Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Five- Membered Ring By Nonionic Bonding Patents (Class 546/279.1)
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Publication number: 20140031341Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.Type: ApplicationFiled: December 19, 2011Publication date: January 30, 2014Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENTInventors: Jerome Aubert, Martin Steinhoff
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Publication number: 20140024665Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: June 5, 2013Publication date: January 23, 2014Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
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Publication number: 20130345211Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A1, X, A2, R1a, R1b, R1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: July 15, 2011Publication date: December 26, 2013Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Chiyou Ni, Minnie Park, Laykea Tafesse
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Publication number: 20130324501Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols according to formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: June 4, 2013Publication date: December 5, 2013Inventors: Elisabetta ARMANI, Carmelida Capaldi, Laura Carzaniga, Oriana Esposito
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Publication number: 20130303773Abstract: This invention relates to the discovery of novel rosuvastatin and atorvastatin analogues.Type: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventors: Derek Lindsay, Peter Jackson, Stephen Hindley, Inder Bhamra
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Publication number: 20130296245Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.Type: ApplicationFiled: November 14, 2011Publication date: November 7, 2013Inventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
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Publication number: 20130289075Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.Type: ApplicationFiled: June 25, 2013Publication date: October 31, 2013Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Publication number: 20130266590Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I), (II), (III) or (IV) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.Type: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: NOVARTIS AGInventors: Christopher Sean Straub, Zhuoliang Chen
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Publication number: 20130267539Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 5, 2013Publication date: October 10, 2013Applicant: THERAVANCE, INC.Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8552003Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: GrantFiled: July 31, 2007Date of Patent: October 8, 2013Assignee: Novartis AGInventors: Mark G. Charest, Christine Hiu-Tung Chen, Zhuoliang Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
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Patent number: 8546336Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: GrantFiled: September 7, 2012Date of Patent: October 1, 2013Assignee: Novartis AGInventors: Zhuoliang Chen, Mark G. Charest, Christine Hiu-Tung Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
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Publication number: 20130217686Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.Type: ApplicationFiled: September 28, 2011Publication date: August 22, 2013Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
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Publication number: 20130211075Abstract: The present invention relates to a novel amide derivative. More specifically, the present invention provides a medicinal agent useful as a prophylactic or therapeutic agent for diseases, which relies on the production of cytokines from T cells, and which comprises an amide derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or the pharmacologically acceptable salt as an active ingredient. Provided is an amide derivative represented by general formula (I) [wherein each symbol is as defined in the description] or a pharmacologically acceptable salt thereof, or a solvate of the derivative or the pharmacologically acceptable salt.Type: ApplicationFiled: October 13, 2011Publication date: August 15, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Hiroyuki Ushio, Maiko Hamada, Masayuki Watanabe, Atsushi Numata, Naoto Fujie, Tooru Takashima, Hiroyuki Furukawa, Junki Ando
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Patent number: 8507535Abstract: The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: June 29, 2011Date of Patent: August 13, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Hasane Ratni, Walter Vifian
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Patent number: 8492111Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 7, 2010Date of Patent: July 23, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
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Publication number: 20130165483Abstract: This invention provides compounds of formula IB: wherein HY, R1, R2, R3, R15, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: Millennium Pharmaceuticals, Inc.
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Publication number: 20130165464Abstract: This invention provides compounds of formula IB: and also provides compounds of formulas ID, IIB, VB, and IIC: wherein HY, R1, R2, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: MILLENNIUM PHARMACEUTICALS, INC.
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Patent number: 8470855Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residuType: GrantFiled: November 10, 2006Date of Patent: June 25, 2013Assignee: IMTM GmbHInventors: Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jürgen Faust, Michael Täger, Petra Fuchs, Bianca Senns
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Publication number: 20130157995Abstract: Embodiments of the present disclosure provide for compounds such as those shown in FIG. 1.1 (compounds A, B, C, and D), 2?substituted nicotine compounds, azetidine compounds, ether linked nicotine compounds (FIG. 1.2, compounds E, F, G, and H), methods of synthesis of the compounds, methods of treatment of a condition using compounds A, B, C, D, 2?substituted nicotine compounds, azetidine compounds, or ether linked nicotine compounds, methods of selectively stimulating alpha7 nAChR and/or alpha4beta2 receptors, and the like.Type: ApplicationFiled: September 2, 2011Publication date: June 20, 2013Inventors: William Reade Kem, Ferenc Soti, Anne Rouchaud, Hong Xing, Jon Lindstrom, Kristin Marie Andrud
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Patent number: 8445440Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.Type: GrantFiled: February 23, 2011Date of Patent: May 21, 2013Assignee: Novartis AGInventors: Christopher Straub, Zhuoliang Chen, Mark Palermo
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Publication number: 20130116230Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: December 20, 2012Publication date: May 9, 2013Applicant: INCYTE CORPORATIONInventor: Incyte Corporation
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Publication number: 20130116430Abstract: 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: ApplicationFiled: December 28, 2012Publication date: May 9, 2013Applicant: 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: 20130109721Abstract: The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders.Type: ApplicationFiled: December 8, 2010Publication date: May 2, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Kevin Sprott, John Jeffrey Talley, Jane Yang, Bo Peng
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Patent number: 8431599Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.Type: GrantFiled: September 12, 2012Date of Patent: April 30, 2013Assignees: Allergan, Inc., ExonHit Therapeutics SAInventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Patent number: 8410279Abstract: The invention relates to substituted pyrrole compounds of Formula (I) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: June 10, 2009Date of Patent: April 2, 2013Assignee: Genentech, Inc.Inventors: Lewis J. Gazzard, Joseph Lyssikatos
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Publication number: 20130079313Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: September 26, 2012Publication date: March 28, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8404679Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.Type: GrantFiled: April 23, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Andreas Koblet, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Publication number: 20130065923Abstract: The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, R4, Q1, Q2, Q3, Q4, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.Type: ApplicationFiled: November 6, 2012Publication date: March 14, 2013Applicant: SANOFIInventor: Sanofi
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Publication number: 20130065880Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.Type: ApplicationFiled: November 9, 2012Publication date: March 14, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Patent number: 8394834Abstract: The present invention relates to a compounds of formula I wherein R1, R2, Ar1, Ar2, R?, R?, m, n, and o are defined in the specification or to a pharmaceutically active salt, racemic mixture, enantiomer, optical isomer or to tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: August 16, 2010Date of Patent: March 12, 2013Assignee: Hoffman-La Roche Inc.Inventors: Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angelique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20130059873Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: April 3, 2012Publication date: March 7, 2013Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
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Publication number: 20130048007Abstract: The present invention relates to a cationic aminopyridine of general formula (I), acid-addition salts thereof and solvates thereof: in which: R1 is a linear or branched, saturated C1-C20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic aminopyridine, compositions, uses, hair dyeing processes and devices using this cationic aminopyridine.Type: ApplicationFiled: December 3, 2010Publication date: February 28, 2013Inventor: Aziz Fadli
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Patent number: 8378109Abstract: Contemplated compositions and methods are employed to bind in vitro and in vivo to an ?4?2 nicotinic acetylcholine receptor in a highly selective manner. Where such compounds are labeled, compositions and methods employing such compounds can be used for PET and SPECT analysis. Alternatively, and/or additionally contemplated compounds can be used as antagonists, partial agonists or agonists in the treatment of diseases or conditions associated with ?4??2 dysfunction.Type: GrantFiled: December 1, 2005Date of Patent: February 19, 2013Assignee: The Regents of the University of CaliforniaInventors: Jogeshwar Mukherjee, Ramaiah Pichika, Steven Potkin, Frances Leslie, Sankha Chattopadhyay
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Patent number: 8367679Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.Type: GrantFiled: December 8, 2009Date of Patent: February 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
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Publication number: 20130028843Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: ApplicationFiled: October 10, 2012Publication date: January 31, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8362262Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosed.Type: GrantFiled: October 7, 2011Date of Patent: January 29, 2013Assignee: Neuralstem, Inc.Inventors: Judith Kelleher-Andersson, Karl K. Johe
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Patent number: 8362003Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: June 16, 2011Date of Patent: January 29, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Patent number: 8362020Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: December 21, 2010Date of Patent: January 29, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Publication number: 20130023539Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.Type: ApplicationFiled: June 18, 2012Publication date: January 24, 2013Applicant: Euroscreen S.A.Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
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Publication number: 20130005663Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Applicant: NOVARTIS AGInventors: Mark G. CHAREST, Christine Hiu-Tung CHEN, Zhuoliang CHEN, Miao DAI, Feng HE, Huangshu LEI, Ly Luu PHAM, Sushil Kumar SHARMA, Christopher Sean STRAUB, Run-Ming David WANG, Fan YANG, Leigh ZAWEL
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Patent number: 8343952Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: August 20, 2010Date of Patent: January 1, 2013Assignee: Akebia Therapeutics Inc.Inventors: Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Richard Masaru Kawamoto
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Patent number: 8344005Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.Type: GrantFiled: May 12, 2009Date of Patent: January 1, 2013Assignee: Glaxo Wellcome Manufacturing Pte LtdInventors: Giuseppe Alvaro, Agostino Marasco
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Publication number: 20120322831Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer's Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.Type: ApplicationFiled: January 22, 2011Publication date: December 20, 2012Applicant: KAREUS THERAPEUTICS SAInventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
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Patent number: 8318777Abstract: The invention discloses a compound of general formula (I) and a process for preparing this compound. The invention discloses a fungicidal composition comprising a compound of general formula (I) and a method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: November 23, 2011Date of Patent: November 27, 2012Assignee: Bayer SASInventors: Pierre-Yves Coqueron, Philippe Desbordes, Darren James Mansfield, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Alain Villier, Pierre Genix
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Patent number: 8318750Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: GrantFiled: August 26, 2011Date of Patent: November 27, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120295906Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 27, 2012Publication date: November 22, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
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Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20120289403Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: ApplicationFiled: November 11, 2010Publication date: November 15, 2012Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
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Patent number: 8309596Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: GrantFiled: June 26, 2008Date of Patent: November 13, 2012Assignee: Novartis AGInventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Patent number: 8299076Abstract: Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: May 17, 2006Date of Patent: October 30, 2012Assignees: Array Biopharma Inc., Astrazeneca ABInventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, Jim Blake, Richard Anthony Storey, Rebecca Jane Booth, John David Pittam, John Leonard, Mark Richard Fielding