The Additional Five-membered Hetero Ring Also Has Chalcogen As A Ring Member Patents (Class 514/254.02)
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Publication number: 20120004213Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Kumar SUNDARESAN, Sandeep N. RAIKAR, Srinivasa Raju SAMMETA, Ganesh PRABHU, Hosahalli SUBRAMANYA, Alexander BISCHOFF
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Publication number: 20120004216Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane 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: July 1, 2011Publication date: January 5, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D.J. Grootenhuis
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Patent number: 8088777Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: its pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen or the like, Y is a group of the formula: Z is —NR7— or the like, R1 is hydrogen or the like, R2 and R3 are each independently hydrogen or the like, n is 0 or 1, p is 0 to 6.Type: GrantFiled: August 28, 2007Date of Patent: January 3, 2012Assignee: Shionogi & Co., Ltd.Inventor: Toshisada Yano
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Patent number: 8088760Abstract: A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: GrantFiled: January 16, 2009Date of Patent: January 3, 2012Assignee: BioMarin Pharmaceutical Inc.Inventors: Daniel Chu, Bing Wang
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Publication number: 20110319423Abstract: The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.Type: ApplicationFiled: September 28, 2009Publication date: December 29, 2011Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Science, P.L.AInventors: Jin Li, Rifang Yang, Rui Song, Hui Zhu, Ning Wu, Liuhong Yun, Ruibin Su, Rusheng Zhao
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Publication number: 20110312969Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.Type: ApplicationFiled: December 8, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotei, Smantha Jayne Bamford
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Publication number: 20110306620Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: October 27, 2010Publication date: December 15, 2011Applicant: Bayer CropScience AGInventors: Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
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Publication number: 20110301149Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: ApplicationFiled: October 12, 2009Publication date: December 8, 2011Applicant: VM DISCOVERY INC.Inventor: Jay Jie-Qiang Wu
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Publication number: 20110301143Abstract: Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, C?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.Type: ApplicationFiled: February 18, 2010Publication date: December 8, 2011Inventors: Elise Isabel, Nicolas Lachance, Jean-Philippe Leclerc, Serge Leger, Renata M. Oballa, David Powell, Yeeman K. Ramtohul, Patrick Roy, Geoffrey K. Tranmer, Renee Aspiotis, Lianhai Li, Evelyn Martins
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Publication number: 20110301176Abstract: There is provided compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. Compounds include imidazothiazole derivatives that can inhibit interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity.Type: ApplicationFiled: July 15, 2011Publication date: December 8, 2011Inventors: Kouichi Uoto, Yuuichi Sugimoto, Hiroyuki Naito, Masaki Miyazaki, Keisuke Yoshida, Masashi Aonuma
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Publication number: 20110301158Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: ApplicationFiled: August 15, 2011Publication date: December 8, 2011Applicant: Novo Nordisk A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce-Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M.M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
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Publication number: 20110294822Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.Type: ApplicationFiled: December 22, 2009Publication date: December 1, 2011Applicant: NHWA PHARMA. CORPORATIONInventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110294813Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: June 30, 2011Publication date: December 1, 2011Applicants: SHIONOGI & CO., LTD., INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20110288088Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: May 17, 2011Publication date: November 24, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.I.Inventors: Tiziano BANDIERA, Andrea LOMBARDI BORGIA, Sten Christian ORRENIUS, Ettore PERRONE, Italo BERIA, Daniele FANCELLI, Arturo GALVANI
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Publication number: 20110288083Abstract: The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK.Type: ApplicationFiled: May 19, 2011Publication date: November 24, 2011Applicant: NEW YORK UNIVERSITYInventors: Timothy CARDOZO, Hong WANG, David Ron
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Patent number: 8063042Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y, R3, R4, R5, R6, R7, R8, R9, R10, m and n are as herein defined, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: GrantFiled: July 10, 2008Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin
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Patent number: 8058299Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 1, 2008Date of Patent: November 15, 2011Assignee: VIA Pharmaceuticals, Inc.Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Apostle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
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Publication number: 20110275636Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: ApplicationFiled: May 4, 2011Publication date: November 10, 2011Applicant: FerroKin BioSciences, Inc.Inventor: James Malecha
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Publication number: 20110275609Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: January 14, 2010Publication date: November 10, 2011Applicant: CARA THERAPEUTICS, INC.Inventor: Robert Zhiyong Luo
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Publication number: 20110269756Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: December 8, 2009Publication date: November 3, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20110269750Abstract: The application relates to specific combinations of Roflumilast and/or Roflumilast N-Oxide and a PPAR-agonist, as well as their use in the treatment of diabetes mellitus type 2.Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Applicant: NYCOMED GMBHInventors: Hans-Peter KLEY, Guido HANAUER, Daniela HAUSER, Beate SCHMIDT, Dirk BREDENBRÖKER, Wilhelm WURST, Jörg KEMKOWSKI
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Publication number: 20110269817Abstract: The invention relates to modulation of circadian rhythm and underlying biological processes.Type: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: The Regents of the University of CaliforniaInventors: Paolo Sassone-Corsi, Yasukazu Nakahata
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Publication number: 20110263571Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.Type: ApplicationFiled: October 27, 2009Publication date: October 27, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Seigo Ishibuchi, Hidemasa Hikawa, Akiko Tarao, Jun-ichi Endoh, Kunitomo Adachi, Kazuhiro Maeda, Kaoru Tashiro
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Publication number: 20110263562Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.Type: ApplicationFiled: April 26, 2011Publication date: October 27, 2011Inventors: Tohru Yamashita, Makoto Kamata, Hideki Hirose, Masataka Murakami, Takuya Fujimoto, Zenichi Ikeda, Tsuneo Yasuma, Ikuo Fujimori, Ryo Mizojiri, Tomoya Yukawa
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Publication number: 20110263596Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 8044079Abstract: The invention relates to novel oxindole derivative of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: December 1, 2006Date of Patent: October 25, 2011Assignee: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Patent number: 8039463Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: March 20, 2009Date of Patent: October 18, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Kumar Sundaresan, Sandeep N. Raikar, Srinivasa Raju Sammeta, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Publication number: 20110251212Abstract: A compound which specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist is provided. It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is —N(R4)—C(?O)—C(?O)—, —N(R4)—(CR5R6)p—C(?O)—, —N(R4)—C(?O)—(CR7R8)q— or —C(?O)—N(R4)—(CR7R8)q—, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 19, 2008Publication date: October 13, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Minoru Tomida, Naotake Kobayashi, Kousuke Anan, Aya Tazawa, Kayoko Hata
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Publication number: 20110251176Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: April 6, 2011Publication date: October 13, 2011Inventor: Xiaojing Wang
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Publication number: 20110251214Abstract: This invention relates to a process for the preparation of 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride, a partial dopamine-D2 receptor agonist and a full serotonin 5-HT1A receptor agonist. This invention also relates to the monohydrate of said compound, as well as to pharmaceutical compositions containing these compounds, to methods for preparing these compounds, to methods for preparing intermediates useful for their synthesis, and to methods for preparing compositions containing these compounds.Type: ApplicationFiled: October 10, 2010Publication date: October 13, 2011Inventors: Jeroen Van Rheenen, Wilhelmus G.H.M. Muijselaar, Hendrik Teunissen
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Patent number: 8030307Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. 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 a compound of the present invention.Type: GrantFiled: November 26, 2008Date of Patent: October 4, 2011Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joel D. Moore, Yat Sun Or, Zhe Wang
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Publication number: 20110224219Abstract: The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.Type: ApplicationFiled: November 10, 2009Publication date: September 15, 2011Applicant: LG LIFE SCIENCES LTD.Inventors: Koo Lee, Sang Dae Lee, Sang Pil Moon, In Ae Ahn, Sung Pil Choi, Hyun Ho Lee, Dong Sup Shim, Soo Yong Chung, Hyun Min Lee
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Publication number: 20110224211Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20110218182Abstract: The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.Type: ApplicationFiled: July 2, 2009Publication date: September 8, 2011Applicant: ASTRAZENECA ABInventors: Leslie Dakin, James Edward Dowling, Michelle Lamb, Jon Read, Qibin Su, Xiaolan Zheng
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Publication number: 20110212964Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: May 9, 2011Publication date: September 1, 2011Applicant: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Allen Yu Hong, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Patent number: 8003790Abstract: The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.Type: GrantFiled: February 17, 2006Date of Patent: August 23, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Tomohiro Yoshida, Hiroshi Sakashita, Naoko Ueda, Shinji Kirihara, Satoru Uemori, Reiko Tsutsumiuchi, Fumihiko Akahoshi
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Publication number: 20110200586Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110201604Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
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Publication number: 20110200687Abstract: The present disclosure provides novel pharmaceutical dosage forms such as a maintenance treatment dose and methods for making the same, and methods for using said compounds and maintenance treatment doses to treat and prevent diseases and/or disorders.Type: ApplicationFiled: March 8, 2011Publication date: August 18, 2011Inventors: Irene EIJGENDAAL, Gerrit Klein, Maria J.L. Terhorst-Van Amstel, Klaas ZWIER, Nico BRUINS, Hendrikus T. RIGTER, Erik GOUT, Caroline BOON, Michiel H. De Vries, Dorte MALLING, Anneke WINSEMIUS, Sangeeta RAJE, Ellen Bech CHRISTENSEN, Jeff PAUL
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Publication number: 20110200587Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110195955Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: ApplicationFiled: August 18, 2008Publication date: August 11, 2011Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
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Publication number: 20110190299Abstract: An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.Type: ApplicationFiled: April 19, 2010Publication date: August 4, 2011Applicants: SBI BIOTECH CO., LTD., CRYSTALGENOMICS, INC.Inventors: Takayuki Irie, Masaaki Sawa, Sayuri Ito, Chika Tanaka, Seong Gu Ro, Choul Hong Park
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Publication number: 20110178063Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: July 21, 2011Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20110172245Abstract: Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: August 22, 2008Publication date: July 14, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaaki Hirose, Masanori Okaniwa, Takashi Imada
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Patent number: 7977489Abstract: Compounds of the following general structure for use in compositions and methods for modulating the activity of nuclear receptors are provided: The compounds are useable in compositions and methods for modulating the estrogen related receptors and are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR?.Type: GrantFiled: October 21, 2005Date of Patent: July 12, 2011Assignee: Exelixis, Inc.Inventors: Richard Martin, Raju Mohan, Brett B. Busch, Michael Charles Nyman, William C. Stevens, Jr.
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Publication number: 20110158940Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: June 2, 2009Publication date: June 30, 2011Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Dennis F. Hruby
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Publication number: 20110160223Abstract: Provided are pharmaceutical compositions and methods of treatment or prophylaxis of certain neuropsychiatric conditions, in particular mood disorders. The compounds are of the general Formula I-V as described herein.Type: ApplicationFiled: November 2, 2010Publication date: June 30, 2011Inventors: Raymond J. Dingledine, Stephen F. Traynelis