Ring Oxygen In The Bicyclo Ring System Patents (Class 514/302)
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Patent number: 8962651Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 11, 2014Date of Patent: February 24, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Kyle J. Eastman, Kyle E. Parcella, John F. Kadow
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Patent number: 8957062Abstract: 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. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: April 5, 2012Date of Patent: February 17, 2015Assignee: 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: 20150038502Abstract: The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 19, 2012Publication date: February 5, 2015Inventors: Dansu Li, Anthony J. Roecker
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Publication number: 20150038509Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: ApplicationFiled: June 12, 2014Publication date: February 5, 2015Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
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Publication number: 20150038527Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupusType: ApplicationFiled: January 22, 2013Publication date: February 5, 2015Applicant: Merck Patent GmbHInventors: Lars Burgdorf, Tatjana Ross, Carl Deutsch
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Publication number: 20150038438Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.Type: ApplicationFiled: August 29, 2012Publication date: February 5, 2015Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
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Publication number: 20150031668Abstract: 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: July 15, 2014Publication date: January 29, 2015Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen
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Patent number: 8940758Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.Type: GrantFiled: July 17, 2013Date of Patent: January 27, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Ando
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Publication number: 20150025070Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.Type: ApplicationFiled: July 13, 2012Publication date: January 22, 2015Applicant: Novartis AGInventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
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Publication number: 20150025106Abstract: The invention provides a drug delivery system for a combination of therapeutic agents. The system includes a water soluble biodegradable ABA-type triblock copolymer that possesses thermosensitive gelation properties. The system can form a stable thermogel that includes a combination of therapeutic agents including, for example, rapamycin, paclitaxel, and 17-AAG. After administration to a subject, the drugs are released at a controlled rate from the thermogel, which biodegrades into non-toxic components. The polymer system can also function to increase the solubility and stability of drugs in the composition.Type: ApplicationFiled: July 22, 2014Publication date: January 22, 2015Inventors: Glen S. Kwon, Hyunah Cho
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Publication number: 20150025075Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, X and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: January 18, 2013Publication date: January 22, 2015Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm
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Publication number: 20150005284Abstract: Compounds of the formula I in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: January 3, 2013Publication date: January 1, 2015Applicant: Merck Patent GmbHInventors: Hans Michael Eggenweiler, Guenter Hoelzemann, Dieter Dorsch
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Publication number: 20140378493Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: September 8, 2014Publication date: December 25, 2014Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
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Patent number: 8916584Abstract: Benzisoxazole and azabenzisoxazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: GrantFiled: February 11, 2011Date of Patent: December 23, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Darren W. Engers
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Publication number: 20140364444Abstract: 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: August 21, 2014Publication date: December 11, 2014Inventors: Hayato TAKYO, Masaki TAKAHASHI, Takamasa TANABE, Yoshihiko NOKURA, Mai ITO, Atsushi IWATA
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Patent number: 8907093Abstract: Carboxylic acid derivatives having an oxazolo[4,5-c]pyridine ring The invention therefore relates to compounds of the formula I in which X, Y, R1, R2 and R3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.Type: GrantFiled: June 25, 2012Date of Patent: December 9, 2014Assignee: SanofiInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Thomas Huebschle, Katrin Hiss
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Patent number: 8889868Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: GrantFiled: November 3, 2009Date of Patent: November 18, 2014Assignee: Syntarga BVInventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgersma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus de Groot
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Patent number: 8871738Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: GrantFiled: October 25, 2012Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
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Publication number: 20140309237Abstract: 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: June 26, 2014Publication date: October 16, 2014Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Patent number: 8859529Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: September 22, 2009Date of Patent: October 14, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Patent number: 8853238Abstract: 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: GrantFiled: December 22, 2011Date of Patent: October 7, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
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Patent number: 8853239Abstract: The present invention relates to compounds of formula I, wherein R1, LP, LQ, X, A, 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 6, 2012Date of Patent: October 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf
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Publication number: 20140296224Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Nicholas D. ADAMS, Joelle Lorraine Burgess, Michael Gerard Darcy, Carla A. Donatelli, Steven David Knight, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Stanley J. Schmidt
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Publication number: 20140294805Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: October 2, 2014Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
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Publication number: 20140275154Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Kyle J. Eastman, Kyle E. Parcella, John F. Kadow
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Publication number: 20140275156Abstract: There is provided now flavonoid compounds, compositions containing these compounds, methods for their synthesis, and uses of these compounds. In particular, there is provided methods of preventing and or mitigating the damage caused by cell apoptosis or cell necrosis by administration of the novel flavonoid compounds. In some aspects, there is provided methods for inhibiting pro-apoptotic signalling kinases activity in a subject while regulating and activating extracelluar signal regulated kinase (ERK).Type: ApplicationFiled: August 13, 2012Publication date: September 18, 2014Applicant: NEUPROTECT PTY LTDInventor: Grant McLachlan
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Publication number: 20140274926Abstract: The present invention provides compounds of Formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: IRM LLCInventors: Arnab Kumar CHATTERJEE, Fang LIANG, Casey Jacob Nelson MATHISON, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh NAGLE, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL
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Publication number: 20140275155Abstract: This invention relates to bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias GRAUERT, Ralf ANDERSKEWITZ, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
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Patent number: 8828998Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).Type: GrantFiled: March 15, 2013Date of Patent: September 9, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Vito J. Palombella, David G. Winkler
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Publication number: 20140249170Abstract: The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections.Type: ApplicationFiled: September 18, 2012Publication date: September 4, 2014Inventors: Radha Rangarajan, Rajinder Kumar, BV Prabhakar, P Chandrasekhar, P Mallikarjuna, Ankita Banerjee
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Publication number: 20140243310Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: October 23, 2012Publication date: August 28, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tohru Yamashita, Takuya Fujimoto, Ryo Mizojiri, Kazuko Yonemori, Hideki Hirose, Zenichi Ikeda, Ikuo Fujimori, Kyoko Toyofuku, Tsuneo Yasuma, Nobuyuki Matsunaga
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Publication number: 20140243302Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.Type: ApplicationFiled: June 26, 2012Publication date: August 28, 2014Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
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Publication number: 20140242135Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: April 25, 2012Publication date: August 28, 2014Applicant: Vanderbilt UniversityInventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
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Patent number: 8809329Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.Type: GrantFiled: July 31, 2008Date of Patent: August 19, 2014Assignees: Tokyo Metropolitan Institute of Medical Science, Renascience Co., Ltd.Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
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Publication number: 20140228320Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: April 15, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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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: 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: 20140228347Abstract: 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: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: IRM LLCInventors: Valentina MOLTENI, Hank Michael James PETRASSI, Xiaolin LI, Xiaodong LIU, Jon LOREN, Juliet NABAKKA, Bao NGUYEN, Vince YEH
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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: 8796271Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 11, 2011Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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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: 8791113Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: GrantFiled: May 31, 2011Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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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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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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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: 20140194462Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on ?7nAChR in a mammal by administering an effective amount of a compound of Formula I.Type: ApplicationFiled: October 8, 2013Publication date: July 10, 2014Applicant: Anvyl LLCInventor: Richard Kanner
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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