The Additional Hetero Ring And The Bicyclo Ring System Are Attached Directly To The Same Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 548/468)
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Publication number: 20130259830Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.Type: ApplicationFiled: June 24, 2011Publication date: October 3, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
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Publication number: 20130253186Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 10, 2013Publication date: September 26, 2013Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Publication number: 20130231373Abstract: The present teachings relate to compounds of Formula (I): and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, R4, R5, ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula (I) and methods of use compounds of Formula (I) in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: August 27, 2010Publication date: September 5, 2013Applicant: Novartis AGInventors: Clinton Alan Brooks, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Gang Liu, Michael David Schultz
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Patent number: 8524709Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: GrantFiled: January 12, 2012Date of Patent: September 3, 2013Assignee: Tyrogenex, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20130225617Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.Type: ApplicationFiled: January 31, 2013Publication date: August 29, 2013Applicant: PULMAGEN THERAPEUTICS (ASTHMA) LIMITEDInventor: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
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Patent number: 8518943Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 6, 2012Date of Patent: August 27, 2013Assignee: UCB Pharma, S.A.Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Publication number: 20130217679Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: ApplicationFiled: March 23, 2011Publication date: August 22, 2013Applicants: THE SCRIPPS RESEARCH INSTITUTE, THE JOHNS HOPKINS UNIVERSITYInventors: Donald J. Zack, Thomas Bannister, Tomas Vojkovsky, Zhiyong Yang, Cynthia Berlinicke
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Publication number: 20130210885Abstract: The present invention relates to crystalline forms of L-malic acid salt of sunitinib and its preparation. The crystalline forms of the present invention are designated as Form V and Form VI of L-malic acid salt of sunitinib. Formula (I).Type: ApplicationFiled: January 28, 2011Publication date: August 15, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Sudhir Singh Sanwal, Saridi Madhava Dileep Kumar, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Patent number: 8501962Abstract: The present invention relates to an improved process for the preparation of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide—Sunitinib base of formula (I) and its pharmaceutically acceptable malate salt of formula (I(a)).Type: GrantFiled: November 17, 2008Date of Patent: August 6, 2013Assignee: Natco Pharma LimitedInventors: Srinivasa Krishna Murthy Konduri, Bhujanga Rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
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Publication number: 20130197242Abstract: The present invention relates to stable crystalline Form II of L-malic acid salt of sunitinib and its preparation.Type: ApplicationFiled: November 19, 2010Publication date: August 1, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Sudhir Singh Sanwal, Saridi Madhava Dileep Kumar, Swargam Sathyanarayana
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Publication number: 20130190512Abstract: The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate.Type: ApplicationFiled: November 1, 2010Publication date: July 25, 2013Applicant: SCINOPHARM TAIWAN, LTD.Inventors: Julian P. Henscheke, Yung-Fa Chen
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Patent number: 8492428Abstract: Small-molecule inhibitors of Botulinum toxin, including BoNTA, BoNTD and BoNTE are provided, as well as methods of using the inhibitors.Type: GrantFiled: September 20, 2006Date of Patent: July 23, 2013Assignees: Mayo Foundation for Medical Education and Research, The United States of America As Represented by the Secretary of the ArmyInventors: Yuan-Ping Pang, Jewn Giew Park, Jing Tang, Charles B. Millard, James J. Schmidt
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Patent number: 8492559Abstract: Substituted indole compounds corresponding to the formula I: In which R8, R9a, R9b, R10, R11, R200, R210, A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).Type: GrantFiled: February 3, 2010Date of Patent: July 23, 2013Assignee: Gruenenthal GmbHInventors: Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Patent number: 8476432Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: GrantFiled: June 30, 2011Date of Patent: July 2, 2013Assignee: Yuhan CorporationInventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Publication number: 20130158030Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).Type: ApplicationFiled: March 31, 2011Publication date: June 20, 2013Applicant: QILU PHARMACEUTICAL CO., LTDInventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Boyan Xu, Shousheng Yan, Zongru Guo, Minghui Zhang, Dong Lin, Zhantao Zhang, Haojie Zhou
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Patent number: 8466190Abstract: The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals.Type: GrantFiled: April 16, 2008Date of Patent: June 18, 2013Assignee: Natco Pharma LimitedInventors: Srinivasa Krishna Murthy Konduri, Bhujanga Rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
