Bicyclo Ring System Having The Oxazine Ring As One Of The Cyclos (e.g., Benzoxazines, Etc.) Patents (Class 544/105)
  • MORPHOLINO SUBSTITUTED UREA DERIVATIVES AS MTOR INHIBITORS
    Publication number: 20130196982
    Abstract: The invention relates to compounds of formula (I) wherein X1, X2, R1 to R4, m, n have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: March 4, 2011
    Publication date: August 1, 2013
    Inventors: Rosemary Lynch, Andrew David Cansfield, Helen Sarah Niblock, Daniel Paul Hardy, Jessica Taylor
  • HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES
    Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • 1, 2, 4-TRIAZOLONE DERIVATIVE
    Publication number: 20130197217
    Abstract: The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.
    Type: Application
    Filed: September 30, 2011
    Publication date: August 1, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Takeshi Kuwada, Mitsukane Yoshinaga, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki, Naoki Miyakoshi
  • COMPOUNDS FOR INHIBITION OF CANCER CELL PROLIFERATION
    Publication number: 20130190258
    Abstract: Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R1, R2, R2?, R3, R4, R5, R6, R7, R8, R9 are as described herein.
    Type: Application
    Filed: January 24, 2013
    Publication date: July 25, 2013
    Inventors: John CASHMAN, Mark MERCOLA, Dennis SCHADE, Masanao TSUDA
  • HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS SELECTIVE JAK INHIBITORS
    Publication number: 20130190292
    Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: August 12, 2011
    Publication date: July 25, 2013
    Applicant: CELLZOME LIMITED
    Inventors: Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe, Nigel Ramsden
  • INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
    Publication number: 20130190491
    Abstract: Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: January 11, 2013
    Publication date: July 25, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • MODULATORS OF AMYLOID BETA
    Publication number: 20130190302
    Abstract: The invention relates to compounds of formula wherein the substituents are as described in claim 1. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Application
    Filed: January 25, 2013
    Publication date: July 25, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffman-La Roche Inc.
  • APOPTOSIS PROMOTERS
    Publication number: 20130190488
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 25, 2013
    Applicant: Abbott Laboratories
    Inventor: Abbott Laboratories
  • Herbicidal Benzoxazinones
    Publication number: 20130184155
    Abstract: The present invention provides benzoxazinones of formula I wherein R1 is hydrogen or halogen; R2 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C3-C6-cycloalkyl, C3-C6-alkenyl, C3-C6-haloalkenyl, C3-C6-alkynyl, C3-C6-haloalkynyl, C1-C6-alkoxy or C3-C6-cycloalkyl-C1-C6-alkyl; R3 is halogen; R4 is halogen; X is O or S; and Y is a substituted or unsubstituted heterocycle; Benzoxazinones of formula I are useful as herbicides.
    Type: Application
    Filed: September 26, 2011
    Publication date: July 18, 2013
    Inventors: Trevor William Newton, Thomas Seitz, Matthias Witschel, Anja Simon, Helmut Walter, Richard Roger Evans
  • HETERO RING-FUSED IMIDAZOLE DERIVATIVE HAVING AMPK ACTIVATING EFFECT
    Publication number: 20130184240
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Application
    Filed: September 8, 2011
    Publication date: July 18, 2013
    Applicant: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • Xinafoate salt of N4-(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]2,4-pyrimidinediamine
    Patent number: 8486935
    Abstract: The present invention relates to the xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine. This compound is a suitable drug substance and is useful in the treatment of conditions including asthma.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: July 16, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventor: Stefan Colin John Taylor
  • SUBSTITUTED (1-(METHYLSULFONYL)AZETIDIN-3-YL)(HETEROCYCLOALKYL)METHANONE ANALOGS AS ANTAGONISTS OF MUSCARINIC ACETYLCHOLINE M1 RECEPTORS
    Publication number: 20130178458
    Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 3, 2012
    Publication date: July 11, 2013
    Applicant: Vanderbilt University
    Inventor: Vanderbilt University
  • Synthesis of 2,4-pyrimidinediamines
    Patent number: 8481724
    Abstract: Disclosed herein are methods for synthesizing 2,4-pyrimidinediamines as well as intermediates used therein.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: July 9, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ulfried Felfer, Karl-Heinz Giselbrecht, Michael Wolberg
  • 3-(3,4-dihydro-2H-benzo [1,4]oxazin-6-yl)-1H-Pyrimidin-2,4-dione compounds as herbicides
    Patent number: 8481723
    Abstract: The present invention relates to uracils of formula I wherein the variables are defined according to the description, processes and intermediates for preparing the uracils of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one uracil of the formula I to act on plants, their seed and/or their habitat.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: July 9, 2013
    Assignee: BASF SE
    Inventors: Anja Simon, Liliana Parra Rapado, Richard Roger Evans, Matthias Witschel, Trevor William Newton, Thomas Seitz, Helmut Walter
  • 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
    Publication number: 20130172335
    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: February 22, 2013
    Publication date: July 4, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • TRPV1 ANTAGONISTS
    Publication number: 20130172334
    Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: December 17, 2012
    Publication date: July 4, 2013
    Applicant: ABBVIE INC.
    Inventor: AbbVie Inc.
  • Phenylacetic acid compound
    Patent number: 8476266
    Abstract: A compound represented by formula (I), wherein R1 represents a hydrogen atom, etc., R2 and R3 each independently represents a hydrogen atom, optionally oxidized C1-4 alkyl group or optionally protected hydroxyl group, or R2 and R3 taken together represent optionally oxidized C2-5 alkylene group, R4 represents an optionally oxidized C1-6 alkyl group, etc., R5 represents an optionally oxidized C1-6 alkyl group, etc., R6 represents an optionally oxidized C1-6 alkyl group, etc., m represents 0 or an integer from 1 to 3, n represents 0 or an integer from 1 to 4, and i represents 0 or an integer from 1 to 7.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: July 2, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Atsushi Naganawa, Toshihiko Nagase
  • Prodrugs of 2,4-pyrimidinediamine compounds and their uses
    Patent number: 8476263
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: July 2, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
    Publication number: 20130165422
    Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Dihydro-Benzo-Oxazine and Dihydro-Pyrido-Oxazine Derivatives
    Publication number: 20130165436
    Abstract: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: NOVARTIS AG
    Inventor: Novartis AG
  • Novel Use
    Publication number: 20130165433
    Abstract: The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 27, 2013
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Zoe Alicia Harrison, Katherine Louise Jones, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Charlotte Jane Mitchell, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christopher Alan Paul Smethurst, Yoshiaki Washio
  • PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL AGENTS
    Publication number: 20130164280
    Abstract: The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventor: Gilead Sciences, Inc.
  • Bicyclic compounds
    Patent number: 8471004
    Abstract: The invention is concerned with novel bicyclic compounds of formula (I), wherein A, L, E, F, G, R1, R2, R3, R4, R5, R6, R7, V, W and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: June 25, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei
  • 2-AMINOPYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR
    Publication number: 20130158259
    Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: February 13, 2013
    Publication date: June 20, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventor: JANSSEN PHARMACEUTICA NV
  • PROTEASE INHIBITORS
    Publication number: 20130158261
    Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: TaiMed Biologics, Inc.
    Inventor: TaiMed Biologics, Inc.
  • 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
  • AMINO ACID-, PEPTIDE-AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF
    Publication number: 20130158021
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
    Publication number: 20130157999
    Abstract: Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Application
    Filed: November 28, 2012
    Publication date: June 20, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES
    Publication number: 20130157941
    Abstract: The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances.
    Type: Application
    Filed: June 17, 2011
    Publication date: June 20, 2013
    Applicant: Sanofi
    Inventors: Stefan Petry, Norbert Tennagels, Karl-Heinz Baringhaus
  • AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
    Publication number: 20130158006
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Application
    Filed: November 28, 2012
    Publication date: June 20, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • HETEROCYCLIC COMPOUND
    Publication number: 20130150344
    Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 13, 2013
    Inventors: Masato Yoshikawa, Shinkichi Suzuki, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo, Haruhi Kamisaki, Takahiko Taniguchi
  • Acyl Piperazine Derivatives as TTX-S Blockers
    Publication number: 20130150356
    Abstract: The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: August 9, 2011
    Publication date: June 13, 2013
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Mikiko Morita, Shuzo Watanabe
  • Fused Tricyclic Inhibitors of Mammalian Target of Rapamycin
    Publication number: 20130150353
    Abstract: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Application
    Filed: August 22, 2011
    Publication date: June 13, 2013
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyum Zhao, Andrew McRiner
  • NEW SELECTIVE CCR2 ANTAGONISTS
    Publication number: 20130150354
    Abstract: The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.
    Type: Application
    Filed: June 14, 2012
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Stefan SCHEUERER
  • 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES
    Publication number: 20130150349
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: February 5, 2013
    Publication date: June 13, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • NOVEL COMPOUNDS
    Publication number: 20130150355
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER
  • 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
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20130142807
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Application
    Filed: January 25, 2013
    Publication date: June 6, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
    Publication number: 20130137648
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: January 23, 2013
    Publication date: May 30, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • HETEROARYL (ALKYL) DITHIOCARBAMATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
    Publication number: 20130136794
    Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.
    Type: Application
    Filed: April 21, 2011
    Publication date: May 30, 2013
    Applicant: PEKING UNIVERSITY
    Inventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
  • 2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds
    Patent number: 8450313
    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: Grant
    Filed: May 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES
    Publication number: 20130131039
    Abstract: Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
    Type: Application
    Filed: April 11, 2011
    Publication date: May 23, 2013
    Applicant: Array BioPharma Inc.
    Inventors: Laurence E. Burgess, Mark Laurence Boys, Robert D. Groneberg, Darren M. Harvey, Timothy Kercher, Christopher F. Kraser, Ellen Laird, Eugene Tarlton, Qian Zhao, Lily Huang
  • FUROPYRIDINYL-SUBSTITUTED 1,4-DIHYDROPYRIDINE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20130131055
    Abstract: This invention relates to novel 4-(furo[3,2-c]pyridin-2-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
    Type: Application
    Filed: November 15, 2010
    Publication date: May 23, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Martin Michels, Hans Briem, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch
  • PYRAZINE KINASE INHIBITORS
    Publication number: 20130131040
    Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: November 23, 2012
    Publication date: May 23, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Bicyclic peptidomimetic inhibitors of aspartyl-proteases for the treatment of infectious diseases
    Patent number: 8445484
    Abstract: The present invention refers to 3-aza-bicyclo [3.2.1] octane derivatives of general formula (I) their preparation, use and pharmaceutical compositions useful in the treatment of pathologies associated with microbial pathogens expressing aspartylprotease activity.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: May 21, 2013
    Assignees: Istituto Superiore di Sanita', Universita' Degli Studi di Firenze
    Inventors: Antonio Cassone, Flavia De Bernardis, Enrico Garaci, Andrea Trabocchi, Antonio Guarna
  • Prodrugs of 2,4-pyrimidinediamine compounds and their uses
    Patent number: 8445485
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: May 21, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
  • Herbicidal tetrahydrophthalimides
    Patent number: 8445407
    Abstract: The present invention relates to tetrahydrophthalimides of formula I wherein the variables are defined according to the description, processes and intermediates for preparing the benzoxazinones of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one tetrahydrophthalimide of the formula I to act on plants, their seed and/or their habitat.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: May 21, 2013
    Assignee: BASF SE
    Inventors: Matthias Witschel, Trevor William Newton, Thomas Seitz, Helmut Walter, Bernd Sievernich, Anja Simon, Ricarda Niggeweg, Klaus Grossmann
  • BENZOXAZINE DERIVATIVES AND USES THEREOF
    Publication number: 20130123251
    Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, Y, Z1, m, n, and p are as defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
    Type: Application
    Filed: December 13, 2012
    Publication date: May 16, 2013
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
  • 2-substituted-ethynylthiazole derivatives and uses of same
    Patent number: 8440837
    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: Grant
    Filed: October 20, 2010
    Date of Patent: May 14, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Mathivanan Packiarajan, Michel Grenon
  • Imidazopyrazine Syk inhibitors
    Patent number: 8440667
    Abstract: Certain imidazopyrazines of Formula (I): and pharmaceutical compositions thereof are provided herein. Methods of treating patients responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity of Formula (I) effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: May 14, 2013
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford