Additional Unsaturated Hetero Ring Attached Directly Or Indirectly To The Triazole Ring By Nonionic Bonding Patents (Class 548/266.2)
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Publication number: 20120129901Abstract: Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.Type: ApplicationFiled: May 20, 2010Publication date: May 24, 2012Inventors: Jorge Antonio Ribeiro Salvador, Rita Catarina Mendes Dos Santos, Marta Cascante Serratosa
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Patent number: 8183262Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.Type: GrantFiled: September 1, 2009Date of Patent: May 22, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
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Publication number: 20120108595Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.Type: ApplicationFiled: June 28, 2010Publication date: May 3, 2012Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
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Publication number: 20120108635Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: ApplicationFiled: May 18, 2010Publication date: May 3, 2012Applicant: Bayer CropScience AGInventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
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Publication number: 20120101072Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: December 21, 2011Publication date: April 26, 2012Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Publication number: 20120022083Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.Type: ApplicationFiled: February 9, 2011Publication date: January 26, 2012Applicant: ADHEREX TECHNOLOGIES, INC.Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
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Publication number: 20120015988Abstract: 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: May 4, 2009Publication date: January 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Renee M. Zindell, Patricia Amouzegh, Monika Ermann, Christopher Francis Palmer, Mark Whittaker
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Publication number: 20110275673Abstract: The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders.Type: ApplicationFiled: September 17, 2009Publication date: November 10, 2011Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
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Publication number: 20110220880Abstract: An m-terphenyl derivative has a structure of formula (I) or (II): wherein A and B are five-membered heterocyclic compounds containing nitrogen, each of substituents R, R1 and R2 is a member independently selected from the group consisting of H, halo, cyano, trifluoromethyl, amino, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl, C1-C20 heterocycloalkyl, C1-C20 heterocycloalkenyl, aryl and heteroaryl. The compound of the present invention may have advantages in good electron affinity, low HOMO and thereby achieving hole blocking and may be used for electron transport material and/or electron injection material.Type: ApplicationFiled: January 6, 2011Publication date: September 15, 2011Inventors: Chien-Hong CHENG, Cheng-An WU, Fang-Iy WU, Cheng-Hung SHIH
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Patent number: 7989637Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted triazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: December 17, 2008Date of Patent: August 2, 2011Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20110144110Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 16, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 7947683Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: 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 drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.Type: GrantFiled: April 12, 2006Date of Patent: May 24, 2011Assignee: Glaxo Group LimtedInventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
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Patent number: 7935693Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: GrantFiled: December 29, 2007Date of Patent: May 3, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Jing Zhang, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Patent number: 7910614Abstract: The present invention relates to azolylmethyloxiranes of the general formula I in which A or B is benzodioxolyl which is optionally substituted by one to five of the following substituents: halogen, CN, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and the respective other substituent A or B is phenyl or 5-membered or 6-membered heteroaryl, these substituents optionally being substituted by one to three of the following substituents: halogen, CN, NO2, amino, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylamino, C1-C4-dialkylamino, thio or C1-C4-alkylthio, and to the plant-compatible acid addition salts or metal salts thereof, to the use of the compounds of the formula I for controlling phytopathogenic fungi and to compositions comprising these compounds.Type: GrantFiled: July 17, 2007Date of Patent: March 22, 2011Assignee: BASF SEInventors: Jochen Dietz, Thomas Grote, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glättli
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Patent number: 7902240Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: GrantFiled: November 8, 2007Date of Patent: March 8, 2011Assignee: Novartis AGInventors: Yi Xia, Kris Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
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Publication number: 20110046194Abstract: The present invention constitutes new 3-triazolylphenyl-substituted sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, X, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.Type: ApplicationFiled: August 19, 2010Publication date: February 24, 2011Applicant: Bayer CropScience AGInventors: Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste, Ulrich Görgens
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Publication number: 20110045104Abstract: The present invention constitutes new 3-[1-(3-haloalkyl)triazolyl]phenyl sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.Type: ApplicationFiled: August 19, 2010Publication date: February 24, 2011Applicant: Bayer CropScience AGInventors: Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste
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Publication number: 20110015404Abstract: Compounds of the general structure: Z-A-(S—B)n where A represents a linear aromatic molecular core, S represent a flexible spacer unit, B represents a crosslinking group such as a methacrylate group, n equals 1 to 3, and Z represents any entity compatible with the B groups, and in which A is a substantially aromatic nucleus containing fluorene ring structures substituted at the 9-position and in which the 9-positions of the fluorenes are not susceptible to oxidation.Type: ApplicationFiled: January 7, 2009Publication date: January 20, 2011Inventor: Gene Carl Koch
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Patent number: 7872000Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 28, 2007Date of Patent: January 18, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingu Ding, Jiaxin Yu, Joane Litvak
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Publication number: 20110003690Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.Type: ApplicationFiled: January 29, 2009Publication date: January 6, 2011Applicant: BAY CROPSCIENCE AGInventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
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Publication number: 20100331335Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 5, 2010Publication date: December 30, 2010Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Patent number: 7829639Abstract: A composition for conductive materials comprises a compound represented by the following general formula (A1): wherein: R1 is the same or different and each independently represents a C2-C8 straight-chain alkyl group; R2 is the same or different and each independently represents a hydrogen atom, a methyl group or an ethyl group; Y represents a group containing at least one substituted or unsubstituted aromatic hydrocarbon ring, or substituted or unsubstituted heterocyle; and X1 is the same or different and each represents a substituent represented by the following general formula (A2): wherein n1 is an integer of from 2 to 8.Type: GrantFiled: September 2, 2005Date of Patent: November 9, 2010Assignee: Seiko Epson CorporationInventors: Koichi Terao, Yuji Shinohara, Takashi Shinohara
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Patent number: 7825142Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: GrantFiled: August 24, 2009Date of Patent: November 2, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D. P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Publication number: 20100267759Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: February 7, 2008Publication date: October 21, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Mark A. Seefeld, Meagan B. Rouse, Dirk A. Heerding, Simon Peace, Dennis S. Yamashita, Kenneth C. McNulty
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Publication number: 20100256386Abstract: An aryl (1H-1,2,4-triazol-1-yl) compound is useful for producing a 3-(1H-1,2,4-triazol-1-yl)phenylsulfide compound (useful, e.g., as an insecticide). Also disclosed is a process for producing the compound. The aryl (1H-1,2,4-triazol-1-yl) compound is represented by the general formula (1), below, wherein R represents a C1-C6 alkyl group or a cyclic C3 alkyl group; A1 represents a hydrogen atom, an amino group, a mono(C1-C6 alkyl amino group or a di(C1-C6 alkyl) amino group; A2 represents a halogen atom, a C1-C6 alkyl group or a cyclic C3 alkyl group; and Z represents a hydrogen atom, a halo-sulfonyl group or a mercapto group.Type: ApplicationFiled: November 28, 2008Publication date: October 7, 2010Applicant: IHARA CHEMICAL INDUSTRY CO., LTD.Inventor: Kentaro Kawazoe
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Publication number: 20100256387Abstract: 2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase Type 1 enzyme (11?-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11?-HSD-1.Type: ApplicationFiled: April 14, 2010Publication date: October 7, 2010Applicant: MERCK SHARP & DOHMEInventors: Susan D. Aster, James M. Balkovec, Donald W. Graham, Xin Gu, Nancy J. Kevin, Gool F. Patel, Mitree Ponpipom
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Publication number: 20100234374Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.Type: ApplicationFiled: December 21, 2006Publication date: September 16, 2010Inventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Raffaele Ingenito, Carsten Schultz-Fademrecht
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Publication number: 20100190762Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: April 2, 2010Publication date: July 29, 2010Applicant: CHEMOCENTRYX, INC.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Publication number: 20100168088Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20100168095Abstract: The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Ar2 represents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, X1 represents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by A?.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: Teiji KIMURA, Noritaka KITAZAWA, Toshihiko KANEKO, Nobuaki SATO, Koki KAWANO, Koichi ITO, Eriko DOI, Mamoru TAKAISHI, Takeo SASAKI, Takehiko MIYAGAWA, Hiroaki HAGIWARA, Takashi DOKO
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Publication number: 20100144812Abstract: Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.Type: ApplicationFiled: February 19, 2010Publication date: June 10, 2010Applicant: Wyeth LLPInventors: Lynn Resnick, Donna M. Huryn, Joan E. Sabalski, Joshua D. Berkowitz, Anthony Frank Kreft, Dennis Martin Kubrak, Thomas Joseph Caggiano, Koi Michele Morris
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Publication number: 20100120714Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R7, R8a, R8b, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: April 4, 2008Publication date: May 13, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Bruce Lawrence Finkelstein, Andrew Edmund Taggi, Jefrey Keith Long, Paula Louise Sharpe, Chi-ping Tseng, Stephen Frederick Mccann, Amy X. Ding, Steven Lewis Swann, JR.
