Plural Piperidine Rings Patents (Class 514/316)
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Patent number: 8952004Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, 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: GrantFiled: January 5, 2011Date of Patent: February 10, 2015Assignee: Boehringer Ingelheim International GmbHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Patent number: 8940774Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.Type: GrantFiled: November 26, 2013Date of Patent: January 27, 2015Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Publication number: 20150025110Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: October 9, 2014Publication date: January 22, 2015Inventors: Henrietta Dehmlow, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Hans Richter
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Publication number: 20150025056Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
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Patent number: 8937086Abstract: The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.Type: GrantFiled: January 14, 2011Date of Patent: January 20, 2015Assignee: University of Pittsburgh—Of the Commonwealth System of Higher EducationInventors: Laura J. Niedernhofer, Paul D. Robbins, Peter Wipf
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Publication number: 20150011526Abstract: The present invention relates to 2-oxo-piperidinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 10, 2012Publication date: January 8, 2015Inventors: Ali Ates, Florian Montel, Anne Valade, Olivier Lorthioir
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Publication number: 20150005279Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 26, 2014Publication date: January 1, 2015Applicant: ABBVIE INC.Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
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Patent number: 8921395Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: GrantFiled: March 19, 2014Date of Patent: December 30, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Sabine Axt, Timothy J. Church
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Patent number: 8921394Abstract: Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: GrantFiled: April 21, 2011Date of Patent: December 30, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Thomas H. Graham, Dong-Ming Shen, Min Shu
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Publication number: 20140378471Abstract: The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.Type: ApplicationFiled: September 9, 2014Publication date: December 25, 2014Inventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20140378429Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein.Type: ApplicationFiled: January 31, 2013Publication date: December 25, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
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Patent number: 8916555Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: GrantFiled: March 14, 2013Date of Patent: December 23, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
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Publication number: 20140371239Abstract: The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.Type: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Inventors: Jolanta Grembecka, Tomasz Cierpicki, Sunil Kumar Upadhyay, Shaun R. Stauffer, Rocco D. Gogliotti, Timothy J. Senter
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Publication number: 20140369961Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
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Patent number: 8912334Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: September 11, 2013Date of Patent: December 16, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
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Publication number: 20140364419Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Robert Shalwitz, Joseph H. Gardner
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Patent number: 8907098Abstract: 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, Y1, Y2, V, W, n, m and o have the meanings given herein, 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: GrantFiled: November 18, 2010Date of Patent: December 9, 2014Assignee: MERCK PATENT GmbHInventors: Frank Stieber, Dirk Wienke
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Publication number: 20140349989Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated with these diseases and disorders.Type: ApplicationFiled: December 20, 2013Publication date: November 27, 2014Applicant: ALZHEIMER'S INSTITUTE OF AMERICAInventors: Dange Vijay Kumar, Paul M. Slattum, Kraig M. Yager, Mark D. Shenderovich, Rajendra Tangallapally, Se-Ho Kim
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Publication number: 20140349918Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.Type: ApplicationFiled: September 10, 2012Publication date: November 27, 2014Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and ResearchInventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan
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Publication number: 20140343074Abstract: The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.Type: ApplicationFiled: March 14, 2014Publication date: November 20, 2014Inventors: Katja Jantos, Wilfred Braje, Herve Geneste, Andreas Kling, Liliane Unger, Berthold Behl, Marcel van Gaalen, Wilfried Hornberger, Loic Laplanche, Silke Weber
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Publication number: 20140341851Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 4, 2014Publication date: November 20, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
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Publication number: 20140343075Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: July 30, 2014Publication date: November 20, 2014Applicant: MERCK PATENT GMBHInventors: Kai SCHIEMANN, Melanie SCHULTZ, Wolfgang STAEHLE
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Patent number: 8889716Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: GrantFiled: May 7, 2012Date of Patent: November 18, 2014Assignee: CHDI Foundation, Inc.Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
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Patent number: 8889670Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: February 16, 2010Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
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Publication number: 20140335074Abstract: Methods are provided herein for enhancing the effectiveness of medical therapies by administering agents that suppress a biological damage response that is inducible by the medical therapy administered to a subject. In certain embodiments, a method is provided for administering an anti-senescent cell agent that suppresses a biological response comprising cellular senescence that is induced by the medical therapy.Type: ApplicationFiled: December 13, 2012Publication date: November 13, 2014Inventors: Judith Campisi, Marco Demaria
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Publication number: 20140336222Abstract: The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: ApplicationFiled: July 24, 2014Publication date: November 13, 2014Inventors: Stephane L. Bogen, Yao Ma, Yaolin Wang, Brian Robert Lahue, Latha G. Nair, Manami Shizuka, Matthew E. Voss, Margarita Kirova-Snover, Weidong Pan, Yuan Tian, Bheemashankar A. Kulkarni, Craig R. Gibeau, Yuan Liu, Giovanna Scapin, Diane Rindgen, Ronald J. Doll, Timothy J. Guzi, Danny J. Hicklin, Amin Nomeir, Cynthia Seidel-Dugan, Gerald W. Shipps, JR., Malcolm MacCoss
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Publication number: 20140336165Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.Type: ApplicationFiled: November 14, 2012Publication date: November 13, 2014Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
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Publication number: 20140336193Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Inventors: Donald W. Landry, Shi-Xian Deng, Stevan Pecic, Kirsten Alison Rinderspacher
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Publication number: 20140336158Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: ApplicationFiled: July 25, 2014Publication date: November 13, 2014Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Publication number: 20140329803Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.Type: ApplicationFiled: November 16, 2012Publication date: November 6, 2014Inventors: Miles Congreve, Giles Brown, Julie Cansfield, Benjamin Tehan
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Publication number: 20140329809Abstract: A process for the characterization of rosacea is disclosed. The process can include identifying for the first time new markers in leukocyte recruitment as well as the therapeutic applications targeting rosacea.Type: ApplicationFiled: October 26, 2012Publication date: November 6, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Isabelle Carlavan, Martin Steinhoff
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Publication number: 20140323460Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
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Publication number: 20140323458Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.Type: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
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Patent number: 8871770Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: February 3, 2014Date of Patent: October 28, 2014Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Publication number: 20140315893Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediType: ApplicationFiled: November 22, 2012Publication date: October 23, 2014Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
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Publication number: 20140315918Abstract: The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Inventors: Katja Jantos, Wilfred Braje, Herve Geneste, Andreas Kling, Liliane Unger, Berthold Behl, Marcel van Gaalen, Wilfried Hornberger, Loic Laplanche, Silke Weber
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Publication number: 20140315914Abstract: The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: ApplicationFiled: April 14, 2014Publication date: October 23, 2014Inventors: Astrid Netz, Thorsten Oost, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Patent number: 8865641Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.Type: GrantFiled: June 14, 2012Date of Patent: October 21, 2014Assignee: The Feinstein Institute for Medical ResearchInventors: Valentin A. Pavlov, Kevin J. Tracey
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Patent number: 8865702Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.Type: GrantFiled: July 23, 2008Date of Patent: October 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20140309193Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.Type: ApplicationFiled: December 5, 2012Publication date: October 16, 2014Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
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Patent number: 8859776Abstract: The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: GrantFiled: October 5, 2010Date of Patent: October 14, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Stephane L. Bogen, Yao Ma, Yaolin Wang, Brian Robert Lahue, Latha G. Nair, Manami Shizuka, Matthew Ernst Voss, Margarita Kirova-Snover, Weidong Pan, Yuan Tian, Bheemashankar A. Kulkarni, Craig R. Gibeau, Yuan Liu, Giovanna Scapin, Diane Rindgen, Ronald J. Doll, Timothy J. Guzi, Danny J. Hicklin, Amin Nomeir, Gerald W. Shipps, Jr., Malcolm MacCoss
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Publication number: 20140296202Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: October 18, 2012Publication date: October 2, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
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Publication number: 20140296196Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: ApplicationFiled: June 13, 2014Publication date: October 2, 2014Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
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Publication number: 20140296212Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: ApplicationFiled: February 10, 2014Publication date: October 2, 2014Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Allison L. Zulli, Brigitte Lesur, Babu G. Sundar, Christophe Yue
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Publication number: 20140296289Abstract: Thiazolyl oxime ethers and hydrazones of the formula (I), in which the symbols A, L1, L2, Y, W, X, R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also methods for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: ApplicationFiled: February 28, 2014Publication date: October 2, 2014Applicant: Bayer CropScience AGInventors: Pierre CRISTAU, Nicola Rahn, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Arnd Voerste, Jürgen Benting
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1H-BENZIMIDAZOLE-4-CARBOXAMIDES SUBSTITUTED WITH PHENYL AT THE 2-POSITION ARE POTENT PARP INHIBITORS
Publication number: 20140296235Abstract: Compounds having formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds having formula (I), methods of treatment comprising compounds having formula (I), and methods of inhibiting the PARP enzyme comprising compounds having formula (I).Type: ApplicationFiled: April 11, 2014Publication date: October 2, 2014Inventors: Thomas D. Penning, Sheela A. Thomas, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda -
Patent number: 8846675Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.Type: GrantFiled: May 3, 2012Date of Patent: September 30, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
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Publication number: 20140288033Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: ApplicationFiled: March 19, 2014Publication date: September 25, 2014Applicant: THERAVANCE, INC.Inventors: Sabine Axt, Timothy J. Church
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Patent number: 8841323Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: GrantFiled: March 15, 2007Date of Patent: September 23, 2014Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma S.A.Inventors: Jose Maria Cid-Nunez, Jose Ignacio Andres-Gil, Andres Avelino Trabanco-Suarez, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Gregor James MacDonald, Shirley Elizabeth Pullan, Robert Johannes Lutjens, Guillaume Albert Jacques Duvey, Vanthea Nhem, Terry Patrick Finn, Gagik Melikyan, Vincent Mutel
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Publication number: 20140275068Abstract: The present invention provides neuronal gap junction blocking compounds according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1. The compounds are useful for the treatment or prevention of a range of conditions including, e.g., migraine, epilepsy, non-epileptic seizures, brain injury, and cardiovascular disease.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Proximagen LimitedInventors: Edward Savory, Daniel Hill, Oldrich Kocian