Abstract: The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH?CH—, *—CO—CH2CH2—, *—CO—CH2—NH—, wherein the asterisks indicate the bond that is linked to the thiophene group of Formula (I), and R1-R3 are as defined in the claims.
Type:
Grant
Filed:
January 10, 2007
Date of Patent:
August 23, 2011
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
Type:
Grant
Filed:
November 5, 2009
Date of Patent:
August 23, 2011
Assignee:
Amgen Inc.
Inventors:
Hilary Beck, Paul Dransfield, Zice Fu, Jonathan B. Houze, XianYun Jiao, Todd J. Kohn, SuJen Lai, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Michael J. Schmitt, Rajiv Sharma, Wang Shen, Marc Vimolratana, Yingcai Wang, Zhongyu Wang
Abstract: The present invention relates to a process for the preparation of 4-[1-(4-cyano phenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile (letrozole), substantially free from its isomeric impurity. The preparation involves reaction of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile with 4-fluorobenzonitrile in the presence of an organic solvent and a silicon amine. The present invention also relates to a process for the preparation of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile which involves: (a) the reaction of a 4-halomethyl benzonitrile with 1,2,4-triazole in the presence of cesium carbonate and an organic solvent to obtain a reaction mass comprising 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile of formula II; and (b) precipitation of 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile (II) from the reaction mass using a suitable organic solvent.
Abstract: Benzo[b]perhydroheterocyclic arylamine compounds have shown to be particularly useful as stabilizers. The compounds may serve as antioxidants, antiozoants, heat stabilizers and ultraviolet light stabilizers and such compounds are oil soluble, thus particularly suited for use as an antioxidant in a lubricating oil composition.
Abstract: The present invention relates to novel aminoalkoxy arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.
Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.
Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.
Type:
Grant
Filed:
July 6, 2007
Date of Patent:
August 23, 2011
Assignees:
Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
Abstract: The present invention relates to modulators of metalloproteinase activity.
Type:
Grant
Filed:
May 14, 2009
Date of Patent:
August 16, 2011
Assignee:
Wyeth LLC
Inventors:
Phaik-Eng Sum, Jerauld Stanley Skotnicki, Steve Yik-Kai Tam, Tarek Suhayl Mansour, David Brian How, Joshua James Sabatini, Jason Shaoyun Xiang, Eric Feyfant
Abstract: Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Type:
Grant
Filed:
December 7, 2007
Date of Patent:
August 16, 2011
Assignee:
Exelixis Patent Company LLC
Inventors:
Brant Clayton Boren, Brett B. Busch, Xiao-Hui Gu, Vasu Jammalamadaka, Shao Po Lu, Richard Martin, Raju Mohan, Edwin Schweiger, William C. Stevens, Tie-Lin Wang, Yinong Xie, Wei Xu
Abstract: The invention relates to biphenyl compounds of formula (I): wherein U, V and W together form a group of the formula *—CH?CH—CH<, *—CH2—CH2—CH< or *—CH2—CH2—N<, in which * means the point of linkage to the phenyl ring; A is O or CH2; and D, E, X, Y, Z, R1, R2, o, n, and p are as defined in the specification. The invention also relates to pharmaceutical compositions of the compound of the compounds. The compounds and pharmaceutical compositions of the invention can be used in the treatment or prevention of cardiovascular disorders.
Type:
Grant
Filed:
October 9, 2006
Date of Patent:
August 16, 2011
Assignee:
Bayer Schering Pharma Aktiengellschaft
Inventors:
Stephan Bartel, Michael Hahn, Wahed Ahmed Moradi, Klaus Münter, Thomas Rölle, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder
Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.
Abstract: The present invention provides a phosphorus-containing compound of formula (I): wherein R1, R2, R3 and R4 are the same or different; and R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, C1-8 alkyl, haloalkyl, and alkoxy. The phosphorus-containing compound is prepared by bonding a bisphenol group to a phosphorus atom to prevent the phosphorus-containing heterocyclic molecule from exhibiting steric hindrance on hydroxyl functional groups, thereby increasing reactivity in the subsequent reactions.
Type:
Grant
Filed:
October 7, 2009
Date of Patent:
August 9, 2011
Assignee:
Chang Chun Plastic Co., Ltd.
Inventors:
Gai-Chi Chen, Ching-Jui Huang, An Pang Tu, Kuen Yuan Hwang
Abstract: The present invention provides an aryl- or heteroaryl compound represented by the formula (Ia) or (Ib) wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. The compound has superior acid secretion inhibitory action, an antiulcer activity and the like.
Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea·¼ Ethanolate Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it is disclosed.
Abstract: The present invention relates to the field of perfumery. More particularly, it concerns specific oxime or nitrite derivatives of 4-dodecene, which are useful perfuming ingredients in particular to impart natural mandarin odor notes.
Abstract: A compound having the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, wherein R1 comprises a chromophore that absorbs light from the visible wavelength range, and wherein n is an integer of at least 12. A solid phase change ink composition is also disclosed containing a colorant comprising a chromophore that absorbs light from the visible wavelength range and has the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, and wherein n is an integer of at least 12. Also disclosed is a method of forming a colorant wherein a first compound having the formula is reacted with a second compound having the formula Z(CH2)nCH3 wherein n is an integer of at least 12 to form a third compound having the formula wherein the third compound comprises a chromophore that absorbs light from the visible wavelength range.
Type:
Grant
Filed:
December 14, 2007
Date of Patent:
July 26, 2011
Assignee:
Xerox Corporation
Inventors:
Jeffrey H Banning, Michael B. Meinhardt, Donald R Titterington, Clifford R King
Abstract: Disclosed herein is a compound represented by a formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Abstract: Disclosed are two new crystalline forms, ? and ?, of perindopril erbumine. Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardiovascular diseases, especially high blood pressure and heart failure. The ? crystalline form is obtained in the crystallization of perindopril erbumine at from 30 to 45° C., preferably from 34 to 45° C., from MTBE containing from 1.5 to 2.5% (v/v) water; the crystallization is advantageously carried out with stirring. If the water is then removed, advantageously by azeotropic distillation, preferably at from 35 to 37° C., and stirring is then continued for at least 15 h at from 30 to 45° C., preferably from 35 to 37° C., the ? crystalline form is converted to the ? crystalline form. The ? crystalline form can also be obtained by stirring the ? or ? crystalline form at from 33 to 38° C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the ? crystalline form.
Type:
Grant
Filed:
March 9, 2010
Date of Patent:
July 19, 2011
Assignee:
Les Laboratoires Servier
Inventors:
Christoph Strassler, Vit Lellek, Roger Fassler
Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.
Type:
Grant
Filed:
November 15, 2006
Date of Patent:
July 19, 2011
Assignee:
BASF SE
Inventors:
Markus Kordes, Christopher Koradin, Deborah L. Culbertson
Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
Type:
Grant
Filed:
October 16, 2006
Date of Patent:
July 19, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Sherman T. Waddell, James M. Balkovec, Nancy J. Kevin, Xin Gu