Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/405)
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Patent number: 8063091Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: July 22, 2009Date of Patent: November 22, 2011Assignee: Abbott LaboratoriesInventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Patent number: 8053459Abstract: The present invention synthesizes a series of selenolo[3,2-c]pyrazole and selenolo[2,3-c]pyrazole derivatives, and discovers their anticancer activity.Type: GrantFiled: July 15, 2010Date of Patent: November 8, 2011Assignee: China Medical UniversityInventors: Sheng-Chu Kuo, Li-Jiau Huang, Li-Chen Chou, Jai-Sing Yang, Mei-Hua Hsu, Shi-Hong Zhuang, Mei-Chi Fang, Hui-Yi Lin
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Publication number: 20110263598Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: ApplicationFiled: April 6, 2011Publication date: October 27, 2011Applicant: UNIVERSITY HEALTH NETWORKSInventors: Peter B. Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Radoslaw Laufer, Guohua Pan
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Publication number: 20110212078Abstract: This invention relates to compounds of the following Formula (I); or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.Type: ApplicationFiled: June 24, 2009Publication date: September 1, 2011Inventors: Panduranga Adulla P. Reddy, Umar Faruk Mansoor, M. Arshad Siddiqui
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Patent number: 7973043Abstract: The present invention relates to a new method of treatment for persons meeting diagnoses for major depressive disorder, or other unipolar (non-bipolar, non-psychotic and non-treatment resistant) depression. The method comprises administering a combination of two categories of drugs, antipsychotics or dopamine system stabilizers, in combination with a newer antidepressant such as a selective serotonin reuptake inhibitor, as initial treatment or as soon as possible. The method targets the prevention of suicide, and provides other benefits including preventing disease progression development of tolerance toward the antidepressants. Another aspect of the invention relates to using the method for alleviating cognitive distortion and related functional impairment or health risks, and/or using the method for smoking cessation or nicotine withdrawal.Type: GrantFiled: July 25, 2003Date of Patent: July 5, 2011Inventor: Peter Migaly
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Patent number: 7968583Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: GrantFiled: December 6, 2006Date of Patent: June 28, 2011Assignee: Nerviano Medical Sciences S.r.l.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Sten Christian Orrenius, Ettore Perrone, Italo Beria, Daniele Fancelli, Arturo Galvani
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Patent number: 7947707Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.Type: GrantFiled: October 3, 2006Date of Patent: May 24, 2011Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Takahiro Toyoshima, Toshinobu Sasaki, Chikara Hoshino, Masakazu Takeda
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Publication number: 20110112147Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 5, 2010Publication date: May 12, 2011Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20110110948Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.Type: ApplicationFiled: July 15, 2008Publication date: May 12, 2011Applicant: SCHERING CORPORATIONInventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien -
Patent number: 7939528Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: GrantFiled: October 12, 2006Date of Patent: May 10, 2011Assignee: GlaxoSmithKline LLCInventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
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Patent number: 7935708Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.Type: GrantFiled: April 25, 2007Date of Patent: May 3, 2011Assignee: MSD K.K.Inventors: Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Toshihiro Sakamoto, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
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Patent number: 7906649Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-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: May 19, 2006Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Ann E. Weber, Jason Cox
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Publication number: 20110034424Abstract: Provided is a method for the long term treatment of a condition or disease which is one of the indications for NSAID use in a human patient, which comprises administering to the patient a pharmaceutically effective amount of a NSAID and at least 36 mcg per day of cobiprostone or its pharmaceutically acceptable salt, ester, ether or amide. By administering cobiprostone or its pharmaceutically acceptable salt, ester, ether or amide in combination with a NSAID, the patient can receive the NSAID for longer time period.Type: ApplicationFiled: June 29, 2010Publication date: February 10, 2011Applicant: SUCAMPO AGInventor: Ryuji Ueno
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Publication number: 20110028470Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.Type: ApplicationFiled: July 31, 2008Publication date: February 3, 2011Applicants: TOKAI UNIVERSITY EDUCATIONAL SYSTEM, RENASCIENCE CO., LTD., MEDICAL & BIOLOGICAL LABORATORIES CO., LTD.Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
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Patent number: 7879890Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: December 18, 2008Date of Patent: February 1, 2011Assignee: Schering CorporationInventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Aneta M. Micula, Robert Feltz
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Patent number: 7863305Abstract: Compounds of formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: June 1, 2005Date of Patent: January 4, 2011Assignee: Roche Palo Alto LLCInventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova, Deborah Carol Reuter, Karin Ann Stein, Robert Weikert
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Patent number: 7846959Abstract: The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.Type: GrantFiled: March 25, 2005Date of Patent: December 7, 2010Assignee: Exelixis, Inc.Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Larisa Dubenko, Abigail R. Kennedy, Steven Charles Defina, Angie I. Kim, Jean-Claire L. Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Anagha Abhijit Joshi
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Patent number: 7842712Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: GrantFiled: August 20, 2007Date of Patent: November 30, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Huan Qiu Li, Ronald Charles Tomlinson, Pan Li
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Publication number: 20100286133Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds as pharmaceutical products.Type: ApplicationFiled: July 20, 2010Publication date: November 11, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Hubert HEUER, Norbert TENNAGELS
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Patent number: 7820707Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: GrantFiled: June 29, 2007Date of Patent: October 26, 2010Assignee: N.V. OrganonInventors: Kevin James Gillen, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
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Patent number: 7816390Abstract: The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol; or 3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: January 29, 2008Date of Patent: October 19, 2010Assignee: Janssen Pharmaceutica NVInventors: Robert A. Galemmo, Dana L. Johnson, Umar S. M. Maharoof, Jay M. Mei, Robert W. Tuman
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Patent number: 7812019Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: GrantFiled: November 22, 2005Date of Patent: October 12, 2010Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
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Patent number: 7807714Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of formula (I) or a tautomer of such a compound; and component (B) and component (C) are pesticides as described in claim 1.Type: GrantFiled: February 7, 2007Date of Patent: October 5, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Franz Brandl, Michael Oostendorp, Ronald Zeun
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Patent number: 7803830Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: October 8, 2008Date of Patent: September 28, 2010Assignee: Roche Palo Alto LLCInventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
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Patent number: 7795440Abstract: The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell proliferative disorders.Type: GrantFiled: January 25, 2007Date of Patent: September 14, 2010Assignee: Janssen Pharmaceutica NVInventors: Chih Yung Ho, Bengt Anders Brunmark, Stuart Emanuel, Robert A. Galemmo, Jr., Dana L. Johnson, Donald W. Ludovici, Umar Maharoof, Jay M. Mei, Jan L. Sechler, Eric D. Strobel, Robert W. Tuman, Hwa Kwo Yen
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Publication number: 20100222275Abstract: Provided are a pharmaceutical product capable of treating vitiligo by thickening the epidermis at a vitiligo-affected site, which has been thinned, to thereby accelerate pigmentation, and a method of accelerating pigmentation by thickening the epidermis. Vitiligo can be treated by using a compound having an epidermis thickening action, for example, a therapeutic agent for a skin ulcer which is used in the treatment of burn ulcer, crural ulcer, diabetic ulcer or post-operative ulcer, or a therapeutic agent for bedsore.Type: ApplicationFiled: October 17, 2008Publication date: September 2, 2010Inventors: Kunihiko Tamaki, Kanako Kikuchi, Mayumi Komine, Seiki Fujimoto
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Publication number: 20100216706Abstract: A method of treating neurodegeneration of substantia nigra pars compacta (SNpc) dopamine neurons and compositions therefor are provided.Type: ApplicationFiled: May 13, 2008Publication date: August 26, 2010Inventors: Tamas L. Horvath, Zane B. Andrews
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Patent number: 7781436Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: GrantFiled: July 25, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7776791Abstract: The invention relates to novel N-heterocyclylphenyl-substituted cyclic ketoenols of the formula (I) in which CKE, W, X, Y and Z are as defined in the disclosure, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides. The invention further relates to selective herbicidal compositions comprising firstly the N-heterocyclylphenyl-substituted cyclic ketoenols and secondly a compound which improves crop plant tolerance.Type: GrantFiled: June 7, 2004Date of Patent: August 17, 2010Assignee: Bayer CropScience AGInventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Stefan Lehr, Klaus Kunz, Jörg Konze, Olga Malsam, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann, Wahed Ahmed Moradi, Guido Bojack, Thomas Auler, Martin Hills, Heinz Kehne
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Patent number: 7776861Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: GrantFiled: January 23, 2006Date of Patent: August 17, 2010Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Xin Wen
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Patent number: 7772268Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds to treat diabetes mellitus, dyslipidemia and atherosclerotic disorders.Type: GrantFiled: April 8, 2008Date of Patent: August 10, 2010Assignee: Sanofi-AventisInventors: Gerhard Zoller, Stefan Petry, Gunter Müller, Hubert Heuer, Norbert Tennagels
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Patent number: 7772263Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: February 3, 2009Date of Patent: August 10, 2010Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
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Patent number: 7767705Abstract: Compounds of formula (I) wherein R3, R7, R9 and L are defined in the description are TRPV1 antagonists that exhibit low inhibitory activity against CYP3A4. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: August 24, 2007Date of Patent: August 3, 2010Assignee: Abbott LaboratoriesInventors: Chih-hung Lee, Richard J Perner, Brian S. Brown, John Darbyshire
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Patent number: 7759344Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as c-Met 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: GrantFiled: January 9, 2008Date of Patent: July 20, 2010Assignee: Amgen Inc.Inventors: Shon Booker, Noel D'Angelo, Julie Germain, Jean-Christophe Harmange, Tae-Seong Kim, Michele Potashman
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Patent number: 7750034Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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 19, 2007Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Patent number: 7750026Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: GrantFiled: January 27, 2005Date of Patent: July 6, 2010Assignee: GlaxoSmithKline LLCInventors: Vipulkumar Kantibhai Patel, Stephen Swanson
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Patent number: 7728030Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.Type: GrantFiled: December 20, 2007Date of Patent: June 1, 2010Assignees: AstraZeneca AB, Bayer Schering Pharma AktiengesellschaftInventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Patent number: 7700636Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: March 19, 2008Date of Patent: April 20, 2010Assignee: Amgen Inc.Inventors: Holger Monenschein, George Erich Wohlhieter, Qingping Zeng
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Patent number: 7696191Abstract: A novel crystalline form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methylethyl)oxy]-N-1H-pyrazol-3-ylbenzamide is described in the specification. This compound is a glucokinase (GLK or GK) activator and useful as a pharmaceutical agent in the treatment or prevention of a disease or medical condition mediated through GLK, leading to a decreased glucose threshold for insulin secretion. Processes for the manufacture of the crystalline form, pharmaceutical compositions comprising the crystalline form and the use of the crystalline form in medical treatment are also described.Type: GrantFiled: December 21, 2007Date of Patent: April 13, 2010Assignee: AstraZeneca ABInventors: James McCabe, Gary Peter Tomkinson
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Patent number: 7691888Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.Type: GrantFiled: October 5, 2005Date of Patent: April 6, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Bodo Betzemeier, Trixi Brandl, Steffen Breitfelder, Ralph Brueckner, Thomas Gerstberger, Michael Gmachl, Matthias Grauert, Frank Hilberg, Christoph Hoenke, Matthias Hoffmann, Maria Impagnatiello, Dirk Kessler, Christian Klein, Bernd Krist, Udo Maier, Darryl McConnell, Charlotte Reither, Stefan Scheuerer, Andreas Schoop, Norbert Schweifer, Oliver Simon, Martin Steegmaier, Steffen Steurer, Irene Waizenegger, Ulrike Weyer-Czernilofsky, Andreas Zoephel
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Patent number: 7687527Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: December 18, 2008Date of Patent: March 30, 2010Assignee: Schering CorporationInventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Umar Faruk Mansoor, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li
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Publication number: 20100075993Abstract: The invention provides flavivirus replication inhibitors of WNV and other flaviviruses, such as, for example, JEV, SLEV, AV, KV, JV, CV, YV, TBEV, DENV-1, DENV-2, DENV-3, DENV-4, YFV and MVEV. The invention further provides pharmaceutical compositions including one or more such flavivirus replication inhibitors. The invention further provides methods of treatment, prevention, inhibition or amelioration of one or more diseases associated with flavivirus replication including administering one or more such inhibitors or pharmaceutical compositions.Type: ApplicationFiled: June 30, 2006Publication date: March 25, 2010Applicant: DREXEL UNIVERSITYInventors: Baohua Gu, Tim Block, Andy Cuconati
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Patent number: 7683085Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF- or combinations thereof.Type: GrantFiled: December 18, 2008Date of Patent: March 23, 2010Assignee: Schering CorporationInventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar
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Patent number: 7642278Abstract: Organic compounds having the structure I are provided where the variables have the values described herein. A method of inhibiting c-ABL in a patient includes administering an effective amount of a compound of structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable salt of the tautomer to the patient.Type: GrantFiled: October 27, 2005Date of Patent: January 5, 2010Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Johanna M. Jansen, Christopher McBride, Paul A. Renhowe, Cynthia Shafer
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Patent number: 7625937Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: September 26, 2007Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Amjad Ali, James M. Balkovec, Donald W. Graham, Christopher F. Thompson, Nazia Quraishi
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Patent number: 7622492Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: August 18, 2006Date of Patent: November 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Bruce Lester Banner, Joseph Anthony Bilotta, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Nancy-Ellen Haynes, Agnieszka Kowalczyk, Alexander Mayweg, Michael Paul Myers, Sherrie Lynn Pietranico-Cole, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Kevin Richard Guertin
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Patent number: 7612106Abstract: The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like.Type: GrantFiled: November 17, 2006Date of Patent: November 3, 2009Assignee: Arena Pharmaceuticals, Inc.Inventors: P. Douglas Boatman, Thomas O. Schrader, Graeme Semple, Philip J. Skinner, Jae-Kyu Jung
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Patent number: 7582669Abstract: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.Type: GrantFiled: December 6, 2006Date of Patent: September 1, 2009Assignee: Aventis Pharma SAInventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney
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Publication number: 20090163546Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: December 1, 2008Publication date: June 25, 2009Inventors: David Robert Bolin, Jianping Cai, Robert Alan Goodnow, JR.