Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/245)
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Patent number: 8058300Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: GrantFiled: June 3, 2010Date of Patent: November 15, 2011Assignee: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Patent number: 8048899Abstract: are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 22, 2009Date of Patent: November 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Markus Ostermeier, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
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Patent number: 8044099Abstract: Bifunctional molecules and methods for their use are provided. The subject bifunctional molecules are conjugates of a drug moiety and a pharmacokinetic modulating moiety, where these two moieties are optionally joined by a linking group. The bifunctional molecules are further characterized in that they exhibit at least one modulated pharmacokinetic property upon administration to a host as compared to a free drug control. The subject bifunctional molecules find use in a variety of therapeutic applications.Type: GrantFiled: December 13, 2004Date of Patent: October 25, 2011Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Roger Briesewitz, Gerald R. Crabtree, Thomas J. Wandless
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Publication number: 20110245221Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 30, 2009Publication date: October 6, 2011Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.Inventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Paolo Carminati, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati, Claudio Pisano
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Publication number: 20110212467Abstract: Evidence demonstrating that elevated expression of dUTPase protects breast cancer cells from the expansion of the intracellular uracil pool, translating to reduced growth inhibition following treatment with 5-FU is provided. The implementation of in silica drug development techniques to identify and develop small molecule inhibitors of dUTPase are reported. As 5-FU and the oral 5-FU pro-drug capecitabine remain central agents in the treatment of a variety of malignancies, the clinical utility of a small molecule inhibitor to dUTPase represents a viable strategy to improve the clinical efficacy of these mainstay chemotherapeutic agents.Type: ApplicationFiled: August 27, 2009Publication date: September 1, 2011Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Robert D. Ladner, Nouri Neamati
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Patent number: 7960588Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: GrantFiled: March 29, 2010Date of Patent: June 14, 2011Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20110124696Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: June 24, 2009Publication date: May 26, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John Regan, Doris Riether
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Patent number: 7947718Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: GrantFiled: September 15, 2009Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20110082181Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: Amira Phamaceuticals, Inc.Inventors: Thomas Jon SEIDERS, Lucy Zhao, Jeannie M. Arruda, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
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Patent number: 7863308Abstract: Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 10, 2008Date of Patent: January 4, 2011Assignee: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100311799Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: June 3, 2010Publication date: December 9, 2010Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Thomas Jon SEIDERS, Bowei WANG, Jeannie M. ARRUDA, Jeffrey Roger ROPPE, Timothy PARR
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Publication number: 20100305200Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: December 10, 2008Publication date: December 2, 2010Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20100168182Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly TrkA, TrkB, TrkC, PDGFR and c-kit.Type: ApplicationFiled: December 11, 2007Publication date: July 1, 2010Applicant: IRM LLCInventors: Yuan Mi, Pamela Albaugh, Yi Fan, Ha-Soon Choi, Zuosheng Liu, Shenlin Huang
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Patent number: 7745458Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.Type: GrantFiled: August 18, 2006Date of Patent: June 29, 2010Assignee: Glaxo Group LimitedInventors: Luca Arista, Anna Checchia, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20100152257Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: December 15, 2009Publication date: June 17, 2010Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Thomas Jon SEIDERS, Bowei WANG, Jeannie M. ARRUDA, Jeffrey Roger ROPPE, Timothy PARR
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Publication number: 20100135960Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: November 17, 2009Publication date: June 3, 2010Inventors: Yat Sun Or, Lu Ying, Ce Wang, Xiaowen Peng, Yao-Ling Qiu
