Polycyclo Ring System Having The 1,2-diazole Ring As One Of The Cyclos Patents (Class 546/275.7)
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Publication number: 20090082359Abstract: 5-pyridinone substituted indazoles of the formula and methods of their use are presented.Type: ApplicationFiled: July 18, 2008Publication date: March 26, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Peter Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden
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Publication number: 20090081123Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)-Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)-Z?; an amide substituent of formula —C(O)—NH-T?.Type: ApplicationFiled: December 8, 2008Publication date: March 26, 2009Applicant: CeNeRx BioPharmaInventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabriele MURINEDDU
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Publication number: 20090076091Abstract: The invention relates to novel indazole derivatives as cited in claim 1, which are inhibitors of CHK1, CHK2 and SGK kinases and can be used to treat cancer and other diseases.Type: ApplicationFiled: January 10, 2007Publication date: March 19, 2009Applicant: MERCK PATENT GMBHInventors: Markus Klein, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
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Publication number: 20090074675Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.Type: ApplicationFiled: April 12, 2006Publication date: March 19, 2009Applicant: GLAXO GROUP LIMITEDInventors: Colin David Eldred, David House, Graham George Adam Inglis, Simon John Fawcett MacDonald, Philip Alan Skone
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Publication number: 20090062347Abstract: The present application describes deuterium-enriched axitinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 25, 2008Publication date: March 5, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090054423Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 7, 2006Publication date: February 26, 2009Inventors: Jason E. Imbriglio, Steven L. Colletti, James R. Tata, Rui Liang, Subharekha Raghavan, Darby R. Schmidt, Abigail L. Smenton, Sook Yee Chan
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Publication number: 20090054397Abstract: The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 designates —(CO)h—(NRa)j—(CRb?CRc)k—Ar (wherein Ra, Rb and Rc each independently designate a hydrogen atom, a halogen atom, hydroxyl group, an optionally substituted C1-6 alkyl group or the like; Cy designates a 5- or 6-membered heteroaryl; and V each independently designate the formula -L-X—Y (wherein L designates a single bond, an optionally substituted C1-6 alkylene group or the like; X designates a single bond or the formula -A- (wherein A designates NR2, O, CO, S, SO or SO2) and so on; and Y designates a hydrogen atom, a halogen atom, nitro group or the like).Type: ApplicationFiled: April 29, 2008Publication date: February 26, 2009Inventors: Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Takashi Doko, Taro Terauchi, Yoshimitsu Naoe, Takafumi Motoki
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Publication number: 20090048219Abstract: The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent.Type: ApplicationFiled: May 23, 2006Publication date: February 19, 2009Applicant: NITROMED INC.Inventor: David S. Garvey
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Patent number: 7482342Abstract: Compound corresponding to general formula (I): in which, R1 represents a hydrogen or halogen atom, an NH2, NHR2, NHCOR2, NO2, CN, CH2NH2 and CH2NHR2; or alternatively R1 represents an optionally substituted phenyl or an optionally substituted heteroaromatic group; Ar represents an optionally substituted phenyl group or an optionally substituted heteroaromatic group; n represents 0, 1, 2 or 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Application in therapy.Type: GrantFiled: April 1, 2005Date of Patent: January 27, 2009Assignee: sanofi-aventisInventors: Hugues D'Orchymont, Luc Van Hijfte, Andre Zimmermann
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Publication number: 20090012123Abstract: As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.Type: ApplicationFiled: April 12, 2006Publication date: January 8, 2009Inventors: Hisayuki Seike, Takeshi Matsugi, Atsushi Shimazaki
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Publication number: 20080293714Abstract: Disclosed are compounds of formula (I): (F) wherein Ri, R2, X and Ar are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: December 6, 2006Publication date: November 27, 2008Inventors: Joerg Martin Bentzien, Brian Nicholas Cook, Hidenori Takahashi
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Publication number: 20080269280Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: March 14, 2008Publication date: October 30, 2008Applicant: ChemoCentryx, Inc.Inventors: Penglie Zhang, Andrew M.K. Pennell, Lianfa Li, Edward J. Sullivan
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Patent number: 7439363Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): R2 is selected from the group consisting of —C1-8alkyl-Z, —C2-8alkenyl-Z and —C2-8alkynyl-Z; wherein the —C1-8alkyl-Z, —C2-8alkenyl-Z and —C2-8alkynyl-Z and Z is a 5 to 6 member aromatic monocyclic heteroaryl ring having from 2 to 4 heteroatoms. These compounds are useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: June 1, 2004Date of Patent: October 21, 2008Assignee: Janssen Parmaceutica N.V.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Hong Ye
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Publication number: 20080242866Abstract: The present invention relates to a novel method of preparing anthranilamides of formula I: in which R1, R2, R3, A, E, Q, X, and W are defined in the claims, to a novel intermediate compound, and to the use of said novel intermediate compound for the preparation of said anthranilamides of formula I.Type: ApplicationFiled: March 27, 2008Publication date: October 2, 2008Inventors: Norbert SCHMEES, Orlin Petrov
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Publication number: 20080234259Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).Type: ApplicationFiled: June 1, 2006Publication date: September 25, 2008Applicant: Glenmark Pharmaceuticals S.A.Inventors: Meyyappan Muthuppalaniappan, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan
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Publication number: 20080234327Abstract: This invention is directed to compounds of formula (I): wherein m, R1, R2, R3 and R4 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.Type: ApplicationFiled: March 21, 2008Publication date: September 25, 2008Applicant: XENON PHARMACEUTICALS INC.Inventors: Jean-Jacques Cadieux, Jianmin Fu, Rajender Kamboj, Zaihui Zhang
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Publication number: 20080227820Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: October 31, 2007Publication date: September 18, 2008Inventors: Markus Berger, Hartmut Rehwinkel, Heike Schaecke, Matti Lepisto, Karl Edmann
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Publication number: 20080227821Abstract: 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: ApplicationFiled: January 29, 2008Publication date: September 18, 2008Inventors: Robert A. Galemmo, Dana L. Johnson, Umar S.M. Maharoof, Jay M. Mei, Robert W. Tuman
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Publication number: 20080194586Abstract: Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dylipidermia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.Type: ApplicationFiled: March 3, 2006Publication date: August 14, 2008Inventors: Harold B. Wood, Peter T. Meinke, Guo Q. Shi, Yong Zhang
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Publication number: 20080188666Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: November 7, 2007Publication date: August 7, 2008Inventors: Markus Berger, Hartmut Rehwinkel, Heike Schaecke, Matti Lepisto, Karl Edmann
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Patent number: 7405299Abstract: The current invention relates to compounds of the formula: (Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.Type: GrantFiled: November 24, 2003Date of Patent: July 29, 2008Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Timothy Paul Burkholder, Todd Vincent Decollo, Alexander Glenn Godfrey, Charles Raymond Heap, Chi-Hsin Richard King, Hong-Yu Li, William Thomas McMillen, Jason Scott Sawyer, Yan Wang, Clive Gideon Diefenbacher, Thomas Albert Engler, Sushant Malhotra, Sreenivasa Reedy Mundla
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Publication number: 20080176833Abstract: This invention provides novel dihydropyridine derivatives of the formula I having protein tyrosine kinase inhibitory activity, to process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions.Type: ApplicationFiled: December 13, 2007Publication date: July 24, 2008Inventors: Marc Adler, Stefan Baeurle, Judi Bryant, Ming Chen, Yuo-Ling Chou, Paul Hrvatin, Seock-Kyu Khim, Monica Kochanny, Wheeseong Lee, Michael Mamounas, Janet Meurer Ogden, Gary Bruce Phillips, Victor Selchau, Christopher West, Bin Ye, Shendong Yuan, Martin Krueger
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080125423Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: ApplicationFiled: July 18, 2007Publication date: May 29, 2008Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. Dewolf, Dalia R. Jakas
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Publication number: 20080119648Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Publication number: 20080108668Abstract: The invention relates to fungicide and insecticide, especifically to the substituted azole compounds and its preparation method and use thereof. The azole compounds of the invention having general formula (I): The compounds of present invention, having broad spectrum fungicidal activity, applied for controlling various disease in plants. For example they have good activity against the diseases such as cucumber downy mildew, cucumber grey mold, cucumber powdery mildew, tomato early blight, tomato late blight, phytophthora blight of pepper, grape downy mildew, grape white rot, apple ring rot, apple alternaria leaf spot, rice sheath blight, rice blast, wheat leaf rust, wheat leaf blotch, wheat powdery mildew, rapesclerotiniose, corn southern leaf blight. Some compounds have good insecticidal or acaricidal activity and can be used to control insects and acacids of various crops. For example they are used to control army worm, diamond backmoth and aphid, and culex mosquito.Type: ApplicationFiled: February 17, 2005Publication date: May 8, 2008Inventors: Changling Liu, Miao Li, Hong Zhang, Lin Li, Mingxing Zhang, Aiying Guan, Chunqing Hou, Zhinian Li, Yonggang Jia
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Publication number: 20080103182Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: ApplicationFiled: October 19, 2007Publication date: May 1, 2008Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20080081815Abstract: A novel heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: ApplicationFiled: September 29, 2006Publication date: April 3, 2008Applicant: GREEN CROSS CorporationInventors: Jinhwa Lee, Jeong Min Kim, Chong-Hwan Jonathan Chang, Suk Youn Kang, Hee Jeong Seo, Kwang-Seop Song, Sung-Han Lee, Kwang-Woo Ahn
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Publication number: 20080058384Abstract: Novel Inhibitors of Rho-kinases are disclosed.Type: ApplicationFiled: February 18, 2005Publication date: March 6, 2008Inventors: Dennis Lee, Krista B. Goodman
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Publication number: 20080058515Abstract: Indazolylacrylamide derivatives, which are useful as SGK-1 inhibitors are described herein. The described invention also includes methods of making such indazolylacrylamide derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate SGK-1 activity.Type: ApplicationFiled: July 23, 2004Publication date: March 6, 2008Inventors: David Harold Drewry, James Andrew Linn, James Marvin Veal
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Patent number: 7329657Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: August 2, 2004Date of Patent: February 12, 2008Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Han-Cheng Zhang, Bruce Maryanoff, Bruce Conway, Kimberly White, Hong Ye, Leonard Robert Hecker, David F. McComsey
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Patent number: 7282498Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: June 1, 2004Date of Patent: October 16, 2007Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 7262200Abstract: 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: October 27, 2003Date of Patent: August 28, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Huan Qui Li, Ronald Charles Tomlinson, Pan Li
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Patent number: 7241779Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.Type: GrantFiled: December 22, 2004Date of Patent: July 10, 2007Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, Allison L. Zulli, Dandu R. Reddy, Ming Tao, Theodore L. Underiner
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Patent number: 7238696Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptorType: GrantFiled: February 13, 2004Date of Patent: July 3, 2007Assignee: WyethInventors: Ronald Charles Bernotas, Yinfa Yan, Albert Jean Robichaud, Guangcheng Liu
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Patent number: 7232910Abstract: The present invention relates to methods for preparing indazole compounds of formula I, which are useful as modulators and/or inhibitors of protein kinases. The present invention also relates to intermediate compounds useful in the preparation of compounds of formula I.Type: GrantFiled: October 31, 2005Date of Patent: June 19, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Brigitte Leigh Ewanicki, Erik Jon Flahive, Annie Judith Kasparian, Mark Bryan Mitchell, Michael David Perry, Stacy Ann O'Neill-Slawecki, Neal William Sach, James Edward Saenz, Bing Shi, Nebojsa Slobodan Stankovic, Jayaram Kasturi Srirangam, Qingping Tian, Shu Yu
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Patent number: 7196109Abstract: The present invention relates to the use of 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, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, 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, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essentialType: GrantFiled: November 23, 2005Date of Patent: March 27, 2007Assignee: Aventis Pharma SAInventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney, Gilles Tiraboschi
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Patent number: 7196082Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: October 14, 2003Date of Patent: March 27, 2007Assignee: Merck & Co. Inc.Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Robert M. Tynebor
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Patent number: 7186720Abstract: The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independently represent a hydrogen atom or a methyl group; n is 0 or 1; A represents an optionally substituted nitrogenous heterocycle; and to their N-oxides and to their salts or solvates, to the pharmaceutical compositions and the medicaments comprising them, and to a process for their preparation.Type: GrantFiled: April 19, 2002Date of Patent: March 6, 2007Assignee: Sanofi-AventisInventors: Marco Baroni, Bernard Bourrie, Pierre Casellas
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Patent number: 7148357Abstract: VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g.Type: GrantFiled: July 31, 2003Date of Patent: December 12, 2006Assignee: Schering AGInventors: Andreas Huth, Ludwig Zorn, Martin Kruger, Stuat Ince, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey, Holger Hess-Stumpp
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Patent number: 7141585Abstract: This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.Type: GrantFiled: April 26, 2004Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Romuald Gaston Corbau, Charles Eric Mowbray, Manoussos Perros, Paul Anthony Stupple, Anthony Wood
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Patent number: 7141587Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: November 18, 2004Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Jr., Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Maria Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
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Patent number: 7141581Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: August 12, 2003Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Bender, Dana Hu-Lowe, David Ray Shalinsky
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Patent number: 7119115Abstract: The present invention relates to novel compounds derived from indazoles or indoles of formula (1) or formula (2), to methods for treating tumors or cancerous cells with compounds of formula (1) or formula (2) and to pharmacaetutical compositions comprising a pharmaceutically acceptable carrier and a compound of formula (1) or formula (2)Type: GrantFiled: January 21, 2004Date of Patent: October 10, 2006Assignee: Aventis Pharma S.A.Inventors: Michel Tabart, Eric Bacqué, Sylvie Wentzler, Cécile Combeau, Conception Nemecek, Patrick Mailliet, Fabienne Thompson
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Patent number: 7105682Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis 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 10, 2002Date of Patent: September 12, 2006Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
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Patent number: 7102009Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis 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: July 17, 2002Date of Patent: September 5, 2006Assignee: Amgen Inc.Inventors: Vinod F. Patel, Benny Askew, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Julie Germain, Gregory J. Habgood, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Babak Riahi, Chester Chenguang Yuan, Daniel Elbaum
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Patent number: 7087626Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.Type: GrantFiled: May 13, 2002Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Todd Vincent DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Jr., Hong-Yu Li, William Thomas McMillen, Shawn Christopher Miller, Jason Scott Sawyer, Edward C. R. Smith, Jonathan Michael Yingling
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Patent number: 7087625Abstract: PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formulas I–III: wherein A, B, D, R1, R2, R3, R7, R8, R9, R10 and R6are as defined herein.Type: GrantFiled: November 19, 2003Date of Patent: August 8, 2006Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Elizabeth Doorly Graham, Allen T. Hopper, Ashok Tehim
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Patent number: 7087603Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Z1 or Z2 is nitrogen, Q is —S—, —O—, —N(R4)—, —C(R6?)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclobutanediyl, and R1 is T-Ring D, wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–7 membered ring having 0–3 heteroatoms; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: December 15, 2003Date of Patent: August 8, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier