Ring Oxygen In The Bicyclo Ring System Patents (Class 546/115)
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Publication number: 20140228395Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Allergan, Inc.Inventors: SANTOSH C. SINHA, LIMING WANG, KEN CHOW, MOHAMMED I. DIBAS, MICHAEL E. GARST
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Publication number: 20140228377Abstract: A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which acts relying on an orexin (OX) receptor antagonistic activity and is useful for the treatment or prevention of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, head ache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases and hypertension.Type: ApplicationFiled: July 4, 2012Publication date: August 14, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Masahito Abe, Aya Futamura, Ryo Suzuki, Dai Nozawa, Hiroshi Ohta, Yuko Araki
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Publication number: 20140221322Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: November 5, 2013Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
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Patent number: 8796306Abstract: A noxious arthropod controlling composition comprising a heterocyclic compound represented by the formula (1) [wherein, A1 and A2 represent ?C(R6)—, nitrogen and so on, R1 represents a halogen and so on, R3 and R4 represent optionally substituted C1 to C4 chain hydrocarbon group and so on, R5 represents a hydrogen and so on, n represents 0 or 1] as an active ingredient has an excellent effect for controlling noxious arthropods.Type: GrantFiled: June 17, 2011Date of Patent: August 5, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsuhiko Iwakoshi, Hayato Takyo
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Patent number: 8796262Abstract: This invention relates to new fused heterocyclic derivatives having affinity to S1P receptors, a pharmaceutical composition containing said compounds, as well as the use of said compounds for the preparation of a medicament for treating, alleviating or preventing diseases and conditions in which any S1P receptor is involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.Type: GrantFiled: July 8, 2011Date of Patent: August 5, 2014Assignees: AbbVie B.V., AbbVie Inc.Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
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Publication number: 20140213538Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: January 15, 2014Publication date: July 31, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
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Patent number: 8790795Abstract: Provided are an organic compound having high heat stability suitable for use in an organic light-emitting device, and an organic light-emitting device using the organic compound. The organic light-emitting device is an organic light-emitting device, including: an anode; a cathode; and an organic compound layer disposed between the anode and the cathode, in which at least one layer of the organic compound layer has a 6,12-dinaphthylchrysene derivative represented by one of the following general formulae (1) and (2): in the formulae (1) and (2), Z represents a naphthyl group, and Q represents an electron-withdrawing substituent selected from the group consisting of the following general formulae (3) to (5): in the formula (5), R1 represents a hydrogen atom or a methyl group.Type: GrantFiled: May 25, 2012Date of Patent: July 29, 2014Assignee: Canon Kabushiki KaishaInventors: Hironobu Iwawaki, Hiroki Ohrui, Yuko Chishina, Masanori Muratsubaki, Tetsuo Takahashi
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Publication number: 20140206872Abstract: There is provided a fluorescent dye which can improve the fluorescent intensity at the time of labeling to thereby detect a biomolecule with higher sensitivity. The fluorescent dye of the present invention includes a nitrogen cation-containing group or a nitrogen-containing group. Its high water solubility can improve the rate of labeling for a biomolecule to thereby detect a biomolecule with high sensitivity.Type: ApplicationFiled: February 18, 2011Publication date: July 24, 2014Inventors: Shinichiro Isobe, Shuntaro Mataka
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Patent number: 8785635Abstract: The invention provides novel derivatives of cyclopamine having the following formula:Type: GrantFiled: August 27, 2008Date of Patent: July 22, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
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Publication number: 20140200216Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, David M. Burns, Hao Feng, Chu-Biao Xue, Anlai Wang, Jun Pan
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Publication number: 20140200227Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
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Publication number: 20140199263Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 16, 2012Publication date: July 17, 2014Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
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Patent number: 8778926Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: January 20, 2012Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Bernd Nosse
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Publication number: 20140194290Abstract: There is provided a compound having an excellent controlling effect on pests represented by the formula (1): wherein, A1 represents —NR7—, etc., A2 represents a nitrogen atom, etc., A3 represents a nitrogen atom, etc., R1 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R2, R3 and R4 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more halogen atoms, etc., R5 and R6 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R7 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group W, etc., n represents 0, 1 or 2, or an N-oxide thereof.Type: ApplicationFiled: August 3, 2012Publication date: July 10, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Masaki Takahashi, Takamasa Tanabe, Mai Ito, Yoshihiko Nokura, Atsushi Iwata
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Patent number: 8771665Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: GrantFiled: December 16, 2011Date of Patent: July 8, 2014Assignee: Cocrystal Discovery, Inc.Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Patent number: 8759523Abstract: The present invention relates to a process comprising the step of dehydrating a compound of Formula (I): with a suitable dehydrating reagent to form a compound of Formula (II): wherein R1-R7 are as defined herein. Compounds of Formula (II) have shown promise as intermediates to compounds useful for treating bacterial infections.Type: GrantFiled: July 19, 2011Date of Patent: June 24, 2014Assignee: Glaxo Group LimitedInventors: Joseph Sisko, Douglas Mans, Hao Yin
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Publication number: 20140163035Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: July 20, 2012Publication date: June 12, 2014Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm, Mark Murphy
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Publication number: 20140135332Abstract: The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: April 20, 2012Publication date: May 15, 2014Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David John Haydon, Lloyd George Czaplewski, Neil Robert Stokes, David Davies, Ian Collins, James T Palmer, Jeffrey Peter Mitchell, Gary Robert William Pitt, Daniel Offermann
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Publication number: 20140134235Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.Type: ApplicationFiled: October 14, 2013Publication date: May 15, 2014Applicant: DR. REDDY'S LABORATORIES LTD.Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
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Publication number: 20140128383Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.Type: ApplicationFiled: April 6, 2012Publication date: May 8, 2014Applicant: LABORATOIRE BIODIMInventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
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Patent number: 8716277Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: May 6, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
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Patent number: 8716479Abstract: The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of ? ketone product and ? ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.Type: GrantFiled: December 24, 2008Date of Patent: May 6, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian C. Austad, Andre Lescarbeau, Lin-Chen Yu
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Patent number: 8703758Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.Type: GrantFiled: April 26, 2011Date of Patent: April 22, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Tohru Yamashita, Makoto Kamata, Hideki Hirose, Masataka Murakami, Takuya Fujimoto, Zenichi Ikeda, Tsuneo Yasuma, Ikuo Fujimori, Ryo Mizojiri, Tomoya Yukawa
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Publication number: 20140094608Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: September 18, 2013Publication date: April 3, 2014Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Wai-Yee LEUNG, Ching-Ying Cheung, Stephen Yue
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Patent number: 8669365Abstract: The invention provides novel derivatives of cyclopamine having the following formula:Type: GrantFiled: August 27, 2008Date of Patent: March 11, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, André B. Charette, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
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Patent number: 8669271Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: December 16, 2011Date of Patent: March 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Niklas Heine, Elke Langkopf, Bernd Nosse
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Publication number: 20140066433Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.Type: ApplicationFiled: September 5, 2013Publication date: March 6, 2014Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Leonardus A.J.M. Sliedregt, Maria J.P. van Dongen, Jacobus A.J. den Hartog, Adrian Hobson
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Publication number: 20140057893Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.Type: ApplicationFiled: April 5, 2012Publication date: February 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Publication number: 20140045855Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: August 2, 2013Publication date: February 13, 2014Applicant: AMGEN INC.Inventors: Kaustav BISWAS, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. HORNE, Matthew R. KALLER, Vu Van MA, Kelvin SHAM, Wenge ZHONG
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Publication number: 20140044806Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.Type: ApplicationFiled: October 16, 2013Publication date: February 13, 2014Applicant: H. Lundbeck A/SInventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
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Publication number: 20140045800Abstract: Certain tetracyclic compounds are described, which may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: February 4, 2013Publication date: February 13, 2014Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20140039100Abstract: The instant invention pertains to novel bi- or tricyclic sterically hindered alkoxyamines, their precursors, a process for their preparation and their use as light stabilizers for polymers or coatings, as flame retardants, as peroxide substitutes (rheology modifiers) or carbon radical scavengers.Type: ApplicationFiled: October 4, 2013Publication date: February 6, 2014Applicant: BASF SEInventors: Stefan Hauck, Walter Fischer, Kai-Uwe Schoening
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Publication number: 20140024671Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: July 9, 2013Publication date: January 23, 2014Inventors: Michael EISSENSTAT, Dehui DUAN
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Publication number: 20140018373Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.Type: ApplicationFiled: December 22, 2011Publication date: January 16, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
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Publication number: 20130345255Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, wherein X1, L, Rx, Ry, Rz, R1, R2, A, m, n, p, q, and r are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: June 20, 2013Publication date: December 26, 2013Inventors: Arthur Gomtsyan, Jerome Daanen, Michael E. Kort, Philip R. Kym, Eric A. Voight, Kevin R. Woller
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Publication number: 20130331410Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LQ and Ar are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Elke LANGKOPF
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Patent number: 8603947Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.Type: GrantFiled: July 20, 2011Date of Patent: December 10, 2013Assignee: Bayer Cropscience AGInventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
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Patent number: 8604028Abstract: This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: GrantFiled: November 15, 2010Date of Patent: December 10, 2013Assignee: Bayer Intellectual Property GmbHInventors: Martin Michels, Hans Briem, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch
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Patent number: 8598156Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: March 23, 2011Date of Patent: December 3, 2013Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20130310391Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: January 9, 2012Publication date: November 21, 2013Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Christian Sirrenberg, Thomas J.J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
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Patent number: 8580956Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: GrantFiled: May 28, 2008Date of Patent: November 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
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Patent number: 8569336Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: November 9, 2009Date of Patent: October 29, 2013Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K. C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
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Patent number: 8569283Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: GrantFiled: August 29, 2012Date of Patent: October 29, 2013Inventors: Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
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Publication number: 20130267521Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Applicants: Intellikine LLC, Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
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Publication number: 20130267554Abstract: 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: ApplicationFiled: November 9, 2012Publication date: October 10, 2013Applicant: CERENIS THERAPEUTICS HOLDING SAInventors: Daniela Carmen ONICIU, Jean-Louis Henri DASSEUX, Otto GEOFFROY, Ronald BARBARAS
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Patent number: 8551982Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 13, 2012Date of Patent: October 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
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Publication number: 20130261107Abstract: In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. 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: August 31, 2011Publication date: October 3, 2013Applicant: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Carrie K. Jones, Jose Manuel Bartolome-Nebreda, Susana Conde-Ceide, James Gregor MacDonald, Manuel Jesus Alcazar Vaca
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Patent number: 8546374Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: GrantFiled: July 9, 2012Date of Patent: October 1, 2013Assignee: Abbvie Inc.Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
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Patent number: 8541595Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: GrantFiled: November 3, 2009Date of Patent: September 24, 2013Assignee: Merch Sharp & Dohme Corp.Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
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Publication number: 20130245025Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 3, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey