Abstract: Disclosed herein are compounds of formula (I) wherein L1, L2, L3, R1, R4, R5, and R6 are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
June 13, 2017
Assignee:
CAYMAN CHEMICAL COMPANY, INC.
Inventors:
Stephen Douglas Barrett, Bradlee David Germain, Adam Uzieblo, Fred Lawrence Ciske, Gregory William Endres, Andriy Kornilov, Kirk M. Maxey, James Paul O'Malley, Thomas Allen Owen
Abstract: The compounds of formula (I) are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumor growth.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
June 13, 2017
Assignee:
Proximagen Limited
Inventors:
Max Espensen, Lee Patient, David Evans, Iain Simpson, Edward Savory
Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
December 5, 2016
Date of Patent:
June 6, 2017
Assignee:
Genentech, Inc.
Inventors:
Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
Abstract: Provided are fused tricyclic amide compounds, pharmaceutical compositions comprising at least one such fused tricyclic compound, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain tricyclic amide compounds that can be useful for inhibiting multiple (specifically BRAF and/or EGFR-T790M) kinases and for treating disorders mediated thereby.
Abstract: [Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an ?7 nicotinic acetylcholine receptor (?7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an ?7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an ?7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an ?7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.
Abstract: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R and R6 are each independently (LQ)mY; R4 is H, halogen, optionally substituted aryl or optionally substituted alkyl; and; each X is independently CR7 or N. The compounds are PI3K inhibitors and therefore have potential utility in therapy.
Type:
Grant
Filed:
March 8, 2013
Date of Patent:
May 30, 2017
Assignee:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Franck Alexandre Silva
Abstract: The invention relates to a method for synthesizing an intermediate of Apixaban comprising reacting a compound of formula I with 5-chloro-valeryl chloride in the presence of inorganic base in an inert solvent to obtain a compound of formula II, with the reaction formula of (A), wherein R is selected from nitro group and the group (B). The method is mild in reaction condition, simple in operation, easy in purification, inexpensive in production cost, environmental-friendly, and suitable for industrial production.
Abstract: The present invention relates to compounds of formula wherein the substituents are described in claim 1 and to the pharmaceutically acceptable salts thereof. These compounds inhibit the enzyme catechol-O-methyltransferase (COMT). The compounds may be used for the treatment of Parkinson's disease, depression, cognitive impairment and motor symptoms, resistant depression, cognitive impairment, mood and negative symptoms of schizophrenia.
Type:
Grant
Filed:
June 26, 2015
Date of Patent:
May 23, 2017
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Caterina Bissantz, René Bonnafous, Bernd Buettelmann, Roland Jakob-Roetne, Christian Lerner, Markus Rudolph
Abstract: Disclosed are compound of Formula (Ia), wherein R2, R12, R16, J, Q, X, Y and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (Ia).
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
May 16, 2017
Assignee:
AbbVie Inc.
Inventors:
Anthony Mastracchio, Milan Bruncko, Chunqiu Lai, Julie M. Miyashiro, Zhi-Fu Tao, Keith W. Woods, Thomas D. Penning, Andrew J. Souers
Abstract: The present invention relates to an improved process for the preparation of Linezolid. More specifically, the present invention relates to an improved process for preparing (S)—N-[[3-[3-fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl] phthalimide and (S)-glycidyl phthalimide intermediates, which are used in the preparation of Linezolid.
Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.
Abstract: The present invention refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (Ia), as well as a intermediate thereof. The process of the invention has simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.
Abstract: The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
May 2, 2017
Assignee:
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
Inventors:
Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Nicoleta Dobri, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
Abstract: The present invention provides trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors. wherein, R1, R2 and R3 have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing trisubstituted benzotriazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.
Type:
Grant
Filed:
February 24, 2014
Date of Patent:
April 25, 2017
Assignees:
UM PHARMAUJI SDN. BHD., AURIGENE DISCOVERY TECHNOLOGIES LIMITED
Abstract: The present invention provides a method for producing a 1H-tetrazole derivative by reacting an azide compound represented by general formula (II) and a cyanide compound represented by general formula (III) in a flow reactor to produce a compound represented by general formula (I) (wherein, Y represents an alkyl group, aryl group, arylalkyl group, substituted silyl group or substituted silylalkyl group, Z represents —CO—, —SO2— or —CRaRb— (wherein, Ra and Rb respectively and independently represent a hydrogen atom, alkyl group or unsubstituted or substituted aryl group), p represents 0 or 1, q represents 0 or 1, r represents 0 or 1 (provided that q is 1 in the case p is 0 or r is 0), R1 represents an alkyl group or hydrogen atom in the case q is 0 or an alkylene group in the case q is 1, and R2 represents an unsubstituted or substituted aryl group).
Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
Type:
Grant
Filed:
October 18, 2013
Date of Patent:
April 11, 2017
Assignee:
ASTEX THERAPEUTICS LIMITED
Inventors:
Gianni Chessari, Christopher Norbert Johnson, Lee William Page, Ildiko Maria Buck, James Edward Harvey Day, Steven Howard, Gordon Saxty, Christopher William Murray, Anna Hopkins
Abstract: The present invention provides thiazole compounds of Formula I wherein X1, X2, X3, X4, X5, R1, R2, R4, R5, R6, R7, and W, and ring AA, are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrugs, or esters or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.