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Publication number: 20100075951Abstract: This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: June 17, 2009Publication date: March 25, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: David P. Cardin, Paul Greenspan, Stepan Vyskocil, Jeffrey Gaulin, Tianlin Xu, Christelle C. Renou
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Patent number: 7674811Abstract: The present invention relates to 5-lipoxygenase inhibitors. Compounds disclosed herein can be useful in the treatment of bronchial asthma, chronic obstructive pulmonary disorder, arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, urticaria, atopic dermatitis, allergic rhinitis, other inflammatory, and autoimmune diseases. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as 5-lipoxygenase inhibitors are also provided.Type: GrantFiled: March 14, 2007Date of Patent: March 9, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Ashwani Kumar Verma, Sanjay Malhotra, Abhijit Ray, Shirumalla Raj Kumar
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Patent number: 7666890Abstract: Synthesis and herbicidal activity of novel 1-(2-substituted benzo[d]thiazol-5-yl)-1H-1,2,4-triazol-5(4H)-one derivatives. Using a dose of 300 gai./h, the compounds of the invention possess significant herbicidal activity for Echinochloa crusgalli, Digiatria sanguinalis, Setaria viridis, Brassica juncea, Amaranthus retroflexus and Chenopodium album.Type: GrantFiled: December 2, 2008Date of Patent: February 23, 2010Assignee: Huazhong Normal UniversityInventors: Guangfu Yang, Yanping Luo, Zuming Liu
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Publication number: 20090326026Abstract: There is provided compounds of formula (I), wherein X1, X2, X3, Y4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: ApplicationFiled: September 3, 2009Publication date: December 31, 2009Inventors: Mathias ALTERMAN, Anders Rudolf HALLBERG
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Publication number: 20090312375Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: ApplicationFiled: August 24, 2009Publication date: December 17, 2009Applicant: LEXICON PHARMACEUTICALS, INC.Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D.P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Patent number: 7618972Abstract: The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).Type: GrantFiled: March 8, 2006Date of Patent: November 17, 2009Assignee: Pfizer IncInventor: Andrew Antony Calabrese
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Patent number: 7612064Abstract: The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.Type: GrantFiled: May 24, 2004Date of Patent: November 3, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Martin Eberle, Philipp Ermert, Daniel Obrecht, Frank Lach, Anatol Luther, Felix Bachmann, Allessandro Strebel
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Patent number: 7598280Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: GrantFiled: February 28, 2008Date of Patent: October 6, 2009Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D. P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Patent number: 7572816Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.Type: GrantFiled: July 21, 2004Date of Patent: August 11, 2009Assignee: Auspex Pharmaceuticals, Inc.Inventors: Bruno Tse, Sepehr Sarshar
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Publication number: 20090111822Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: October 24, 2008Publication date: April 30, 2009Applicant: AstraZeneca ABInventors: Emma BRATT, Kenneth Granberg
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Publication number: 20090111823Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: October 24, 2008Publication date: April 30, 2009Applicant: AstraZeneca ABInventors: Kenneth GRANBERG, Bjorn Holm
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Publication number: 20090111821Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: October 24, 2008Publication date: April 30, 2009Applicant: AstraZeneca ABInventors: Methvin ISAAC, Andreas WALLBERG
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Patent number: 7521470Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: GrantFiled: June 20, 2005Date of Patent: April 21, 2009Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Publication number: 20090088570Abstract: An organic electroluminescent device, which has, between a pair of electrodes, at least one organic layer including a light-emitting layer, in which the organic layer contains a specific tetraphenylene compound, and in which the light-emitting layer contains a phosphorescent material; and a specific tetraphenylene compound that can be used in the device.Type: ApplicationFiled: November 20, 2008Publication date: April 2, 2009Applicant: FUJIFILM CORPORATIONInventors: Jun OGASAWARA, Tatsuya Igarashi, Satoshi Sano
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Publication number: 20090030050Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: ApplicationFiled: February 28, 2008Publication date: January 29, 2009Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D.P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Publication number: 20080311075Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: May 14, 2008Publication date: December 18, 2008Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Lawrence G. Hamann, Clint A. James, David R. Langley, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Gan Wang, Fukang Yang
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Publication number: 20080299080Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: November 15, 2007Publication date: December 4, 2008Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson, Constantin G. Yannopoulos, Guy Falardeau, Louis Vaillancourt, Real Denis
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Publication number: 20080255202Abstract: The present application relates to novel phenylthioacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, in particular dyslipidaemias and arteriosclerosis.Type: ApplicationFiled: March 26, 2005Publication date: October 16, 2008Applicant: Bayer HealthCare AGInventors: Hilmar Bischoff, Elke Dittrich-Wengenroth, Nils Griebenow, Axel Kretschmer, Joachim Kruger, Elisabeth Woltering, Lars Barfacker, Claudia Hirth-Dietrich, Peter Ellinghaus, Martin Raabe, Stephen Bartel, Christian Pilger, Ulrich Rosentreter, Klemens Lustig, Armin Kern, Dieter Lang