Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/316)
The nitrogen is bonded directly at 4- or 6-position (Class 544/317)
  • OXAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH
    Publication number: 20130018048
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: April 4, 2011
    Publication date: January 17, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
  • New Positive allosteric modulators of nicotinic acetylcholine receptor
    Publication number: 20130012530
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide
    Patent number: 8343984
    Abstract: Polymorphic forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: January 1, 2013
    Assignees: Novartis AG, Novartis Pharma GmbH
    Inventors: Paul W Manley, Wen-Chung Shieh, Paul Allen Sutton, Piotr “Peter” H Karpinski, Raeann Wu, Stéphanie M. Monnier, Jörg Brozio
  • AMINO-TETRAZOLES ANALOGUES AND METHODS OF USE
    Publication number: 20120329772
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Application
    Filed: July 9, 2012
    Publication date: December 27, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biqin C. Li
  • METALLOENZYME INHIBITOR COMPOUNDS
    Publication number: 20120329788
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: June 19, 2012
    Publication date: December 27, 2012
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • Pyridones useful as inhibitors of kinases
    Patent number: 8338597
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: December 25, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, Sharn Ramaya, Juan-Miguel Jimenez, Alistair Rutherford
  • Compounds, pharmaceutical compositions and uses thereof
    Publication number: 20120322784
    Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE
  • Pyrimidine compounds and methods of making and using same
    Patent number: 8334292
    Abstract: Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: December 18, 2012
    Assignee: Cystic Fibrosis Foundation Therapeutics, Inc.
    Inventor: Phoebe Chiang
  • 5-CYANO-4- (PYRROLO [2,3B] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
    Publication number: 20120309963
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: May 22, 2012
    Publication date: December 6, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Stephen Clinton Young, Simon Robert Lorrie Everitt, Ronald Knegtel, Joanne Louise Pinder, Alistair Peter Rutherford, Steven Durrant, Guy Brenchley, Jean-Damien Charrier, Michael O'Donnell
  • CYCLIC AMINE COMPOUND AND ACARICIDE
    Publication number: 20120309964
    Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.
    Type: Application
    Filed: February 24, 2011
    Publication date: December 6, 2012
    Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
  • CYTOCHROME P450 OXIDASE INHIBITORS AND USES THEREOF
    Publication number: 20120309762
    Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 6, 2012
    Applicant: Abbott Laboratories
    Inventors: Larry L. Klein, Hui-Ju Chen, Ming C. Yeung, Charles A. Flentge, John T. Randolph, Peggy P. Huang, Douglas K. Hutchinson, Dale J. Kempf
  • 4-azetidinyl-1-heteroatom linked-cyclohexane antagonists of CCR2
    Patent number: 8324186
    Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: December 4, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Zhihua Sui
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 8324384
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: February 3, 2010
    Date of Patent: December 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
  • Pyrimidinones as casein kinase II (CK2) modulators
    Patent number: 8324231
    Abstract: A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways.
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: December 4, 2012
    Assignee: Exelixis, Inc.
    Inventors: Elena S. Koltun, Patrick Kearney, Naing Aay, Arlyn Arcalas, Wai Ki Vicky Chan, Jeffry Kimo Curtis, Hongwang Du, Ping Huang, Brian Kane, Moon Hwan Kim, Michael Pack, Amy L. Tsuhako, Wei Xu, Cristiana A. Zaharia, Peiwen Zhou
  • Substituted isoxazoline compound and pest control agent
    Patent number: 8318757
    Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted isoxazoline compound of General Formula (1): where A1, A2 and A3 independently are CH or N, etc., X1, X2 and X3 are independently are H, a halogen atom, etc., Y1 is H, etc., R1 is —C(O)R1a, —C(S)R1a, R1a is —C(R9)(R9a)—S(O)rR10, —C(R9)(R9a)—S(O)t(R10)?NR11, etc., R2 is H, etc., R3 is CF3, CClF2, etc., R4 is H, etc., R9 is H, etc., R9a is H, etc., R10 is C1-2 alkyl, etc., R11 is H, etc., r is an integer of 0-2, t is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: November 27, 2012
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Kazushige Maeda, Youko Yamada, Eitatsu Ikeda, Ken-ichi Toyama, Mitsuaki Komoda
  • Tricyclic Derivatives and Their Pharmaceutical Use and Compositions
    Publication number: 20120295882
    Abstract: This application relates to tricyclic compounds of Formula I: including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula I and uses therefore.
