Chalcogen Bonded Directly To A Ring Carbon Of The Six-membered Hetero Ring Patents (Class 514/335)
-
Publication number: 20090286786Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: ApplicationFiled: March 10, 2009Publication date: November 19, 2009Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
-
Publication number: 20090270360Abstract: The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, Rc, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: ApplicationFiled: January 16, 2009Publication date: October 29, 2009Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Jacques Himber, Roland Humm, Hans Iding, Dietmar Knopp, Narendra Panday, Fabienne Ricklin, Christoph Martin Stahl
-
Patent number: 7605164Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: February 14, 2006Date of Patent: October 20, 2009Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
-
Publication number: 20090258884Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: ApplicationFiled: April 16, 2009Publication date: October 15, 2009Inventors: William K. Hagmann, Linus S. Lin, Shrenik K. Shah, Ravindra N. Guthikonda, Hongbo Qi, Linda L. Chang, Ping Liu, Helen M. Armstrong, James P. Jewell, Thomas J. Lanza, JR.
-
Publication number: 20090192196Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a 6-membered heterocycle, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 12, 2007Publication date: July 30, 2009Inventors: Isabelle Christian, Marie-Claire Grosjean-Cournoyer, Pierre Hutin, Philippe Rinolfi, Arounarith Tuch, Jacky Vidal
-
Publication number: 20090149439Abstract: The present invention relates to a novel compound having an effect of inhibiting production/secretion of ?-amyloid protein. The present invention provides a compound represented by the general formula (1): or a salt thereof, or a solvate of the compound or the salt; and a medicament comprising thereof.Type: ApplicationFiled: April 7, 2006Publication date: June 11, 2009Applicant: Daiichi Sankyo Company LimitedInventors: Satoru Miyauchi, Hideki Kubota, Kayoko Motoki, Masayuki Ito
-
Patent number: 7544702Abstract: Bisaryl-sulfonamide compounds having the formula wherein Ar, R1, R2, L, B, W, X, Y, and Z, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR? or PPAR?. In particular, the compounds of the invention modulate the function of PPAR? or PPAR?. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.Type: GrantFiled: August 11, 2005Date of Patent: June 9, 2009Assignee: Amgen Inc.Inventors: Philippe Bergeron, Christopher N. Farthing, Stuart D. Jones, John W. Liebeschuetz, Sarah E. Lively, Lawrence R. McGee, Sharon McKendry, David Sheppard, Stephen C. Young
-
Patent number: 7544703Abstract: A novel cyclic compound having a 4-pyridylalkylthio group having an (un)substituted amino group introduced therein or a salt thereof. They are useful as a medicine. The cyclic compound is a compound represented by the following formula (1), which is useful for the treatment of diseases in which angiogenesis participates. In the following formula (1), ring A represents a benzene ring or a 5- or 6-membered aromatic heterocycle optionally fused with a cycloalkane ring; B represents alkylene; R1 and R2 each represents H, (substituted) aryl, (substituted) heterocyclic group, etc.; R3 and R4 each represents H, (substituted) alkyl, (substituted) cycloalkyl, -Z-R5, etc.; R5 represents (substituted) alkyl, (substituted) aryl, (substituted) heterocyclic group, etc.; X and Y each represents H, etc.; Z represents —CO—, —COO—, —CONR6—, —SO2—, etc.; R6 represents H, etc.; p is 0, 1, or 2; and q is 0 or 1.Type: GrantFiled: February 17, 2005Date of Patent: June 9, 2009Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takahiro Honda, Hisashi Tajima, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Takaaki Inaba, Yuriko Takeno
-
Publication number: 20090131435Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, and X are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 20, 2009Publication date: May 21, 2009Applicant: Array BioPharma Inc.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
-
Publication number: 20090118333Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Weichuan Caroline Chen, Paul Krenitsky, Andreas Termin, Dean Wilson
-
Publication number: 20090111852Abstract: A carboxamide compound represented by the formula (1): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, one of ring constitutional atoms of the heterocyclic group is a nitrogen atom and the heterocyclic group may be substituted with a group selected from the group consisting of a C1-C3 alkyl and the like, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom or the like] and a plant disease controlling agent comprising this as an active ingredient.Type: ApplicationFiled: July 12, 2006Publication date: April 30, 2009Applicant: Sumitomo Chemical Company, LimitedInventors: Shin-ichiro Souma, Yoshiharu Kinoshita
-
Publication number: 20090105255Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: December 17, 2007Publication date: April 23, 2009Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
-
Publication number: 20090099184Abstract: Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.Type: ApplicationFiled: February 15, 2007Publication date: April 16, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephane Delombaert, Anne Bettina Eldrup, Neil Alexander Farrow, Jennifer A. Kowalski, Ingo Andreas Mugge, Fariba Soleymanzadeh, Alan David Swinamer, Steve John Taylor
-
Patent number: 7507767Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: February 6, 2002Date of Patent: March 24, 2009Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
-
