The Other Cyclo In The Bicyclo Ring System Is Five-membered Patents (Class 544/280)
Ring nitrogen is shared by the two cyclos (Class 544/281)
  • PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS
    Publication number: 20130253193
    Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
    Type: Application
    Filed: February 7, 2013
    Publication date: September 26, 2013
    Applicant: Incyte Corporation
    Inventor: Jiacheng Zhou
  • PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS
    Publication number: 20130253190
    Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
    Type: Application
    Filed: February 7, 2013
    Publication date: September 26, 2013
    Applicant: Incyte Corporation
    Inventor: Jiacheng Zhou
  • PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS
    Publication number: 20130253191
    Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
    Type: Application
    Filed: February 7, 2013
    Publication date: September 26, 2013
    Applicant: Incyte Corporation
    Inventor: Jiacheng Zhou
  • Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
    Patent number: 8541425
    Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: September 24, 2013
    Assignee: Incyte Corporation
    Inventors: James D. Rodgers, Stacey Shepard, Jordan S. Fridman, Krishna Vaddi
  • Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
    Patent number: 8541427
    Abstract: In its many embodiments, the present invention provides certain 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds Formula (II): and include tautomers, steroisomers, or pharmaceutically acceptable salts or solvates of said compounds, stereoisomers, or said tautomers, wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's Disease, are also disclosed.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: September 24, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Andrew W. Stamford, Zhaoning Zhu, Mihirbaran Mandal, Yusheng Wu, Jared N. Cumming, Xiaoxiang Liu, Guoqing Li, Ulrich Iserloh
  • KINASE INHIBITORS
    Publication number: 20130237538
    Abstract: The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 12, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Clarence E. Hull, III, Thomas C. Malone
  • Enzyme inhibiting compounds
    Patent number: 8530653
    Abstract: The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: September 10, 2013
    Assignee: Chelsea Therapeutics, Inc.
    Inventor: Michael J. Roberts
  • Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
    Patent number: 8530485
    Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: September 10, 2013
    Assignee: Incyte Corporation
    Inventors: James D. Rodgers, Stacey Shepard
  • Triazinone and diazinone derivatives useful as HSP90 inhibitors
    Patent number: 8524712
    Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: March 24, 2008
    Date of Patent: September 3, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Chi-Wan Lee, Teresa Przewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
  • Pyrrolidine derivatives
    Patent number: 8524710
    Abstract: The invention relates to a compound of formula (I) wherein A1 to A4 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used, for example, as inhibitors of the cysteine protease cathepsin.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: September 3, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Banner, Uwe Grether, Wolfgang Haap, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Substituted N-(pyrazol-5-yl)-pyrrolo[3,2-D]pyrimidin-4-amine useful as protein kinase inhibitors
    Patent number: 8524720
    Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: January 4, 2010
    Date of Patent: September 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M.C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
  • AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS
    Publication number: 20130225556
    Abstract: The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Application
    Filed: March 29, 2013
    Publication date: August 29, 2013
    Applicant: Incyte Corporation
    Inventor: Incyte Corporation
  • BICYCLIC DIAMINES AS JANUS KINASE INHIBITORS
    Publication number: 20130225577
    Abstract: The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: October 17, 2011
    Publication date: August 29, 2013
    Inventors: David Joseph Guerin, Jason D. Brubaker, Michelle Martinez, Joon O. Jung, Neville J. Anthony, Mark E. Scott, Carolyn Michele Cammarano, Dawn Marie Mampreian Hoffman, Hyun Chong Woo, Christopher J. Dinsmore, Philip Jones
  • SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF
    Publication number: 20130217698
    Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
    Type: Application
    Filed: November 9, 2011
    Publication date: August 22, 2013
    Applicants: Astex Therapeutics LTD, Novartis AG
    Inventors: John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
  • ENHANCED TREATMENT REGIMENS USING MTOR INHIBITORS
    Publication number: 20130209543
    Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 15, 2013
    Applicant: Intellikine LLC
    Inventor: Intellikine LLC
  • Substituted fused imidazoles and pyrazoles and use thereof
    Publication number: 20130210824
    Abstract: The present application relates to novel substituted fused imidazoles and pyrazoles, 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 producing medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: January 8, 2013
    Publication date: August 15, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: BAYER INTELLECTUAL PROPERTY GMBH
  • PYRROLOPYRIMIDINE COMPOUNDS AND USES THEREOF
    Publication number: 20130210831
    Abstract: The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer.
    Type: Application
    Filed: August 18, 2011
    Publication date: August 15, 2013
    Inventors: Wei-Guo Su, Wei Deng, Jinshui Li, Jianguo Ji
  • Solid forms of pemetrexed
    Patent number: 8507508
    Abstract: There is provided polymorphs and amorphous form of pemetrexed or its pharmaceutical acceptable salts and process for making thereof.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: August 13, 2013
    Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.
    Inventors: Raghavendracharyulu Venkata Palle, Sekhar Munaswamy Nariyam, Vijay Bhailalbhai Patel, Raghupati Rama Subrahmanyam Vinjamuri, Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Venu Nalivela
  • Substituted pyrrolo[2,3-d]pyrimidines as LIM kinase 2 inhibitors
    Patent number: 8507672
    Abstract: Substituted pyrrolo[2,3-d]pyrimidine-based compounds useful as inhibitors of LIM kinase 2 are disclosed. Also disclosed are pharmaceutical compositions comprising the compounds and methods of their use to treat, manage and prevent inflammatory diseases and disorders, cancer, and diseases and disorders of the eye.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: August 13, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins, Dennis S. Rice, Michael Victor Voronkov, Yulian Zhang
  • SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES
    Publication number: 20130203786
    Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds 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: Application
    Filed: May 16, 2011
    Publication date: August 8, 2013
    Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
  • DEUTERATED PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6
    Publication number: 20130203765
    Abstract: The invention is directed to novel deuterated pyrrolopyrimidine compounds of formula (I) wherein R1 and R2 are defined below and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: February 17, 2011
    Publication date: August 8, 2013
    Applicant: Novartis AG
    Inventors: Christopher Thomas Brain, Lawrence Blas Perez
  • Useful pharmaceutical salts of 7-[(3R, 4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3, 5-dihydro-pyrrolo [3, 2-D] pyrimidin-4-one
    Patent number: 8501753
    Abstract: The present disclosure provides novel hemi- and mono-salts of 7-[(3R,4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3,5-dihydro-pyrrolo[3,2-d]pyrimidin-4-one (Compound 1) with various organic and inorganic acids. In one embodiment, the organic acid is a C4 organic diacids. The present disclosure further provides novel methods for preparing these salts. The novel monohydrates hemisalts of the C4 organic diacids are isostructural and can be prepared with different properties. Multiple acids can be used simultaneously and the proportion of acids can be varied offering the opportunity to select hemi-salts of compound 1 with desired properties.
    Type: Grant
    Filed: March 24, 2010
    Date of Patent: August 6, 2013
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Gary Bartley, Thomas Cleary, John Lang
  • HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS
    Publication number: 20130190320
    Abstract: 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: Application
    Filed: January 12, 2013
    Publication date: July 25, 2013
    Applicant: ACEA BIOSCIENCES, INC.
    Inventor: ACEA Biosciences, Inc.
  • SERINE/THREONINE KINASE INHIBITORS
    Publication number: 20130178486
    Abstract: Compounds having the formula I wherein A, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, Ra, Rb, X1, X2, X3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 11, 2013
    Applicant: Genentech, Inc.
    Inventor: Genentech, Inc.
  • Heteroaryl compounds useful as inhibitors of E1 activating enzymes
    Patent number: 8481550
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: August 24, 2011
    Date of Patent: July 9, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • RING-FUSED 4-AMINOPYRIMIDINES AND USE THEREOF AS STIMULATORS OF SOLUABLE GUANYLATE CYCLASES
    Publication number: 20130172372
    Abstract: The present application relates to novel fused 4-aminopyrimidines, 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 the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: July 5, 2011
    Publication date: July 4, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
  • PYRAZOLO[3,4-d]PYRIMIDINE AND PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20130172314
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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: Application
    Filed: September 14, 2012
    Publication date: July 4, 2013
    Applicant: Pharmacyclics, Inc.
    Inventors: Wei CHEN, David J. Loury
  • HETEROCYCLIC FLAVIVIRIDAE VIRUS INHIBITORS
    Publication number: 20130171102
    Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: May 20, 2011
    Publication date: July 4, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor
  • Benzoxazole kinase inhibitors and methods of use
    Patent number: 8476282
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of using such compounds or compositions, and methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications such as treatment of cancer.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: July 2, 2013
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
  • Benzoxazole kinase inhibitors and methods of use
    Patent number: 8476431
    Abstract: The present invention provides chemical entities, compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of making such compounds or compositions, and methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications such as treatment of cancer.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: July 2, 2013
    Assignee: Itellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
  • FUSED BICYCLIC mTOR INHIBITORS
    Publication number: 20130165651
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 27, 2013
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
  • INHIBITORS OF E1 ACTIVATING ENZYMES
    Publication number: 20130165457
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: June 19, 2012
    Publication date: June 27, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Steven P. Langston, Edward J. Olhava, Stepan Vyskocil
  • 1,4-SUBSTITUTED PIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20130164259
    Abstract: The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 27, 2013
    Inventors: Cliff C. Cheng, Xiaohua Huang, Gerald W. Shipps, JR.
  • PROCESSES FOR PREPARING PEMETREXED
    Publication number: 20130165654
    Abstract: The present invention relates to pemetrexed disodium substantially free from specific process-related impurities, and processes for the preparation thereof.
    Type: Application
    Filed: February 13, 2012
    Publication date: June 27, 2013
    Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES LTD.
    Inventors: Rajasekhar Kadaboina, Sekhar Munaswamy Nariyam, Veerender Murki, Amarendhar Manda, Raghupati Rama Vinjamuri, Nageshwar Gunda
  • Inhibitors of VEGF receptor and HGF receptor signalling
    Patent number: 8470850
    Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: June 25, 2013
    Assignee: MethylGene Inc.
    Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
  • TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS
    Publication number: 20130157996
    Abstract: Compounds of Formula I are useful as antagonists 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: Application
    Filed: June 21, 2012
    Publication date: June 20, 2013
    Applicant: Amgen Inc.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • DIAZAINDOLE INHIBITORS OF CRAC
    Publication number: 20130158040
    Abstract: Disclosed are compounds of Formula (I): useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.
    Type: Application
    Filed: December 17, 2012
    Publication date: June 20, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • (aza)indole derivative and use thereof for medical purposes
    Patent number: 8466152
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: June 18, 2013
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6
    Publication number: 20130150342
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: February 17, 2011
    Publication date: June 13, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas Brain, Young Shin Cho, John William Giraldes, Bharat Lagu, Julian Roy Levell, Michael J. Luzzio, Lawrence Blas Perez, Yaping Wang, Fan Yang
  • 2-Substituted phenyl-5,7-dihydrocarbyl-3,7-dihydropyrrolo[2,3-d] pyrimidin-4-one derivatives, the preparation and the pharmaceutical use thereof
    Patent number: 8461165
    Abstract: The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: June 11, 2013
    Assignees: Yangtze River Pharmaceutical (Group) Co., Ltd, Tianjin North Pharma Sci-Tech Co., Ltd
    Inventors: Yongfeng Wang, Kejun Zhao
  • Pyrrolopyrimidinedione and its therapeutic use
    Patent number: 8455505
    Abstract: The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: June 4, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Christine Edwards, Janus Kulagowski, Harry Finch
  • Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith
    Publication number: 20130137709
    Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.
    Type: Application
    Filed: May 5, 2011
    Publication date: May 30, 2013
    Inventors: Nathanael S. Gray, Wenjun Zhou
  • HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
    Publication number: 20130137681
    Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
    Type: Application
    Filed: January 30, 2013
    Publication date: May 30, 2013
    Applicant: INCYTE CORPORATION
    Inventor: INCYTE CORPORATION
  • Benzoxazole kinase inhibitors and methods of use
    Patent number: 8450329
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of using such compounds or compositions, and methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications such as treatment of cancer.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: May 28, 2013
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
  • Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
    Patent number: 8450331
    Abstract: In its many embodiments, the present invention provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's Disease, are also disclosed.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: May 28, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, Andrew Stamford, Mihirbaran Mandal, Xiaoxiang Liu
  • Benzoxazole kinase inhibitors and methods of use
    Patent number: 8450480
    Abstract: The present invention provides chemical entities, compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of making such compounds or compositions, and methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications such as treatment of cancer.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: May 28, 2013
    Assignee: Itellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
  • Substituted 7-carboxamido-pyrrolo[3,2-d]pyrimidines
    Patent number: 8445501
    Abstract: The compounds of Formula (I), in which R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: May 21, 2013
    Assignee: Takeda GmbH
    Inventors: Josef Stadlwieser, Beate Schmidt, Heiko Bernsmann, Alexander Sudau, Torsten Dunkern, Degenhard Marx, Jörg Diefenbach
  • HETEROCYCLIC COMPOUNDS USEFUL FOR KINASE INHIBITION
    Publication number: 20130123284
    Abstract: Provided herein are compounds useful for kinase inhibition.
    Type: Application
    Filed: March 24, 2011
    Publication date: May 16, 2013
    Applicant: AMITECH THERAPEUTIC SOLUTIONS INC
    Inventors: Lee Daniel Arnold, Eric A. Murphy
  • Fused heteroaromatic pyrrolidinones
    Patent number: 8440689
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: May 14, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yasuyoshi Arikawa, Qing Dong, Victoria Feher, Benjamin Jones, Betty Lam, Zhe Nie, Christopher Smith, Masashi Takahashi
  • FUSED HETEROAROMATIC PYRROLIDINONES AS SYK INHIBITORS
    Publication number: 20130116260
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.
    Type: Application
    Filed: December 17, 2010
    Publication date: May 9, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yasuyoshi Arikawa, Benjamin Jones, Betty Lam, Zhe Nie, Christopher Smith, Masashi Takahashi, Qing Dong, Victoria Feher