Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
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Patent number: 9012443Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: December 6, 2012Date of Patent: April 21, 2015Assignee: Amgen Inc.Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
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Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation
Patent number: 9012450Abstract: Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.Type: GrantFiled: December 28, 2012Date of Patent: April 21, 2015Assignees: Global Blood Therapeutics, Inc., Cytokinetics, Inc., The Regents of the University of CaliforniaInventors: Brian Metcalf, Chihyuan Chuang, Jeffrey Warrington, Kumar Paulvannan, Matthew P. Jacobson, Lan Hua, Bradley Morgan -
Patent number: 9012642Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).Type: GrantFiled: September 18, 2012Date of Patent: April 21, 2015Assignee: ViiV Healthcare UK LimitedInventors: Simon N. Haydar, Brian Alvin Johns, Emile Johann Velthuisen
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Patent number: 9012659Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.Type: GrantFiled: December 10, 2010Date of Patent: April 21, 2015Assignee: Johannes Gutenberg—Universitat MainzInventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
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Patent number: 9012646Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: GrantFiled: July 9, 2014Date of Patent: April 21, 2015Assignee: Nivalis Therapeutics, Inc.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20150104384Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.Type: ApplicationFiled: March 1, 2013Publication date: April 16, 2015Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
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Publication number: 20150105367Abstract: This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.Type: ApplicationFiled: March 5, 2013Publication date: April 16, 2015Inventors: Daniel L. Flynn, Michael D, Kaufman, Lakshminarayana Vogeti, Scott Wise, Wei-Ping Lu, Bryan Smith, Timothy Malcolm Caldwell, William C. Patt, James R. Henry, Philip A. Hipskind, Sheng-Bin Peng
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Publication number: 20150105418Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20150105405Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.Type: ApplicationFiled: March 25, 2013Publication date: April 16, 2015Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber, Wolfgang Von Deyn, Swetlana Derksen, Deborah L. Culberston, Nancy B. Rankl
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Publication number: 20150105401Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: October 7, 2014Publication date: April 16, 2015Applicant: The University of RochesterInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
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Publication number: 20150105377Abstract: The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: March 12, 2013Publication date: April 16, 2015Inventors: Joseph M. Gozgit, Victor M. Rivera, William C. Shakespeare, Xiaotian Zhu, David C. Dalgarno
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Publication number: 20150105380Abstract: The present invention provides methods for treating polycystic kidney disease by administering a compound or pharmaceutical composition thereof having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein.Type: ApplicationFiled: September 23, 2014Publication date: April 16, 2015Applicant: ANGION BIOMEDICA CORP.Inventors: Prakash NARAYAN, Brian HUANG, Prani PAKA, Latha PAKA, Itzhak D. GOLDBERG
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Publication number: 20150099777Abstract: A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent for the prophylaxis or treatment of diabetes mellitus are provided.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Hideki Hirose, Takeshi Yamasaki, Tohru Yamashita, Asato Kina, Yoichi Nishikawa
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Patent number: 9000175Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).Type: GrantFiled: November 24, 2011Date of Patent: April 7, 2015Assignee: Lupin LimitedInventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 8999968Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: GrantFiled: July 3, 2013Date of Patent: April 7, 2015Assignee: University Health NetworkInventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
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Patent number: 8999966Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).Type: GrantFiled: October 24, 2011Date of Patent: April 7, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr.
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Patent number: 8999957Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: GrantFiled: June 22, 2011Date of Patent: April 7, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Yongqi Deng, Liang Zhu, Gerald W. Shipps, Jr., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
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Publication number: 20150093338Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: October 8, 2014Publication date: April 2, 2015Inventor: Michael Farber
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Publication number: 20150094328Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.Type: ApplicationFiled: September 30, 2014Publication date: April 2, 2015Inventors: Andrew Payne, Jose Luis Castro Pineiro, Louise Michelle Birch, Afzal Khan, Alan James Braunton, James Edward Kitulagoda, Motohiro Soejima
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Publication number: 20150094327Abstract: The invention provides a fluorescence polarization (FP)-based assay to identify inhibitors of resolvase's DNA cleavage activity. The invention also provides resolvase inhibitors identified by the assay, as well as derivatives and analogs thereof. In certain embodiments, the compounds of the invention are useful to treat a poxvirus infection in an infected subject.Type: ApplicationFiled: April 29, 2013Publication date: April 2, 2015Inventors: Frederic D. Bushman, Young Hwang, Matt Culyba
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Publication number: 20150094310Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.Type: ApplicationFiled: April 23, 2013Publication date: April 2, 2015Inventor: Florian Holsboer
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Publication number: 20150094306Abstract: The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: April 25, 2013Publication date: April 2, 2015Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
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Publication number: 20150094311Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: December 1, 2014Publication date: April 2, 2015Inventors: HENRICUS JACOBUS MARIA GIJSEN, ADRIANA INGRID VELTER, GREGOR JAMES MACDONALD, FRANCOIS PAUL BISCHOFF, TONGFEI WU, SVEN FRANCISCUS ANNA VAN BRANDT, MICHEL SURKYN, MIRKO ZAJA, SERGE MARIA ALOYSIUS PIETERS, DIDIER JEAN-CLAUDE BERTHELOT, MICHEL ANNA JOZEF DE CLEYN, DANIEL OEHLRICH
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Patent number: 8993589Abstract: The present invention relates to substituted imidazo [1,2-a]pyridines of formula I where R is —CH2COOH or —COOH, which inhibits exogenously or endogenously stimulated gastric acid secretion and can be used in the prevention and treatment of gastric acid related diseases and gastrointestinal inflammatory diseases.Type: GrantFiled: February 19, 2014Date of Patent: March 31, 2015Inventor: Mikael Dahlström
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Patent number: 8993779Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 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 metabotropic glutamate receptors are involved, such as schizophrenia.Type: GrantFiled: August 5, 2011Date of Patent: March 31, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
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Patent number: 8993564Abstract: Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed treatment of tumours.Type: GrantFiled: May 29, 2012Date of Patent: March 31, 2015Assignee: Merck Patent GmbHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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Patent number: 8993612Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: GrantFiled: October 6, 2010Date of Patent: March 31, 2015Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V S Varanasi, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
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Patent number: 8993590Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.Type: GrantFiled: March 12, 2014Date of Patent: March 31, 2015Assignee: Galapagos NVInventors: Nicolas Desroy, Bertrand Heckmann, Reginald Christophe Xavier Brys, Agnès Marie Joncour, Christophe Peixoto, Xavier Marie Bock
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Publication number: 20150087648Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 10, 2014Publication date: March 26, 2015Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
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Publication number: 20150087605Abstract: Disclosed are compositions and methods for treating anthrax, inhibiting anthrax toxins and inhibiting anthrax toxin-induced cytotoxicity. Carboxylic acid-containing small molecules can be used in the methods and compositions disclosed herein, for example, sulindac and derivatives thereof may be used. Methods of screening for carboxylic acid-containing small molecules that can be used to treat anthrax are disclosed. Targeting the anthrax toxin reduces the risks of anthrax spores.Type: ApplicationFiled: September 19, 2014Publication date: March 26, 2015Inventors: J. Manuel Perez Figueroa, Oscar Santiesteban, Charalambos Kaittanis
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Patent number: 8987297Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: GrantFiled: August 6, 2014Date of Patent: March 24, 2015Assignee: Wockhardt Ltd.Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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Publication number: 20150080413Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Jerome Emile Georges Guillemont, David Francis Alain Lancois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Publication number: 20150080410Abstract: Developed here is a mitotic network comprising a signature of up to 54 genes, and including also sub-sets of genes within the signature, which can identify members by requiring higher correlation values for a signature gene. The present mitotic network provides for methods for prognosis and diagnosis of various cancers. The mitotic network is conserved across cancers exhibiting aberrant mitotic activity and several genes in the network act as therapeutic targets. Development of other inhibitors of mitosis can apply expression values of the genes in the mitotic network from patient tissue to select patients during clinical validation of the new drugs.Type: ApplicationFiled: May 19, 2014Publication date: March 19, 2015Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Zhi Hu, Jian-hua Mao, Wen-Lin Kuo, Ge Huang, Joe W. Gray
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Publication number: 20150080372Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.Type: ApplicationFiled: October 14, 2014Publication date: March 19, 2015Inventors: Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang
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Publication number: 20150080377Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, aType: ApplicationFiled: August 31, 2013Publication date: March 19, 2015Inventor: Daljit Singh Dhanoa
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Publication number: 20150080387Abstract: The invention relates to pharmaceutical formulations in liquid form, containing fluoroquinolones and antioxidative sulphur compounds. The formulations are particularly suitable for parenteral uses and are distinguished, inter alia, by good tolerance.Type: ApplicationFiled: November 21, 2014Publication date: March 19, 2015Inventors: Iris HEEP, Kristine FRAATZ, Hans-JĂĽrgen HAMANN, Markus EDINGLOH
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Patent number: 8980895Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: GrantFiled: August 9, 2012Date of Patent: March 17, 2015Assignee: Mercury Therapeutics, Inc.Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Patent number: 8980888Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: GrantFiled: September 4, 2014Date of Patent: March 17, 2015Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Akihiro Okano, Muneyoshi Makabe, Kouki Ogawa
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Patent number: 8980910Abstract: A method is provided for treating patients suffering from elevated intraocular pressure or fluctuation in intraocular pressure, including for example glaucoma patients. The method comprises administering to the patient an inhibitor of orexin activity in an amount sufficient to reduce intraocular pressure or intraocular pressure fluctuation in one or both eyes of the patient.Type: GrantFiled: March 29, 2012Date of Patent: March 17, 2015Assignee: Indiana University Research and Technology CorporationInventors: Brian C. Samuels, Anantha Shekhar, Philip L. Johnson
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Patent number: 8980887Abstract: Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification.Type: GrantFiled: June 9, 2011Date of Patent: March 17, 2015Assignees: Institute of Pharmacology, Toxicology Academy of Military Medical Sciences P.L.A., ChinaInventors: Rifang Yang, Yunfeng Li, Yongzhen Li, Nan Zhao, Liuhong Yun, Juanjuan Qin, Zhongyao Feng, Youzhi Zhang
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Patent number: 8980911Abstract: The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A? B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.Type: GrantFiled: November 22, 2013Date of Patent: March 17, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Ashwani Kumar Verma, Kumaragurubaran Nagaswamy, Lalima Sharma, Soma Ghosh, Balkrishna Ramchandra Kale, Aniruddha Mondal, Punit Kumar Srivastava, Sunanda Ghosh Dastidar, Rijwan Jaffer Momin, Pradip Balu Wagh, Sonali Nanasaheb Pansare, Pramod Raosaheb Markad, Yogesh Balasaheb Khairnar, Rie Miyauchi, Takeshi Murata, Masayuki Ishizaki, Masatoshi Nagamochi, Shin Iimura
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Patent number: 8980893Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.Type: GrantFiled: November 21, 2013Date of Patent: March 17, 2015Assignee: Merial, Inc.Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
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Patent number: 8981101Abstract: 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 tumors.Type: GrantFiled: January 9, 2012Date of Patent: March 17, 2015Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
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Publication number: 20150072978Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: November 17, 2014Publication date: March 12, 2015Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew J. Souers
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Publication number: 20150072955Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: October 14, 2014Publication date: March 12, 2015Applicant: Resverlogix Corp.Inventor: Henrik C. Hansen
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Publication number: 20150073011Abstract: The present invention is directed to compounds which are beta-lacatamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R2, R3 and R4 are described herein.Type: ApplicationFiled: April 2, 2013Publication date: March 12, 2015Applicant: ASTRAZENECA ABInventors: Helen McGuire, Shanta Bist, Neil Bifulco, Liang Zhao, Ye Wu, Hoan Huynh, Hui Xiong, Janelle Comita-Prevoir, Daemian Dussault, Bolin Geng, Brendan Chen, Thomas Durand-Reville, Satenig Guler
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Publication number: 20150072974Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.Type: ApplicationFiled: May 9, 2013Publication date: March 12, 2015Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
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Patent number: 8975276Abstract: PDE10 inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit PDE10 are also disclosed.Type: GrantFiled: June 25, 2012Date of Patent: March 10, 2015Assignee: Bristol-Myers Squibb CompanyInventors: William D. Schmitz, Mikkel V. DeBenedetto, S. Roy Kimura
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Patent number: 8975261Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: May 21, 2012Date of Patent: March 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo