At Least Three Hetero Rings Containing Patents (Class 544/364)
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Publication number: 20130102608Abstract: The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: ApplicationFiled: June 7, 2011Publication date: April 25, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Guenter Hoelzemann, Dieter Dorsch, Alfred Jonczyk, Christiane Amendt, Frank Zenke
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Publication number: 20130102607Abstract: Medicinal use The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of respiratory syncitial virus (RSV) infection in particular viral exacerbation of a respiratory disorder such as bronchitis, asthma, COPD and/or cystic fibrosis, methods of treating or preventing RSV infection employing said compounds or pharmaceutical composition comprising the same.Type: ApplicationFiled: June 17, 2011Publication date: April 25, 2013Applicant: Respivert LimitedInventors: Lindsey Cass, Kazuhiro Ito, William Garth Rapeport, Peter Strong
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Patent number: 8426422Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: January 18, 2010Date of Patent: April 23, 2013Assignee: Abbvie Inc.Inventors: Laura A. Hexamer, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Michael D. Wendt
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Patent number: 8426420Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 17, 2010Date of Patent: April 23, 2013Assignee: SanofiInventors: Marc Nazaré, Gernot Zech, Melitta Just, Tilo Weiss, Gerhard Hessler, Markus Kohlmann
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Patent number: 8426401Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: April 23, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130096117Abstract: 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: October 2, 2012Publication date: April 18, 2013Inventors: Julie Nicole HAMBLIN, Paul Spencer JONES, Suzanne Elaine KEELING, Joelle LE, Nigel James PARR
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Patent number: 8420643Abstract: The present invention is directed to methods of use of a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, or combination thereof, a composition comprising the thiosemicarbazone, a method of administration thereof, and use thereof to treat a cancer.Type: GrantFiled: December 2, 2011Date of Patent: April 16, 2013Assignee: Critical Outcome Technologies Inc.Inventors: Wayne R. Danter, Martyn Brown, Franck LePifre
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Publication number: 20130090309Abstract: The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: April 30, 2012Publication date: April 11, 2013Inventors: Eric Thomas Romeo, Michelle R. Machacek, Benjamin Wesley Trotter, Thomas Allen Miller, Brian Michael Andresen, Neville John Anthony, Brandon M. Taoka, Yuan Liu
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Patent number: 8415341Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica, NVInventors: Kristen Chevalier, Jose Clemente, Scott Dax, Chris Flores, Li Liu, Mark Macielag, Mark McDonnell, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang, Bin Zhu
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Publication number: 20130085126Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.Type: ApplicationFiled: September 25, 2012Publication date: April 4, 2013Applicant: National Health Research InstitutesInventors: Kak-Shan Shia, Chun-Ping Chang, Yu-Sheng Chao
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Patent number: 8410088Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: April 13, 2012Date of Patent: April 2, 2013Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Masashi Seki, Syuji Shirotori
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Patent number: 8410090Abstract: The invention relates to heterocyclylamide-substituted thiazoles, pyrroles and thiophenes and processes for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: July 1, 2006Date of Patent: April 2, 2013Assignee: AiCuris GmbH & Co. KGInventors: Holger Zimmermann, David Brueckner, Kerstin Henninger, Martin Hendrix, Martin Radtke
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Publication number: 20130079354Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein W, V, x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Applicant: Xenon Pharmaceuticals Inc.Inventors: Melwyn ABREO, Daniel F. HARVEY, Mikhail A. KONDRATENKO, Wenbao LI, Rajender KAMBOJ, Vishnumurthy KODUMURU, Michael D. WINTHER, Heinz W. GSCHWEND, Nagasree CHAKKA, Shifeng LIU, Serguei SVIRIDOV, Shaoyi SUN
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Publication number: 20130079343Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: ApplicationFiled: November 24, 2012Publication date: March 28, 2013Applicant: Korea Institute of Science and TechnologyInventor: Korea Institute of Science and Technology
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Publication number: 20130079325Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 14, 2012Publication date: March 28, 2013Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20130079329Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: September 13, 2012Publication date: March 28, 2013Inventors: John Hood, Sunil Kumar Kc
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Publication number: 20130079320Abstract: The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: September 25, 2012Publication date: March 28, 2013Applicant: Gruenenthal GmbHInventor: Gruenenthal GmbH
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Patent number: 8404683Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.Type: GrantFiled: November 3, 2010Date of Patent: March 26, 2013Assignee: Janssen Pharmaceutical N.V.Inventors: Jean Ferand Armand Lacrampe, Christophe Meyer, Yannick Aimè Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
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Patent number: 8404691Abstract: There is provided compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. Compounds include imidazothiazole derivatives that can inhibit interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity.Type: GrantFiled: July 15, 2011Date of Patent: March 26, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Kouichi Uoto, Yuuichi Sugimoto, Hiroyuki Naito, Masaki Miyazaki, Keisuke Yoshida, Masashi Aonuma
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Publication number: 20130072468Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Inventors: Eric J. Gilbert, William J. Greenlee, Michael W. Miller, Jack D. Scott, Andrew W. Stamford
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Publication number: 20130072467Abstract: The present invention provides a novel compound having a superior activity as an ERR-? modulator and useful as an agent for the prophylaxis or treatment of ERR-? associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: August 3, 2012Publication date: March 21, 2013Inventors: Shigemitsu MATSUMOTO, Koji Ono, Yusuke Tominari, Taisuke Katoh, Kazuhiro Miwa, Atsushi Hasuoka, Shinichi Imamura
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
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Publication number: 20130066075Abstract: Provided is a compound useful in the prevention and treatment of non-alcoholic steatohepatitis. A prophylactic and/or therapeutic agent for non-alcoholic steatohepatitis which contains, as the active ingredient, 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, an acid-addition salt thereof, or a solvate of the same.Type: ApplicationFiled: May 18, 2011Publication date: March 14, 2013Applicant: KOWA COMPANY, LTD.Inventors: Haruki Shibata, Yasunobu Yoshinaka, Kimiyuki Shibuya
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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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Publication number: 20130064770Abstract: The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.Type: ApplicationFiled: May 26, 2011Publication date: March 14, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Ian Martin Newington, Duncan George Wynn, Robert James Domett Nairne, Benedicte Guilbert, Subrata Mandal, Jinto Jose, Sunderaraman Varadarajan, Chitralekha Rangaswamy, Helen Betts, Rebecca Davis
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PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE
Publication number: 20130059839Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: April 18, 2011Publication date: March 7, 2013Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Nicholas J. Lawrence, Roberta Pireddu, Said M. Sebti -
Publication number: 20130053383Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: May 5, 2011Publication date: February 28, 2013Inventors: Celine Duquenne, 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: 20130053369Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: ApplicationFiled: October 26, 2012Publication date: February 28, 2013Applicant: Astellas Pharma Inc.Inventor: Astellas Pharma Inc.
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Publication number: 20130053398Abstract: 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). A method of synthesizing 4-(2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1-carboxylic acid (4-chloro-pyridin-3-yl)-amide is also disclosed.Type: ApplicationFiled: May 2, 2011Publication date: February 28, 2013Applicant: Janssen Pharmaceutica NVInventors: John M. Keith, Jing Liu
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Publication number: 20130053372Abstract: The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.Type: ApplicationFiled: February 15, 2011Publication date: February 28, 2013Inventors: Prashant Bhimrao Kapadnis, Robert Glen, Robin Hiley, James Bell, David Spring
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Publication number: 20130053397Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful in treating cancer.Type: ApplicationFiled: May 5, 2011Publication date: February 28, 2013Inventors: 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: 20130053345Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Inventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Patent number: 8383660Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: GrantFiled: January 3, 2007Date of Patent: February 26, 2013Assignee: Pfizer Inc.Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
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Patent number: 8377938Abstract: The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor.Type: GrantFiled: February 14, 2008Date of Patent: February 19, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Tomohiro Matsushima, Shuji Shirotori, Keiko Takahashi, Atsushi Kamada, Kazunori Wakasugi, Takahisa Sakaguchi
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Patent number: 8378095Abstract: 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 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: GrantFiled: May 9, 2008Date of Patent: February 19, 2013Assignee: Saruem LimitedInventors: John Charles Reader, John Mark Ellard, Michael Cherry
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Patent number: 8377924Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure 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: GrantFiled: January 21, 2010Date of Patent: February 19, 2013Assignee: Rigel Pharmaceuticals Inc.Inventors: Rajinder Singh, Huí Li, Haoran Zhao, Rao Kolluri, Kin Tso, John Ramphal, Shihai Gu, Carlos Valdez, Jing Zhang, Emily Stauffer, Matthew Duncton, Salvador Alvarez
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Patent number: 8378108Abstract: The present invention relates to compounds of Formula (I): where in X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 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 and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: GrantFiled: July 12, 2010Date of Patent: February 19, 2013Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte
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Patent number: 8378092Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: August 18, 2010Date of Patent: February 19, 2013Assignee: SanofiInventors: Markus Follmann, Volkmar Wehner, Jerome Meneyrol, Jean-Michel Altenburger, Frédéric Petit, Gilbert Lassalle, Jean-Pascal Herault
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Publication number: 20130040359Abstract: Nitric oxide synthase (NOS) inhibitor compounds comprising bi-terminal aromatic ring moieties, and related methods of NOS inhibition.Type: ApplicationFiled: October 1, 2012Publication date: February 14, 2013Applicant: Northwestern UniversityInventor: Northwestern University
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Publication number: 20130040962Abstract: There is provided a compound of formula (I): wherein: J represents (A): or (B): compositions comprising same, processes for preparing said compounds and use thereof in treatment, particularly in the treatment of inflammatory disease, such as asthma, COPD and 15 rheumatoid arthritis.Type: ApplicationFiled: April 8, 2011Publication date: February 14, 2013Inventors: John King-Underwood, Peter John Murray, Jonathan Gareth Williams, Ildiko Buck, Stuart Thomas Onions
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Publication number: 20130040961Abstract: Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) PEG) oligomers. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over non-oligomer modified diaromatic substituted compounds.Type: ApplicationFiled: February 22, 2011Publication date: February 14, 2013Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Publication number: 20130040948Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: ApplicationFiled: February 10, 2012Publication date: February 14, 2013Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20130040930Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Patent number: 8372849Abstract: This invention relates to heterocyclic compounds of the formulas shown in the specification. It also relates to methods for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, and tissue injuries with one of the heterocyclic compounds.Type: GrantFiled: November 3, 2008Date of Patent: February 12, 2013Assignee: Taigen Biotechnology Co., Ltd.Inventors: Chi-Feng Yen, Cheng-Kung Hu, Chang-Pin Huang, Ying-Huey Huang, Gholam Hossein Hakimelahi, Chi-Hsin Richard King
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Patent number: 8372844Abstract: The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.Type: GrantFiled: April 24, 2012Date of Patent: February 12, 2013Assignee: Korea Research Institute of Chemical TechnologyInventors: Jae Yang Kong, Woo-Kyu Park, Heeyeong Cho, Daeyoung Jeong, Gildon Choi, Hun Yeong Koh, Sang Hee Kim, Ae Nim Pae, Yong Seo Cho, Joo Hwan Cha, Hyunah Choo, Sang Eun Chae, Hee-Yoon Lee
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Publication number: 20130035339Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are 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 and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: September 13, 2012Publication date: February 7, 2013Applicant: Gilead Sciences, IncInventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
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Patent number: 8367664Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: January 23, 2007Date of Patent: February 5, 2013Assignee: Allergan, Inc.Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
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Patent number: 8367676Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.Type: GrantFiled: June 28, 2010Date of Patent: February 5, 2013Assignee: AstraZeneca ABInventors: Johan Andersson, Helena Gybäck, Anh Johansson, Christian Erik Linde, Jonas Malmström, Gunnar Nordvall, Tatjana Weigelt, Gitte Terp
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Patent number: 8367844Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: GrantFiled: August 6, 2010Date of Patent: February 5, 2013Assignee: Syngenta Crop Protection LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
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Patent number: 8367653Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: February 5, 2013Assignee: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark MacIelag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu