The Five-membered Nitrogen Hetero Ring Has Chalcogen As A Ring Member Patents (Class 514/253.1)
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Publication number: 20140179663Abstract: The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: Gilead Sciences, Inc.Inventor: Gregory Notte
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Publication number: 20140179698Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, A, Q, W and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.Type: ApplicationFiled: July 24, 2012Publication date: June 26, 2014Applicant: AB SCIENCEInventors: Abdellah Benjahad, Alain Moussy, Emmanuel Chevenier, Willy Picoul, Anne Lermet, Didier Pez, Jason Martin, Franck Sandrinelli
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Publication number: 20140147415Abstract: The present invention relates to the treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, in particular in an appropriate dosage regimen.Type: ApplicationFiled: November 3, 2011Publication date: May 29, 2014Applicant: AB SCIENCEInventors: Alain Moussy, Jean-Pierre Kinet
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Publication number: 20140148457Abstract: Compounds of the formula I in which R, R1, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: April 12, 2012Publication date: May 29, 2014Applicant: MERCK PATENT GMBHInventors: Srinivasa R. Karra, Wolfgang Staehle, Eike Staub, Margarita Wucherer-Plietker
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Publication number: 20140142112Abstract: A compound of formula: wherein Ar1, A, R3, X, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: ApplicationFiled: December 6, 2013Publication date: May 22, 2014Applicant: Purdue Pharma L.P.Inventors: Qun SUN, Laykea Tafesse, Sam Victory
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Patent number: 8729081Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: GrantFiled: October 12, 2009Date of Patent: May 20, 2014Assignee: VM Discovery Inc.Inventor: Jay Jie-Qiang Wu
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Publication number: 20140135305Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.Type: ApplicationFiled: December 12, 2013Publication date: May 15, 2014Applicant: PTC THERAPEUTICS, INC.Inventors: Sergey V. Paushkin, Charles Romfo, Ellen Welch, Nikolai Naryshkin
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Patent number: 8722663Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: GrantFiled: January 28, 2011Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Patent number: 8722681Abstract: This invention provides thiazolylpiperazine derivatives, and N-sulfonyl heterocyclic derivatives including phenyl- and benzyl-thiazolylpiperidine derivatives, and pharmaceutically acceptable salts thereof, which are useful active ingredients for administration in a method for the treatment of an ?-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides methods for making such derivatives, and pharmaceutical compositions including such derivatives together with pharmaceutically acceptable excipients.Type: GrantFiled: February 5, 2010Date of Patent: May 13, 2014Assignee: NV reMYNDInventors: Gerard Griffioen, Veronica Rojas De La Parra, Annick Lauwers
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Publication number: 20140128404Abstract: The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.Type: ApplicationFiled: June 29, 2012Publication date: May 8, 2014Applicant: REMYND NVInventors: Gerard Griffioen, Matthias Nettekoven, Katrien Princen, Hasane Ratni, Walter Vifian
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Publication number: 20140127157Abstract: Antiviral activity of Nilotinib against Hepatitis C virus.Type: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Inventors: Erica Canino, Adam Feire, Christopher Jones, Paul W. Manley
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Patent number: 8716312Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: November 17, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme CorporationInventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Publication number: 20140121213Abstract: In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.Type: ApplicationFiled: July 3, 2012Publication date: May 1, 2014Inventors: Jeffrey Charles Boehm, Roderick S. Davis, Jeffrey Kerns, Guoliang Lin, Robert D. Murdoch, Hong NIE
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Patent number: 8703961Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: November 9, 2010Date of Patent: April 22, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Hannes Koolman
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Publication number: 20140088108Abstract: Novel compounds selected from 2-(3-aminoaryl) amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: AB SCIENCEInventors: Marco CIUFOLINI, Camille WERMUTH, Bruno GIETHLEN, Alain MOUSSY
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Publication number: 20140080830Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: November 25, 2013Publication date: March 20, 2014Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Publication number: 20140073634Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 13, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
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Publication number: 20140073624Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: February 19, 2013Publication date: March 13, 2014Applicant: RIB-X PHARMACEUTICALS, INC.Inventor: Rib-X Pharmaceuticals, Inc.
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Publication number: 20140073622Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.Type: ApplicationFiled: September 13, 2013Publication date: March 13, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
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Publication number: 20140066424Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 6, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Christopher L. Carroll, Joe Marszalek, Barbara Czako, Ryan Johnson, Jay Theroff
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Publication number: 20140057882Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.Type: ApplicationFiled: October 8, 2013Publication date: February 27, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta ARMANI, GABRIELE AMARI, LAURA CARZANIGA, CARMELIDA CAPALDI, ORIANA ESPOSITO, GINO VILLETTI, RENATO DE FANTI
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Publication number: 20140057914Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: February 27, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu
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Publication number: 20140051662Abstract: The present invention relates to the treatment of multiple myeloma, especially for the treatment of those patients with refractory or first relapsed multiple myeloma, and in particular patients with t(4;14) multiple myeloma, comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, administered in association with an additional care in multiple myeloma; for example, autologous stem-cell transplantation, targeted therapies, anti-myeloma agents such as alkylating agents, corticosteroids, or immunomodulatory agents, including bortezomib, lenalidomide, and dexamethasone.Type: ApplicationFiled: April 4, 2012Publication date: February 20, 2014Applicant: AB SCIENCEInventors: Alain Moussy, Jean-Pierre Kinet
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Patent number: 8653082Abstract: Heterocyclic compounds of formula (I), (II), (III) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are each independently selected from hydrogen, halogen, C1-6alkyl, C2-6alkenyl, N—(C1-6alkyl)2, and N—(C2-6alkenyl)2, the C1-6alkyl and C2-6alkenyl being straight or branched; and Y1 and Y2 are selected from N and CH where one of Y1 and Y2 is N and the other is CH, are provided. Also provided are the synthesis of and pharmaceutical compositions including these compounds. These compounds and pharmaceutical compositions thereof can be used for the treatment of disorders, and in particular, cancer.Type: GrantFiled: February 25, 2010Date of Patent: February 18, 2014Assignee: Urifer Ltd.Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
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Publication number: 20140045800Abstract: Certain tetracyclic compounds are described, which may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: February 4, 2013Publication date: February 13, 2014Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20140038964Abstract: Methods of using compounds of the invention, such as compounds of Formulae IIa, IIb, IIc, or IId and pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in treating, preventing, inhibiting or ameliorating the symptoms of a disease or disorder that is modulated or otherwise affected by nuclear receptor activity, or in which nuclear receptor activity is implicated.Type: ApplicationFiled: July 25, 2013Publication date: February 6, 2014Applicant: Exelixis Patent Company LLCInventors: Brett B. Busch, Brenton T. Flatt, Xiao-Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin J. Schweiger, William C. Stevens, JR., Tie-Lin Wang, Yinong Xie
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Publication number: 20140038982Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.Type: ApplicationFiled: May 31, 2013Publication date: February 6, 2014Applicant: GlaxoSmithKline LLCInventor: Connie L. ERICKSON-MILLER
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Publication number: 20140031334Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
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Publication number: 20140024649Abstract: Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.Type: ApplicationFiled: October 10, 2011Publication date: January 23, 2014Applicants: Auckland UniServices Limited, The Board of Trustees of the Leland Stanford Junior UniversityInventors: Amato Giaccia, Edwin Lai, Olga Razorenova, Denise Chan, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Ray Tabibiazar, Po-wai Yuen
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Publication number: 20140005103Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.Type: ApplicationFiled: June 25, 2013Publication date: January 2, 2014Inventors: Craig A. Coburn, Milana Maletic, Richard Soll, Chunsing Li, Yunfu Luo, Zhiqi Qi
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Patent number: 8618110Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: GrantFiled: February 9, 2010Date of Patent: December 31, 2013Assignee: VM Discovery Inc.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20130345200Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: August 7, 2013Publication date: December 26, 2013Applicant: GlaxoSmithKline LLCInventors: James Brackley, III, Joelle Lorraine Burgess, Seth Grant, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20130338111Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Applicants: Icagen, Inc., Pfizer LimitedInventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20130324551Abstract: Thiazolylphenyl-benzenesulfonamido 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: February 21, 2012Publication date: December 5, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Gabriella Traquandi, Chiara Marchionni, Alessandra Scolaro, Nicoletta Colombo
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Publication number: 20130316999Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: August 7, 2013Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
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Publication number: 20130317020Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 2, 2013Publication date: November 28, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20130310357Abstract: Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: May 26, 2011Publication date: November 21, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventor: Gang Liu
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Publication number: 20130296335Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: March 29, 2013Publication date: November 7, 2013Inventors: Bradley P. MORGAN, Erica A. KRAYNACK, Pu-Ping LU, Alex MUCI, David J. MORGANS
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Publication number: 20130289045Abstract: The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.Type: ApplicationFiled: May 10, 2013Publication date: October 31, 2013Applicant: AB SCIENCEInventor: AB Science
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Publication number: 20130289047Abstract: Heteroarylthio compounds covalently linked to an arylpiperazine moiety for the treatment of neurological conditions.Type: ApplicationFiled: October 14, 2011Publication date: October 31, 2013Applicant: EPIOMED THERAPEUTICS, INC.Inventors: David Helton, David Fick
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Patent number: 8569282Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: GrantFiled: December 11, 2008Date of Patent: October 29, 2013Assignee: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130281434Abstract: Compounds of formula I?: or salts thereof are provided. Pharmaceutical compositions comprising a compound of formula I?, processes for preparing compounds of formula I?, intermediates useful for preparing compounds of formula I? and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Applicant: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130267506Abstract: Compositions for therapy of a diabetic symmetrical polyneuropathy a subject in need thereof, the compositions comprising: an effective amount of a muscarinic acetylcholine receptor antagonist exemplified by pirenzepine, telenzepine, atropine, or derivatives thereof or salts thereof or analogs thereof or derivatives thereof, and a pharmacologically acceptable carrier. The composition may be injectable or alternatively, may be applied topically or alternatively, may be delivered orally. A suitable topical composition may comprise a lotion, a cream, a gel, or a viscous fluid. The muscarinic acetylcholine receptor antagonist may be a muscarinic acetylcholine receptor antagonist salt or a muscarinic acetylcholine receptor antagonist derivative or a muscarinic acetylcholine receptor antagonist analog.Type: ApplicationFiled: October 24, 2011Publication date: October 10, 2013Applicant: UNIVERSITY OF MANITOBAInventors: Paul Fernyhough, Nigel A. Calcutt, Lakshmi Kotra
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Publication number: 20130267484Abstract: The present invention relates to a tyrosine kinase inhibitor or a mast cell inhibitor, and in particular masitinib or a pharmaceutically acceptable salt thereof, for the treatment of human rheumatoid arthritis.Type: ApplicationFiled: June 1, 2011Publication date: October 10, 2013Applicant: AB SCIENCEInventors: Alain Moussy, Jean-Pierre Kinet
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Patent number: 8551999Abstract: The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5—Z1—, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group —CO—, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.Type: GrantFiled: October 29, 2008Date of Patent: October 8, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takumi Sumida, Fujio Tabusa, Kazuo Sekiguchi, Takeshi Kodama, Koichi Yasumura, Yutaka Kojima, Masaaki Motoyama, Keisuke Miyajima, Kenji Yoshida, Keizo Kan, Makoto Sakamoto, Hideki Takasu, Takashi Nakagawa, Naoto Ohi, Yasuo Harada, Norikazu Hashimoto, Hironori Matsuyama, Masatoshi Iida, Shigekazu Fujita, Tae Fukushima
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Patent number: 8536177Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: GrantFiled: August 8, 2011Date of Patent: September 17, 2013Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Publication number: 20130217680Abstract: This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 24, 2011Publication date: August 22, 2013Inventors: Alexander Pasternak, Reynalda K. deJesus, Yuping Zhu, Lihu Yang, Shawn Walsh, Haifeng Tang, Dooseop Kim, Barbara Pio, Aurash Shahripour, Kevin Belyk
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Publication number: 20130202555Abstract: The present invention relates to a tyrosine kinase inhibitor or a mast cell inhibitor, and in particular masitinib or a pharmaceutically acceptable salt thereof, for the treatment of human multiple sclerosis.Type: ApplicationFiled: April 20, 2011Publication date: August 8, 2013Applicant: AB SCIENCEInventors: Alain Moussy, Jean-Pierre Kinet
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Publication number: 20130203729Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: August 9, 2012Publication date: August 8, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Todd BOSANAC, Angela BERRY, John David GINN, Tamara Denise HOPKINS, Sabine SCHLYER, Fariba SOLEYMANZADEH, John WESTBROOK, Maolin YU, Zhonghua ZHANG