Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
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Publication number: 20130059847Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: April 1, 2012Publication date: March 7, 2013Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Publication number: 20130059824Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from Mild Cognitive Impairment.Type: ApplicationFiled: November 23, 2010Publication date: March 7, 2013Applicant: AFRAXis, Inc.Inventors: Jay Lichter, David Campbell, Benedikt Vollrath, Sergio G. Durón
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Patent number: 8389520Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: GrantFiled: October 12, 2007Date of Patent: March 5, 2013Assignee: Bayer Intellectual Property GmbHInventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
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Patent number: 8389521Abstract: The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceuticals compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. formula (I).Type: GrantFiled: April 24, 2008Date of Patent: March 5, 2013Assignee: Ingenium Pharmaceuticals GmbHInventors: Heike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
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Patent number: 8383621Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.Type: GrantFiled: October 20, 2010Date of Patent: February 26, 2013Assignee: FAB Pharma S.A.S.Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Francois Moreau
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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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Publication number: 20130045955Abstract: The present invention provides compounds of formula (I) herein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 16, 2012Publication date: February 21, 2013Inventors: Nicholas J. Bennett, Thomas MCINALLY, Tobias MOCHEL, Stephen Thom, Anna-Karin Tidén
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Publication number: 20130045962Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.Type: ApplicationFiled: November 6, 2008Publication date: February 21, 2013Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
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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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Publication number: 20130040949Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: December 29, 2010Publication date: February 14, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
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Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
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Publication number: 20130035329Abstract: Compounds and compositions comprising compounds useful in the treatment of cancer are described herein.Type: ApplicationFiled: June 8, 2012Publication date: February 7, 2013Inventors: Jeffrey O. Saunders, Francesco G. Salituro
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Publication number: 20130034520Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: October 12, 2012Publication date: February 7, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8367658Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. 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 CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: GrantFiled: September 23, 2011Date of Patent: February 5, 2013Assignee: Cancer Research Technology LimitedInventors: Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
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Publication number: 20130029987Abstract: Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.Type: ApplicationFiled: April 20, 2012Publication date: January 31, 2013Inventors: Brydon L. Bennett, Jan Elsner, Paul Erdman, Robert Hilgraf, Laurie Ann LeBrun, Meg McCarrick, Mehran F. Moghaddam, Mark A. Nagy, Stephen Norris, David A. Paisner, Marianne Sloss, William J. Romanow, Yoshitaka Satoh, Jayashree Tikhe, Won Hyung Yoon, Mercedes Delgado
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Publication number: 20130029981Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.Type: ApplicationFiled: June 18, 2012Publication date: January 31, 2013Applicant: Katholieke Universiteit LeuvenInventors: Sigrid De Keersmaecker, Dirk De Vos, Denis Ermolatev, Hans Steenackers, Erik Van Der Eycken, Jozef Vanderleyden, Bharat S. Savaliya
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Patent number: 8362013Abstract: ABT-263 bis-HCl and crystalline polymorphs thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: GrantFiled: April 29, 2010Date of Patent: January 29, 2013Assignee: AbbVie Inc.Inventors: Thomas Borchardt, Paul Brackemeyer, Nathaniel Catron, Rodger Henry, Xiaochun Lou, Matthew Ravn, Geoff G. Z. Zhang, Deliang Zhou
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Patent number: 8362014Abstract: ABT-263 free base and crystalline forms thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: GrantFiled: September 15, 2010Date of Patent: January 29, 2013Assignee: AbbVie Inc.Inventors: Geoff G. Z. Zhang, Paul J. Brackemeyer, Nathaniel D. Catron, Thomas B. Borchardt
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Publication number: 20130023519Abstract: 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.Type: ApplicationFiled: January 24, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Tobias WUNBERG, Oliver KRAEMER, Lars van der VEEN
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Publication number: 20130023527Abstract: The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.Type: ApplicationFiled: September 14, 2012Publication date: January 24, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Graeme Semple, Beatriz Fioravanti, Guilherme Pereira, Imelda Calderon, Jane Laguerta Uy, Kameshwari Duvvuri, Jin Sun Karoline Choi, Yifeng Xiong, Vibha Dave, Mihai D. Azimioara
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Publication number: 20130023526Abstract: The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.Type: ApplicationFiled: April 30, 2012Publication date: January 24, 2013Applicant: Abbott LaboratoriesInventors: David J. Calderwood, Eric C. Breinlinger, Steven L. Swann, Venkata Srikanth Chitty, Subramanyah Seetharama Shastry Hosahalli, Subhendu Mukherjee, Siva Sanjeeva Rao Thunuguntla
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Publication number: 20130023533Abstract: 5-alkynyl-pyridine of general formula (I) which are inhibitors of the activity of PI3K alpha, and their use in the treatment of diseases characterized by excessive or abnormal cell proliferation, such as cancer.Type: ApplicationFiled: January 24, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Tobias WUNBERG, Oliver KRAEMER, Lars van der VEEN
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Publication number: 20130017196Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
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Publication number: 20130018046Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
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Publication number: 20130017194Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.Type: ApplicationFiled: July 6, 2012Publication date: January 17, 2013Applicant: Cancer Therapeutics CRC Pty LimitedInventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
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Patent number: 8354407Abstract: The present invention relates to 2-arylamino-4-(heterocyclic)aminopyrimidines inhibitors which are inhibitors and therefore inhibit Protein Kinase C-alpha (PKC-?). The PKC-? inhibitors of the present invention are important for improving myocardial intracellular calcium cycling, resulting in improved myocardial contraction and relaxation performance and thereby slowing the progression of heart failure. The present invention further relates to compositions comprising said 2-arylamino-4-(heterocyclic)amino-pyrimidines and to methods for controlling, abating, or otherwise slowing the progression of heart failure.Type: GrantFiled: May 14, 2009Date of Patent: January 15, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Jane Far-Jine Djung, Adam Golebiowski, Jack A. Hunter, Gary P. Schrum
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Publication number: 20130012490Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20130012476Abstract: The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Inventors: Qiang DING, Nathanael Schiander GRAY, Bing LI, Yi LIU, Taebo SIM, Tetsuo UNO, Guobao ZHANG, Carole Pissot Soldermann, Werner BREITENSTEIN, Guido BOLD, Giorgio CARAVATTI, Pascal FURET, Vito GUAGNANO, Marc LANG, Paul W. MANLEY, Joseph SCHOEPFER, Carsten SPANKA
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Publication number: 20130012500Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Inventors: Gurdip BHALAY, Emma BUDD, Graham Charles BLOOMFIELD, Stephen Paul COLLINGWOOD, Andrew DUNSTAN, Lee EDWARDS, Peter GEDECK, Catherine HOWSHAM, Peter HUNT, Thomas Anthony HUNT, Paul OAKLEY, Nichola SMITH
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Patent number: 8349833Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.Type: GrantFiled: October 18, 2011Date of Patent: January 8, 2013Assignee: Cerenis Therapeutics Holding SAInventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Ronald Barbaras, Valery Kochubey, Dmitry Kovalsky, Oleg Gennadievich Rodin, Otto Geoffroy, Anna Rzepiela
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Publication number: 20130005710Abstract: The present invention provides a novel aminopyridine derivative that is excellent in pharmaceutical effects such as a neuroprotective effect, a neurogenesis or nerve regeneration promoting effect, and a cognitive function improving effect and, preferably, is low toxic and delivered at a high rate to the central nervous system.Type: ApplicationFiled: November 17, 2010Publication date: January 3, 2013Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Norihito Tokunaga, Yuhei Miyanohana
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Publication number: 20130004518Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Applicant: Merck, Sharp & Dohme Corp.Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Publication number: 20130005728Abstract: The present invention is directed to a substituted pyrimidine compound of formula (I) or an enantiomer thereof, or a prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such a compound. The invention also includes a method of treatment of a patient by the administration of a pharmaceutically effective amount of such a compound.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Keith J. HARRIS, Joacy C. AGUIAR, Patrick Wai-Kwok SHUM, Zhicheng ZHAO, Gregory B. POLI, Gregory STOKLOSA, Yong-Mi CHOI-SLEDESKI, Stephan REILING, David STEFANY, Charles GARDNER
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Patent number: 8343969Abstract: This invention relates to a bromo-phenyl substituted thiazolyl dihydropyrimidine, its preparation method and use as a medicament for treating and preventing hepatitis B infections. The invention also relates to a composition comprising the dihydropyrimidine, one or more antiviral agents and, optionally, an immunomodulator for treating and preventing HBV infections.Type: GrantFiled: July 17, 2012Date of Patent: January 1, 2013Assignee: Sunshine Lake Pharma Co., Ltd.Inventors: Siegfried Goldman, Jing Li, Yi Song Liu
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Publication number: 20120328627Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: ApplicationFiled: August 28, 2012Publication date: December 27, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20120328570Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20120329784Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, and R6 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 11, 2011Publication date: December 27, 2012Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp, Yongdong Zhao
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Patent number: 8338614Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: January 13, 2006Date of Patent: December 25, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
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Patent number: 8338417Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases.Type: GrantFiled: May 2, 2008Date of Patent: December 25, 2012Assignees: IRM LLC, Novartis AGInventors: Xiaolin Li, Xiaodong Liu, Valentina Molteni, Donatella Chianelli, Jon Loren, Juliet Nabakka, Timothy Ramsey, Werner Breitenstein
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Patent number: 8338413Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.Type: GrantFiled: March 7, 2012Date of Patent: December 25, 2012Assignee: Novartis AGInventor: Heinrich Rueeger
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Publication number: 20120322802Abstract: The present invention relates to novel 2,4-pyrimidine derivatives and a use thereof, and more particularly, to pyrimidine derivatives which are effective for systemic lupus erythematosus, a composition for preventing and treating systemic lupus erythematosus comprising the same as an active ingredient and a method for screening the same. The present inventors found novel materials inhibiting surface translocation of gp96 by mimicking a function of AIMP1 which is a molecular anchor for an intracellular residence of gp96, and identified in vitro and in vivo activity of the materials for preventing and treating SLE by alleviating SLE plasma in autoimmune diseases. Therefore, the present invention provides a novel method for screening a therapeutic agent for SLE, and preventing or treating SLE using the mechanism.Type: ApplicationFiled: November 2, 2010Publication date: December 20, 2012Applicants: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, SNU R&DB FOUNDATIONInventors: Sunghoon Kim, Jung Min Han, Hyeong Rae Kim, Dong Ju Jeon, Jong Hwan Song, Kyung Eun Park
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Publication number: 20120322799Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.Type: ApplicationFiled: November 30, 2010Publication date: December 20, 2012Applicant: PHARMATROPHIX, INC.Inventor: Gopal Damodara
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Publication number: 20120322795Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b 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: December 14, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Zhidong CHEN, Stephane DE LOMBAERT, Michel Jose EMMANUEL, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Hidenori TAKAHASHI
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Publication number: 20120316155Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger
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Publication number: 20120316170Abstract: To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): or the general formula (II): or an isotope thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: Daiichi Sankyo Company LimitedInventors: Nobuo Machinaga, Jun Chiba, Fumihito Muro, Hiroshi Yuita, Jun Watanabe
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Publication number: 20120316159Abstract: This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: December 13, 2011Publication date: December 13, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
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Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
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Publication number: 20120316169Abstract: (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.Type: ApplicationFiled: October 28, 2010Publication date: December 13, 2012Applicant: DOMPÉ S.P.A.Inventors: Andrea Beccari, Andrea Aramini, Gianluca Bianchini, Alessio Moriconi
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Publication number: 20120316165Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, X, Z, Ar, and n are as described in the claims, Ar is phenyl or heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, 1H-pyrazole-3-yl, 1H-pyrazole-4-yl and 1H-pyrazole-5-yl; or to a pharmaceutically suitable acid addition salt thereof, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Guido Galley, Roger Norcross, Philippe Pflieger
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Patent number: 8329691Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: GrantFiled: October 14, 2008Date of Patent: December 11, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Tawada