Hetero Ring Is Seven-membered Consisting Of Two Nitrogens And Five Carbon Atoms Patents (Class 514/218)
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Patent number: 8435981Abstract: Compounds of the formula (I) in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1 are inhibitors of tyrosine kinases, in particular of met kinase and can be employed inter alia for the treatment of tumors.Type: GrantFiled: July 12, 2007Date of Patent: May 7, 2013Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
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Publication number: 20130109678Abstract: The invention relates to novel compounds, processes for their preparation and their use in protecting biological materials from radiation damage (radioprotection).Type: ApplicationFiled: April 6, 2011Publication date: May 2, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Roger Francis Martin, Jonathan White, Pavel Lobachevsky, David Winkler, Colin Skene, Sebastian Maruccio
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Publication number: 20130109670Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: ApplicationFiled: December 18, 2012Publication date: May 2, 2013Applicant: PFIZER INC.Inventor: PFIZER INC.
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Patent number: 8431567Abstract: The present invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, A, B and Y are as defined in claim 1, medicinal products containing them and use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.Type: GrantFiled: August 24, 2007Date of Patent: April 30, 2013Assignee: Abbott GmbH & Co. KGInventors: Herve Geneste, Thorsten Oost, Astrid Netz, Charles W. Hutchins, Wolfgang Wernet, Wilfred Lubisch, Liliane Unger, Wilfried Hornberger
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Patent number: 8431564Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: July 27, 2010Date of Patent: April 30, 2013Assignee: Merck Sharp & Dohme B.V.Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20130102592Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: December 5, 2012Publication date: April 25, 2013Applicant: SAREUM LIMITEDInventor: Sareum Limited
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Publication number: 20130102590Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicant: AbbVie IncInventor: AbbVie Inc.
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Publication number: 20130096100Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.Type: ApplicationFiled: September 14, 2012Publication date: April 18, 2013Applicant: ASTELLAS PHARMA INC.Inventors: Yutaka KONDOH, Kazuhiko Iikubo, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani, Itsuro Shimada, Takahiro Matsuya, Kazuo Kurosawa, Akio Kamikawa, Hiroyuki Mano
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Publication number: 20130096084Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: ApplicationFiled: June 22, 2011Publication date: April 18, 2013Inventors: Yongqi Deng, Liang Zhu, Gerald W. Shipps, JR., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
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Patent number: 8420630Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.Type: GrantFiled: February 24, 2010Date of Patent: April 16, 2013Assignees: Boehringer Ingelheim Pharma GmbH & Co. KG, Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schnapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoop, Steffen Steurer
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Patent number: 8420632Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: June 28, 2010Date of Patent: April 16, 2013Assignee: Galderma Research & DeveloplmentInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marléne Schuppli
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Publication number: 20130090326Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.Type: ApplicationFiled: October 15, 2010Publication date: April 11, 2013Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Yanming Du, Sandra Sinishtaj, Yuanqing Tang, Brian T. Wimberly
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N3-HETEROARYL SUBSTITUTED TRIAZOLES AND N5-HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20130090330Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: October 4, 2012Publication date: April 11, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC. -
Patent number: 8415340Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.Type: GrantFiled: July 24, 2008Date of Patent: April 9, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Upender Velaparthi, Peiying Liu, Mark D. Wittman, David R. Langley
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Patent number: 8415336Abstract: The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, wherein R, Ra, R10, R20, R30, R40, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.Type: GrantFiled: January 19, 2012Date of Patent: April 9, 2013Assignee: SanofiInventors: Henning Steinhagen, Bodo Scheiper, Hans Matter, Gary McCort, Guillaume Begis, Pascale Goberville, Berangere Thiers
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Publication number: 20130085134Abstract: Quinoxaline compounds of formula (I) have a PDE9-inhibiting action and are useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: ApplicationFiled: November 27, 2012Publication date: April 4, 2013Applicant: ASTELLAS PHARMA INC.Inventor: ASTELLAS PHARMA INC.
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Publication number: 20130085128Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 27, 2012Publication date: April 4, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130085127Abstract: A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.Type: ApplicationFiled: May 23, 2011Publication date: April 4, 2013Applicant: ASKA Pharmaceutical Co., LtdInventors: Makoto Okada, Koichi Hasumi, Takahiro Nishimoto, Miwa Yoshida, Kouki Ishitani, Tomoji Aotsuka, Hashime Kanazawa
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Publication number: 20130085135Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, 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: November 15, 2012Publication date: April 4, 2013Applicants: Genentech, Inc., Array BioPharma Inc.Inventors: Array BioPharma Inc., Genentech, Inc.
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Patent number: 8410088Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: April 13, 2012Date of Patent: April 2, 2013Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Masashi Seki, Syuji Shirotori
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Patent number: 8410091Abstract: The present invention is related to a process of preparing substituted 2-amino-5-(5-(heterocyclemethyl)pyridin-2-yloxy)benzoic acid compound of formula (I) or a salt thereof,Type: GrantFiled: September 9, 2010Date of Patent: April 2, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Magnus Carl Arne Eriksson, Dhileepkumar Krishnamurthy, Xiao-Jun Wang, Li Zhang
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Patent number: 8410090Abstract: The invention relates to heterocyclylamide-substituted thiazoles, pyrroles and thiophenes and processes for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: July 1, 2006Date of Patent: April 2, 2013Assignee: AiCuris GmbH & Co. KGInventors: Holger Zimmermann, David Brueckner, Kerstin Henninger, Martin Hendrix, Martin Radtke
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Publication number: 20130079321Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, 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: September 26, 2012Publication date: March 28, 2013Applicant: GENENTECH, INC.Inventor: GENENTECH, INC.
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Publication number: 20130079337Abstract: The invention relates to compounds corresponding to formula (I) in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.Type: ApplicationFiled: September 26, 2011Publication date: March 28, 2013Applicant: SANOFIInventors: ALEXANDRE BENAZET, OLIVIER DUCLOS, NATHALIE GUILLO, GILBERT LASSALLE, KARIM MACARY, VALÉRIE VIN
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Patent number: 8404677Abstract: The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.Type: GrantFiled: October 29, 2010Date of Patent: March 26, 2013Assignees: Genosco, Oscotec, Inc.Inventors: Hong Woo Kim, Jong Sung Koh, Jaekyoo Lee, Ho-Juhn Song, Youngsam Kim, Hee Kyu Lee, Jang-Sik Choi, Sun-Hee Lim, Sunhwa Chang
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Patent number: 8399455Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer, and osteolytic bone disorders.Type: GrantFiled: October 13, 2009Date of Patent: March 19, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Gerard Rosse, Linli Wei, Kenneth G. Carson
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Patent number: 8399456Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: April 21, 2010Date of Patent: March 19, 2013Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Raaum
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Patent number: 8399449Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: GrantFiled: February 25, 2009Date of Patent: March 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
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Patent number: 8394805Abstract: Novel compounds of which the following is exemplary:Type: GrantFiled: August 12, 2008Date of Patent: March 12, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Patent number: 8394789Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-?]isoquinoline and pyrrolo[2,1-?]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: February 6, 2009Date of Patent: March 12, 2013Assignee: MSD Oss B.V.Inventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lars Anders van der Veen, Willem Frederik Johan Karstens
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Publication number: 20130059836Abstract: Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.Type: ApplicationFiled: May 12, 2011Publication date: March 7, 2013Inventors: Xiaodong Wang, Jing Liu, Chao Yang, Weihe Zhaug, Stephen Frye, Dmitri Kireev
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Publication number: 20130059829Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.Type: ApplicationFiled: July 20, 2012Publication date: March 7, 2013Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
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PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE
Publication number: 20130059839Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: April 18, 2011Publication date: March 7, 2013Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Nicholas J. Lawrence, Roberta Pireddu, Said M. Sebti -
Patent number: 8389522Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: GrantFiled: October 19, 2009Date of Patent: March 5, 2013Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Publication number: 20130053371Abstract: There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: January 24, 2011Publication date: February 28, 2013Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLÓGICAS (CNIO)Inventors: Joaquin Pastor Fernández, Sonia Martinez Gonzalez, Rosa Maria Alvarez Escobar, Antonlo Rodriguez Hergueta, José Ignacio Martin Hernando, Francisco Ramos Lima
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Publication number: 20130053370Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.Type: ApplicationFiled: January 31, 2011Publication date: February 28, 2013Applicants: HANMI SCIENCE CO., LTD., CATHOLIC UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Jung Beom Son, Seung Hyun Jung, Wha ll Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
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Publication number: 20130053361Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: July 5, 2012Publication date: February 28, 2013Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20130053363Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.Type: ApplicationFiled: October 26, 2012Publication date: February 28, 2013Applicant: Astellas Pharma Inc.Inventor: Astellas Pharma Inc.
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Publication number: 20130053348Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: September 12, 2012Publication date: February 28, 2013Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Sing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
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Publication number: 20130053346Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: ApplicationFiled: August 23, 2012Publication date: February 28, 2013Applicant: Endo Pharmaceuticals IncInventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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Publication number: 20130053372Abstract: The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.Type: ApplicationFiled: February 15, 2011Publication date: February 28, 2013Inventors: Prashant Bhimrao Kapadnis, Robert Glen, Robin Hiley, James Bell, David Spring
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Patent number: 8383660Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: GrantFiled: January 3, 2007Date of Patent: February 26, 2013Assignee: Pfizer Inc.Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
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Publication number: 20130045955Abstract: The present invention provides compounds of formula (I) herein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 16, 2012Publication date: February 21, 2013Inventors: Nicholas J. Bennett, Thomas MCINALLY, Tobias MOCHEL, Stephen Thom, Anna-Karin Tidén
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Publication number: 20130046009Abstract: The disclosure is directed to methods of treating hematologic malignancies. More particularly, the disclosure is directed to methods of treating hematologic malignancies using Rho kinase (ROCK) inhibitors and myosin light chain-specific inhibitory RNA molecules. The disclosure is further directed to methods of identifying drug candidates for inhibiting ROCK in hematologic malignancies.Type: ApplicationFiled: August 15, 2012Publication date: February 21, 2013Inventor: Reuben Kapur
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Publication number: 20130045975Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.Type: ApplicationFiled: February 10, 2012Publication date: February 21, 2013Applicant: KALYPSYS, INC.Inventors: Steven P. Govek, Clay Beauregard, Daniel A. Gamache, Mark R. Hellberg, Stewart A. Noble, Andrew K. Shiau, David J. Thomas, John M. Yanni
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Patent number: 8377925Abstract: The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.Type: GrantFiled: February 24, 2009Date of Patent: February 19, 2013Assignee: Mimetica Pty LtdInventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
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Patent number: 8377957Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: November 29, 2011Date of Patent: February 19, 2013Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Patent number: 8377926Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: February 4, 2011Date of Patent: February 19, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francois Maltais, Guy W. Bemis, Tiansheng Wang, Juan-Miguel Jimenez, Luca Settimo, Stephen Young, Dean Boyall, Damien Fraysse, Christopher John Davis
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Publication number: 20130040930Abstract: 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, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Patent number: RE44205Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compType: GrantFiled: April 6, 2012Date of Patent: May 7, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil