Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
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Publication number: 20140275026Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Le Wang, John Pratt, Lisa A. Hasvold, Dachun Liu, Yujia Dai, Steven D. Fidanze, James H. Holms, Robert A. Mantei, Keith F. McDaniel, George S. Sheppard, William J. McClellan
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Publication number: 20140275033Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
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Publication number: 20140275065Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
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Publication number: 20140275027Abstract: Disclosed are compounds of Formula (IIIa), wherein R1, R2, R3, X1, X2, X3, X4, X5, have any of the values defined therefore in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIIa).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Jianchun Gong, Zhi-Fu Tao, Thomas D. Penning, Andrew J. Souers, Yunsong Tong, Guidong Zhu
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Publication number: 20140275061Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
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Publication number: 20140275018Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: WOCKHARDT LIMITEDInventors: Mahesh Vithalbhai PATEL, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Snjeev Joshi
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Publication number: 20140275019Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHDInventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
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Patent number: 8835444Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).Type: GrantFiled: January 31, 2011Date of Patent: September 16, 2014Assignee: Novartis AGInventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
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Patent number: 8835455Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.Type: GrantFiled: May 24, 2013Date of Patent: September 16, 2014Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
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Patent number: 8835454Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group of: are useful as HIV attachment inhibitors.Type: GrantFiled: August 28, 2012Date of Patent: September 16, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhongxing Zhang, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20140256768Abstract: The present document describes novel compounds which may inhibit the activity of anti-apoptotic proteins such as Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases involving a defect in apoptosis, such as, for example, in the treatment of cancer.Type: ApplicationFiled: October 11, 2012Publication date: September 11, 2014Inventor: Zhaoyin Wang
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Publication number: 20140256658Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256707Abstract: The present invention provides compounds of Formula I or II, 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 channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: August 16, 2012Publication date: September 11, 2014Applicant: AMGEN INC.Inventors: Thomas Dineen, Isaac E. Marx, Hanh Nho Nguyen, Matthew Weiss
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Publication number: 20140256713Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: February 21, 2014Publication date: September 11, 2014Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin JOHNS, Eric Eugene BOROS, Takashi KAWASUJI, Cecilia S. KOBLE, Noriyuki KUROSE, Hitoshi MURAI, Ronald George SHERRILL, Jason Gordon WEATHERHEAD
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Publication number: 20140256666Abstract: The present invention describes single drug entities, formed by connecting an antibiotic moiety via a linker with a non-steroidal anti-inflammatory drug (NSAID) moiety. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual antibiotic and NSAID drug.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256705Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George S. Sheppard, Carol K. Wada, Kevin R. Woller
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Publication number: 20140256736Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Applicant: XENON PHARMACEUTICALS INC.Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
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Publication number: 20140255392Abstract: The present invention relates to substituted imidazopyridine compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: March 28, 2012Publication date: September 11, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Antje Margret Wengner, Roland Neuhaus, Gerhard Siemeister
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Publication number: 20140256734Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.Type: ApplicationFiled: March 10, 2014Publication date: September 11, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: John David Lawson, Mark Sabat, Nicholas Scorah, Christopher Smith, Phong H. Vu, Haixia Wang
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Publication number: 20140255517Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.Type: ApplicationFiled: March 5, 2014Publication date: September 11, 2014Applicant: EMORY UNIVERSITYInventors: Kerry J. Ressler, Paul J. Marvar
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Patent number: 8829199Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: GrantFiled: August 5, 2010Date of Patent: September 9, 2014Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AGInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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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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Patent number: 8829026Abstract: The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPMb8 receptor.Type: GrantFiled: October 3, 2011Date of Patent: September 9, 2014Assignee: RaQualia Pharma Inc.Inventors: Kiyoshi Kawamura, Yuji Shishido, Masashi Ohmi
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Publication number: 20140249177Abstract: The present invention provides novel solid forms of pharmaceutically active agents and therapeutic uses thereof. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: February 21, 2014Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Ian BRUCE, Sylvie CHAMOIN, Stephen Paul COLLINGWOOD, Pascal FURET, Vikki FURMINGER, Sarah LEWIS, Jon Christopher LOREN, Lin LV, Valentina MOLTEN, Alex Michael SAUNDERS, Duncan SHAW, Roy Maxwell TURNER, Vince YEH
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Publication number: 20140249138Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: February 18, 2014Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Publication number: 20140248240Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: September 4, 2014Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Judith D. Kuntz, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
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Publication number: 20140249178Abstract: Substituted perhydro pyrrolopyridines and methods for their use in the treatment of HIV infections, AIDS, and AIDS-related diseases, and in the treatment of BVDV infections are described herein. Also, pharmaceutical compositions comprising the substituted perhydro pyrrolopyridines are useful for the treatment of HIV infections, AIDS, and AIDS-related diseases. The compositions include one or more carriers, diluents, or excipients, or a combination thereof.Type: ApplicationFiled: August 23, 2012Publication date: September 4, 2014Applicant: NOVADRUG, LLCInventor: Eliezer Huberman
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Publication number: 20140249162Abstract: The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).Type: ApplicationFiled: May 15, 2014Publication date: September 4, 2014Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Jong Chan SON, Bong Jin KIM, Jae Hak KIM, Ill Young LEE, Chang Soo YUN, Sang Ho LEE, Chong Kgo LEE
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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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Patent number: 8822493Abstract: The present invention relates to SNS-595 and methods of treating cancer using the same.Type: GrantFiled: March 11, 2013Date of Patent: September 2, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Michelle Arkin, Jennifer Hyde, Duncan Walker, Jasmin Wright
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Patent number: 8822446Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: GrantFiled: April 14, 2011Date of Patent: September 2, 2014Assignee: AbbVie Inc.Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
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Patent number: 8822689Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.Type: GrantFiled: September 19, 2012Date of Patent: September 2, 2014Assignees: Merial Limited, Aventis AgricultureInventors: Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Robert Toms Jacobs
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Patent number: 8822467Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.Type: GrantFiled: December 14, 2012Date of Patent: September 2, 2014Assignee: Ligand Pharmaceuticals IncorporatedInventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
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Patent number: 8822494Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.Type: GrantFiled: November 5, 2013Date of Patent: September 2, 2014Assignee: Pfizer Inc.Inventors: Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Chakrapani Subramanyam, Lei Zhang
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Patent number: 8822460Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: April 4, 2013Date of Patent: September 2, 2014Assignee: Janssen Pharmaceutica NVInventors: Michael P. Winters, Nagy E. Fawzy, Fu-An Kang, Zhihua Sui
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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: 20140243366Abstract: 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: May 1, 2014Publication date: August 28, 2014Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20140243365Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.Type: ApplicationFiled: April 10, 2014Publication date: August 28, 2014Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Ryan Bremer
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Publication number: 20140243334Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d 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: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20140243348Abstract: Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed.Type: ApplicationFiled: January 22, 2014Publication date: August 28, 2014Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: David M. Knipe, Kevin Bryant, David H. Dreyfus
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Publication number: 20140243346Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.Type: ApplicationFiled: April 30, 2014Publication date: August 28, 2014Applicant: NOVARTIS AGInventors: Steven John CHARLTON, Catherine LEBLANC, Stephen Carl McKEOWN
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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: 8816085Abstract: The compounds of Formula (I), wherein R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.Type: GrantFiled: August 24, 2010Date of Patent: August 26, 2014Assignee: Takeda GmbHInventors: Josef Stadlwieser, Beate Schmidt, Heiko Bernsmann, Alexander Sudau, Torsten Dunkern, Ragna Hussong, Ewald Benediktus, Andreas Pahl
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Patent number: 8815892Abstract: The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.Type: GrantFiled: July 24, 2012Date of Patent: August 26, 2014Assignee: Affectis Pharmaceuticals AGInventor: Michael Bös
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Patent number: 8815893Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: January 10, 2011Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
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Patent number: 8815869Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: March 10, 2011Date of Patent: August 26, 2014Assignee: AbbVie Inc.Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
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Publication number: 20140235646Abstract: The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described.Type: ApplicationFiled: May 5, 2014Publication date: August 21, 2014Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
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Publication number: 20140235654Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.Type: ApplicationFiled: February 12, 2014Publication date: August 21, 2014Applicants: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Catherine GUILLOU, Frank KOZIELSKI, Christophe LABRIERE, Francoise GUERITTE, Sergey TCHERNIUK, Dimitrios SKOUFIAS, Claude THAL, Henri-Philippe HUSSON
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Publication number: 20140235647Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: September 27, 2012Publication date: August 21, 2014Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
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Publication number: 20140234254Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: February 15, 2014Publication date: August 21, 2014Applicants: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLCInventor: Ning Xi