The Additional Hetero Ring Is Six-membered And Contains Nitrogen Patents (Class 540/597)
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Publication number: 20130039906Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
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Publication number: 20130029971Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: January 5, 2011Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Patent number: 8362008Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: GrantFiled: December 11, 2008Date of Patent: January 29, 2013Assignee: The University Of EdinburghInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20130023521Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.Type: ApplicationFiled: January 17, 2011Publication date: January 24, 2013Applicant: HYBRIGENICS SAInventors: Roman Lopez, Frederic Colland
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Publication number: 20130018043Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: ApplicationFiled: July 11, 2012Publication date: January 17, 2013Inventors: Joseph A. Bilotta, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Stuart Hayden, Nancy-Ellen Haynes, Christine M. Lukacs-Lesburg, Nicholas Marcopulos, Eric Mertz, Lida Qi, Yimin Qian, Sung-Sau So, Jenny Tan, Kshitij C. Thakkar
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Publication number: 20130012499Abstract: The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: ApplicationFiled: March 23, 2011Publication date: January 10, 2013Applicant: GlaxoSmithKline LLCInventors: Carl A. Brooks, Mui Cheung, S. Eidam Hilary, Ryan M. Fox, Mark A. Hilfiker, Eric S. Manas
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Publication number: 20130005709Abstract: The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.Type: ApplicationFiled: March 24, 2010Publication date: January 3, 2013Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Rajesh Kumar Badange, Veena Reballi, Anil Kashinath Chindhe, Rambabu Namala, Mohamad Sadik Abdulhamid Mulla, Ishtiyaque Ahmad, Renny Abraham, Venkateswarlu Jasti
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Patent number: 8338590Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substitutes A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.Type: GrantFiled: May 20, 2011Date of Patent: December 25, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Hervé Geneste, Andrea Hager-Wernet, legal representative
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Patent number: 8334283Abstract: Compositions for treating, reducing, ameliorating, or preventing infections comprise a fluoroquinolone having Formulae I-VIII and an additional anti-infective agent. Methods for treating, reducing, ameliorating, or preventing such infection use such compositions. Such compositions and methods can be effective against mixed types of pathogens including certain antibiotic-resistant microbial pathogens found in such infections.Type: GrantFiled: April 3, 2012Date of Patent: December 18, 2012Assignee: Bausch & Lomb IncorporatedInventors: Praveen Tyle, Erning Xia, Hongna Wang, Susan E. Norton, Pramod Kumar Gupta, Keith W. Ward, Lynne Brunner
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Publication number: 20120309746Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: May 24, 2012Publication date: December 6, 2012Inventors: Johannes Cornelius Hermann, Matthew C. Lucas, Kin-Chun Thomas Luk, Fernando Padilla, Jutta Wanner, Wenwei Xie, Xiaohu Zhang
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Publication number: 20120309742Abstract: The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of cognitive dysfunction.Type: ApplicationFiled: August 8, 2012Publication date: December 6, 2012Inventors: Ralf GLATTHAR, Donald JOHNS, Daniel UMBRICHT
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Patent number: 8318769Abstract: Substituted sulfonamide compounds corresponding to formula I: processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor.Type: GrantFiled: April 8, 2009Date of Patent: November 27, 2012Assignee: Gruenethal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Franz-Martin Engels, Ruth Jostock, Tieno Germann, Jean De Vry, Klaus Schiene, Sabine Hees
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Publication number: 20120295889Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: Merck Serono S.A.Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20120289696Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.Type: ApplicationFiled: July 26, 2012Publication date: November 15, 2012Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
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Publication number: 20120289497Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: ApplicationFiled: January 17, 2011Publication date: November 15, 2012Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Publication number: 20120277214Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: November 24, 2010Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Patent number: 8299056Abstract: Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.Type: GrantFiled: September 8, 2009Date of Patent: October 30, 2012Assignee: Signal Pharmaceuticals, LLCInventors: Sogole Bahmanyar, R.J. Bates, Kate Blease, Andrew Calabrese, Thomas Daniel, Mercedes Delgado, Jan Elsner, Paul Erdman, Bruce Fahr, Gregory Ferguson, Branden Lee, Lisa Nadolny, Garrick Packard, Patrick Papa, Veronique Plantevin-Krenitsky, Jennifer Riggs, Patricia Rohane, Sabita Sankar, John Sapienza, Yoshitaka Satoh, Victor Sloan, Randall Stevens, Lida Tehrani, Jayashree Tikhe, Eduardo Torres, Andrew Wallace, Brandon Wade Whitefield, Jingjing Zhao
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Publication number: 20120264737Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.Type: ApplicationFiled: March 8, 2012Publication date: October 18, 2012Applicant: 3-V BIOSCIENCES, INC.Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
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Publication number: 20120258959Abstract: Novel compounds 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. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: June 12, 2012Publication date: October 11, 2012Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120252789Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.Type: ApplicationFiled: November 22, 2010Publication date: October 4, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Frank Stieber, Dirk Wienke
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Publication number: 20120245344Abstract: A compound represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes: wherein each of R23, R24, and R25 is hydrogen, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylsulfonyl, or the like; each of Q0 and T0 is CH2 or the like, or Q0 and T0 are combined to form CH?CH or the like; A0 is (CH2)p, C(O), or a bond; B0 is a bond or the like; one of U0 and V0 is N, and the other is CR31 or the like; each of X0 and Y0 is CH2CH2 or the like; Z0 is C(O)OR32 or the like; and each of R21 and R22 is hydrogen, a halogen atom, hydroxyl, C1-8 alkyl, or the like.Type: ApplicationFiled: August 30, 2010Publication date: September 27, 2012Applicant: NIPPON CHEMIPHAR CO., LTD.Inventors: Tsuyoshi Endo, Hiroto Tanaka, Toshihiro Takahashi, Toshihiro Kunigami
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Patent number: 8273736Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 20, 2009Date of Patent: September 25, 2012Assignee: Abbott LaboratoriesInventors: Patrick Betschmann, Andrew F. Burchat, David J. Calderwood, Michael L. Curtin, Steven K. Davidsen, Heather M. Davis, Robin R. Frey, Howard R. Heyman, Gavin C. Hirst, Peter Hrnciar, Michael R. Michaelides, Melanie A. Muckey, Kelly D. Mullen, Paul Rafferty, Carol K. Wada
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Publication number: 20120232062Abstract: Azaindazole compounds are useful for treating Flaviviridae virus infection, including HCV infection.Type: ApplicationFiled: October 19, 2010Publication date: September 13, 2012Applicant: EIGER BIOPHARMACEUTICALS, INC.Inventors: Wenjin Yang, Ingrid Choong
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Publication number: 20120226033Abstract: The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I) below: and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.Type: ApplicationFiled: September 16, 2010Publication date: September 6, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Clary, Jean-Claude Pascal
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Publication number: 20120225847Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylType: ApplicationFiled: June 24, 2009Publication date: September 6, 2012Inventors: Mette Knak Christensen, Fredrik Bjorkling
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Publication number: 20120225862Abstract: Provided are certain heteroaryl benzamides, compositions, and methods of their manufacture and use.Type: ApplicationFiled: July 21, 2010Publication date: September 6, 2012Applicants: AUCKLAND UNIVSERVICES LIMITED, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Patrick D. Sutphin, Denise A. Chan, Sandra Turcotte, William Alexander Denny, Michael Patrick Hay, Anna Claire Giddens, Muriel Marie Bonnet, Amato J. Giaccia
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Patent number: 8258301Abstract: Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, W, and Y are as described herein, or a tautomer, prodrug, solvate, or salt thereof. These compounds are useful as inhibitors of Urotensin II and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the interaction of Urotensin II with its receptor, including cardiovascular diseases. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds, and intermediates useful in these processes.Type: GrantFiled: May 12, 2008Date of Patent: September 4, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Anne Bettina Eldrup, Ingo Andreas Mugge, Fariba Soleymanzadeh, Sanxing Sun, Yunlong Zhang
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Publication number: 20120214790Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 11, 2011Publication date: August 23, 2012Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
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Publication number: 20120208809Abstract: The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c?]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers anType: ApplicationFiled: November 30, 2009Publication date: August 16, 2012Applicant: SANOFIInventors: Didier Babin, Olivier Bedel, Thierry Gouyon, Serge Mignani, David Papin
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Publication number: 20120196849Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: ApplicationFiled: April 10, 2012Publication date: August 2, 2012Applicant: IRM LLCInventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
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Publication number: 20120178741Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noélle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
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Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Patent number: 8217032Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.Type: GrantFiled: June 23, 2011Date of Patent: July 10, 2012Assignee: Eli Lilly and CompanyInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
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Patent number: 8211884Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: July 23, 2009Date of Patent: July 3, 2012Assignee: Madrigal Pharmaceuticals, Inc.Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian
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Publication number: 20120157447Abstract: A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.Type: ApplicationFiled: September 28, 2007Publication date: June 21, 2012Inventor: Arthur E. Harms
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Publication number: 20120157433Abstract: The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.Type: ApplicationFiled: September 2, 2010Publication date: June 21, 2012Inventors: Keith B. Pfister, Martin Sendzik
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Publication number: 20120142635Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: February 8, 2012Publication date: June 7, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Publication number: 20120135961Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.Type: ApplicationFiled: January 10, 2011Publication date: May 31, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt
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Patent number: 8183366Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the variants R, R9, Z, X, Q and Y are defined in the specification.Type: GrantFiled: September 20, 2010Date of Patent: May 22, 2012Assignee: Novartis AGInventors: Rene Hersperger, Philipp Janser, Emil Pfenninger, Hans J Wuethrich, Wolfgang Miltz
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Publication number: 20120122848Abstract: A novel (+)-3-hydroxymorphinan derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating a neurodegenerative disease, are provided.Type: ApplicationFiled: July 28, 2010Publication date: May 17, 2012Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Jong Yup Kim, Kwang-Seop Song, Jeongmin Kim, Kwang Woo Ahn, Yonggyu Kong
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Publication number: 20120121651Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, and prodrugs thereof, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
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Patent number: 8178131Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: May 13, 2009Date of Patent: May 15, 2012Assignee: Array BioPharma Inc.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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Publication number: 20120116072Abstract: Benzenesulfonamide compounds having a structure of the following general formula (I) are described. Also described, are methods for synthesizing the compounds, and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: June 28, 2010Publication date: May 10, 2012Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlene Schuppli
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Patent number: 8173638Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: November 15, 2007Date of Patent: May 8, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu
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Patent number: 8173640Abstract: Compositions for treating, reducing, ameliorating, or preventing infections comprise a fluoroquinolone having Formulae I-VIII and an additional anti-infective agent. Methods for treating, reducing, ameliorating, or preventing such infection use such compositions. Such compositions and methods can be effective against mixed types of pathogens including certain antibiotic-resistant microbial pathogens found in such infections.Type: GrantFiled: May 6, 2008Date of Patent: May 8, 2012Assignee: Bausch & Lomb IncorporatedInventors: Praveen Tyle, Erning Xia, Honga Wang, Susan E. Norton, Pramod Kumar Gupta, Keith W. Ward, Lynne Brunner
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Publication number: 20120108572Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: ApplicationFiled: August 26, 2009Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
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Publication number: 20120094944Abstract: For the prevention and/or treatment of chymase-mediated diseases such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like, a drug is provided having as an active ingredient a compound having extremely strong chymase inhibitory activity, high safety, and high metabolic stability. The compound represented by the formula (I): wherein all symbols have the same meanings as in the description, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a pharmaceutical ingredient having chymase inhibitory activity for preventing and/or treating of chymase-mediated disease, such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like.Type: ApplicationFiled: June 16, 2010Publication date: April 19, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Jun Takeuchi, Takayuki Inukai, Masaru Sakai
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Publication number: 20120083602Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: September 28, 2011Publication date: April 5, 2012Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: RE43481Abstract: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4?-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.Type: GrantFiled: September 3, 2008Date of Patent: June 19, 2012Assignee: Astellas Pharma Inc.Inventors: Fukushi Hirayama, Hiroyuki Koshio, Tsukasa Ishihara, Norio Seki, Shunichiro Hachiya, Keizo Sugasawa, Ryota Shiraki, Yuji Koga, Yuzo Matsumoto, Takeshi Shigenaga, Souichirou Kawazoe