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Publication number: 20130144059Abstract: The present invention relates to the use of PDGF-R inhibitors for the treatment of lymph node metastasis of gastric cancers and to a method of treating mammals including humans suffering from gastric cancer.Type: ApplicationFiled: April 28, 2011Publication date: June 6, 2013Inventor: Yasuhiko Kitadai
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Patent number: 8450361Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: August 4, 2011Date of Patent: May 28, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20130123511Abstract: The present invention relates to a process for the direct preparation of malic acid salt of sunitinib.Type: ApplicationFiled: February 25, 2011Publication date: May 16, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Sudhir Singh Sanwal, Saridi Madhava Dileep Kumar, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Publication number: 20130116298Abstract: The present invention provides an antitumor agent or postoperative adjuvant chemotherapeutic agent for a hepatocellular carcinoma patient who has been treated by transarterial embolization. An antitumor agent or postoperative adjuvant chemotherapeutic agent comprising TSU-68 or a salt thereof, which can be administered to a hepatocellular carcinoma patient within 2 weeks after transarterial embolization, is provided.Type: ApplicationFiled: December 24, 2010Publication date: May 9, 2013Inventor: Toshinori Oka
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Publication number: 20130102776Abstract: An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6 alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6 alkyl group and the like; R4 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6 alkyl group and the like; R8 represents hydrogen atom, a C1-6 alkyl group and the like; A represents —O—, —S—, or —CH2—; D represents —C? or —N?; X represents methylene group, —O—, or —CO—; Q represents —N? or —C(R8)?; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.Type: ApplicationFiled: April 28, 2011Publication date: April 25, 2013Applicants: RIKEN, THE UNIVERSITY OF TOKYOInventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Nae Saito, Hirofumi Nakano, Masanao Abe, Akiko Tanaka, Teruki Honma, Shigeyuki Yokoyama, Keiko Tsuganezawa, Hitomi Yuki
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Patent number: 8426612Abstract: The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.Type: GrantFiled: November 9, 2009Date of Patent: April 23, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Siro Serafini, Andrea Castellin, Claudio Dal Santo
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Publication number: 20130096303Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: ApplicationFiled: June 30, 2011Publication date: April 18, 2013Inventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Patent number: 8415349Abstract: The invention provides derivatives of azabicyclo alkane having formula (ID), and the method for making them, wherein each substitute in formula (ID) is same as defined in the description.Type: GrantFiled: September 14, 2012Date of Patent: April 9, 2013Assignee: Jiangsu Hansoh Pharmaceuticals Co., Ltd.Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
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Patent number: 8389562Abstract: The invention relates to new crystalline polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (i.e., sunitinib base), including Form I, Form II, and Form IV, processes for preparing crystalline polymorphic forms of sunitinib base, and pharmaceutically acceptable salts of new crystalline polymorphic forms of sunitinib base and pharmaceutical compositions comprising new crystalline polymorphic forms of sunitinib base, salts of new crystalline polymorphic forms of sunitinib base and mixtures thereof.Type: GrantFiled: December 12, 2008Date of Patent: March 5, 2013Assignee: Medichem, S.A.Inventors: Stephen Benedict David Winter, Bernardino Mangion
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Patent number: 8383830Abstract: Cyanine compounds having the general formula I for staining biological samples, wherein R1, R2, X, Y, A1 and A2 are as defined in the specification. These kinds of compounds may show good light illumination stability, have a maximum absorption peak around 640 nm that may not change as a function of ambient temperature, have rapidly increased fluorescence intensity upon binding to nucleic acids to form compound/nucleic acid complexes, and have a light spectrum in the near-infrared region, thereby effectively reducing interference from background fluorescence and increasing the accuracy of the detection when used as a staining agent for nucleic acids in a flow cytometer. The compounds provided can be used as a staining agent for erythroblasts in the blood.Type: GrantFiled: October 28, 2009Date of Patent: February 26, 2013Assignee: Shenzhen Mindray Bio-Medical Electronics Co., LtdInventors: Jianhui Shao, Bing Xu
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Publication number: 20130040865Abstract: The present invention provides a succinimide compound represented by the following formula (1-1) or (1-2), and a lubricating oil additive and a lubricating oil composition which contain the succinimide compound. wherein R represents an alkyl group or an alkenyl group having a number-average molecular weight of 500 or greater and less than 5000. wherein R represents an alkyl group or an alkenyl group having a number-average molecular weight of 500 or greater and less than 5000.Type: ApplicationFiled: March 29, 2011Publication date: February 14, 2013Applicant: JX NIPPON OIL & ENERGY CORPORATIONInventors: Kazuo Tagawa, Miho Endou
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Publication number: 20130023672Abstract: A process for preparation of eletriptan hydrobromide having a-form of formula (I) is described that includes reducing 3-((R)-1-methylpyrrolidin-2-yl)methyl)-5-((E)-2-(phenylsulfonyl)vinyl)-1H-indole of formula (II) in presence of a metal catalyst to the product of formula (III) and then converting to hydrobromide salt having a-form of formula (I).Type: ApplicationFiled: March 31, 2010Publication date: January 24, 2013Inventors: Srinivasa Rao Venturi, Hari Prasad Kodali, Hariharakrishnan Venkata Subhramanian, Vankata Srihari Tadimalla, Ramesh Babu Potluri
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Publication number: 20120322844Abstract: The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: August 23, 2012Publication date: December 20, 2012Inventors: Xiong Cai, Changgeng Qian, Stephen Gould
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Publication number: 20120316193Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.Type: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Inventors: Megan Foley, Bradley Tait, Matthew Cullen
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Patent number: 8329740Abstract: The present invention provides a novel crystalline form of sunitinib malate, process for its preparation and to pharmaceutical composition containing it. The present invention also provides a process for preparation of sunitinib malate crystal form I. Thus, for example, sunitinib malate was added to water, the mixture was heated to 80 deg C. to obtain a clear solution and stirred for 30 minutes at 80 deg C., slowly cooled to room temperature and the solution was subjected to freeze drying at about ?90 deg C. for 8 hours to give sunitinib malate crystalline form III.Type: GrantFiled: January 2, 2009Date of Patent: December 11, 2012Assignee: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
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Publication number: 20120289571Abstract: The present invention relates to releasable urea linker systems involving amine-containing chemical compounds and biologically active agents. In particular, the present invention relates to reversibly releasable linkers based on intramolecular cyclization-assisted releasable urea linkages to aromatic amine-containing compounds. The present invention also relates to polymeric conjugates of indolinone-based tyrosine kinase inhibitors.Type: ApplicationFiled: December 30, 2010Publication date: November 15, 2012Applicant: ENZON PHARMACEUTICALS, INC.Inventors: Hong Zhao, Dechun Wu, Snehlata Tripathi, Jing Xia
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Patent number: 8304411Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.Type: GrantFiled: May 20, 2008Date of Patent: November 6, 2012Assignees: Jiangsu Hansoh Pharmaceutical Co., Ltd., Shanghai Hengrui Pharmaceutical Co. Ltd.Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lu, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
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Publication number: 20120277238Abstract: The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is —O—, etc., n is an integer of 0 to 6; X is —N(R7)— or —O—; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is —C(R8)? or —N?; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is ?O, ?S, etc.; B ring is a ring represented by the following formula: wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: July 29, 2010Publication date: November 1, 2012Applicant: Shionogi & Co., LtdInventors: Yuuki Tachibana, Masayoshi Miyagawa, Tsutomu Masuda, Tsuyoshi Hasegawa
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Publication number: 20120264803Abstract: The present invention provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining sufficient therapeutic effects from such chemotherapy. The present invention also provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization using the expression level of PDGF-BB or IL-8 as an indicator and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining therapeutic effects by such prediction method.Type: ApplicationFiled: December 24, 2010Publication date: October 18, 2012Inventor: Toshinori Oka
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Patent number: 8277920Abstract: An optical recording material comprising at least one kind of chalcone type compound represented by the following general formula (I) or a metal complex using the chalcone type compound as a ligand: wherein ring A represents a 5- or 6-membered heterocyclic ring or an aromatic ring; ring B represents a 5- or 6-membered heterocyclic ring, an aromatic ring, or a metallocene structure; the above-mentioned heterocyclic and aromatic ring may be condensed with other rings or may be substituted; n is 0 or 1.Type: GrantFiled: April 24, 2007Date of Patent: October 2, 2012Assignee: Adeka CorporationInventors: Toru Yano, Yohei Aoyama
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Publication number: 20120238752Abstract: Provided is a colored photosensitive curing composition useful for color filters in primary colors, including blue, green, and red, having a high molar absorption coefficient and allowing a reduction in film thickness and superior color purity and fastness. A colored photosensitive curing composition, comprising, as its colorant, a dipyrromethene-based metal complex compound obtained from a metal or metal compound and a dipyrromethene-based compound represented by the following Formula (I): wherein in Formula (I), R1 to R6 each independently represent a hydrogen atom or a substituent group; and R7 represents a hydrogen or halogen atom, or an alkyl, aryl or heterocyclic group.Type: ApplicationFiled: May 23, 2012Publication date: September 20, 2012Applicant: FUJIFILM CORPORATIONInventors: Yuki MIZUKAWA, Ryoji GOTO, Hideki TAKAKUWA, Masashi OGIYAMA, Toru FUJIMORI
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Publication number: 20120232070Abstract: Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Applicant: Laboratoires Fournier SAInventors: Jerome Amaudrut, Benaissa Boubia, Maria Johanna Petronella Van Dongen, Fabrice Guillier, Olivia Poupardin-Olivier
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Publication number: 20120220783Abstract: The present invention relates to salts of sunitinib and their preparation.Type: ApplicationFiled: September 16, 2010Publication date: August 30, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Sudhir Singh Sanwal, Saridi Madhava Dileep Kumar, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Publication number: 20120214815Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 23, 2012Applicant: UCB Pharma, S.A.Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
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Publication number: 20120209003Abstract: Methods for identifying MarR family inhibiting compounds are described. The methods include the use of computer aided rational based drug design programs and three dimensional structures of MarR family polypeptides.Type: ApplicationFiled: September 9, 2011Publication date: August 16, 2012Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Stuart B. Levy, Brent L. Podlogar, Roger Frechette
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Publication number: 20120196866Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 2, 2012Applicant: UCB PHARMA, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
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Publication number: 20120196893Abstract: The present invention provides a method of optical electrophysiological probing, including: providing a fluorescing chemical probe; contacting a thick portion of tissue with the fluorescing chemical probe to create a thick portion of treated tissue; applying a first range of wavelengths of electromagnetic radiation to the treated portion of tissue; and detecting a plurality of depth-specific emission wavelengths emitted from the thick portion of treated tissue.Type: ApplicationFiled: April 9, 2012Publication date: August 2, 2012Applicants: The University of Connecticut, The Research Foundation of State University of New YorkInventors: Arkady M. Pertsov, Arvydas Matiukas, Leslie M. Loew, Joseph P. Wuskell
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Publication number: 20120190669Abstract: The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.Type: ApplicationFiled: January 20, 2012Publication date: July 26, 2012Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Mustapha Haddach, Johnny Yasuo Nagasawa
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Patent number: 8222274Abstract: [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).Type: GrantFiled: February 19, 2007Date of Patent: July 17, 2012Assignee: Astellas Pharma Inc.Inventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
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Publication number: 20120178780Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: 8206806Abstract: A cyanine compound is represented by formula (I): A1: benzene or naphthalene ring. A3: 5- or 6-membered ring. R1, R2: hydrogen atom and the like. R7: an alkyl group and the like. R12: a substituent by formula (II) or (II?). R20: a hydrogen atom and the like. Anq-: a q-valent anion. q: 1 or 2; p: a coefficient for neutral charge. In formula (II): bond between L and T is a double, conjugated double, or triple bond. L: carbon atom. T: carbon, oxygen, sulfur, or nitrogen atom. x, y, z: 0 or 1. s: 0-4. R13: hydrogen atom and the like. R14, R15, and R16: hydrogen atom and the like. In formula (II?), the bond between L? and T? is a double or conjugated double bond. L?: carbon atom. T?: carbon, oxygen, nitrogen atom. s?: 0-4. Ring containing L? and T?: 5-membered ring, may contain a heteroatom.Type: GrantFiled: March 23, 2007Date of Patent: June 26, 2012Assignee: Adeka CorporationInventors: Toru Yano, Satoshi Yanagisawa, Yohei Aoyama, Koichi Shigeno
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Publication number: 20120156213Abstract: The present application relates to a method for treating or preventing Th17 inflammatory disease mediated with IL-6 or IL-17 by administration of medication which inhibits vascular endothelial growth factor receptors, and a pharmaceutical composition therefor.Type: ApplicationFiled: May 20, 2010Publication date: June 21, 2012Applicant: POSTECH ACADEMY-INDUSTRY FOUNDATIONInventors: Yoon Keun Kim, Yong Song Gho, Yu Sun Kim
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Publication number: 20120142749Abstract: The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1, 2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.Type: ApplicationFiled: February 6, 2012Publication date: June 7, 2012Applicants: PFIZER PRODUCTS INC., PFIZER INC.Inventors: Changquan C. Sun, Michael Hawley
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Publication number: 20120122948Abstract: The invention relates to a compound of formula (Ia) wherein n is an integer between 2 and 10, R1 and R2 independently represent a substituent selected from the group consisting of hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl and aminoalkyl, or R1 and R2 are taken together with the nitrogen atom to which they are attached to form a four to ten-membered heterocycle, R5 represents independently in each of the n units a substituent selected from the group consisting of hydrogen, C1-C10 alkyl, halogen, alkoxy, aminoalkyl and alkylamino; or a pharmaceutically acceptable salt thereof, with the proviso that the 5-fluorotryptamine is excluded, for the treatment or the prophylaxis of neuroinflammatory diseases or disorders. The invention also relates to a pharmaceutical composition, a method for inhibiting myeloperoxidase enzyme activity, to a method for inhibiting Low density lipoproteins oxidation.Type: ApplicationFiled: May 27, 2010Publication date: May 17, 2012Applicant: UNIVERSITE LIBRE DE BEUXELLESInventors: Jalal Soubhye, François Dufrasne, Pierre Van Antwerpen