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Patent number: 7696215Abstract: The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: February 23, 2006Date of Patent: April 13, 2010Assignee: AstraZeneca ABInventors: Ian Alun Nash, Jonathan Erle Finlayson, Caroline Rachel Thompson
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Publication number: 20100075348Abstract: The invention relates to a method for diagnosis of a disease, wherein presence or absence of an anti-endothelin-receptor antibody is determined in a sample from a patient to be diagnosed more in particular an anti-endothelin-receptor-A antibody. The disease according to the invention is in particular selected from diabetes, preferably type I diabetes, graft rejection, pre-eclampsia, hypertension, vasculitis, collagenosis, Raynaud-Syndrom (Morbus Raynaud), and inflammatory rheumatic disease and arteriosclerosis. The invention further relates to the use of an inhibitor of an anti-endothelin-receptor antibody or an inhibitor of an endothelin-receptor for the production of a medicament as well as a method for removing anti-endothelin-receptor antibodies from isolated blood by means of plasmapheresis.Type: ApplicationFiled: July 31, 2007Publication date: March 25, 2010Applicant: CELLTREND GMBHInventors: Kai Schulze-Forster, Harald Heidecke
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Patent number: 7652021Abstract: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).Type: GrantFiled: February 28, 2006Date of Patent: January 26, 2010Assignee: Sanofi-AventisInventors: Peter Aranyi, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Zoltan Kapui, Edit Susan, Tibor Szabo, Katalin Urban-Szabo, Marton Varga
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Publication number: 20090227790Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: April 7, 2009Publication date: September 10, 2009Inventor: Leu-Fen H. Lin
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Patent number: 7557133Abstract: The present invention relates to an isoxazoline derivative as an inhibitor against various caspases, a process for preparing the same, and a therapeutic composition for preventing inflammation and apoptosis comprising the same.Type: GrantFiled: August 26, 2004Date of Patent: July 7, 2009Assignee: LG Life Sciences Ltd.Inventors: Hye-Kyung Chang, Yeong-Soo Oh, Cheol-Won Park, Yong-Jin Jang, Tae-Kyo Park, Sung-Sub Kim, Min-Jung Kim, Mi-Jeong Park, Jung-Gyu Park, Hee-Dong Park, Kyeong-Sik Min, Tae-Soo Lee, Sang-Kyun Lee, Soo-Hyeon Kim, Hee-Kyung Jeong, Sun-Hwa Lee, Hwa-Dong Kim, Ae-Ri Kim, Ki-Sook Park, Hyun-Ik Shin, Hyeong-Wook Choi, Kyu-Woong Lee, Jae-Hoon Lee, Tae-Ho Heo, Ho-Jun Kim, Tae-Sik Kwon, Jeong Hui Seong
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Publication number: 20090170911Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.Type: ApplicationFiled: February 20, 2009Publication date: July 2, 2009Applicant: AJINOMOTO CO. INCInventors: Takashi YAMAMOTO, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
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Publication number: 20090163497Abstract: The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: June 25, 2009Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Patent number: 7517996Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.Type: GrantFiled: February 3, 2006Date of Patent: April 14, 2009Assignee: Ajinomoto Co., Inc.Inventors: Takashi Yamamoto, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
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Publication number: 20090069288Abstract: Disclosed herein are novel compounds of Formula (I), wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases as well as proliferative disorders such as cancer.Type: ApplicationFiled: July 15, 2008Publication date: March 12, 2009Inventors: Eric C. Breinlinger, Kevin P. Cusack, Adrian D. Hobson, Bin Li, Thomas D. Gordon, Robert H. Stoffel, Grier A. Wallace, Pintipa Grongsaard, Lu Wang, Lu Wang
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Patent number: 7396838Abstract: A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1: wherein R1, R2, R3, R4, and n are as defined herein.Type: GrantFiled: June 6, 2005Date of Patent: July 8, 2008Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Patent number: 7368578Abstract: The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic actiType: GrantFiled: September 9, 2003Date of Patent: May 6, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Nobuyuki Takakura, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Publication number: 20080096943Abstract: Compounds of formula I in free or salt form, wherein T, X, R1, R2, Ra, R3, R4, R5 and U have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: August 9, 2005Publication date: April 24, 2008Inventors: Gurdip Bhalay, Andrew Dunstan, Angela Glen, Trevor John Howe, Clive McCarthy
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Patent number: 7354919Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein, kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: July 24, 2003Date of Patent: April 8, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, James W. Janetka, Francois Maltais, Jingrong Cao
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Patent number: 7348322Abstract: The present invention relates to compounds of formula I: wherein A, X, R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: December 8, 2006Date of Patent: March 25, 2008Assignee: Roche Palo Alto LLCInventors: Leyi Gong, Counde O'Yang, Yun-chou Tan
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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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Publication number: 20080045560Abstract: Compounds of the following structure are described: wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.Type: ApplicationFiled: August 13, 2007Publication date: February 21, 2008Applicant: WyethInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
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Publication number: 20070238710Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Applicant: ARDEA BIOSCIENCESInventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
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Publication number: 20070232648Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where A, B, and R1-R3 are defined herein.Type: ApplicationFiled: March 30, 2007Publication date: October 4, 2007Inventors: Russell Dahl, Sara Sabine Hadida-Ruah, Leslie A. Robinson
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Patent number: 7241786Abstract: The present invention relates to compounds of the Formula wherein R1, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, Z and n are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: May 12, 2004Date of Patent: July 10, 2007Assignee: Pfizer IncInventor: Yuhpyng Liang Chen
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Patent number: 7081538Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, X is O, S or NH; HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are describedType: GrantFiled: November 28, 2000Date of Patent: July 25, 2006Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Michael John Betts
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Patent number: 7060710Abstract: The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6? and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4; one of R6 and R6? is hydrogen; either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon; and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.Type: GrantFiled: November 22, 2002Date of Patent: June 13, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
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Patent number: 7041670Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.Type: GrantFiled: April 8, 2003Date of Patent: May 9, 2006Assignee: Schering-Plough Animal Health CorporationInventors: Constantine G. Boojamra, Lee S. Chong, Scott J. Hecker, Tomasz W. Glinka, Dale E. Shuster
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Patent number: 6987122Abstract: 2-(1H-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.Type: GrantFiled: July 12, 2001Date of Patent: January 17, 2006Assignee: Novuspharma S.p.A.Inventors: Ernesto Menta, Nicoletta Pescalli
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Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6964975Abstract: The present invention relates to novel isoxazole and thiazole compounds having an excellent lysophosphatidic acid (LPA) receptor antagonistic activity represented by general formula [1] or salts thereof: wherein R1 and R2 represents an optionally substituted alkyl group or the like; R3 represents a hydrogen atom or the like; R4 represent a group selected from the group consisting of (I) optionally substituted phenyl, aryl, or heterocycle, (II) substituted or nonsubstituted alkyl, and (III) substituted or nonsubstituted alkenyl, alternatively, R3 and R4 may form a ring structure together with a carbon atom to which they bind; and X represents an oxygen atom or a sulfur atom, provided that, when R3 is a hydrogen atom, R4 represents a group other than methyl, and the use thereof as a medicine.Type: GrantFiled: February 19, 2001Date of Patent: November 15, 2005Assignee: Kirin Beer Kabushiki KaishaInventors: Akihiro Ueno, Rika Nagao, Tomoko Watanabe, Hideo Ohta, Mikio Yagi
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Patent number: 6958348Abstract: Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by Structural Formula (I) (preferably an effective amount). Also disclosed is a method of treating a subject with cancer by administering to the subject an effective amount of a compound represented by Structural Formula (I).Type: GrantFiled: August 29, 2002Date of Patent: October 25, 2005Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, Guiqing Liang, David James, Hao Li, Zhi-Qiang Xia
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Patent number: 6903104Abstract: The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formula, each R1 is independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R5; or when taken together with R2 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R2 is independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R5; or when taken together with R1 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5.Type: GrantFiled: December 5, 2002Date of Patent: June 7, 2005Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Patent number: 6852745Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.Type: GrantFiled: September 26, 2003Date of Patent: February 8, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, John E. Tellew, John E. Macor, Zhengxiang Gu
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Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji