Four Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 544/184)
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Publication number: 20090163468Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: ApplicationFiled: December 2, 2008Publication date: June 25, 2009Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joesph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
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Publication number: 20090156594Abstract: The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.Type: ApplicationFiled: May 21, 2008Publication date: June 18, 2009Applicant: SGX Pharmaceuticals, Inc.Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth A. Jefferson, Jorg Hendle, Patrick S. Lee, Angelina Marie Thayer, Gavin Charles Hirst
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Publication number: 20090156604Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: ApplicationFiled: August 14, 2008Publication date: June 18, 2009Inventors: Swen HOLDER, Armin Zulch, Thomas Bar, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
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Publication number: 20090143356Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.Type: ApplicationFiled: October 26, 2006Publication date: June 4, 2009Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090124609Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 15, 2008Publication date: May 14, 2009Applicant: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20090082564Abstract: Magenta chromophore dyes which are stabilized by adding steric hindering groups to protect the imino carbons; nonlimiting examples of the steric hindering groups being phenyl, methyl, ethyl, isopropyl, fluoride, chloride, bromide and iodide groups.Type: ApplicationFiled: September 24, 2008Publication date: March 26, 2009Inventor: Larrie A. Deardurff
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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
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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
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Patent number: 7473669Abstract: This invention relates to substituted dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad spectrum fungicides. This invention also teaches methods of preparing these compounds as well as methods of using the compounds as fungicides.Type: GrantFiled: May 3, 2006Date of Patent: January 6, 2009Assignee: Dow AgroSciences LLCInventors: Steven Howard Shaber, Maurice Chee Hoong Yap, Kevin Gerald Meyer, Noormohamed Mohamed Niyaz, Brent Jeffrey Rieder, Michael Thomas Sullenberger, William Randal Erickson, Frisby Davis Smith
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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
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Publication number: 20080312218Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.Type: ApplicationFiled: September 21, 2006Publication date: December 18, 2008Inventors: Duane A. Burnett, Wen-Lian Wu
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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
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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
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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
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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
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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
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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
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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
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Publication number: 20080167304Abstract: 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: ApplicationFiled: March 13, 2008Publication date: July 10, 2008Inventors: Jagabandhu Das, John Hynes, Katerina Leftheris, Shuqun Lin, Stephen T. Wrobleski, Hong Wu
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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
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Publication number: 20080103149Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim 1Type: ApplicationFiled: October 30, 2006Publication date: May 1, 2008Inventors: Philippe GUEDAT, Xavier Jacq, Frederic Colland, Laurent Daviet, Etienne Formstecher, Jean-Christophe Rain, Matteo Colombo
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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
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Publication number: 20080076921Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: March 28, 2007Publication date: March 27, 2008Applicant: PHARMACYCLICS, INC.Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 7326475Abstract: The present invention provides: an organic EL element exhibiting high luminance, a high external quantum efficiency and a long high temperature driving life at 50° C.; an illuminator and a display device employing the organic EL element; and a material preferably used for the organic EL element.Type: GrantFiled: April 20, 2004Date of Patent: February 5, 2008Assignee: Konica Minolta Holdings, Inc.Inventors: Eisaku Katoh, Hiroshi Kita, Tomohiro Oshiyama, Mitsuhiro Fukuda, Yoshiyuki Suzuri, Noriko Ueda
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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
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Publication number: 20070213300Abstract: Compounds having the Formula (I), including pharmaceutically acceptable salts thereof, wherein at least one of X1, X2 or X3 is and any remaining X1, X2 or X3 is hydrogen, which are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, A1, A2 and m are as described herein.Type: ApplicationFiled: March 6, 2007Publication date: September 13, 2007Inventors: Chunjian Liu, Katerina Leftheris, Vivekananda M. Vrudhula, James Lin
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Patent number: 7253167Abstract: The present invention relates to compounds having the formula, wherein, Q is optionally substituted aryl or heteroaryl, R1 is hydrogen or C1-4alkyl, and R2, R3, R4 and R5 are hydrogen or optional substituents as defined in the specification.Type: GrantFiled: June 29, 2005Date of Patent: August 7, 2007Assignee: Bristol-Myers Squibb CompanyInventors: James Lin, Stephen T. Wrobleski, Chunjian Liu, Katerina Leftheris
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Patent number: 7241763Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein, the use of such compounds as inhibitors of cyclin-dependent serine/threonine kinases (Cdks), as well as kinases and phosphatases involved in cell cycle regulation such as the tyrosine kinases Wee1, Mik1 and Myt1 or the tyrosine dephosphatases such as Cdc25 and Pyp3. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating cell proliferative disorders such as atherosclerosis, restenosis and cancer.Type: GrantFiled: July 8, 2003Date of Patent: July 10, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Jean Fernand Armand LaCrampe, Richard William Connors, Chih Yung Ho, Alan Richardson, Eddy Jean Edgard Freyne, Peter Jacobus Johannes Buijnsters, Annette Cornelia Bakker
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Patent number: 7232822Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: March 17, 2004Date of Patent: June 19, 2007Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Patent number: 7202243Abstract: The invention relates to new substituted imidazotriazines, processes for their preparation and their use for the production of medicaments for the treatment and/or prophylaxis of cancer and neurodegenerative disorders, in particular of Parkinson's disease and of schizophrenia.Type: GrantFiled: June 25, 2003Date of Patent: April 10, 2007Assignee: Bayer HealthCare AGInventors: Martin Hendrix, David Brückner, Arno Friedl, Irene Gerlach, Volker Hinz, Jörg Keldenich, Frank Mauler, Maria Niewöhner, legal representative, Dagmar Karthaus, Karl-Heinz Schlemmer, Adrian Tersteegen, Özkan Yalkinoglu, Ulrich Niewöhner, deceased
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Patent number: 7199121Abstract: Use of a compound of formula (I): wherein each R, which are the same or different, is H or C1–C6 alkyl, and X completes a ring which is a substituted triazine having one of the following formulae (II) to (IV): wherein R? is H or C1–C6 alkyl; or an enol tautomer of a compound of formula (I) in which any of the groups R or R? is hydrogen; in the manufacture of a medicament for use as a protein tyrosine phosphatase (PTP) inhibitor. Formula (I) embraces 2-methylfervenulone, which can be produced by fermentation of a novel microbial strain. Fermentation of the said strain also produces novel precursors to 2-methylfervenulone having utility as prodrugs.Type: GrantFiled: September 7, 2001Date of Patent: April 3, 2007Assignee: Institute of Molecular and Cell BiologyInventors: Catherine J. Pallen, Haishan Wang, Kah Leong Lim, Su Ling Yeo, Yue Wang, Yin Hwee Tan
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Patent number: 7196095Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosisType: GrantFiled: June 21, 2002Date of Patent: March 27, 2007Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Richard Beresis, Richard Berger, Steven L. Colletti, James B. Doherty, Dennis D. Feng, Gui-Bai Liang, Dennis M. Schmatz, Xiaoxia Qian, David A. Claremon, Nigel J. Liverton, Charles J. McIntyre, Ernest W. Kovacs
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Patent number: 7176203Abstract: A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: May 1, 2003Date of Patent: February 13, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Robert James Maxey, Michael Geoffrey Neil Russell, Leslie Joseph Street
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Patent number: 7122548Abstract: The present invention relates to compounds of the Formula (I), and their pharmaceutically acceptable salts.Type: GrantFiled: June 24, 2004Date of Patent: October 17, 2006Assignee: Sugen, Inc.Inventors: Fang-Jie Zhang, Tomas Vojkovsky, Ping Huang, Congxin Liang, Steven Huy Do, Marcel Koenig, Jingrong Cui
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Patent number: 7115602Abstract: The invention relates to 7-(4-tert butyl-cyclohexyl)-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.Type: GrantFiled: May 30, 2002Date of Patent: October 3, 2006Assignee: Bayer AktiengesellschaftInventors: Cristina Alonso-Alija, Heike Gielen, Martin Hendrix, Maria Niewöhner, Dagmar Schauss, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel J. Cuthbert, Mary F. Fitzgerald, Graham Sturton, Ulrich Niewöhner
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Patent number: 7098207Abstract: Novel imidazotriazinones of general formula a method for the production and the pharmaceutical use thereof are disclosed.Type: GrantFiled: January 5, 2005Date of Patent: August 29, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Maria Niewohner, legal representative, Mazen Es-Sayed, Thomas Lampe, Helmut Haning, Gunter Schmidt, Karl-Heinz Schlemmer, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Ulrich Niewohner, deceased
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Patent number: 7087605Abstract: The invention relates to novel 5-Ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.Type: GrantFiled: May 21, 2002Date of Patent: August 8, 2006Assignee: Bayer AktiengesellschaftInventors: Cristina Alonso-Alija, Heike Gielen, Martin Hendrix, Maria Theresia Niewohner, legal representative, Dagmar Schauss, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel J. Cuthbert, Mary F. Fitzgerald, Richard Graham Sturton, Martin Michels, Ulrich Niewohner, deceased
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Patent number: 7074790Abstract: The invention relates to novel 5-ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.Type: GrantFiled: May 5, 2003Date of Patent: July 11, 2006Inventors: Cristina Alonso-Alija, Heike Gielen-Haertwig, Martin Michels, Dagmar Karthaus, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel Cuthbert, Mary F. Fitzgerald, Graham Sturton, Maria Theresia Niewöhner, legal representative, Ulrich Niewöhner, deceased
