Abstract: A compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof: (wherein each symbol is as defined in the description.) The compounds represented by formula (I) has the antagonistic activity against CCR5, so they are useful in preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, inflammatory bowel disease such as ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation (rejection of graft of solid organ, rejection of graft of pancreatic islet cells in therapy for diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, infection with RSV, etc.
Abstract: The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.
Type:
Grant
Filed:
October 27, 2008
Date of Patent:
March 12, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Gerald W. Shipps, Jr., Matthew Richards, Cliff C. Cheng, Xiaohua Huang
Abstract: The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.
Type:
Grant
Filed:
September 10, 2010
Date of Patent:
March 5, 2013
Assignee:
North Carolina State University
Inventors:
Daniel L. Comins, Florence F. Wagner, Pauline Ondachi
Abstract: Provided is a compound useful as a therapeutic drug for pain and inflammation caused by various pathological conditions such as neuropathic pain and rheumatoid arthritis. The compound of the formula (I) or a salt thereof [wherein R1 is a methyl group or a hydrogen atom, R2 represents a hydrogen atom, an alkyl group, an alkylcarbonyl group or an aryl carbonyl group, A represents a cycloalkyl group, a cycloalkenyl group, an aryl group or a heteroaryl group (each group may be substituted with a substituent selected from the group consisting of alkyl, alkenyl, cycloalkyl and halogen), n and m each represent an integer of 1, 2 or 3, and p represents an integer of 0, 1, 2 or 3].
Abstract: Method for producing 4-formylaminopiperidine derivatives of the formula (I) and also the acid addition salts of these compounds, comprising the reaction of 4-aminopiperidine derivatives of the formula (II) or the acid addition salts of these compounds in the presence of compounds of the formula (III) and the use of 4-formylaminopiperidine derivatives of the formula (I) produced in such a way for protecting inanimate organic material against the effect of light.
Abstract: Crystalline raloxifene hydrochloride in hydrated form, particularly the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and uses thereof.
Type:
Grant
Filed:
October 17, 2007
Date of Patent:
January 1, 2013
Assignee:
Cipla Limited
Inventors:
Srinivas Laxminarayan Pathi, Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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.
Type:
Grant
Filed:
June 9, 2010
Date of Patent:
January 1, 2013
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Kevin Michael Cottrell, Alex Aronov, Robert J. Davies, Jon H. Come, David Messersmith, Jinwang Xu, Upul Keerthi Bandarage, Jingrong Cao
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.
Abstract: A process is described for catalytically preparing optionally substituted aromatic or heteroaromatic nitrites of the general formula (I) Ar—CN??(I) by reacting the corresponding aryl halides of the general formula (II) Ar—X??(II) in which X is chlorine, bromine, iodine, triflate, nonaflate, mesylate or tosylate and Ar is an optionally substituted aromatic or heteroaromatic radical, characterized in that the reaction is performed in the presence of a palladium compound, a phosphine of the general formula (III) or (IV) where R is an alkyl radical and R?, R? and R?? are each an alkyl radical or an aryl radical or heteroaryl radical and A is an alkylene or arylene radical, and potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III), optionally in a solvent and optionally with addition of a base.
Type:
Grant
Filed:
November 21, 2007
Date of Patent:
November 20, 2012
Assignee:
Saltigo GmbH
Inventors:
Nikolaus Müller, Wolfgang Mägerlein, Alain Cotté, Matthias Beller, Thomas Schareina, Alexander Zapf
Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.
Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
Type:
Grant
Filed:
September 18, 2008
Date of Patent:
October 30, 2012
Assignee:
Glaxo Group Limited
Inventors:
David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
Type:
Grant
Filed:
October 5, 2010
Date of Patent:
October 16, 2012
Assignee:
Adolor Corporation
Inventors:
Bertrand Le Bourdonnec, Roland E. Dolle
Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
Type:
Grant
Filed:
July 17, 2009
Date of Patent:
October 16, 2012
Assignee:
University of Pittsburgh - Of the Commonwealth System of Higher Education
Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.
Type:
Grant
Filed:
February 10, 2012
Date of Patent:
September 25, 2012
Assignee:
Schering Corporation
Inventors:
Tiruvettipuram K. Thiruvengadam, Anantha Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green