Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
-
Patent number: 7514435Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as antiproliferative agents.Type: GrantFiled: November 16, 2006Date of Patent: April 7, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Ping Chen, Yufen Zhao, Brian E. Fink, Soong-Hoon Kim
-
Publication number: 20090082354Abstract: A pyrazolo[5,1-c][1,2,4]triazine compound of formula A: and pharmaceutically acceptable sats thereof. The multiply-substituted pyrazolo[5,1-c][1,2,4]triazine compounds of the invention selectively inhibit B-Raf kinase activity and are useful for treating disorders mediated by B-Raf kinase.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Applicant: WyethInventors: Dan Maarten Berger, Minu Dhanjisha Dutia, Darrin William Hopper, Nancy Torres
-
Patent number: 7507734Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).Type: GrantFiled: November 16, 2006Date of Patent: March 24, 2009Assignee: Aventis Pharma S.A.Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
-
Publication number: 20090076011Abstract: The present application describes deuterium-enriched tirapazamine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 15, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Publication number: 20090062288Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: ApplicationFiled: October 28, 2008Publication date: March 5, 2009Inventors: Harold Mastalerz, Dolatrai M. Vyas, George L. Trainor, Ashvinikumar V. Gavai
-
Patent number: 7494996Abstract: This invention relates to dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad spectrum fungicides and insecticides. This invention also teaches methods of preparing these compounds as well as methods of using the compounds as fungicides and insecticides.Type: GrantFiled: October 26, 2001Date of Patent: February 24, 2009Assignee: Dow AgroSciences LLCInventors: Martha Jean Kelly, Karen Anderson Evans, James Joseph Gallagher, Mark Joseph Mulvihill
-
Publication number: 20090048244Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: ApplicationFiled: September 24, 2008Publication date: February 19, 2009Inventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
-
Publication number: 20090047243Abstract: The invention features compositions and methods employing combinations of an A2A receptor agonist and a PDE inhibitor for the treatment of a B-cell proliferative disorder, e.g., multiple myeloma.Type: ApplicationFiled: July 17, 2008Publication date: February 19, 2009Inventors: Richard Rickles, Laura Pierce, Margaret S. Lee
-
Publication number: 20090041675Abstract: A medicament comprising, separately or together, (A) a compound of formula I in free or salt or solvate form, where W, Rx, Ry, R1, R2, R3, R4, R5, R6 and R7 have the meanings as indicated in the specification, and (B) one or more of compounds selected from the group consisting of PDE4 inhibitors and PDE5 inhibitors, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.Type: ApplicationFiled: May 30, 2006Publication date: February 12, 2009Inventor: Alexandre Trifilieff
-
Patent number: 7485640Abstract: The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH?CH—, or —CH2—CH2—, —N?CH— or —CH?N—; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— or —OCH2— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.Type: GrantFiled: October 29, 2003Date of Patent: February 3, 2009Assignee: Merck Sharp & Dohme LimitedInventors: William Robert Carling, Jose Luis Castro Pineiro, Simon Charles Goodacre, David James Hallett, Leslie Joseph Street
-
Patent number: 7485654Abstract: The amide compound of the formula (I) [each symbol is as defined in the description] has a promoting action on neuritogenesis of trigeminal nerve cells, and the compound is useful as a corneal neuritogenesis promoter, an agent for recovering corneal sensitivity by promotion of corneal neuritogenesis, and an agent for treating dry eye.Type: GrantFiled: June 3, 2005Date of Patent: February 3, 2009Assignees: Senju Pharmaceutical Co., Ltd., Mitsubishi Tanabe Pharma CorporationInventors: Yoshiko Takayama, Yoshikuni Nakamura, Jun Inoue, Mitsuyoshi Azuma
-
Publication number: 20090018136Abstract: The present invention is directed to a novel methods and compositions for the therapeutic intervention of vascular complications associated with diabetes, hyperlipidemias, and various cardiovascular disorders including but not limited to recalcitrant hypertension, coronary artery disease, pulmonary arterial hypertension, congestive heart failure, and hemolytic anemias. More specifically, the specification describes methods and compositions for treating such vascular disorders using compositions comprising BH4 and derivative thereof. Combination therapies of BH4 and other therapeutic regimens are contemplated.Type: ApplicationFiled: June 5, 2008Publication date: January 15, 2009Inventors: Daniel I. Oppenheimer, Emil D. Kakkis, Alejandro Dorenbaum
-