Publication number: 20090069179Abstract: The present invention relates to pyridin-4-ylmethylamides of the general formula (I), where R1 to R6 and n are as defined in the claims and to the N-oxides and the agriculturally acceptable salts of the compounds I. The invention also relates to a process for preparing these compounds. Furthermore, the invention relates to the use of the compounds I and the N-oxides and the agriculturally acceptable salts thereof for combating phytopathogenic fungi (hereinafter referred to as harmful fungi). Furthermore the compounds I, their N-oxides and salts can be used for controlling arthropodal pests.Type: ApplicationFiled: February 13, 2007Publication date: March 12, 2009Applicant: BASF SEInventors: Jan Klaas Lohmann, Wassilios Grammenos, Michael Puhl, Jochen Dietz, Bernd Muller, Joachim Rheinheimer, Jens Renner
-
Publication number: 20090054352Abstract: Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli. Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.Type: ApplicationFiled: November 7, 2006Publication date: February 26, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Fukushi Hirayama, Jiro Fujiyasu, Daisuke Kaga, Kenji Negoro, Daisuke Sasuga, Norio Seki, Ken-ichi Suzuki
-
Publication number: 20090048269Abstract: The invention relates to chemical compounds of the formula (I), or pharmaceutically acceptable salts thereof, which possess ALK5 (TGF?R1) inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal such as man.Type: ApplicationFiled: August 12, 2008Publication date: February 19, 2009Applicant: AstraZeneca ABInventors: Maurice Raymond Finlay, Frederick Woolf Goldberg, Craig Anthony Roberts, Nicola Jane Roberts, David Alan Rudge
-
Patent number: 7485641Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.Type: GrantFiled: June 18, 2007Date of Patent: February 3, 2009Assignee: Pfizer, Inc.Inventors: David W. Piotrowski, Yu Hui, John W. Benbow
-
Publication number: 20090018145Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreating carcinomas) and mesotheliomas.Type: ApplicationFiled: October 18, 2005Publication date: January 15, 2009Applicant: Compass Pharmaceuticals LLCInventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
-
Publication number: 20080306108Abstract: Compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising a pyridoxine analogue.Type: ApplicationFiled: June 6, 2008Publication date: December 11, 2008Applicant: MEDICURE INTERNATIONAL INC.Inventors: Wasimul Haque, James Diakur, Vinh Pham, Wenlian Zhang
-
Patent number: 7459562Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: GrantFiled: April 21, 2005Date of Patent: December 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Lyndon A. M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
-
Publication number: 20080293684Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: July 26, 2005Publication date: November 27, 2008Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
-
Publication number: 20080280905Abstract: The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: ApplicationFiled: May 8, 2008Publication date: November 13, 2008Applicant: Bristol Myers Squibb CompanyInventors: Hannguang J. Chao, Huji Tuerdi, Timothy F. Herpin, Jaques Yves Roberge, Yalei Liu, R. Michael Lawrence, Robert P. Rehfuss, Charles G. Clark, Jennifer X. Qiao, Timur Gungor, Patrick Y. S. Lam, Tammy Wang, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Gilles Bouthillier, Dora M. Schnur
-
Publication number: 20080280904Abstract: Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.Type: ApplicationFiled: October 4, 2006Publication date: November 13, 2008Inventors: Anne Bettina Eldrup, Fariba Soleymanzadeh, Steven John Taylor
-
Patent number: 7442702Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 25, 2002Date of Patent: October 28, 2008Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
-
Publication number: 20080249133Abstract: The present invention relates to the use of substituted 2-thio-3,5-dicyano-4-phenyl-6-amino-pyridines of the formula (I) for production of a medicament for the prophylaxis and/or treatment of nausea and vomiting.Type: ApplicationFiled: June 23, 2005Publication date: October 9, 2008Applicant: Bayer Healthcare AGInventors: Thomas Krahn, Wolfgang Thielemann, Ulrich Rosentreter, Nicole Diedrichs, Thomas Kramer
-
Publication number: 20080207695Abstract: There is provided a compound of formula (I) wherein R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6 to R8, A and G have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).Type: ApplicationFiled: June 14, 2006Publication date: August 28, 2008Applicant: ASTRAZENECA ABInventors: Ingemar Nilsson, Magnus Polla
-
Publication number: 20080171692Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: ApplicationFiled: February 1, 2008Publication date: July 17, 2008Inventors: William K. Hagmann, Linus S. Lin, Shrenik K. Shah, Ravindra N. Guthikonda, Hongbo Qi, Linda L. Chang, Ping Liu, Helen M. Armstrong, James P. Jewell, Thomas J. Lanza
-
Publication number: 20080139557Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: September 11, 2007Publication date: June 12, 2008Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Tony Lee, James W. Darrow, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt
-
Publication number: 20080114033Abstract: The invention is directed to pyridinone compounds useful for modulating Met kinase, having the following structure: and is further directed to pharmaceutical compositions comprising the compound; and methods for treating proliferative diseases, such as cancer by the administration of this compound.Type: ApplicationFiled: November 8, 2007Publication date: May 15, 2008Inventors: Robert M. Borzilleri, Gretchen M. Schroeder, Zhen-Wei Cai
-
Patent number: 7262209Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: October 2, 2002Date of Patent: August 28, 2007Assignee: Novartis Animal Health US, Inc.Inventors: Thomas Goebel, Pierre Ducray
-
Patent number: 7074742Abstract: Compounds of Formula (I), their N-oxides and agriculturally suitable salts are disclosed which are useful as fungicides formula (I), (II) wherein A is a substituted pyridinyl ring; B is a substituted pyridinyl ring; W is C=L or SOn is O or S; R1 and R2 are each independently H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; R3 is H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl or C3-C8 dialkylaminocarbonyl; R4 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; X is O or S; and n is 1 or 2; provided that when W is C?O and R1, R2 and R3 are H; then B is other than 4-trifluoromethyl-3-pyridinyl, 2-chloro-4-pyridinyl and 2,6-dihalo-4-pyridinyl.Type: GrantFiled: September 17, 2001Date of Patent: July 11, 2006Assignee: E. I. du Pont de Nemours and CompanyInventors: Timothy Donald Neubert, David Walter Piotrowski, Michael Paul Walker
-
Patent number: 7067539Abstract: The invention relates to compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: August 7, 2002Date of Patent: June 27, 2006Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
-
Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
-
Patent number: 7053094Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: January 20, 2005Date of Patent: May 30, 2006Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
-
Patent number: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
-
Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
-
Patent number: 6953798Abstract: Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra?)R??(1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of ?4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: November 29, 1999Date of Patent: October 11, 2005Assignee: Celltech R&D LimitedInventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
-
Patent number: 6943180Abstract: Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, rhinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: March 15, 2002Date of Patent: September 13, 2005Assignee: Merck & Co., Inc.Inventors: George Doherty, Linus S Lin, William K. Hagmann, Ginger Xu-qiang Yang, Linda L. Chang, Shrenik K. Shah, Richard A. Mumford, Theodore Kamenecka
-
Patent number: 6939881Abstract: Methods for preventing ulcers, such as gastric ulcers, in a horse about to undergo stress that causes gastric ulcers and prior to occurrence of a gastric ulcer condition in the horse involving administering a proton pump inhibitor (PPI) are disclosed and claimed.Type: GrantFiled: May 29, 2001Date of Patent: September 6, 2005Inventor: Frank Pipers
-
Patent number: 6927225Abstract: The present invention relates to compounds of Formula I: wherein: represents a 6-membered heterocyclic aromatic ring in which X1 is N, and X2, X3 and X4 are CR?; wherein R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORz in which Rz is H or C1-C3 alkyl; and c) A represents (i) C2-C14 alkenyl, or C2-C14 alkynyl, all of which may be branched or unbranched, unsubstituted or substituted with halogen, hydroxy, nitro, aroyl, aryloxy, C1-C8 acyloxy, C1-C6 alkylthio, arylthio, aryl, heteroaryl, heteroarylthio, heteroaryloxy, C1-C6 acyl, C1-C6 haloalkyl, C1-C6 alkoxy or C1-C6 haloalkoxy, and (ii) C3-C14 cycloalkyl, containing 0 heteroatoms and 0-2 unsaturations, substituted with aryloxy, heteroaryloxy, C1-C6 alkylthio, aType: GrantFiled: December 2, 2002Date of Patent: August 9, 2005Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
-
Patent number: 6921756Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
-
Patent number: 6919343Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: January 30, 2003Date of Patent: July 19, 2005Assignee: Merck & Co., Inc.Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Dong-Mei Feng, Scott D. Kuduk, Dai-Shi Su, Jenny Miu-chun Wai
-
Patent number: 6908923Abstract: Certain substituted benzamide derivatives of Formula I: selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 20, 2002Date of Patent: June 21, 2005Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
-
Patent number: 6903118Abstract: The invention relates to new piperazinyl-substituted pyridylalkane, alkene, and alkine acid amides substituted with saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to the general formula (I) as well as methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: June 7, 2005Assignee: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
-
Patent number: 6884791Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
-
Patent number: 6881736Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: wherein R1 is Het or Ar R2 is or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 7, 2000Date of Patent: April 19, 2005Assignee: SmithKline Beecham CorporationInventors: Peter J. Manley, William H. Miller, Irene N. Uzinskas
-
Patent number: 6878723Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.Type: GrantFiled: April 6, 2000Date of Patent: April 12, 2005Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), BioprojetInventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
-
Patent number: 6833378Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: January 17, 2001Date of Patent: December 21, 2004Assignee: Pfizer IncInventor: Yuhpyng L. Chen
-
Patent number: 6821963Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: June 4, 2002Date of Patent: November 23, 2004Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle