Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 544/250)
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Patent number: 7786131Abstract: The present invention relates to pyrimido [5,4-d] pyrimidine compounds of Formula II or a pharmaceutically acceptable salt thereof, wherein Q is and X, E1, E2, E3, R6 and p are as defined herein. The compounds of this invention are irreversible inhibitors of tyrosine kinases and are useful in the treatment of cancer, atherosclerosis, restenosis, endometriosis and psoriasis.Type: GrantFiled: May 20, 2003Date of Patent: August 31, 2010Assignee: Warner-Lambert CompanyInventors: Alexander James Bridges, William Alexander Denny, Ellen Myra Dobrusin, Annette Marian Doherty, David William Fry, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Jeffrey B. Smaill, Hairong Zhou
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Publication number: 20100216807Abstract: Novel heterocyclic compounds of formula I: A-B-D??Formula I or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III: B is a moiety selected from the group consisting of: D is a moiety selected from the group consisting of: which exhibit a dopamine receptor (preferably a D4 receptor) and/or a serotonine receptor (preferably 5HTA1 agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.Type: ApplicationFiled: September 24, 2007Publication date: August 26, 2010Applicant: ATIR Holding S.AInventor: Vladimir Kogan
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Publication number: 20100210639Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4?,3?:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: July 1, 2008Publication date: August 19, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, Suki Klair, Jane Scanlon, Glynn Addison, Michael Cherry
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Publication number: 20100204226Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: February 10, 2010Publication date: August 12, 2010Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, JR., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Publication number: 20100187515Abstract: Use of a precursor of an n-dopant for doping an organic semiconductive material, as a blocking layer, as a charge injection layer, as an electrode material, as a storage material or as a semiconductor material itself in electronic or optoelectronic components, the precursor being selected from the following formulae 1-3c:Type: ApplicationFiled: June 20, 2008Publication date: July 29, 2010Applicant: NOVALED AGInventors: Michael Limmert, Andrea Lux, Horst Hartmann
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Publication number: 20100190808Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis.Type: ApplicationFiled: January 23, 2009Publication date: July 29, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLC.Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharmo Rao, Matthew Kostura, Mustafa Guzel
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Publication number: 20100179127Abstract: The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, in which R1, R2, R3, R4 and A are as defined in the specification, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Philipp Floersheim, Wolfgang Froestl, Sebastien Guery, Kiemens Kaupmann, Manuel Koller
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Patent number: 7750017Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly hyperproliferative diseases such as cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly hyperproliferative diseases such as cancer.Type: GrantFiled: October 14, 2005Date of Patent: July 6, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Chengzhi Zhang, Roger Smith, Jason Duquette, Qian Zhao, Jacques Dumas, Georgiy Bondar, Yingfu Li, Dongping Fan
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Patent number: 7741333Abstract: The present invention relates to a quinazoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).Type: GrantFiled: June 21, 2007Date of Patent: June 22, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Olaf Prien, Knut Eis, Wolfgang Schwede, Judith Guenther, Dieter Zopf, Dominic E. A. Brittain
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Publication number: 20100145041Abstract: Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Trixi BRANDL, Udo MAIER, Matthias HOFFMANN, Stefan SCHEUERER, Anne T. JOERGENSEN, Alexander PAUTSCH, Steffen BREITFELDER, Matthias GRAUERT, Christoph HOENKE, Klaus ERB, Michael PIEPER, Ingo PRAGST
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Publication number: 20100144714Abstract: The present invention relates to new derivatives of imidazo, pyrimido and diazepine-pyrimidine-dione of the general formula (I) in which R1, R2, L1, L2, Y, Z and A are various and varying groups. These products exhibit a good affinity for certain sub-types of cannabinoid receptors, in particular the CB2 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said products, and to the use thereof for preparing a drug.Type: ApplicationFiled: December 17, 2007Publication date: June 10, 2010Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)Inventors: Lydie Poitout, Valérie Brault
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Publication number: 20100137343Abstract: This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: February 1, 2010Publication date: June 3, 2010Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding
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Publication number: 20100120805Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.Type: ApplicationFiled: November 9, 2009Publication date: May 13, 2010Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
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Publication number: 20100121056Abstract: The present invention relates to intercalator pseudonucleotides. Intercalator pseudonucleotides according to the invention are capable of being incorporated into the backbone of a nucleic acid or nucleic acid analogue and they comprise an intercalator comprising a flat conjugated system capable of co-stacking with nucleobases of DNA. The invention also relates to oligonucleotides or oligonucleotide analogues comprising at least one intercalator pseudo nucleotide. The invention furthermore relates to methods of synthesising intercalator pseudo nucleotides and methods of synthesising oligonucleotides or oligonucleotide analogues comprising at least one intercalator pseudonucleotide.Type: ApplicationFiled: August 3, 2009Publication date: May 13, 2010Applicant: Human Genetic Signatures Pty. Ltd.Inventors: Ulf Bech Christensen, Erik Bjerregaard Pedersen
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Publication number: 20100113485Abstract: The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno[2,3-d]pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypertension, congestive heart failure, and hypertension.Type: ApplicationFiled: October 30, 2009Publication date: May 6, 2010Inventors: Dale S. Dhanoa, Oren Becker, Silvia Noiman, Sekar Reddy Alla, Srinivasa Rao Cheruku, Rosa E. Mele'ndez, Anurag Sharadendu, Dongli Chen, Yael Marantz, Sharon Shacham, Alexander Heifetz, Boaz Inbal, Venkitasamy Kesavan, Shay Bar-Haim
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Patent number: 7700609Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: October 14, 2004Date of Patent: April 20, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
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Patent number: 7700608Abstract: A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof.Type: GrantFiled: August 3, 2005Date of Patent: April 20, 2010Assignee: Shire Holdings AGInventor: Richard Franklin
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Publication number: 20100087420Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: December 4, 2009Publication date: April 8, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur G. Taveras
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Publication number: 20100087453Abstract: The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associated with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: October 9, 2007Publication date: April 8, 2010Applicants: President and Fellows of Harvard College, Shanghai Institute of Organic ChemistryInventors: Junying Yuan, Chengye Yuan, Alexei Degterev
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Patent number: 7691868Abstract: Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.Type: GrantFiled: March 23, 2007Date of Patent: April 6, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Trixi Brandl, Udo Maier, Matthias Hoffmann, Stefan Scheuerer, Anne T. Joergensen, Alexander Pautsch, Steffen Breitfelder, Matthias Grauert, Christoph Hoenke, Klaus Erb, Michael Pieper, Ingo Pragst
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Publication number: 20100075999Abstract: The invention relates to a process for the preparation of anagrelide, and for the preparation of intermediates for use in preparing anagrelide. The invention also relates to the intermediates per se, in particular compounds of Formula (V): where R constitutes a suitable leaving group, which may not be hydrogen. The R group may be selected from: (i) —SiR13, (ii) —CH2Ar, (iii) —COOR2, and (iv) sulfonates such as —SO2R3.Type: ApplicationFiled: February 6, 2008Publication date: March 25, 2010Applicant: CIPLA LIMITEDInventors: Srinivas Laxminarayan Pathi, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
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Publication number: 20100075998Abstract: The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.Type: ApplicationFiled: November 23, 2007Publication date: March 25, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
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Publication number: 20100069374Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3Type: ApplicationFiled: November 17, 2009Publication date: March 18, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
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Patent number: 7678790Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 23, 2005Date of Patent: March 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
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Publication number: 20100056549Abstract: The present invention features pyrimido-dione-quinoline compounds having improved solubility, pharmaceutical compositions of substituted pyrimido-dione-quinoline compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more pyrimido-dione-quinoline compounds of the invention.Type: ApplicationFiled: June 13, 2007Publication date: March 4, 2010Applicant: Government of the US, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Allan Weissman, Yili Yang
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Publication number: 20100048593Abstract: The present invention features 5-deazaflavin compounds, pharmaceutical compositions of 5-deazaflavin compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more 5-deazaflavin compounds of the invention.Type: ApplicationFiled: February 23, 2009Publication date: February 25, 2010Applicants: Government of the US, as represented by the Secretary, Department of Health & Human Services, BioVeris CorporationInventors: Allan M. Weissman, Karen H. Vousden, Jane P. Jensen, Yili Yang, Shengyun Fang, Douglas Woods, John H. Kenten, Ilia Davydov, Yassamin J. Safiran, Pankaj Oberoi
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Publication number: 20100036123Abstract: The invention relates to a method of preparing 2,4-dichloro-7H-pyrrolo[2,3-h]quinazoline (II): from 1H-pyrrolo[2,3-h]quinazoline-2,4-dione.Type: ApplicationFiled: August 7, 2009Publication date: February 11, 2010Applicant: WyethInventors: Kenneth Alfred Martin Kremer, Uresh Shantilal Shah, Aranapakam Mudumbai Venkatesan, Zecheng Chen, Osvaldo dos Santos
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Publication number: 20100016341Abstract: Disclosed are compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof or wherein R1, R2, R3, R4, R6, R7, R14, W, V, X, Y, A and b are as described above in the specification. Also disclosed is a method of inhibiting aspartyl protease, methods of treating cardiovascular diseases, cognitive diseases, neurodegenerative diseases, and other biological processes and indications. Combination treatments and compositions are also disclosed.Type: ApplicationFiled: December 10, 2007Publication date: January 21, 2010Inventors: Zhaoning Zhu, Andrew Stamford, Guoqing Li, Mihirbaran Mandal
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Publication number: 20100008913Abstract: Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.Type: ApplicationFiled: July 22, 2009Publication date: January 14, 2010Inventor: Stephen R. Hanson
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Publication number: 20090325944Abstract: The invention relates to methods and products for modulating glycosylation of proteins. The invention is useful for treating glycosylation-associated disorders such as neurodegeneration, diabetes, including complications of diabetes such as insulin resistance, nephropathy, microvascular damage, and endothelial dysfunction. The invention also relates in part to assays that are useful for identifying and testing candidate compounds for modulating glycosylation of proteins.Type: ApplicationFiled: April 11, 2007Publication date: December 31, 2009Inventors: Suzanne Walker Kahne, Benjamin Gross
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Publication number: 20090325927Abstract: Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: July 2, 2009Publication date: December 31, 2009Inventors: Frank Chavez, Michael P. Curtis, James P. Edwards, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Brad M. Savall
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Publication number: 20090318421Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: April 28, 2006Publication date: December 24, 2009Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090306107Abstract: The present invention relates to compounds that are useful to inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway. The application is also concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy, and with other subject matter.Type: ApplicationFiled: March 17, 2006Publication date: December 10, 2009Applicant: NOVARTIS AGInventors: Lawrence Blas Perez, Tao Sheng
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Publication number: 20090293764Abstract: A dye compound has the following general formula (1). In the general formula (1), A1 denotes N or CR2. When A1 denotes N, R1 denotes an amino group. When A1 denotes CR2, R1 and R2 form an aromatic ring that has an anionic group. R3 denotes an alkyl group, an aryl group, or an aralkyl group. Cy denotes a substituted or unsubstituted aromatic ring.Type: ApplicationFiled: April 29, 2009Publication date: December 3, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Waka Hasegawa, Yasuaki Murai, Masashi Hirose, Takeshi Miyazaki
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Publication number: 20090298858Abstract: The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs.Type: ApplicationFiled: June 2, 2009Publication date: December 3, 2009Applicant: ABBOTT LABORATORIESInventors: Thomas D. Penning, Sheela A. Thomas, Philip J. Hajduk, Daryl R. Sauer, Kathy Sarris, Vincent L. Giranda
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Publication number: 20090286814Abstract: This invention relates to macrocyclic compounds of formula (I) or (II) shown in the specification. These compounds can be used to treat hepatitis C virus infection.Type: ApplicationFiled: November 4, 2008Publication date: November 19, 2009Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Chu-chung Lin, Kuang-Yuan Lee, Yo-chin Liu, Pin Lo, Rong-Jiunn Chen, Chen-Fu Liu, Chih-Ming Chen, Chi-Hsin Richard King
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Publication number: 20090286815Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: ApplicationFiled: May 19, 2009Publication date: November 19, 2009Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
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Publication number: 20090286811Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: April 9, 2009Publication date: November 19, 2009Inventors: Prasada Rao V.S. Lingham, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20090275533Abstract: Fused bicyclic pyrimidine compounds of formula (I): wherein R1, R3, R4, X1, X2, Y, Z, A, B, C, D, n, and the two bonds are defined herein. Also disclosed are a method for inhibiting Aurora kinase activity and a method for treating cancer with these compounds.Type: ApplicationFiled: April 22, 2009Publication date: November 5, 2009Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Su-Ying Wu, Yu-Sheng Chao
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Publication number: 20090270388Abstract: The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-? inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-? activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.Type: ApplicationFiled: March 30, 2009Publication date: October 29, 2009Applicant: Bayer Pharmaceuticals CorporationInventors: Mitsuyuki Shimada, Toshiki Murata, Kinji Fuchikami, Hideki Tsujishita, Naoki Omori, Issei Kato, Mami Miura, Klaus Urbahns, Florian Gantner, Kevin Bacon
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Patent number: 7598255Abstract: Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.Type: GrantFiled: July 27, 2006Date of Patent: October 6, 2009Assignee: Janssen Pharmaceutica NVInventor: Curt A. Dvorak
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Patent number: 7595324Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.Type: GrantFiled: November 9, 2007Date of Patent: September 29, 2009Assignee: Ardea Biosciences, Inc.Inventors: Jean-Luc Girardet, Zhi Hong, Stephanie Shaw, Yung-hyo Koh
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Publication number: 20090221597Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: February 25, 2009Publication date: September 3, 2009Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Publication number: 20090214529Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat a kinesin Eg5 protein-mediated disorder.Type: ApplicationFiled: May 22, 2008Publication date: August 27, 2009Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Ching-Cheng Wang, Hung-Chuan Chen, Shu-Huei Wang, Mei-Chun Lin, Tien-Lan Shieh, Ying-Huey Huang, Shih-Chieh Chuang, Chi-Hsin Richard King
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Publication number: 20090215746Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.Type: ApplicationFiled: October 31, 2008Publication date: August 27, 2009Applicant: Takeda Pharmaceuticals Company LimitedInventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
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Publication number: 20090215741Abstract: The disclosure concerns compounds of general formula (I): wherein n, X, Y, R1 and R2 are as defined herein. The disclosure also concerns a method for preparing the compounds and their therapeutic use.Type: ApplicationFiled: May 6, 2009Publication date: August 27, 2009Applicant: SANOFI-AVENTISInventors: Jacques FROISSANT, Frank MARGUET, Anne OLIVIER-BANDINI, Frederic PUECH
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Publication number: 20090212280Abstract: A method of using a metal complex as an n-dopant for doping an organic semiconducting matrix material in order to alter the latter's electrical characteristics is provided. In order to provide n-doped organic semiconductors with matrix materials having a low reduction potential, while achieving high conductivities, the n-dopant is a neutral electron-rich metal complex with a neutral or charged transition metal atom as a central atom and having at least 16 valence electrons. The complex can be polynuclear and can possess at least one metal-metal bond. At least one ligand can form a ? complex with the central atom, which can be a bridge ligand, or it can contain at least one carbanion-carbon atom or a divalent atom. Methods for providing the novel n-dopants are provided.Type: ApplicationFiled: March 3, 2005Publication date: August 27, 2009Inventors: Ansgar Werner, Olaf Kühl, Simon Gessler, Horst Hartmann, Andre Grüssing, Michael Limmert, Andrea Lux, Kentaro Harada
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Patent number: 7576091Abstract: A compound of formula 1, or a pharmaceutically acceptable salt thereof, wherein: X is S, O, or NH; “a” is a single bond; or “a” is a double bond and one of R3 and R4, and one of R5 and R6 are absent; R1 is H; or is selected from an alkyl group, a cycloalkyl group, a heteroaryl group, an aralkyl group, CO-alkyl, SO2-alkyl, CO2R13 and an aryl group, each of which optionally contains one or more heteroatoms, and is optionally substituted with one or more groups selected from R8 and R9; R2 is H, R8, or an alkyl group optionally substituted with one or more R8 groups; R3, R4, R5, and R6 are each independently selected from H, R8, an alkyl group and an alkenyl group, wherein said alkyl and alkenyl groups are optionally substituted with one or more R8 groups; or R3 and R4, and/or R5 and R6 together represent ?O; R7 is H, R8, NH(CH2)nR9, CO(CH2)nR9, NHCO(CH2)nR9, O(CH2)nR9, or an alkyl or phenyl group, each of which is optionally substituted with one or more groups selected from R8 and R9; R8 is OR10, NR10R11, haType: GrantFiled: January 6, 2006Date of Patent: August 18, 2009Assignee: Cyclacel LimitedInventors: Campbell McInnes, Mark Peter Thomas, Shudong Wang, Neil McIntyre, Nicholas Westwood, Peter Martin Fischer
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Patent number: 7576092Abstract: Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: July 10, 2007Date of Patent: August 18, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frank Chavez, Michael P. Curtis, James P. Edwards, Anne E. Fitzgerald, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Jing Liu, Neelakandha S. Mani, Brad M. Savall
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Publication number: 20090197901Abstract: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHCOR?, NHSO2R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.Type: ApplicationFiled: January 7, 2009Publication date: August 6, 2009Applicant: PHARMA MAR, S.A.Inventors: Modesto Remuinan, Juan Jose Gonzalez, Carlos del Pozo, Andres Francesh, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Regan James Anderson, Jonathan Charles Morris