    Type: Application
    Filed: June 21, 2012
    Publication date: November 22, 2012
    Applicant: Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Derek D. Dunn, Greg A. Hostetler, Robert J. McHugh, George C. Morton, Gerard C. Rosse, Joseph M. Salvino, Babu G. Sundar, Rabindranath Tripathy
  • CERTAIN HETEROCYCLES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE
    Publication number: 20120289698
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: November 15, 2012
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • IMIDAZOLIDINEDIONE DERIVATIVES
    Publication number: 20120289526
    Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.
    Type: Application
    Filed: December 6, 2010
    Publication date: November 15, 2012
    Inventors: Giuseppe Alvaro, Anne Décor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
  • THIAZOLYL MGLUR5 ANTAGONISTS AND METHODS FOR THEIR USE
    Publication number: 20120289696
    Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
    Type: Application
    Filed: July 26, 2012
    Publication date: November 15, 2012
    Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
  • Oxazolidinones as Modulators of MGLUR5
    Publication number: 20120283264
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: November 2, 2011
    Publication date: November 8, 2012
    Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
  • NOVEL 3-HYDROXYISOTHIAZOLE 1-OXIDE DERIVATIVE
    Publication number: 20120277150
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Application
    Filed: April 11, 2012
    Publication date: November 1, 2012
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventor: Munetaka OHKOUCHI
  • Pyrimidine derivatives
    Patent number: 8299086
    Abstract: The invention relates to novel pyrimidine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: October 30, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
  • Crystalline forms of 2-(2-flouro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide
    Patent number: 8299076
    Abstract: Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: October 30, 2012
    Assignees: Array Biopharma Inc., Astrazeneca AB
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, Jim Blake, Richard Anthony Storey, Rebecca Jane Booth, John David Pittam, John Leonard, Mark Richard Fielding
  • Arginine Derivatives with NP-I Antagonistic Activity
    Publication number: 20120269864
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
  • NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME
    Publication number: 20120258978
    Abstract: Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, or an amino group; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, or —CO—; and Q is a hydrogen atom or a phenyl group.
    Type: Application
    Filed: May 29, 2012
    Publication date: October 11, 2012
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Naohiro TAKEMOTO, Kenji MURATA, Norihito MURAYAMA, Chikaomi YAMADA
  • Substituted Aminobutyric Derivatives as Neprilysin Inhibitors
    Publication number: 20120252830
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to 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 7, 2012
    Publication date: October 4, 2012
    Applicant: NOVARTIS AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
    Patent number: 8278316
    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 2, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Saleem Ahmad
  • TRPV3 Modulators
    Publication number: 20120245124
    Abstract: Disclosed herein are modulators of TRPV3 of formula (I) wherein X1, X2, R1, R2, Rx, and n are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Application
    Filed: March 23, 2012
    Publication date: September 27, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Bruce Clapham, Phil B. Cox, Michael J. Dart, Arthur Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark Matulenko, Robert G. Schmidt, Clara I. Villamil, Eric A. Voight, Kevin R. Woller
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20120245174
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
  • New Compounds 806
    Publication number: 20120238579
    Abstract: The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.
    Type: Application
    Filed: March 23, 2012
    Publication date: September 20, 2012
    Inventors: Yevgeni Besidki, Inger Kers, Martin Nylôf, Lars Sandberg, Karin Skogholm
  • 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
    Publication number: 20120232071
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • NOVEL SULFONAMIDES AS L-CPT1 INHIBITORS
    Publication number: 20120232104
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Urotensin II receptor antagonists
    Patent number: 8258301
    Abstract: Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, W, and Y are as described herein, or a tautomer, prodrug, solvate, or salt thereof. These compounds are useful as inhibitors of Urotensin II and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the interaction of Urotensin II with its receptor, including cardiovascular diseases. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds, and intermediates useful in these processes.
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: September 4, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Anne Bettina Eldrup, Ingo Andreas Mugge, Fariba Soleymanzadeh, Sanxing Sun, Yunlong Zhang
  • SUBSTITUTED BIARYL DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20120220614
    Abstract: The present invention relates to Substituted Biaryl Derivatives, compositions comprising a Substituted Biaryl Derivative, and methods of using the Substituted Biaryl Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Application
    Filed: November 16, 2010
    Publication date: August 30, 2012
    Inventors: Craig D. Boyle, Claire M. Lankin, William J. Greenlee, Joel M. Harris
  • AZA-BICYCLOALKYL ETHERS AND THEIR USE AS ALPHA7-NACHR AGONISTS
    Publication number: 20120220599
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 2, 2012
    Publication date: August 30, 2012
    Inventors: Dominik FEUERBACH, Konstanze HURTH, Timothy John RITCHIE
  • Novel Dihydropyrimidin-2(1H)-one Compounds as S-Nitrosoglutathione Reductase Inhibitors
    Publication number: 20120208817
    Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: September 24, 2010
    Publication date: August 16, 2012
    Applicant: N30 PHARMACEUTICALS, LLC
    Inventors: Xicheng Sun, Jian Qiu
  • Process and catalyst
    Patent number: 8242044
    Abstract: Aromatic or heteroaromatic nitro compounds are catalytically hydrogenated to the corresponding amines in the presence of a platinum catalyst comprising elemental platinum on a support; the platinum catalyst is modified with a molybdenum compound and a phosphorus compound wherein the phosphorus has an oxidation state of less than +5, e.g. hypophosphorous acid; the catalyst is particularly useful in the hydrogenation of nitro compounds with halogen and/or sulfur-containing substituents.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: August 14, 2012
    Assignee: AstraZeneca AB
    Inventors: Wilhelm Quittman, Thomas Peter Belser, Rhony Niklaus Aufdenblatten
  • 6-phenylpyrimidinones as PIM modulators
    Patent number: 8242129
    Abstract: A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: August 14, 2012
    Assignee: Exelixis, Inc.
    Inventors: Amy L. Tsuhako, Naing Aay, S. David Brown, Wai Ki Vicky Chan, Hongwang Du, Ping Huang, Brian Kane, Patrick Kearney, Moon Hwan Kim, Elena S. Koltun, Michael Pack, Wei Xu, Peiwen Zhou
  • UREA SUBSTITUTED SULPHONAMIDE DERIVATIVES
    Publication number: 20120196884
    Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).
    Type: Application
    Filed: June 14, 2010
    Publication date: August 2, 2012
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
  • PYRIDONES USEFUL AS INHIBITORS OF KINASES
    Publication number: 20120190699
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.
    Type: Application
    Filed: December 14, 2011
    Publication date: July 26, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Steven Durrant, Sharn Ramaya, Juan-Miguel Jimenez, Alistair Rutherford
  • C-Met Modulators and Method of Use
    Publication number: 20120184523
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 19, 2012
    Applicant: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takbuchi, Yong Wang, Wei Xu
  • Preparation of aminopyrimidine compounds
    Patent number: 8222412
    Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: July 17, 2012
    Assignee: AstraZeneca UK Limited
    Inventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
  • PHENYL SULPHONAMIDES AS MODULATORS OF ION CHANNELS
    Publication number: 20120178713
    Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Application
    Filed: March 14, 2012
    Publication date: July 12, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
  • REGIOSELECTIVE PREPARATION OF 2-AMINO-5-TRIFLUOROMETHYLPYRIMIDINE DERIVATIVES
    Publication number: 20120172596
    Abstract: The present invention relates to a method of making pyrimidines of formula (III) said method comprising reacting a compound of formula (I) with an oxygen, sulfur or nitrogen nucleophile of formula T-H; and reacting the compound obtained with an amine of formula (II) [HN(R1)R2] to form a compound of formula (III) wherein X1, X2, T, R1 and R2 have the meanings as defined herein.
    Type: Application
    Filed: August 13, 2010
    Publication date: July 5, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Guenter Linz, Gerd Kraemer
  • Novel compounds
    Publication number: 20120165348
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: July 21, 2011
    Publication date: June 28, 2012
    Applicant: AstraZeneca AB
    Inventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
  • Substituted cyclic urea derivatives and the use thereof as vanilloid receptor 1 modulators
    Patent number: 8207182
    Abstract: The present invention relates to substituted cyclic urea derivatives corresponding to formula I, to processes for the preparation thereof, to medicinal drugs containing such compounds, to the use of such compounds in the preparation of medicinal drugs and in related treatment methods.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: June 26, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Bernd Sundermann, Hans Schick, Helmut Sonnenschein
  • NOVEL 3-HYDROXY-5-ARYLISOTHIAZOLE DERIVATIVE
    Publication number: 20120157459
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: December 24, 2010
    Publication date: June 21, 2012
    Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
  • NEPRILYSIN INHIBITORS
    Publication number: 20120157383
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: December 14, 2011
    Publication date: June 21, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Roland GENDRON, Melissa FLEURY, Adam D. HUGHES
  • USE OF AZABICYCLOALKYL DERIVATIVES OR PYRROLIDINE-2-ONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF ATAXIA
    Publication number: 20120157464
    Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.
    Type: Application
    Filed: July 21, 2010
    Publication date: June 21, 2012
    Inventors: Dominik Feuerbach, Baltazar Gomez-Mancilla
  • ETHER BENZOTRIAZOLE DERIVATIVES
    Publication number: 20120149677
    Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: August 16, 2010
    Publication date: June 14, 2012
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek