Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba(bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.
Abstract: Novel p75 receptor antagonist compounds and compositions and uses thereof for the prevention and treatment of p75-associated disorders, such as neurodegenerative diseases, are described.
Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
Type:
Grant
Filed:
March 26, 2013
Date of Patent:
March 29, 2016
Assignee:
Pfizer Inc.
Inventors:
Kay Ahn, Markus Boehm, Shawn Cabral, Philip A. Carpino, Kentaro Futatsugi, David Hepworth, Daniel W. Kung, Suvi Orr, Jian Wang
Abstract: The compositions and methods of described herein comprise novel ingredients effective to reduce unwanted pigmentation, such as skin discoloration, freckles, age spots, liver spots, sun damage, tans, pigmented acne marks, scars, pigmented birthmarks, hyperpigmentation, post-inflammatory hyperpigmentation, post-injury hyperpigmentation, melasma, cholasma, after-burn scar, nail stain, yellowing of skin, dark circles under eyes, and the like. The composition may include additional ingredients accordingly for a colored cosmetic, moisturizer, cleanser, toner, and the like.
Type:
Grant
Filed:
December 30, 2014
Date of Patent:
March 22, 2016
Assignee:
Avon Products, Inc.
Inventors:
Hong Hu, Sunghan Yim, Uma Santhanam, John W. Lyga
Abstract: Provided is a compound having at least one selected from the group consisting of cell growth promoting activity, angiogenesis promoting activity, lumen formation promoting activity, cell migration promoting activity, and neurocyte growth promoting activity, which is a chemically stable low-molecular-weight substance that has high absorbability and can be supplied stably at a low cost because of its low molecular weight. A cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof according to the present invention is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof.
Type:
Grant
Filed:
November 27, 2009
Date of Patent:
March 1, 2016
Assignee:
National University Corporation Kagawa University
Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
Abstract: The present invention discloses a xanthine derivative having the structure of the following general formula (I) or a pharmaceutically acceptable salt thereof; further discloses a preparation method for the xanthine derivative or a pharmaceutically acceptable salt thereof; and further discloses the use of the xanthine derivative or a pharmaceutically acceptable salt thereof. Through experiments of DPP-IV activity inhibition experiments in vitro, impact on glucose tolerance in normal mice and impact on blood glucose in spontaneous diabetic mice, it proves that the compounds and pharmaceutically acceptable salts thereof show good DPP-IV inhibition activity, can be applied to prepare medicines for treating dipeptidyl peptidase IV-related diseases, and more particularly, can be applied to the use of medicines for treating type II diabetes or diseases of abnormal glucose tolerance.
Type:
Grant
Filed:
May 15, 2013
Date of Patent:
February 9, 2016
Assignee:
Chengdu Easton Pharmaceutical Co., Ltd.
Inventors:
Ying Wang, Yongzhe Xiang, Guodong Cen, Long Huang, Jian Liu, Ning Zhou, Jibing Zhang
Abstract: The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof which comprises oxidizing a compound of formula (IV) or a salt thereof with an oxidizing agent in an organic or inorganic solvent or solvent mixture, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. Further aspects of the invention include the novel intermediary compound of formula (IV), and a process for the preparation thereof.
Abstract: The present invention provides a novel compound which has a broad antibacterial spectrum and particularly exhibits a high antibacterial activity on ?-lactamase-producing gram-negative bacteria. Specifically provided are: a compound represented by formula (I) wherein the meaning of each symbol is as defined in the description, an amino-group-protected form of a type of the compound which has the amino group on a ring in a position-7 side chain, or a pharmaceutically acceptable salt of the compound or the amino-group-protected form; and a pharmaceutical composition containing the compound, the amino-group-protected form or the pharmaceutically acceptable salt.
Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
Type:
Grant
Filed:
May 16, 2014
Date of Patent:
January 12, 2016
Assignee:
GlaxoSmithKline LLC
Inventors:
Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
Abstract: The present invention relates to an improved method for synthesizing meropenem trihydrate[(1R,5S,6S)-2-[((2?S,4?S)-2?-dimethylaminocarbozyl)pyrrolidin-4?-ylthio]-6-[(R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid, trihydrate], which is a novel carbapenem antibiotic.
Type:
Grant
Filed:
March 11, 2010
Date of Patent:
January 12, 2016
Assignees:
DAEWOONG PHARMACEUTICAL CO., LTD., DAEWOONG BIO, INC.
Inventors:
Yoon Seok Song, Sung Woo Park, Yeon Jung Yoon, Hee Kyoon Yoon, Seong Cheol Moon, Byung Goo Lee, Soo Jin Choi, Sun Ah Jun
Abstract: The invention relates to 6-substituted 9-halogenalkyl purine derivatives of the general formula I wherein R6 is selected from the group comprising —NH-furfuryl, —NH-(4-hydroxy-3-methylbut-2-en-1-yl), —NH-(3-methylbut-2-en-1-yl), —NH-(4-hydroxy-3-methylbutyl), —NH-(4-hydroxy-1,3-dimethylbut-2-en-1-yl), —NH-(4-hydroxy-1,3-dimethylbutyl), —NH-benzyl, —NH-phenyl, wherein benzyl, furfuryl and phenyl can be unsubstituted or optionally substituted with 1 to 3 substituents selected from the group comprising hydroxy, halogen, methyl and methoxy, and R9 is selected from the group comprising C1-C3 alkyl or C1-C3 alkenyl wherein each of the groups is substituted with one or more halogen atoms, for use in the regulation of growth and development of plant cells, organs and/or whole plants. The invention also relates to preparations containing these derivatives and to novel to 6-substituted 9-halogenalkyl purines.
Type:
Grant
Filed:
September 2, 2011
Date of Patent:
December 29, 2015
Assignee:
UNIVERZITA PALACKEHO V OLOMOUCI
Inventors:
Vaclav Mik, Lucie Szucova, Karel Dolezal, Lukas Spichal, Petr Galuszka, Miroslav Strnad, Jiri Gruz
Abstract: A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like.
Type:
Grant
Filed:
November 25, 2011
Date of Patent:
December 22, 2015
Assignee:
Medpacto, Inc.
Inventors:
Eun Kyong Shim, Nam Doo Kim, Tae Bo Shim, Seung Yong Kim
Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
Type:
Grant
Filed:
June 5, 2014
Date of Patent:
December 22, 2015
Assignee:
Intellikine LLC
Inventors:
Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
Abstract: Synthesis of many proteins is tightly controlled at the level of translation and plays an essential role in fundamental processes such as cell growth and proliferation, signaling, differentiation or death. Methods that allow imaging and identification of nascent proteins allow for dissecting regulation of translation, both spatially and temporally, including in whole organisms. Described herein are robust chemical methods for imaging and affinity-purifying nascent polypeptides in cells and in animals, based on puromycin analogs. Puromycin analogs of the present invention form covalent conjugates with nascent polypeptide chains, which are rapidly turned over by the proteasome and can be visualized and specifically captured by a bioorthogonal reaction (e.g., [3+2] cycloaddition). The methods of the present invention have broad applicability for imaging protein synthesis and for identifying proteins synthesized under various physiological and pathological conditions in vivo.
Type:
Grant
Filed:
November 9, 2012
Date of Patent:
December 15, 2015
Assignee:
President and Fellows of Harvard College
Abstract: The present invention relates to novel azetidinone-containing compounds having a novel side-chain which is attached to the aryl ring at C4 via a C—C bond and comprises a 3,3-disubstituted oxetane ring and a polar group A, and which are useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels.
Type:
Grant
Filed:
March 5, 2010
Date of Patent:
December 15, 2015
Assignee:
Lipideon Biotechnology AG
Inventors:
Thomas Fessard, Dong-Bo Li, Damien Barbaras, Susanne Wolfrum, Erick Carreira
Abstract: Substituted isoquinolin-1(2H)-one compounds that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
Type:
Grant
Filed:
August 20, 2013
Date of Patent:
December 8, 2015
Assignee:
Intellikine LLC
Inventors:
Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
Abstract: The present invention relates to a process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Y1 and Y2 are independently F or Cl, preferably F, said compound of formula (I) containing the cis-isomer and the trans-isomer, wherein the process comprises (1) providing the compound of formula (I) comprised in a first suitable solvent; and (2) treating the compound of formula (I) comprised in the first suitable solvent with HCl comprised in a second suitable solvent to obtain the HCl salt of the compound of formula (I).
Type:
Grant
Filed:
May 18, 2011
Date of Patent:
December 8, 2015
Assignee:
SANDOZ AG
Inventors:
Martin Langner, Dominic De Souza, Abhinay C. Pise, Sachin Bhuta
Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Type:
Grant
Filed:
July 15, 2014
Date of Patent:
December 1, 2015
Assignee:
Allergan, Inc.
Inventors:
Liming Wang, Mohammed I. Dibas, Michael E. Garst, Ken Chow, Santosh C. Sinha
Abstract: The present invention provides fused derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.