The Additional Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/337)
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Publication number: 20140219960Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.Type: ApplicationFiled: April 23, 2012Publication date: August 7, 2014Applicant: Industry-Academic Cooperation Foundation, Yonsei UniversityInventor: Jong-Won Oh
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Publication number: 20140221431Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.Type: ApplicationFiled: June 26, 2012Publication date: August 7, 2014Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., LtdInventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
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Patent number: 8796271Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 11, 2011Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Patent number: 8796467Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: December 7, 2012Date of Patent: August 5, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
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Patent number: 8796275Abstract: The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.Type: GrantFiled: July 28, 2009Date of Patent: August 5, 2014Assignees: The Trustees of the University of Pennsylvania, Cellceutix CorporationInventors: Richard W. Scott, Doron Greenbaum, Dahui Liu, Xiaodong Fan, Yongjiang Xu, Haizhong Tang, Ehab Khalil
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Publication number: 20140213591Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: December 23, 2013Publication date: July 31, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
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Patent number: 8791263Abstract: A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(?O)OR3 or C(?O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.Type: GrantFiled: September 16, 2011Date of Patent: July 29, 2014Assignee: Osaka UniversityInventors: Motomasa Kobayashi, Naoyuki Kotoku, Masayoshi Arai, Satoru Tamura
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Patent number: 8785445Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: GrantFiled: December 18, 2009Date of Patent: July 22, 2014Assignee: Array BioPharma Inc.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
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Publication number: 20140194469Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: December 5, 2013Publication date: July 10, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
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Patent number: 8772320Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: GrantFiled: December 28, 2012Date of Patent: July 8, 2014Assignee: FUJIFILM CorporationInventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
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Publication number: 20140187557Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.Type: ApplicationFiled: March 10, 2014Publication date: July 3, 2014Applicant: Janssen Pharmaceutica NVInventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
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Publication number: 20140187504Abstract: The present embodiments relate to methods for the prevention and treatment of inflammatory conditions such as alcoholic liver disease (ALD). More specifically the present embodiments relate to the prevention and treatment of ALD through the administration of an Retinoic Acid Receptor (RAR) agonist. Some embodiments relate to use of tazarotene in the prevention and treatment of alcohol-induced liver injury, alcohol-related liver disease, fatty liver disease, hepatic steatosis, alcoholic hepatitis or alcoholic cirrhosis.Type: ApplicationFiled: June 22, 2012Publication date: July 3, 2014Applicant: GLYCOREREGIMMUNE, INC.Inventor: Vipin Kumar Chaturvedi
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Patent number: 8765791Abstract: The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1?-cyclohexane]-4?-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof.Type: GrantFiled: March 10, 2009Date of Patent: July 1, 2014Assignee: University Health NetworkInventor: Guohua Pan
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Publication number: 20140179735Abstract: A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.Type: ApplicationFiled: April 25, 2012Publication date: June 26, 2014Inventors: Zhong-Yin Zhang, Yantao He, Li-Fan Zeng
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Publication number: 20140163025Abstract: The present invention relates to compounds of general formula I, wherein the groups (Het)Ar and R1 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: December 2, 2013Publication date: June 12, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Sara FRATTINI, Elke LANGKOPF, Holger WAGNER
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Publication number: 20140155381Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.Type: ApplicationFiled: July 27, 2012Publication date: June 5, 2014Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
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Publication number: 20140155415Abstract: The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 4, 2012Publication date: June 5, 2014Inventors: Michael David Bartberger, Michael D. Croghan, Christopher H. Fotsch, Mark H. Norman, Lewis Dale Pennington, Andreas Reichelt, David J. St. Jean, JR., Christopher M. Tegley
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Publication number: 20140155407Abstract: The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.Type: ApplicationFiled: October 21, 2011Publication date: June 5, 2014Inventors: Rolf Hartmann, Ulrike Hille, Christina Zimmer, Carsten A. Vock, Qingzhong Hu
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Publication number: 20140148480Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2— amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.Type: ApplicationFiled: January 15, 2014Publication date: May 29, 2014Applicant: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6)Inventors: Michele REBOUD-RAVAUX, Chahrazade YERROUM-EL AMRI, Xiao TAN, Lixian QIN, Maurice PAGANO, Alain HOVNANIAN, Laetitia FURIO, Bernard PIROTTE
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Publication number: 20140148462Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: November 25, 2013Publication date: May 29, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Elke LANGKOPF, Holger WAGNER
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Publication number: 20140142142Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Patent number: 8729068Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: GrantFiled: October 26, 2012Date of Patent: May 20, 2014Assignee: Astellas Pharma Inc.Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
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Patent number: 8715710Abstract: A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.Type: GrantFiled: July 18, 2012Date of Patent: May 6, 2014Assignee: Heron Therapeutics, Inc.Inventors: Steven Y. Ng, Hui Rong Shen, Jorge Heller
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Publication number: 20140113897Abstract: The present invention embraces compounds that modulate the activity of Epstein-Barr Nuclear Antigen 1 (BBNA1) protein and use thereof in methods for treating latent Epstein-Barr virus infection. R7 is a substituted or unsubstituted phenyl, pyridyl, or pyrimidinyl group. A pharmaceutical composition comprising a compound of the invention in admixture with a pharmaceutically acceptable carrier is also provide as are methods for modulating the activity of Epstein-Barr Nuclear Antigen 1 (EBNA1) protein and treating a latent EpsteinBarr virus infection with a composition of the present invention.Type: ApplicationFiled: May 22, 2012Publication date: April 24, 2014Applicant: THE WISTAR INSTITUTEInventors: Paul M. Lieberman, Troy Messick
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Publication number: 20140107139Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.Type: ApplicationFiled: June 7, 2012Publication date: April 17, 2014Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe Alvaro, Anne Decor, Dieter Hamprecht, Agostino Marasco
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Publication number: 20140107106Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: April 25, 2013Publication date: April 17, 2014Applicant: Affinium Pharmaceuticals, Inc.Inventor: Affinium Pharmaceuticals, Inc.
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Publication number: 20140105920Abstract: Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives.Type: ApplicationFiled: May 23, 2013Publication date: April 17, 2014Inventor: David Sherris
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Publication number: 20140107149Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: Eli Lilly and CompanyInventors: Zengyun AN, Liang CHEN, Shuhui CHEN, Jean Marie DEFAUW, Scott Dale HOLMSTROM, Ping HU, Chongzhi TANG, William Hunter WHITE, Wentao WU, Yang ZHANG
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Patent number: 8691780Abstract: Methods and compositions for enhancing taxane sensitivity are provided. Aspects of the subject methods include administering to a subject a txr1 pathway modulatory agent in conjunction with a taxane. Also provided are txr1 polypeptides and nucleic acids encoding the same. The subject methods and compositions find use in a variety of different applications.Type: GrantFiled: February 16, 2006Date of Patent: April 8, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Chih Jian Lih, Stanley N. Cohen
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Publication number: 20140088148Abstract: Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.Type: ApplicationFiled: April 4, 2012Publication date: March 27, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Sivanesan Dakshanamurthy, Milton L. Brown, Robert Clarke, Ayesha N. Shahjahan, Jaqueline Smith
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Publication number: 20140088117Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and 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 25, 2013Publication date: March 27, 2014Applicant: Genentech, Inc.Inventors: Jason Burch, Minghua Sun, Xiaojing Wang, Wesley Blackaby, Alastair James Hodges, Andrew Sharpe
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Publication number: 20140080803Abstract: Disclosed herein are modulators of TRPV3 of Formula (I) wherein p is 1, 2, 3, or 4, and G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: October 23, 2012Publication date: March 20, 2014Applicant: AbbVie Inc.Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Eric A. Voight
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Publication number: 20140057950Abstract: The present invention relates to compounds of the general formula (I) which show a specific activity against cancer cell lines, the use of these compounds for prophylaxis and treatment of cancer as well as to pharmaceutical compositions containing at least one compound of general formula (I).Type: ApplicationFiled: December 22, 2011Publication date: February 27, 2014Applicant: MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DE WISSENSCHAFTEN E.V.Inventors: Mathias Christmann, Lea Radtke, Herbert Waldmann, Matthieu Willot, Slava Ziegler, Hongyan Sun
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Publication number: 20140057916Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20140057919Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: ApplicationFiled: October 31, 2013Publication date: February 27, 2014Applicant: Pfizer Inc.Inventors: Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
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Publication number: 20140057920Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Patent number: 8648097Abstract: The present invention provides a novel pyridylaminoacetic acid compound represented by the following formula (1): (wherein R1, R2, R3, Y and Z are as defined in the description and claims), or a pharmacologically acceptable salt thereof. The pyridylaminoacetic acid compound has EP2 agonistic action and is therefore useful as a therapeutic and/or prophylactic agent for respiratory diseases such as asthma or chronic obstructive pulmonary disease.Type: GrantFiled: March 12, 2009Date of Patent: February 11, 2014Assignee: Ube Industries, Ltd.Inventors: Ryo Iwamura, Masayuki Tanaka, Tetsushi Katsube, Manabu Shigetomi, Eiji Okanari, Yasunori Tokunaga, Hiroshi Fujiwara
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Publication number: 20140038970Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A??I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: HUBERT B. JOSIEN, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
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Patent number: 8642643Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: GrantFiled: December 18, 2008Date of Patent: February 4, 2014Assignee: SanofiInventors: Stephanie Hachtel, Juergen Dedio, Josef Pernerstorfer, Stephen Shimshock, Carolina Lanter, Raymond Kosley
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Patent number: 8642585Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: GrantFiled: March 14, 2013Date of Patent: February 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
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Publication number: 20140031348Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: July 9, 2013Publication date: January 30, 2014Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
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Publication number: 20140024671Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: July 9, 2013Publication date: January 23, 2014Inventors: Michael EISSENSTAT, Dehui DUAN
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Publication number: 20140024639Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.Type: ApplicationFiled: July 19, 2013Publication date: January 23, 2014Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
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Publication number: 20140005150Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, 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 a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: August 20, 2013Publication date: January 2, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Fabio Zuccotto, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Chiara Marchionni, Michele Modugno
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Publication number: 20130345240Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 16, 2013Publication date: December 26, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130338093Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 19, 2013Publication date: December 19, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.
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Publication number: 20130338106Abstract: Disclosed are compounds of Formula I: and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRa-, and Ra, and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.Type: ApplicationFiled: February 23, 2012Publication date: December 19, 2013Inventors: John A. McCauley, Thomas J. Greshock, John Sanders, Heather H. Stevenson, Jonathan T. Kern, Ronald K. Chang
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Publication number: 20130337082Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a Noggin blocker.Type: ApplicationFiled: February 23, 2012Publication date: December 19, 2013Applicant: EMORY UNIVERSITYInventors: Scott D. Boden, Sreedhara Sangadala
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Patent number: 8604061Abstract: The invention relates to compounds of formula I wherein X, Y, R1, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: GrantFiled: March 22, 2012Date of Patent: December 10, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20130324577Abstract: Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.Type: ApplicationFiled: January 26, 2012Publication date: December 5, 2013Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Tohru Kambe, Isamu Sugimoto