH2, —S—CH2—CH2—CH2—, —S—CH═CH—, —CH═CH—CH═CH—, —C(═CHR3)—CH2—CH2—CH2—, —CH═CH—O—, —CHR4—CH2—CH2—, —CHR4—CH2—CH2—CH2—, —CHR4—CH2—CH2—CH2—CH2—; in said bivalent radicals one hydrogen may be replaced by C1-4alkyl; R3 is phenyl or halophenyl; each R4 independently represents hydrogen, hydroxy, phenylmethyl or halophenylmethyl.Type: GrantFiled: January 5, 1995Date of Patent: February 19, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis, Albertus Henricus Maria Theresia Van Heertum
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Patent number: 6340752Abstract: Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite. Such agents are also employed in the recrystallization and reprocessing of the mercaptoalkanoylamino lactam acids.Type: GrantFiled: December 9, 1998Date of Patent: January 22, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Theodor Denzel, Bang-Chi Chen, James H. Simpson, Rajendra P. Deshpande
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Patent number: 6331623Abstract: A pyrrolesulfonamide compound having formula (I) wherein the ring P represented by &agr; is a pyrrole ring having structure &bgr; or &psgr; wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group &dgr; in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl.Type: GrantFiled: August 26, 1999Date of Patent: December 18, 2001Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Publication number: 20010044436Abstract: New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: ApplicationFiled: December 15, 2000Publication date: November 22, 2001Inventors: John M. Nuss, Xiaohui A. Zhou
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Publication number: 20010031871Abstract: A pyridine alcohol derivative represented by General Formula III 1Type: ApplicationFiled: May 23, 2001Publication date: October 18, 2001Applicant: KURARAY CO., LTD.Inventors: Hideki Matsuda, Goro Asanuma, Takanobu Shin, Manzo Shiono, Shigeki Kikuyama
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Patent number: 6274619Abstract: A compound of the formula: in which R1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl, R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, R3 is hydrogen or amidino-protective group, A is lower alkylene or carbonyl, X is Y is lower alkylene, —S— or —SO2—, Z is —S— or —O—, and the line: is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.Type: GrantFiled: May 31, 2000Date of Patent: August 14, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Akito Tanaka, Hiroaki Mizuno, Minoru Sakurai
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Patent number: 6271223Abstract: A pyrrolesulfonamide derivative having the following formula (I): is provided wherein P, A, Y, l, Z1 and Z2 are as described herein, wherein the derivative has strong serotonin-2 receptor antagonistic action, low toxicity and fewer side effects, and its use as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.Type: GrantFiled: August 26, 1999Date of Patent: August 7, 2001Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6200971Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: October 18, 1999Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Müller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Gr{umlaut over (u )}tzmann, Stefan Wohlfeil
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Patent number: 6133258Abstract: Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.Type: GrantFiled: May 13, 1998Date of Patent: October 17, 2000Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Jun-ichi Shishikura, Hiroshi Inami, Tomoyuki Yasunaga, Masaaki Hirano, Shuichi Sakamoto, Kazushige Ohno, Masamichi Okada, Shin-ichi Tsukamoto