Patent number: 7470689Abstract: Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).Type: GrantFiled: August 31, 2006Date of Patent: December 30, 2008Assignee: Aventis Pharma S.A.Inventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Günter Müller, Cécile Combeau, Christine Delaisi, Anke Steinmetz, Ingrid Sassoon
-
Publication number: 20080312239Abstract: A method of treatment of erectile dysfunction (ED) comprises the step of administering fispemifene to a subject in need thereof in an amount effective to raise the subject's testosterone level. Fispemifene may be used in combination with a PDE-5 inhibitor in individuals who have failed to respond sufficiently to conventional ED treatment. Methods are also disclosed of treating ED by administering clomifene, enclomifene, ospemifene, toremifene and mixtures thereof in combination with a PDE-5 inhibitor.Type: ApplicationFiled: June 13, 2008Publication date: December 18, 2008Applicant: QUATRX PHARMACEUTICALS COMPANYInventors: Robert L. Zerbe, Alexander Bridges, Risto Lammintausta, Rochelle Hanley, Stuart Dombey
-
Patent number: 7462614Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: GrantFiled: March 29, 2004Date of Patent: December 9, 2008Assignee: Smithkline Beecham CorporationInventors: Mui Cheung, Nigel Paul King, Kevin Wayne Kuntz, Robert Anthony Mook, Jr., Mark Andrew Pobanz, James Michael Salovich, Brian John Wilson
-
Patent number: 7462615Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.Type: GrantFiled: December 8, 2005Date of Patent: December 9, 2008Assignee: Hybrigenics SAInventors: Philippe Guedat, Guillaume Boissy, Catherine Borg-Capra, Frédéric Colland, Laurent Daviet, Etienne Formstecher, Xavier Jacq, Jean-Christophe Rain, Rémi Delansorne, Ilaria Peretto, Stefano Vignando
-
Patent number: 7462616Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: GrantFiled: October 24, 2006Date of Patent: December 9, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, John T. Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
-
Publication number: 20080293723Abstract: There are provided spiroindolinone derivatives of the formula and pharmaceutically acceptable salts and esters thereof wherein R1, R2, R3, R4 and R are as herein described. The compounds exhibit anticancer activity.Type: ApplicationFiled: April 11, 2008Publication date: November 27, 2008Inventors: Jin-Jun Liu, Zhuming Zhang
-
Publication number: 20080292626Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat a kinesin Eg5 protein-mediated disorder.Type: ApplicationFiled: May 22, 2008Publication date: November 27, 2008Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Ching-Cheng Wang, Hung-Chuan Chen, Shu-Huei Wang, Mei-Chun Lin, Tien-Lan Shieh, Ying-Huey Huang, Shih-Chieh Chuang, Chi-Hsin Richard King
-
Patent number: 7456176Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.Type: GrantFiled: April 7, 2005Date of Patent: November 25, 2008Assignee: TargeGen, Inc.Inventors: Glenn Noronha, Kathy Barrett, Jianguo Cao, Colleen Gritzen, Xianchang Gong, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Binqi Zeng, Ningning Zhao, Elena Dneprovskaia
-
Publication number: 20080269110Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I where R1, R1a, R1b, A, R3, R4, R5, R5b and R6 are as defined herein.Type: ApplicationFiled: April 25, 2008Publication date: October 30, 2008Inventors: William N. Washburn, Saleem Ahmad, Andres S. Hernandez
-
Publication number: 20080268046Abstract: The present invention relates to novel pharmaceutical dosage forms with controlled release of active ingredient which comprise the PDE 5 inhibitor vardenafil and/or pharmaceutically acceptable salts, hydrates, solvates and/or polymorphic forms thereof as active ingredient, and to the production thereof. The invention further relates to the use of these novel pharmaceutical dosage forms as medicaments, and to their use for producing medicaments for the treatment and/or prevention of disorders in humans and animals.Type: ApplicationFiled: April 29, 2005Publication date: October 30, 2008Applicant: BAYER HEALTHCARE AGInventors: Susanne Zuleger, Peter Serno, Helmut Haning, Kerstin Pauli, Roland Heinig
-
Patent number: 7442700Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: GrantFiled: June 27, 2006Date of Patent: October 28, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Harold Mastalerz, Dolatrai M. Vyas, George L. Trainor, Ashvinikumar V. Gavai
-
Publication number: 20080261974Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.Type: ApplicationFiled: September 22, 2006Publication date: October 23, 2008Inventors: Kevin J Duffy, Duke M. Fitch, Rosanna Tedesco, Michael N. Zimmerman
-
Publication number: 20080253988Abstract: A compound of formula (I): wherein the substituents are as defined in the specification as inhibitor of C-Jun N terminal Kinases (JNK) and P-38 Kinases.Type: ApplicationFiled: October 25, 2005Publication date: October 16, 2008Applicant: NOVARTIS AGInventor: Qing Dong
-
Publication number: 20080249096Abstract: The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.Type: ApplicationFiled: February 16, 2006Publication date: October 9, 2008Applicant: BAYER HEALTHCARE AGInventors: Peter Serno, Roland Heinig, Kerstin Pauli, Yutaka Hayauchi
-
Publication number: 20080234276Abstract: The invention relates to novel heterocyclic triazines which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation by administering effective amounts of such compounds.Type: ApplicationFiled: February 1, 2006Publication date: September 25, 2008Applicant: SENTINEL ONCOLOGY LIMITEDInventors: Robert George Boyle, Stuart Travers
-
Publication number: 20080234277Abstract: The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, X1, X2, X3, Y, Z, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used in treating or preventing diseases which are modulated by HM74A agonists.Type: ApplicationFiled: March 17, 2008Publication date: September 25, 2008Inventors: Aurelia Conte, Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Holger Kuehne, Robert Narquizian, Constantinos G. Panousis, Jens-Uwe Peters, Fabienne Ricklin
-
Publication number: 20080221108Abstract: Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2 and W, are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.Type: ApplicationFiled: February 14, 2006Publication date: September 11, 2008Inventors: Richard Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto, Ian Edward David Smith
-
Patent number: 7419978Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.Type: GrantFiled: October 21, 2004Date of Patent: September 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, John Hynes, Katerina Leftheris, Shuqun Lin, Stephen T. Wrobleski, Hong Wu
-
Publication number: 20080200449Abstract: Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.Type: ApplicationFiled: May 14, 2007Publication date: August 21, 2008Inventors: Horst Olschewski, Robert Roscigno, Lewis J. Rubin, Thomas Schmehl, Werner Seeger, Carl Sterritt, Robert Voswinckel
-
Publication number: 20080200468Abstract: Therapeutically active heteroaryl carboxylic acid derivatives of Formula (I) wherein R1, R2, W, X, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.Type: ApplicationFiled: February 14, 2006Publication date: August 21, 2008Inventors: Juliet Kay Simpson, Ivan Leo Pinto
-
Patent number: 7405213Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: GrantFiled: June 27, 2006Date of Patent: July 29, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ping Chen, Derek J. Norris, Ashvinikumar V. Gavai
-
Publication number: 20080176844Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or pharmaceutically acceptable salt, stereoisomer, or hydrate thereof, wherein R1 is lower alkyl, R2 and R3 are independently selected from lower alkyl, and lower alkenyl and lower alkynyl, wherein the lower alkyl, lower alkenyl, and lower alkynyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio, A is N or C—H, B is N, C—H, C—(SO2—R4), or C—CO—R4, D is N, C—H, C—(SO2—R4) or C—CO—R4, E is N or C—H, wherein only one of A, B or E may be N, and one of B or D is C—(SO2—R4) or C—CO—R4, R4 is a group having the formula: in which each R5, R6, R7 and R8 are independently selected from H and lower alkyl, wherein the lower alkyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio; and additionally or alternatively R6 and R5Type: ApplicationFiled: February 21, 2006Publication date: July 24, 2008Inventors: Stewart Campbell, David Duffy, Michael Grogan, Steven Kates, Emanuele Ostuni, Olivier Schueller, Paul Sweetnam
-
Patent number: 7402582Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: GrantFiled: June 27, 2006Date of Patent: July 22, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ashvinikumar V. Gavai, Ping Chen, Derek J. Norris
-
Publication number: 20080171745Abstract: The invention provides ?-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, R1 and R2 as set out in the description and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of fibrotic diseases, such as pulmonary fibrosis.Type: ApplicationFiled: September 25, 2007Publication date: July 17, 2008Applicants: UNIVERSITY OF WASHINGTON, INSTITUTE FOR CHEMICAL GENOMICSInventors: William R. HENDERSON, Michael KAHN
-
Publication number: 20080171746Abstract: The invention relates to a method for selecting COX-2 selective NSAIDs which have a salutary therapeutic profile. The invention further relates to the use of these selected COX-2 selective NSAIDs in the treatment of certain diseases. The invention yet further relates to combinations comprising COX-2 selective NSAIDs and the use of these combinations.Type: ApplicationFiled: March 14, 2006Publication date: July 17, 2008Inventors: Thomas Klein, Manfrid Eltze, Armin Hatzelmann
-
Publication number: 20080171741Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: October 25, 2007Publication date: July 17, 2008Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
-
Publication number: 20080167287Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: ApplicationFiled: November 19, 2007Publication date: July 10, 2008Applicant: INCYTE CORPORATIONInventors: Jincong Zhuo, Meizhong Xu, Chunhong He, Colin Zhang, Ding-Quan Qian, David M. Burns, Yun-Long Li, Brian Metcalf, Wenqing Yao
-
Publication number: 20080167291Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulation angiotensin activity to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: May 9, 2007Publication date: July 10, 2008Applicant: BrainCells, Inc.Inventors: Carolee Barlow, Todd A. Carter, Kai Treuner, Kym I. Lorrain
-
Publication number: 20080161249Abstract: The present invention relates to the use of novel antibacterial compounds, and pharmaceutical compositions containing these compounds.Type: ApplicationFiled: November 17, 2005Publication date: July 3, 2008Applicant: SMITHKLINE BEECHAM CORPORATIONInventor: Jianzhong Huang
-
Patent number: 7388019Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 27, 2004Date of Patent: June 17, 2008Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Charles G. Caldwell, Joseph L. Duffy, Robert J. Mathvink, Liping Wang, Ann E. Weber
-
Patent number: 7388009Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: GrantFiled: October 3, 2003Date of Patent: June 17, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Katerina Leftheris, Stephen T. Wrobleski, Alaric J. Dyckman
-
Publication number: 20080139565Abstract: Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2, W, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.Type: ApplicationFiled: February 14, 2006Publication date: June 12, 2008Inventors: Matthew Campbell, Andrew McMurtrie Mason, Ivan Leo Pinto, Ian Edward David Smith
-
Publication number: 20080096880Abstract: The invention relates to novel uses of imidazo[1,2,4]triazinones for producing a medicament for the treatment and/or prophylaxis of coronary cardiopathy, heart failure, pulmonary hypertension, bladder complaints, prostatic hyperplasia, nitrate-induced tolerance, or diseases of the eye, such as glaucoma, for the treatment or prophylaxis of central, retinal or posterior ciliary artery occlusion, central retinal vein occlusion, optical neuropathy, such as anterior ischaemic optical neuropathy and glaucomatous optical neuropathy, in addition to macular degeneration, diabetes, in particular diabetic gastroparesis, for the treatment of dysperistalsis of the stomach and oesophagus, female infertility, premature contractions, pre-eclampsia, alopecia, psoriasis associated with renal syndrome, cystic fibrosis, cancer and for improving cognition, powers of concentration, learning skills or hypermnesia, in particular if the disorder is a symptom of dementia.Type: ApplicationFiled: June 24, 2003Publication date: April 24, 2008Applicant: Bayer Heakthcare AGInventors: Helmut Haning, Erwin Bischoff, Ulrich Niewohner, Maria Niewohner
-
Patent number: 7348325Abstract: In general, the instant invention comprises compounds having Formulae I and II: including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.Type: GrantFiled: November 28, 2006Date of Patent: March 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Zhen-Wei Cai, Kyoung S. Kim, Robert M. Borzilleri
-
Patent number: 7332485Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: July 8, 2004Date of Patent: February 19, 2008Assignee: SmithKline Beecham CorpInventors: Kelly M. Aubart, Siegfried Benjamin Christensen, IV, Chaya Duraiswami, Joseph M. Karpinski
-
Patent number: 7317012Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formulas I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein B, R1, R2, R3 and x are described herein.Type: GrantFiled: June 16, 2006Date of Patent: January 8, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Chongqing Sun, Yanting Huang, Doree F. Sitkoff, Guixue Yu, Amarendra Mikkilineni, William R. Ewing
-
Patent number: 7314876Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are surprisingly advantageous as p38 kinase inhibitors, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, NH2, or NH(CH3), preferably methyl; X is N or CH; and R1 through R6 are as described in the specification.Type: GrantFiled: April 22, 2003Date of Patent: January 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, Katerina Leftheris, John Hynes, Arthur M P. Doweyko
-
Patent number: 7314871Abstract: The application claims a method for treating hypertension by administering an effective amount of a compound of the formula (I) wherein the variable groups are as defined in the specification and claims. These 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: GrantFiled: April 21, 2006Date of Patent: January 1, 2008Assignee: Bayer AktiengesellschaftInventors: Maria Niewöhner, legal representative, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski, Ulrich Niewöhner, deceased