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Patent number: 7037909Abstract: The present invention relates to compounds of the Formulae (I) and (II), wherein R1-R10 and G are defined herein, and their pharmaceutically acceptable salts. These compounds modulate the activity of c-Met and are therefore expected to be useful in the prevention and treatment of c-Met related disorders such as cancer.Type: GrantFiled: June 29, 2004Date of Patent: May 2, 2006Assignee: Sugen, Inc.Inventors: Tomas Vojkovsky, Marcel Koenig, Fang-Jie Zhang, Jingrong Cui
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Patent number: 7037910Abstract: 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 Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, and R4 are described herein.Type: GrantFiled: December 17, 2004Date of Patent: May 2, 2006Assignee: Bristol-Myers SquibbInventors: William R. Ewing, Guixue Yu, Bruce A. Ellsworth
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Patent number: 7022847Abstract: The invention relates to a method for the production of 2-phenyl-substituted imidazotriazinones of general formula (I), comprising the reaction of compounds of formula (II) with compounds of formula (III) and subsequent reaction with iodine or bromine, then with a metal cyanide and reaction with an acid.Type: GrantFiled: December 5, 2001Date of Patent: April 4, 2006Assignee: Bayer HealthCare AktiengesellschaftInventors: Marc Nowakowski, Alexander Vetter
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Patent number: 7005431Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: May 1, 2003Date of Patent: February 28, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Michela Bettati, Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Michael Geoffrey Neil Russell, Leslie Jospeh Street
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Patent number: 6998402Abstract: The invention relates to novel substituted imidazotriazinones, to a method for their production and to the use thereof for producing medicaments, in particular to improve perception, powers of concentration, learning capacity and/or memory retentiveness.Type: GrantFiled: February 11, 2002Date of Patent: February 14, 2006Assignee: Bayer AktiengesellschaftInventors: Maria Theresia Niewöhner, legal representative, Dagmar Schauss, Gerhard König, Martin Hendrix, Frank-Gerhard Böss, Franz-Josef van der Staay, Rudy Schreiber, Karl-Heinz Schlemmer, Toshiya Moriwaki, Ulrich Niewöhner, deceased
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Patent number: 6998483Abstract: The present invention relates to a process for the preparation of sulphonamide-substituted imidazotriazinones of the general formula (I) characterized in that compounds of the formula (II) are reacted with sulphuric acid and the products obtained are then reacted with thionyl chloride and converted in situ in an inert solvent using an amine into the compounds according to the invention and, if appropriate, reacted to give the corresponding salts, hydrates or N-oxides.Type: GrantFiled: May 5, 2005Date of Patent: February 14, 2006Assignee: Bayer HealthCare AktiengesellschaftInventors: Marc Nowakowski, Reinhold Gehring, Werner Heilmann, Karl-Heinz Wahl
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Patent number: 6984641Abstract: Selective inhibitors of cGMP-specific PDE, and use of the compounds and salts and solvates thereof as therapeutic agents, are disclosed.Type: GrantFiled: May 2, 2002Date of Patent: January 10, 2006Assignee: Lilly Icos LLC.Inventors: Mark W. Orme, Jason S. Sawyer, Alain C. Daugan, Agnes Bombrun, Françoise Gellibert, Lisa M. Schultze, Raymond F. Brown, Romain L. Gosmini
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Patent number: 6977261Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, Y, R2, R3, R4, R5, and n are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition.Type: GrantFiled: August 5, 2003Date of Patent: December 20, 2005Assignee: Warner-Lambert Company LLCInventors: Amy Mae Bunker, Joseph Armand Picard
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Patent number: 6960583Abstract: The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.Type: GrantFiled: March 18, 2004Date of Patent: November 1, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Paul J. Gilligan, Richard G. Wilde
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Patent number: 6951851Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: October 4, 2005Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6943158Abstract: Compounds of formula I are p38 inhibitors: or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen or alkyl; R2 alkyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkyl, cyanoalkyl, heterocyclyl, heterocyclylalkyl, or —Y1—C(O)—Y2—R11 (where Y1 and Y2 are independently either absent or an alkylene group and R11 is hydrogen, alkyl, haloalkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino); R3 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterosubstituted cycloalkyl, heterocyclyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(?O)—R4 (where R4 is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino), or acyl; Ar1 is aryl; X1 is O, NR5 or S, where R5 is hydrogen or alkyl; and X2 is a bond, O, NR6, S or CH2, where R6 is hydrogen or alkyl.Type: GrantFiled: November 18, 2003Date of Patent: September 13, 2005Assignees: Roche Palo Alto LLC, Hoffmann-La Roche Inc.Inventors: Jian Jeffrey Chen, Kin-Chun Thomas Luk
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Patent number: 6943163Abstract: The present invention relates to 7-alkyl- and cycloalkyl-substituted imidazotriazinones, to processes for their preparation and to their use as medicaments, in particular as inhibitors of cGMP-metabolizing phosphodiesterases.Type: GrantFiled: May 20, 2004Date of Patent: September 13, 2005Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Gunter Schmidt, Karl-Heinz Schlemmer, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn