The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
-
Patent number: 8759361Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: August 22, 2011Date of Patent: June 24, 2014Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
-
Publication number: 20140170110Abstract: Compounds having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: May 21, 2012Publication date: June 19, 2014Applicant: ALMIRALL, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach Taña
-
Publication number: 20140155394Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: June 21, 2013Publication date: June 5, 2014Applicant: Astrazeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
-
Publication number: 20140148433Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: August 31, 2011Publication date: May 29, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
-
Publication number: 20140142113Abstract: A method of treating inflammatory diseases with Adenosine 2B receptor antagonists in particular with xanthine derived inhibitors. The method involves supplying a therapeutically active amount of the compounds of FIG. 1 and in particular compound 1.Type: ApplicationFiled: November 11, 2013Publication date: May 22, 2014Inventors: Michael W. Burnet, Thomas Stohr, Martin Donsbach
-
Publication number: 20140135301Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 22, 2014Publication date: May 15, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
-
Publication number: 20140128389Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: October 15, 2010Publication date: May 8, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Randall L. Halcomb, Paul A. Roethle
-
Publication number: 20140120083Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating cancers or hematologic disorders.Type: ApplicationFiled: March 15, 2013Publication date: May 1, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Howard M. STERN, Jeffery L. KUTOK
-
Publication number: 20140120060Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating rheumatoid arthritis or asthma.Type: ApplicationFiled: March 15, 2013Publication date: May 1, 2014Applicant: INFINITY PHARMACEUTICALS, INC.Inventors: Vito J. Palombella, Jeffrey L. Kutok
-
Patent number: 8703777Abstract: Provided herein are substituted bicyclic compounds, e.g., compounds of Formula IV, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for inhibiting phosphatidyl inositol-3 kinase (PI3 kinase), e.g., for the treatment of various diseases and conditions associated with PI3 kinase activity, including but not limited to, cancer, inflammatory disease, immune disease, and respiratory disease.Type: GrantFiled: January 5, 2009Date of Patent: April 22, 2014Assignee: Intellikine LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Katrina Chan, Christian Rommel, Liansheng Li
-
Patent number: 8703754Abstract: The present invention relates to a compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: GrantFiled: February 8, 2011Date of Patent: April 22, 2014Assignee: GlaxoSmithKline LLCInventors: Robert Hermann Gibbon, Amanda Lucas, Stephen Andrew Hermitage
-
Publication number: 20140107098Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
-
Publication number: 20140100224Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: June 26, 2013Publication date: April 10, 2014Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of CaliforniaInventors: Frank M. Longo, Stephen M. Massa
-
Publication number: 20140100237Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: October 1, 2013Publication date: April 10, 2014Applicant: ChemoCentryx, Inc.Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
-
Publication number: 20140088099Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: November 20, 2013Publication date: March 27, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Pingda REN, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
-
Patent number: 8680076Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.Type: GrantFiled: October 20, 2011Date of Patent: March 25, 2014Assignee: Signal Pharmaceuticals, LLCInventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
-
Publication number: 20140057901Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: February 21, 2013Publication date: February 27, 2014Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
-
Publication number: 20140045825Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: Exelixis, Inc.Inventor: James William Leahy
-
Publication number: 20140031355Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: ApplicationFiled: November 4, 2011Publication date: January 30, 2014Applicant: Amgen Inc.Inventor: Amy Kaizerman
-
Patent number: 8637530Abstract: The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.Type: GrantFiled: January 9, 2012Date of Patent: January 28, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Peter Sieger
-
Patent number: 8637527Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: September 12, 2012Date of Patent: January 28, 2014Assignee: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
-
Publication number: 20140024664Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH2)n— moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: September 20, 2013Publication date: January 23, 2014Applicant: GlaxoSmithKline LLCInventors: Helene Bazin-Lee, Diane Mary Coe, Charlotte Jane Mitchell, Stephen Allan Smith
-
Publication number: 20140018344Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 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 immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.Type: ApplicationFiled: July 8, 2013Publication date: January 16, 2014Inventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
-
Publication number: 20140005198Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: August 28, 2013Publication date: January 2, 2014Applicant: AMGEN INC.Inventors: Adrian L. SMITH, Elizabeth M. DOHERTY, Qi HUANG, Gang LIU
-
Publication number: 20140005164Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: March 23, 2012Publication date: January 2, 2014Applicant: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
-
Patent number: 8618135Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.Type: GrantFiled: March 11, 2011Date of Patent: December 31, 2013Assignee: The Trustees of the University of PennsylvaniaInventor: Daniel J. Rader
-
Publication number: 20130344061Abstract: 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: ApplicationFiled: March 15, 2013Publication date: December 26, 2013Applicant: INFINITY PHARMACEUTICALS, INC.Inventors: Vito J. PALOMBELLA, David G. WINKLER
-
Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
-
Publication number: 20130345216Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 20, 2013Publication date: December 26, 2013Applicant: INTELLIKINE LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
-
Publication number: 20130338174Abstract: The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.Type: ApplicationFiled: December 14, 2011Publication date: December 19, 2013Inventors: Phillip Abbott, Roger Victor Bonnert, Thomas Mcinally, Stephen Thom, Hiroki Wada, Satoshi Onuma
-
Patent number: 8604032Abstract: Provided herein are compounds of formula (I), pharmaceutical compositions comprising the compounds, and methods of use thereof The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including diseases and conditions associated with PI3 kinase activity.Type: GrantFiled: May 20, 2011Date of Patent: December 10, 2013Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
-
Publication number: 20130324562Abstract: The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: March 1, 2012Publication date: December 5, 2013Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
-
Publication number: 20130317023Abstract: A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like.Type: ApplicationFiled: November 25, 2011Publication date: November 28, 2013Applicant: YOUAI CO., LTD.Inventors: Eun Kyong Shim, Nam Doo Kim, Tae Bo Shim, Seung Yong Kim
-
Patent number: 8592581Abstract: The present invention relates to compounds of formula (I) wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl or cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and each R9 is other than H. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula (I), and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.Type: GrantFiled: October 5, 2009Date of Patent: November 26, 2013Assignees: Cyclacel Limited, Cancer Research Technology LimitedInventors: Peter William Sheldrake, Butrus Atrash, Simon Green, Edward McDonald, Sheelagh Frame
-
Publication number: 20130310398Abstract: Combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.Type: ApplicationFiled: July 24, 2013Publication date: November 21, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael MARK, Peter EICKELMANN, Gerd LUIPPOLD, Leo THOMAS
-
Patent number: 8586566Abstract: This invention relates to specific compounds and their pharmaceutically acceptable salts of the general formula: wherein Q is —CR?CR?— and Ring A is an aryl, heteroaryl or heterocyclic ring or ring system. This invention also relates to pharmaceutical compositions comprising such specific compounds or their pharmaceutically acceptable salts and a pharmaceutically acceptable carrier or adjuvant.Type: GrantFiled: December 5, 2011Date of Patent: November 19, 2013Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
-
Patent number: 8586739Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: GrantFiled: May 10, 2012Date of Patent: November 19, 2013Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
-
Publication number: 20130296333Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: July 9, 2013Publication date: November 7, 2013Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
-
Patent number: 8575182Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts of the general formula are provided wherein R6 and R9 are as defined in the specification. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for treating mammalian cells, and especially human skin cells, in order to ameliorate the adverse effects of aging, treat skin disease states, treat immunological responses resulting from or associated with inflammation, and the like.Type: GrantFiled: May 26, 2011Date of Patent: November 5, 2013Assignee: Institute of Experimental Botany, Academy of Sciences of the Czeck RepublicInventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
-
Patent number: 8575340Abstract: The present invention relates to compounds of formula (I): wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.Type: GrantFiled: February 8, 2011Date of Patent: November 5, 2013Assignee: GlaxoSmithKline LLCInventors: Helene Bazin-Lee, Diane Mary Coe, David A. Johnson, Charlotte Jane Mitchell
-
Publication number: 20130289015Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.Type: ApplicationFiled: June 28, 2013Publication date: October 31, 2013Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio Rodriguez Escrich, Maria Cristina Sicre Gonzalez
-
Publication number: 20130281517Abstract: Cyclopropanecarboxylate esters of purine analogues, method of making and using the same for treating herpes virus infections and tumors are disclosed.Type: ApplicationFiled: April 2, 2013Publication date: October 24, 2013Inventors: Ji-Wang CHERN, Shin-yu LAI, Pei-Teh CHANG
-
Patent number: 8563570Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: January 20, 2012Date of Patent: October 22, 2013Assignee: Incyte CorporationInventors: Wenqing Yao, Chunhong He, David M. Burns, Jincong Zhuo, Meizhong Xu, Colin Zhang, Ding-Quan Qian, Brian Metcalf
-
Patent number: 8557830Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: June 5, 2008Date of Patent: October 15, 2013Assignee: Amgen Inc.Inventors: Adrian L. Smith, Elizabeth M. Doherty, Qi Huang, Gang Liu
-
Publication number: 20130267526Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoblType: ApplicationFiled: December 16, 2011Publication date: October 10, 2013Applicant: Amgen, Inc.Inventors: Yi Chen, Timothy David Cushing, Benjamin Fisher, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Youngsook Shin
-
Patent number: 8524777Abstract: A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.Type: GrantFiled: July 17, 2012Date of Patent: September 3, 2013Assignee: Allergan Inc.Inventors: Chin-Ming Chang, James N. Chang, Rhett M. Schiffman, R. Scott Jordan, Joan-En Chang-Lin
-
Publication number: 20130225487Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).Type: ApplicationFiled: March 12, 2013Publication date: August 29, 2013Applicant: Pfizer Inc.Inventor: Pfizer Inc.
-
Patent number: 8507491Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: GrantFiled: August 24, 2009Date of Patent: August 13, 2013Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
-
Publication number: 20130197014Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: April 30, 2012Publication date: August 1, 2013Applicant: Pharmacyclics, Inc.Inventors: Wei CHEN, David J. LOURY
-
Publication number: 20130190320Abstract: The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: ApplicationFiled: January 12, 2013Publication date: July 25, 2013Applicant: ACEA BIOSCIENCES, INC.Inventor: ACEA Biosciences, Inc.