Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Bicyclo Ring System Patents (Class 546/120)
  • Patent number: 9718779
    Abstract: The present invention provides a novel intermediate as well as novel polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide compound represented by the following structural formula-1 and processes for their preparation.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: August 1, 2017
    Assignee: MSN Laboratories Limited
    Inventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Mummadi Venkatesh
  • Patent number: 9056858
    Abstract: Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1, X and G are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: June 16, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Daniel Kuzmich, Can Mao, Hossein Razavi
  • Publication number: 20150148374
    Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Publication number: 20150148349
    Abstract: The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Publication number: 20150141455
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 21, 2015
    Applicant: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Patent number: 9034897
    Abstract: The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: May 19, 2015
    Assignee: SANOFI
    Inventors: Laurent Bialy, Josef Pernerstorfer, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150099709
    Abstract: The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.
    Type: Application
    Filed: May 27, 2013
    Publication date: April 9, 2015
    Inventors: Nobuyuki Takahashi, Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Publication number: 20150065477
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 5, 2015
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
  • Publication number: 20150065482
    Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: GENENTECH, INC.
    Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
  • Publication number: 20150065483
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 8969561
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: March 3, 2015
    Assignee: Dipharma Francis S.r.l.
    Inventors: Emanuele Attolino, Alessandro Lombardo, Simone Tambini
  • Patent number: 8962620
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: February 24, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 8957211
    Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 17, 2015
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Publication number: 20150045327
    Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 12, 2015
    Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
  • Patent number: 8946445
    Abstract: 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: Grant
    Filed: October 11, 2012
    Date of Patent: February 3, 2015
    Assignee: Nanjing Allgen Pharma Co., Ltd.
    Inventor: Zhaoyin Wang
  • Publication number: 20150025242
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 22, 2015
    Applicant: DIPHARMA FRANCIS S.r.l.
    Inventors: Emanuele ATTOLINO, Alessandro LOMBARDO, Simone TAMBINI
  • Publication number: 20150018388
    Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
    Type: Application
    Filed: December 11, 2013
    Publication date: January 15, 2015
    Inventors: Richard B. Silverman, Yinan Zhang
  • Publication number: 20150018386
    Abstract: The present invention discloses an amorphous form of apixaban, process of preparation and compositions thereof.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 15, 2015
    Inventors: Shriprakash Dhar Dwivedi, Kamlesh Kumar Singh, Jitendra Maganbhai Gajera, Nitin Tandon, Digambar Ware
  • Publication number: 20150011579
    Abstract: The invention relates to novel heterocyclic compounds which are pyrazolopyridine derivatives that induce fibroblast growth factor receptor (FGFR) dimerization, having the general formula: M1-L-M2 in which M1 or M2, which may be identical or different, each represent, independently of one another, a monomer unit M and L represents a linker group which links M1 and M2 covalently with the monomer unit which follows: Process for the preparation thereof and therapeutic use thereof.
    Type: Application
    Filed: December 26, 2012
    Publication date: January 8, 2015
    Inventors: Marie-Line Clary-Ceccato, Nathalie Guillo
  • Publication number: 20140378686
    Abstract: The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
    Type: Application
    Filed: September 12, 2011
    Publication date: December 25, 2014
    Applicant: SANOFI
    Inventors: Laurent Bialy, Josef Pernerstorfer, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Publication number: 20140357633
    Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.
    Type: Application
    Filed: December 12, 2012
    Publication date: December 4, 2014
    Inventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
  • Publication number: 20140350006
    Abstract: The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 27, 2014
    Inventors: Chantal Alcouffe, Kirsten Bjegarde, Jacques Mauger
  • Publication number: 20140350260
    Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and/or a superior ?-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Inventors: Tatsuki KOIKE, Minoru Nakamura, Yoshihide Tomata, Takafumi Takai, Yasutaka Hoashi, Yuichi Kajita, Tetsuya Tsukamoto, Makoto Kamata
  • Publication number: 20140343056
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: November 20, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Dominic Suarez, Xinrong Tian, Sharad Kumar Verma
  • Publication number: 20140336385
    Abstract: Provided herein are organic compounds useful in a variety of OLED applications.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 13, 2014
    Inventors: Ivan Abrahamian, Xin Su
  • Publication number: 20140335178
    Abstract: The present invention relates to a Factor Xa inhibitor dosage form comprising apixaban in a solubility-improved form wherein the dosage form provides controlled release of apixaban and methods for preventing or treating venous thromboembolisms, deep vein thrombosis and acute coronary syndrome with said dosage form.
    Type: Application
    Filed: May 19, 2014
    Publication date: November 13, 2014
    Applicants: BRISTOL-MYERS SQUIBB COMPANY, PFIZER INC.
    Inventor: Richard G. Nause
  • Patent number: 8884016
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: November 11, 2014
    Assignee: Dipharma Francis S.r.l.
    Inventor: Chiara Vladiskovic
  • Publication number: 20140330009
    Abstract: The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
    Type: Application
    Filed: September 16, 2011
    Publication date: November 6, 2014
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler, Josef Pernerstorfer, Joachim Brendel
  • Patent number: 8871786
    Abstract: Disclosed are CCR1 inhibitor compounds of the formula (I): which are useful in the treatment of autoimmune and other diseases. Also disclosed a pharmaceutical compositions containing the same, and methods of making and using same.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: October 28, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: John D. Huber
  • Patent number: 8846712
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4 and R5 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: September 30, 2014
    Assignee: Sanofi
    Inventors: Matthias Loehn, Maria Mendez-Perez, Stefania Pfeiffer-Marek, Aimo Kannt, Guillaume Begis, Olivier Duclos, Federic Jeannot
  • Patent number: 8841462
    Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: September 23, 2014
    Inventors: Robert A. Heald, Philip Jackson, Joseph P. Lyssikatos, Stephen Price, Pascal Pierre Alexandre Savy
  • Patent number: 8829190
    Abstract: The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH2, CH2—CH2, CH2—NH, or NH; R1 is halogen, or R1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkyl, alkoxycarbonyl, aryl, all of which are optionally substituted; R2 is hydrogen, or R2 is alkyl, cycloalkyl, alkoxy, heterocycloalkyl, aryl, heteroaryl, alkoxycarbonyl, aminocarbonyl, amino, all of which are optionally substituted; A is aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocycloalkyl or heterocycloalkenyl, all of which are optionally substituted; and pharmaceutically acceptable salts, hydrates, or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments, in particular for the treatment of dermal diseases.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: September 9, 2014
    Assignee: Leo Pharma A/S
    Inventors: Jakob Felding, Morten Dahl Sørensen
  • Publication number: 20140206679
    Abstract: The present invention relates to a heterocyclic pyridone compound represented by General Formula (I), where the heterocyclic pyridone compound is used as a tyrosine kinase inhibitor, and particularly a c-Met inhibitor. The present invention also relates to intermediates for preparing heterocyclic pyridone compound and a preparation method. The present invention further relates to a pharmaceutical composition containing the heterocyclic pyridone compound as an active ingredient, and a use of the pharmaceutical composition in treatment of diseases associated with tyrosine kinase c-Met, especially cancer associated with c-Met, as a medicament.
    Type: Application
    Filed: May 28, 2012
    Publication date: July 24, 2014
    Applicant: SHANGHAI HUILUN LIFE SCIENCE & TECHNOLOGY CO., LTD
    Inventors: Jianjun Cheng, Jihong Qin, Bin Ye
  • Publication number: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Patent number: 8686150
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: April 1, 2014
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Oliver Plettenburg, Christian Schoenau, Matthias Loehn, Stefania Pfeiffer-Marek, Maria Mendez-Perez, Aimo Kannt, Juergen Dedio, Markus Kohlmann, Alexander Schiffer, Guillaume Begis, Olivier Duclos, Frederic Jeannot
  • Patent number: 8685967
    Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ginny D. Ho, Elizabeth M. Smith, Eugenia Y. Kiselgof, Kallol Basu, Zheng Tan, Brian McKittrick, Deen Tulshian
  • Publication number: 20140058107
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Application
    Filed: June 7, 2012
    Publication date: February 27, 2014
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Chiara Vladiskovic, Emanuele Attolino, Alessandro Lombardo, Simone Tambini
  • Publication number: 20140057937
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: August 27, 2013
    Publication date: February 27, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Yandong Li, Jay P. Powers, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Publication number: 20140057891
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 8653260
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • Publication number: 20140038942
    Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
    Type: Application
    Filed: February 10, 2012
    Publication date: February 6, 2014
    Applicants: Merck Sharp & Dohme B.V., Merck Sharp & Dohme Corp.
    Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
  • Publication number: 20140030330
    Abstract: The present invention relates to a Factor Xa inhibitor dosage form comprising apixaban in a solubility-improved form wherein the dosage form provides controlled release of apixaban and methods for preventing or treating venous thromboembolisms, deep vein thrombosis and acute coronary syndrome with said dosage form.
    Type: Application
    Filed: July 2, 2013
    Publication date: January 30, 2014
    Inventor: Richard G. Nause
  • Patent number: 8637509
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: January 28, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
  • Publication number: 20140005221
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 2, 2014
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Publication number: 20130296307
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: July 10, 2013
    Publication date: November 7, 2013
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Publication number: 20130245267
    Abstract: The present application relate to amorphous form of Apixaban useful in making pharmaceutically acceptable dosage forms, and to processes for their preparation.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 19, 2013
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Subba Reddy Peddi Reddy, Md Arshad Alam
  • Publication number: 20130231321
    Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.
    Type: Application
    Filed: April 16, 2013
    Publication date: September 5, 2013
    Applicant: H. LUNDBECK A/S
    Inventors: Mathivanan Packiarajan, Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Michel Grenon
  • Publication number: 20130211090
    Abstract: The present invention relates to a process for preparing 5-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile of the formula (I) which serves as a synthesis intermediate for production of medicaments, especially for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: August 31, 2011
    Publication date: August 15, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Jens Ackerstaff