Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazine Ring Patents (Class 544/58.4)
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Publication number: 20090215746Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.Type: ApplicationFiled: October 31, 2008Publication date: August 27, 2009Applicant: Takeda Pharmaceuticals Company LimitedInventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
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Publication number: 20090198052Abstract: The present invention relates to a method for preparing a syn-form piperidine compound represented by general formula [I]: wherein, bold lines represent bonds in which substituents at positions 2 and 4 of a piperidine ring are in the syn configuration, and the other symbols have the same meaning as defined below, or a salt thereof, comprising: reducing a compound represented by general formula [II]: wherein, ring A represents an optionally substituted benzene ring, R2 represents a hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, and M represents an alkaline metal or hydrogen atom.Type: ApplicationFiled: June 1, 2007Publication date: August 6, 2009Inventors: Hiroaki Matsumae, Yoshikazu Mori, Koji Matsuyama, Noriaki Moriyama
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Patent number: 7557112Abstract: There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.Type: GrantFiled: October 5, 2005Date of Patent: July 7, 2009Assignee: Astellas Pharma Inc.Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
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Publication number: 20090143358Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: ApplicationFiled: March 20, 2008Publication date: June 4, 2009Applicants: ICAgen, Inc., Pfizer LimitedInventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
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Publication number: 20090137570Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: January 28, 2009Publication date: May 28, 2009Applicant: IRM LLCInventors: Hong LIU, Arnab K. CHATTERJEE, David C. TULLY, Phillip B. ALPER, Badry BURSULAYA, Jianhua GUO, David H. WOODMANSEE, Daniel MUTNICK, Donald S. KARANEWSKY, Yun HE
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Publication number: 20090041723Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: ApplicationFiled: October 15, 2007Publication date: February 12, 2009Inventors: Guolin Li, Reza Fathi, Zhen Yang, Yun Liao, Qiang Zhu, Angela Man Iu Lam, Anthony Sandrasagra, Kenneth Nawoschik, Hyun-Joon Cho, Jie Cao, Wu Rouqiu, C. Richard Wobbe
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Publication number: 20090036436Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.Type: ApplicationFiled: January 25, 2006Publication date: February 5, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Publication number: 20090029973Abstract: The present invention relates to a compound represented by the formula: wherein W is C(R1) or N, each A is an optionally substituted aryl group or a heteroaryl group, X1 is —NR3—Y1—, —O—, —S—, —SO—, —SO2— or —CHR3— wherein R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 is optionally bonded to A to form an optionally substituted ring structure, R1 is a hydrogen atom or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom, R2 is a hydrogen atom or optionally substituted group bonded via a carbon atom or a sulfur atom, or R1 and R2, or R2 and R3 are optionally bonded to form an optionally substituted ring structure, or a salt thereof, and a tyrosine kinase inhibitor or an agent for the prophylaxis or treatment of cancer, which contains this compound or a prodrug thereof.Type: ApplicationFiled: July 14, 2008Publication date: January 29, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tomoyasu ISHIKAWA, Takahiko TANIGUCHI, Hiroshi BANNO, Masaki SETO
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Publication number: 20080319188Abstract: A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.Type: ApplicationFiled: August 23, 2006Publication date: December 25, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Tomohiro Matsushima, Keiko Takahashi, Setsuo Funasaka, Hiroshi Obaishi, Shuji Shirotori
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Publication number: 20080287424Abstract: The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: ApplicationFiled: July 15, 2008Publication date: November 20, 2008Applicant: WyethInventors: Derek Cecil Cole, Eric Steven Manas, Lee Dalton Jennings, Frank Eldridge Lovering, Joseph Raymond Stock, William Jay Moore, John Watson Ellingboe, Jeffrey Scott Condon, Mohani Nirmala Sukhdeo, Ping Zhou, Junjun Wu, Koi Michele Morris
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Patent number: 7435732Abstract: This invention relates to crystalline polymorphs of (3S)-N-hydroxy4-({4-[(4-hydroxy-2-butynyl)oxy]phenyl}sulfonyl)-2,2-dimethyl-3-thiomorpholine carboxamide, and preparation and uses thereof.Type: GrantFiled: June 7, 2005Date of Patent: October 14, 2008Assignee: WyethInventors: Wei Tong, Abdolsamad Tadayon, Peter John Larkin, Lalitha Krishnan, Subodh S. Deshmukh, Jean Marie Akin
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Publication number: 20080221086Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(heType: ApplicationFiled: November 8, 2007Publication date: September 11, 2008Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20080132495Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 30, 2005Publication date: June 5, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Maria Grazia Carr, Adrian Liam Gill, Steven Howard, Eva Figueroa Navarro, Gary Trewartha, David Charles Rees, Mladen Vinkovic, Paul Graham Wyatt
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Patent number: 7381260Abstract: A thiazineindigo pigment dispersant represented by Formula (1) or (2): where E denotes a basic group. A pigment composition contains a pigment material, and the thiazine indigo pigment dispersant. A colored composition contains the pigment composition and a pigment carrier. A color filter includes a filter segment prepared from the colored composition.Type: GrantFiled: April 18, 2007Date of Patent: June 3, 2008Assignee: Toyo Ink Mfg. Co., Ltd.Inventors: Masayuki Fujiki, Shoko Goto
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Patent number: 7323563Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:Type: GrantFiled: August 22, 2005Date of Patent: January 29, 2008Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Michael George Hunter, Paul Raymond Beckett, John Martin Clements, Mark Whittaker, Zoe Marie Spavold
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Patent number: 7282496Abstract: Compounds of the formula are useful in treating disease conditions mediated by TNF-?, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, graft rejection, cachexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease and HIV.Type: GrantFiled: November 1, 2002Date of Patent: October 16, 2007Assignee: Wyeth Holdings CorporationInventors: Vincent Premaratna Sandanayaka, Efren Guillermo Delos Santos
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Patent number: 7183276Abstract: The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or —NR2—W—D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.Type: GrantFiled: February 27, 2003Date of Patent: February 27, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Nozomu Sakai, Yu Momose, Katsuhito Murase, Masatoshi Hazama
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Patent number: 7179911Abstract: Processes for using a compound of formula III: to make compounds of formulae I and II: and processes for making the compound of formula III, where R1-5 and J are as defined herein.Type: GrantFiled: June 7, 2005Date of Patent: February 20, 2007Assignee: WyethInventors: Ting-Zhong Wang, Lalitha Krishnan, Joseph Zeldis, Jeremy I. Levin, Jean Schmid, Mellard Jennings, Huan-Qiu Li, Zhixin Wen
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Patent number: 7166590Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.Type: GrantFiled: May 28, 2002Date of Patent: January 23, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7122675Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.Type: GrantFiled: August 1, 2002Date of Patent: October 17, 2006Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
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Patent number: 7022846Abstract: Metabolites of a matrix metalloproteinase inhibitor prinomastat and their synthesis. These metabolites are: (3S)-N-hydroxy-4-(4-((1-oxy-pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl-tetrahydro-2H-1,4-thiazine-3-carboxamide (M6); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(1-oxy-pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M7); (3S)-2,2-dimethyl-4-[4-(1-oxypyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M8); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M2); and (3S)-2,2-dimethyl-4-[4-(pyridin-4yloxy)-benzenesulfonyl)-thiomorphpline-3-carboxylic acid amide (M3).Type: GrantFiled: June 10, 2003Date of Patent: April 4, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael A. Ouellette, Barbara C. M. Potts, Jayaram K. Srirangam, Anthony R. Tibbetts, Kanyin E. Zhang
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Patent number: 6849732Abstract: The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.Type: GrantFiled: November 18, 2002Date of Patent: February 1, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Scott E. Zook, Raymond Dagnino, Jr., Michael E. Deason, Steven L. Bender, Michael J. Melnick
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Patent number: 6756372Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: November 2, 2001Date of Patent: June 29, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Michel Jose Emmanuel, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward
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Patent number: 6685617Abstract: The present invention relates to compound of formula (I), that are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.Type: GrantFiled: March 9, 2001Date of Patent: February 3, 2004Assignees: Pharmacia & Upjohn Company, Tanabe Seiyaku Co., Ltd.Inventors: James Blinn, Robert Chrusciel, Jed Fisher, Steven Tanis, Edward Thomas, Thomas Lobl, Bradley Teegarden
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Patent number: 6649771Abstract: A pyrrolotriazole compound of the following formula (I), and a silver halide color photographic light-sensitive material containing the pyrrolotriazole compound as a cyan coupler: wherein R1 and R2 each independently are an alkyl, cycloalkyl, alkenyl, aryl or heterocyclic group, provided that R1 and R2 may bond together to form a 5- or 6-membered nitrogen-containing heterocycle; R3 is an alkyl, cycloalkyl, alkenyl, aryl or heterocyclic group; R4 is an alkyl, cycloalkyl, alkenyl, alkoxy or amino group; R5 is a hydrogen atom, an alkyl or aryl group; R6 is an alkyl, cycloalkyl or alkenyl group; and X is an oxygen or sulfur atom.Type: GrantFiled: March 26, 2001Date of Patent: November 18, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Takeshi Nakamine, Nobuo Seto, Hideaki Sato, Yasuaki Deguchi
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Publication number: 20030192138Abstract: This relates to a dye represented by Formulae II and IIA below: 1Type: ApplicationFiled: February 8, 2002Publication date: October 16, 2003Applicant: Eastman Kodak CompanyInventors: Margaret J. Helber, Douglas M. Willis, John DiCillo
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Patent number: 6599902Abstract: The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.Type: GrantFiled: May 30, 2002Date of Patent: July 29, 2003Assignee: Sugen, Inc.Inventors: Jingrong Cui, John Ramphal, Congxin Liang, Connie Li Sun, Chung Chen Wei, Peng Cho Tang
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Patent number: 6500948Abstract: The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.Type: GrantFiled: September 29, 2000Date of Patent: December 31, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Scott E. Zook, Raymond Dagnino, Jr., Michael E. Deason, Steven L. Bender, Michael J. Melnick
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Patent number: 6492421Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 30, 1998Date of Patent: December 10, 2002Assignees: Athena Neurosciences, Inc., American Home Products Corp.Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Louis John Lombardo, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen, Reinhardt Bernhard Baudy, Susan Ashwell
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Patent number: 6492394Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.Type: GrantFiled: December 22, 1999Date of Patent: December 10, 2002Assignee: Syntex (U.S.A.) LLCInventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
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Patent number: 6472526Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1): and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.Type: GrantFiled: December 3, 2001Date of Patent: October 29, 2002Assignee: LG Chemical Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6472527Abstract: New heterocyclic compounds are disclosed which are used as intermediates for the preparation of trans-thiazine-indigo pigments which are in part new compounds and can be used for the mass pigmentation of organic substrates. Also disclosed are different environmentally friendly water-based processes for the preparation of the new heterocyclic compounds and the corresponding pigments.Type: GrantFiled: March 15, 2000Date of Patent: October 29, 2002Assignee: Clariant Finance (BVI) LimitedInventors: Till Borchert, Bansi Lal Kaul, Bruno Piastra, Valérie Wolf
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Patent number: 6436980Abstract: Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.Type: GrantFiled: November 28, 2000Date of Patent: August 20, 2002Assignee: Essential Therapeutics, Inc.Inventors: Roger Leger, Ving J. Lee, Miles She
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Patent number: 6387896Abstract: The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R1, R2 and n are as defined in thereof.Type: GrantFiled: May 17, 2000Date of Patent: May 14, 2002Assignee: Pharmacia & Upjohn Co.Inventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Jr., Paul D. Johnson
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Patent number: 6384219Abstract: There is disclosed a 1H-pyrrolo-[1,2-b][1,2,4]triazole compound represented by formula (I): wherein R is an alkyl group; R1, R2, R3, R1′, R2′, and R3′ each are a hydrogen atom or an alkyl group; R1 and R2, and R1′ and R2′ may bond together to form a ring, respectively; R4 is a hydrogen atom or an alkyl group, and X is heterocyclic group, a substituted amino group, or an aryl group. The compound is useful as a photographic cyan coupler. There is also disclosed synthetic intermediates of the compound and a production method of the intermediates.Type: GrantFiled: January 7, 1998Date of Patent: May 7, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Yasuhiro Shimada, Hideki Maeta, Yoshio Shimura
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Publication number: 20020049193Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: ApplicationFiled: August 10, 2001Publication date: April 25, 2002Applicant: GPI NIL HOLDINGS, INC.Inventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
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Patent number: 6365587Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.Type: GrantFiled: May 13, 1999Date of Patent: April 2, 2002Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
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Patent number: 6355640Abstract: The present invention relates to a novel pyrazolopyridine compound of the following formula: wherein R1 is aryl, and R2 is cyclo(lower)alkyl which may have one or more suitable substituent(s), etc; and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said pyrazolopyridine compound or a salt thereof; a pharmaceutical composition comprising said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof; etc.Type: GrantFiled: May 6, 1998Date of Patent: March 12, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Atsushi Akahane, Shintaro Nishimura, Hiromichi Itani, Kieran P. M. Durkin
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Patent number: 6310080Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 1, 1999Date of Patent: October 30, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6303652Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: March 19, 1999Date of Patent: October 16, 2001Assignee: Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6268363Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.Type: GrantFiled: May 17, 2000Date of Patent: July 31, 2001Assignee: LG Chemical Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6265228Abstract: Combinatorial chemical libraries of the Formula [S]—C(O)—L′—Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and —L′—Z is a linker/ligand residue. In these libraries, Z is and Y is —P(O)(OR6)(OR7), —CH(OH)—COR8, —CH,CH═CH2—CH2CH(OH)CH2OH, —CH2CHO, —CH2CH2OH, —CH2CH2OC(O)NHR26, —CH2CH2NR27R28, or The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.Type: GrantFiled: June 18, 1999Date of Patent: July 24, 2001Assignee: Pharmacopeia, Inc.Inventors: Roland Ellwood Dolle, III, Timothee Felix Herpin, Yvonne Class Shimshock, Cullen Lee Cavallaro
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Patent number: 6262060Abstract: The invention relates to azacycloalkane derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to methods for the treatment of hyperglycaemia, diabetes, obesity or inflammation utilizing them.Type: GrantFiled: November 27, 2000Date of Patent: July 17, 2001Assignee: Sanofi-SynthelaboInventors: Manuel Bedoya-Zurita, Juan Antonio Diaz Martin, Marc Daumas
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Patent number: 6255305Abstract: Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.Type: GrantFiled: November 10, 1998Date of Patent: July 3, 2001Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, William Robert Carling, Jose Luis Castro Pineiro, Alexander Richard Guiblin, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Leslie Joseph Street