The 1,3-diazole Ring Is Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/274.1)
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Publication number: 20140081025Abstract: The compound represented by formula (IA) or a pharmaceutically acceptable salt thereof is based on orexin (OX) receptor antagonist activity, is useful in the treatment and prevention of illnesses including sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependency, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, pain, gastrointestinal disease, epilepsy, inflammation, immunological disease, endocrinological related disease, and hypertension.Type: ApplicationFiled: May 8, 2012Publication date: March 20, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Ryo Suzuki, Aya Futamura, Masahito Abe, Shuhei Kashiwa, Nobutaka Hattori, Dai Nozawa, Hiroshi Ohta, Yuko Araki
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Publication number: 20140066425Abstract: Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.Type: ApplicationFiled: March 8, 2012Publication date: March 6, 2014Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.Inventor: Youzhi Tong
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Publication number: 20140057910Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: February 22, 2012Publication date: February 27, 2014Applicant: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Publication number: 20140045790Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: October 15, 2013Publication date: February 13, 2014Applicant: Pfizer Inc.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
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Publication number: 20140045901Abstract: Disclosed are imidazole derivatives as represented by formula (I), and preparation method and use thereof. The compounds can inhibit cyclooxygenase and treat diseases mediated by cyclooxygenase.Type: ApplicationFiled: October 14, 2011Publication date: February 13, 2014Applicant: BEIJING ORBIEPHARM CO., LTDInventor: Jin LI
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Publication number: 20140024583Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: July 15, 2013Publication date: January 23, 2014Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Patent number: 8623857Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.Type: GrantFiled: May 24, 2011Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
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Publication number: 20130338105Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: August 20, 2013Publication date: December 19, 2013Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
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Publication number: 20130289020Abstract: Disclosed are compounds that are antagonists of the CXCR4 receptor.Type: ApplicationFiled: October 13, 2011Publication date: October 31, 2013Applicant: Proximagen LimitedInventors: Edward Daniel Savory, Allson Stewart, Allison Cartey, Giles Brown, Iain Simpson, Kathryn Oliver, Lee Patient, Michael Higginbottom, Andrew Graham Cole
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Publication number: 20130289072Abstract: The present invention relates to provision of a novel indazole compound which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells. The present invention also relates to provision of a drug useful for preventing and/or treating, on the basis of an HSP90 inhibitory effect, a disease in which HSP90 participates, in particular, cancer. A compound represented by the general formula (I) or a salt thereof: wherein X represents CH or N; any one or two of Y1, Y2, Y3, and Y4 represent C—R3 or N, and the others represent CH; A and B are the same or different and represent an optionally substituted monocyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R1 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R2 represents a hydrogen atom, a halogen atom etc.; R3 represents a hydrogen atom, a halogen atom etc.; R4 and R5 are the same or different and represent a hydroxyl group etc.Type: ApplicationFiled: January 6, 2012Publication date: October 31, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto Kitade, Shuichi Ohkubo, Chihoko Yoshimura
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Patent number: 8563734Abstract: 2-[(1-cyanopropyl)carbamoyl]-5-chloromethyl nicotinic acids of formula (I) where Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; R1 is C1-C4 alkyl; R2 is C1-C4 alkyl, C3-C6 cycloalkyl or R1 and R2, when taken together with the atom to which they are attached, represent a C3-C6 cycloalkyl group optionally substituted with methyl, and R3 is hydrogen or a cation preferably selected from the group consisting of alkali metals, alkaline earth metals, manganese, copper, iron, zinc, cobalt, lead, silver, nickel, ammonium and organic ammonium; are useful intermediates for the synthesis of herbicidal imidazolinones.Type: GrantFiled: November 3, 2009Date of Patent: October 22, 2013Assignee: BASF SEInventors: Frederik Menges, Joachim Gebhardt, Michael Rack, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schröder
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Publication number: 20130267510Abstract: 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: December 6, 2011Publication date: October 10, 2013Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
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Publication number: 20130266895Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more hydantoin derivatives represented by the following formula (1): wherein R1 and R2, which may be identical to or different from each other, represent a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4, to R8, which may be identical to or different from each other, represent a hydrogen atom, a chlorine atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc.; R3, to R8 may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of V, W, X, Y and Z are nitrogen atoms which have no substituent of R4 to R8.Type: ApplicationFiled: January 17, 2012Publication date: October 10, 2013Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Ikuo Kimura, Motonori Tsuji, Masaya Tojo, Masafumi Asakai
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Publication number: 20130261128Abstract: This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Osamu Sakurai, Kunio Saruta, Norimitsu Hayashi, Takashi Goi, Kenji Morokuma, Hidekazu Tsujishima, Hiroaki Sawamoto, Hiroaki Shitama, Ritsuo Imashiro
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Publication number: 20130253012Abstract: The present invention relates to a method for controlling invertebrate pests, in particular arthropod pests and nematodes, by using pyrazole compounds of formula I and the salts thereof, the tautomers thereof, the N-oxides thereof and the salts of the tautomers or N-oxides thereof, wherein X is N or CH, Y is N or CH, Z is N or CH, provided that either only one of X, Y and Z is N or only two adjacent groups of X, Y and Z are N; and wherein Q is a bivalent 5- or 6-membered carbocyclic radical or a 5- or 6-membered heterocyclic radical having one heteroatom moiety which is selected from the group consisting of O, S, N or N—RQN as ring member and 0, 1 or 2 further heteroatom moieties N as ring members, wherein 0, 1, 2 or 3 of the ring members that are carbon atoms may carry a radical RQ, provided that the pyrazole radical and the 6-membered heteroaromatic radical are bound in ortho- or meta-position of Q with respect to each other, if Q is a 6-membered radical; and wherein RA, if present, is C1-C3-alkyl, C1-CType: ApplicationFiled: December 9, 2011Publication date: September 26, 2013Applicant: BASF SEInventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Daniel Saelinger, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh, Koshi Gunjima
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Publication number: 20130245063Abstract: 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: April 26, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Jonathan Grey, Jianguo Cao, Zhijun Wang, Evan Rogers
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Publication number: 20130244262Abstract: The present invention provides a cardiomyocyte- and/or cardiac progenitor cell-proliferating agent comprising at least one compound selected from the group consisting of: a GSK3? inhibitor, ERK dephosphorylation inhibitor, Raf activator, CaMK2 inhibitor and p38 inhibitor; and a method for proliferating cardiomyocytes and/or cardiac progenitor cells using the agent.Type: ApplicationFiled: November 17, 2011Publication date: September 19, 2013Applicant: KYOTO UNIVERSITYInventors: Jun Yamashita, Hideki Uosaki
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Publication number: 20130225638Abstract: Disclosed are imidazole derivatives as represented by formula (I), and preparation method and use thereof. The compounds can inhibit cyclooxygenase and treat diseases mediated by cyclooxygenase.Type: ApplicationFiled: October 14, 2011Publication date: August 29, 2013Applicant: BEIJING ORBIEPHARM CO., LTDInventor: Jin LI
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Publication number: 20130210818Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: February 14, 2012Publication date: August 15, 2013Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
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Publication number: 20130203656Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: May 23, 2011Publication date: August 8, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Min Zhong, Leping Li
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Publication number: 20130196952Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: ApplicationFiled: May 4, 2011Publication date: August 1, 2013Applicant: PFIZER INC.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Publication number: 20130190363Abstract: An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient.Type: ApplicationFiled: July 15, 2011Publication date: July 25, 2013Applicants: WAKUNAGA PHARMACEUTICAL CO., LTD., NEUGEN PHARMA INC.Inventors: Joh-E Ikeda, Noriaki Hirayama, Satoshi Inoue, Kazunori Tanaka, Takuya Kanno
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Publication number: 20130190179Abstract: The present invention relates generally to the use of biological or chemical control agents with for controlling insects and nematodes and to methods particularly useful for combating insects or nematodes and/or increasing crop yield in plants that are at least partially resistant to one or more parasitic nematodes or insects.Type: ApplicationFiled: October 13, 2011Publication date: July 25, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ruediger Hain, Gerhard Johann, Guenter Donn
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Patent number: 8486951Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: GrantFiled: August 21, 2012Date of Patent: July 16, 2013Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20130178456Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: ApplicationFiled: February 28, 2013Publication date: July 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130177632Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.Type: ApplicationFiled: February 27, 2013Publication date: July 11, 2013Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
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Publication number: 20130178480Abstract: The present invention provides compounds of the formula, wherein A, B, G, R2, R6, and X are defined herein, pharmaceutical compositions of the same, and methods for treating or inhibiting development of AGE- and/or ALE-associated complications in subjects in need thereof.Type: ApplicationFiled: February 14, 2013Publication date: July 11, 2013Applicant: NephroGenex, Inc.Inventor: NephroGenex, Inc.
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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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Patent number: 8470856Abstract: Anthranilamide compounds, a process for their production, and pesticides containing these compounds as active ingredients. This Abstract is not intended to define the invention disclosed in the specification, nor intended to limit the scope of the invention in any way.Type: GrantFiled: June 29, 2011Date of Patent: June 25, 2013Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Toru Koyanagi, Masayuki Morita, Kenichi Nakamoto, Akihiro Hisamatsu
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Publication number: 20130143929Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R3 and R4 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: September 28, 2011Publication date: June 6, 2013Applicant: EI DU PONT DE NEMOURS AND COMPANYInventors: Jeffrey Keith Long, James Francis Bereznak, Moumita Kar, Andrew Edmund Taggi, Yuzhong Chen
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Patent number: 8445507Abstract: A hydantoin compound useful for the prevention or treatment of hyperproliferative diseases or disorders.Type: GrantFiled: March 27, 2007Date of Patent: May 21, 2013Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Charles L. Sawyers, Samedy Ouk, Chris Tran, John Wongvipat
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Publication number: 20130102592Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: December 5, 2012Publication date: April 25, 2013Applicant: SAREUM LIMITEDInventor: Sareum Limited
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Patent number: 8420661Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: GrantFiled: April 5, 2011Date of Patent: April 16, 2013Assignee: Hoffmann-la Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 8420685Abstract: A compound of the formula: Wherein A1, A2, X, R2 and R3 are as defined herein, or a composition containing the same, which compound is useful in treating renal-, liver- or pulmonary fibrosis.Type: GrantFiled: June 12, 2008Date of Patent: April 16, 2013Assignees: SK Chemicals Co., Ltd., Ewha University Industry Collaboration FoundationInventors: Dae-Kee Kim, Yung-Jue Bang, Hun-Taek Kim, Ii-Sang Cho, Myoung-Soon Park, Young Jae An, Joon Hun Choi
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Publication number: 20130090332Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: ApplicationFiled: September 27, 2012Publication date: April 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8410146Abstract: 2-pyridyl substituted imidazoles of the formula (I) as shown in claim 1, are provided, which are useful in the treatment of diseases mediated by ALK5 or ALK4 inhibitors or both.Type: GrantFiled: June 11, 2009Date of Patent: April 2, 2013Assignee: SK Chemicals Co., Ltd.Inventors: Ju Young Lee, Jae-Sun Kim, Jung-Hoon Oh, Hoe-chul Jung, Hyun Jung Lee, Sang-hwan Kang, Yong-Hyuk Kim, Sung-hoon Park, Keun-Ho Ryu, Jung Bum Yi, Hun-Taek Kim, Key-An Um, Bong-yong Lee
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Publication number: 20130079362Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: ApplicationFiled: August 21, 2012Publication date: March 28, 2013Applicant: DECIPHERA PHARMACEUTICALS, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20130066081Abstract: The present invention provides Chalcone linked Imidazolone compounds of formula A as anti cancer agent against fifty three human cancer cell lines.Type: ApplicationFiled: December 14, 2010Publication date: March 14, 2013Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Kamal Ahmed, Ramakrishna Gadupudi, Balakishan Gorre, Raju Paidakula, Viswanath Arutla, Balakrishna Moku
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Publication number: 20130012532Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.Type: ApplicationFiled: March 14, 2011Publication date: January 10, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
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Publication number: 20130005744Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: January 3, 2013Inventors: Scott Wolkenberg, James C. Barrow, Scott T. Harrison, B. Wesley Trotter, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao
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Publication number: 20120322803Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: December 19, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Steffen STEURER
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Patent number: 8334287Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.Type: GrantFiled: July 9, 2010Date of Patent: December 18, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Eric Vieira, Juergen Wichmann
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Publication number: 20120302608Abstract: The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.Type: ApplicationFiled: May 10, 2012Publication date: November 29, 2012Applicant: ELI LILLY AND COMPANYInventors: Norman Earle Hughes, Bryan Hurst Norman, Timothy Andrew Woods
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Publication number: 20120289551Abstract: Mineralocorticoid receptor antagonists, of which the following is exemplary.Type: ApplicationFiled: November 7, 2011Publication date: November 15, 2012Inventors: Xin GUO, Stephen J. BOYER, Di WU, Frank WU
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Patent number: 8293916Abstract: The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.Type: GrantFiled: November 5, 2009Date of Patent: October 23, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Paul Spurr, Eric Vieira
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Publication number: 20120251551Abstract: The invention relates to substituted (heteroarylmethyl) thiohydantoin compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, and their use for the preparation of medicaments for the treatment and/or prophylaxis of disorders, in particular of prostate cancer.Type: ApplicationFiled: August 28, 2010Publication date: October 4, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Lücking, Arwed Cleve, Bernard Haendler, Hortensia Faus Gimenez, Silke Köhr, Horst Irlbacher
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Publication number: 20120252758Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: March 29, 2012Publication date: October 4, 2012Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William Am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
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Publication number: 20120238566Abstract: Use of cell autophagy (type II cell apoptosis) inhibitors for preventing and/or treating avian influenza, injury of lungs caused by avian influenza virus or nanometer materials. The cell autophagy (type II cell apoptosis) inhibitors are selected from 3-methyladenine, SB203580, LY294002, and or wortmannin. The injury of lungs includes acute respiratory distress syndrome. The avian influenza virus is H5N1, H5N2 or H9N2 avian influenza virus. The nanometer materials include PAMAM G3, G4, G5, G5.5, G6, G7, or G8.Type: ApplicationFiled: April 27, 2010Publication date: September 20, 2012Inventors: Chengyu Jiang, Shuan Rao, Haolin Liu, Feng Guo, Hongliang Wang, Yang Sun, Chenggang Li
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Publication number: 20120220587Abstract: Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 6, 2010Publication date: August 30, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Ulrich Emde, Hans Peter Buchstaller, Markus Klein, Christina Esdar, Joerg Bomke
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Publication number: 20120220463Abstract: The present invention relates to crystalline complexes of 4-hydroxy benzoic acid and selected pesticides. It also relates to agriculturally useful compositions of the complexes.Type: ApplicationFiled: October 28, 2010Publication date: August 30, 2012Applicant: BASF SEInventors: Heidi Emilia Saxell, Rafel Israels, Ansgar Schaefer, Matthias Bratz, Hans Wolfgang Hoeffken, Ingo Brode, Elisa Nauha, Maija Nissinen