Abstract: Compounds represented by formula (II): wherein M is a hydrogen atom, sodium, potassium, or lithium; P is a hydrogen atom, an alkyl group, and the like; and the wavy line indicates a cis form, a trans form, or a mixture thereof for the double bond to which it is attached, may be prepared by hydrolyzing a compound represented by formula (I), or a salt thereof: wherein R1 and R2 are the same or different and each is an alkyl group, or R1 and R2 together with the adjacent nitrogen atom may form an aliphatic heterocycle, and P and the wavy line are as defined above, in the presence of alkali metal hydroxide.
Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
Type:
Grant
Filed:
October 18, 2005
Date of Patent:
April 8, 2008
Assignee:
Amgen Inc.
Inventors:
Qingping Zeng, Guomin Yao, George Erich Wohlhieter, Vellarkad N. Viswanadhan, Andrew Tasker, James Thomas Rider, Holger Monenschein, Celia Dominguez, Matthew Paul Bourbeau
Abstract: Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g., depression and pain.
Type:
Grant
Filed:
August 11, 2006
Date of Patent:
March 25, 2008
Assignee:
Gruenenthal GmbH
Inventors:
Stefan Oberboersch, Corinna Sundermann, Bernd Sundermann, Edward Bijsterveld
Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Type:
Grant
Filed:
February 3, 2006
Date of Patent:
March 25, 2008
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
Abstract: Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.
Type:
Grant
Filed:
July 28, 2006
Date of Patent:
March 25, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca
Abstract: Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.
Type:
Grant
Filed:
April 1, 2005
Date of Patent:
March 18, 2008
Assignee:
Miikana Therapeutics
Inventors:
Sampath K. Anandan, Xiao-Yi Xiao, Dinesh V. Patel, John Ward
Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical uses of these compounds are related to contraception, the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minication of side effects of cyclid menstrual bleeding. Additional uses of the invention include stimulation of food intake.
Type:
Grant
Filed:
January 16, 2007
Date of Patent:
March 18, 2008
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Weiqin Jiang, James J. Fiordeliso, Zhihua Sui
Abstract: The present invention provides a compound of the following formula I: R3—NH—C(?X)—P(?O)OR1OR2 including pharmaceutically acceptable salts, solvates, hydrates and polymorphs of the compounds of formula I, as well as geometrical isomers and optically active forms of the compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates and polymorphs of said isomers and forms, wherein R1 and R2 may be the same or different and are each selected from hydrogen, acyloxyalkyl and aryl or R1 and R2 may form together with the oxygen and phosphorus atoms a dioxaphosphacycloalkane ring; X is O or S; and R3 is selected, when X is O, from bicycloalkyl, cycloalkylalkyl and substituted cycloalkyl by at least one of alkyl, amino, amidino and guanidino; and R3 is selected, when X is S, from bicycloalkyl, cycloalkylalkyl and cycloalkyl optionally substituted by at least one of alkyl, amino, amidino and guanidino; with the proviso that: when X is O, R3 is not cyclohexylmethyl, and when X is S, R3 is not cycl
Type:
Grant
Filed:
October 6, 2005
Date of Patent:
March 18, 2008
Assignee:
Yissum Research Development Company of the Hebrew University of Jerusalem
Inventors:
Eli Breuer, Reuven Reich, Gershon Golomb, Yiffat Katz
Abstract: The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using such compounds as anti-infective, anti-proliferative agents, anti-inflammatory, and/or prokinetic agents.
Type:
Grant
Filed:
February 21, 2006
Date of Patent:
February 26, 2008
Assignee:
Rib-X Pharmaceuticals, Inc.
Inventors:
Deping Wang, Joyce A. Sutcliffe, Adegboyega K. Oyelere, Timothy S. McConnell, Joseph A. Ippolito, John N. Abelson, Dane M. Springer, Joseph M. Salvino, Rongliang Lou, Joel A. Goldberg, Jay J. Farmer, Erin M. Duffy, Ashoke Bhattacharjee
Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.
Type:
Grant
Filed:
November 4, 2005
Date of Patent:
February 19, 2008
Assignee:
Renopharm Ltd.
Inventors:
Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
Abstract: Compounds of formula (I): wherein: X is a group of formula (B): and R1, R2, R4, n, x, y and z are as defined within are described. Processes for their preparation and their use in the treatment of disorders mediated by the neuropeptide Y5 receptor in a warm-blooded animal, such as a human being, are also described.
Type:
Grant
Filed:
May 12, 2005
Date of Patent:
February 19, 2008
Assignee:
AstraZeneca AB
Inventors:
Michael Howard Block, Kevin Michael Foote
Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R6
Type:
Grant
Filed:
December 16, 2003
Date of Patent:
February 19, 2008
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Joannes Theodorus Maria Linders, Gustaaf Henri Maria Willemsens, Ronaldus Arnodus Hendrika Joseph Gilissen, Christophe Francis Robert Nestor Buyck, Greta Constantia Peter Vanhoof, Louis Jozef Elisabeth Van Der Veken, Libuse Jaroskova
Abstract: There are provided novel compounds of formula (I) wherein R1, R2, R3, R10, M, Q, T, U, Y, V and W are as defined in the specification and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.
Abstract: This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.
Type:
Grant
Filed:
September 21, 2005
Date of Patent:
February 12, 2008
Assignee:
H. Lundbeck A/S
Inventors:
Mohammad R. Marzabadi, Yu Jiang, Chien-An Chen, Kai Lu, Kim Andersen
Abstract: The present invention relates to inhibitors of protein kinases, particularly to inhibitors of JAK2 and JAK3. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
September 19, 2005
Date of Patent:
February 12, 2008
Assignee:
Vertex Pharamaceuticals Incorporated
Inventors:
Francesco Salituro, Mark Ledeboer, Brian Ledford, Jian Wang, Albert Pierce, John Duffy, David Messersmith
Abstract: The invention provides pyrrole-containing compounds and methods of use thereof. Kits and pharmaceutical compositions comprising the pyrrole compounds of the invention are also provided. The compounds and compositions disclosed herein are preferably used in the treatment of neurodegenerative diseases, cardiovascular diseases, proliferative diseases, and visual disorders. In particular, methods and compositions for the treatment of stroke are disclosed herein.
Type:
Grant
Filed:
May 17, 2004
Date of Patent:
January 29, 2008
Assignee:
Ambit Biosciences Corporation
Inventors:
David J. Lockhart, Hitesh K. Patel, Zdravko V. Milanov, Shamal Anil Mehta, Patrick Parvis Zarrinkar, William H. Biggs, III, Pietro Ciceri, Miles A. Fabian, Daniel K. Treiber
Abstract: The present invention is directed to certain novel triazole compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity, and eating disorders.
Type:
Grant
Filed:
May 24, 2005
Date of Patent:
January 29, 2008
Assignee:
Metabolex, Inc.
Inventors:
Yan Zhu, Jingyuan Ma, Peng Cheng, Zuchun Zhao, Francine M. Gregoire, Vera A. Rakhmanova
Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
July 20, 2005
Date of Patent:
January 8, 2008
Assignee:
Theravance, Inc.
Inventors:
Robert Murray McKinnell, Edmund J. Moran
Abstract: A process for the production of dialkyl carbonates from the reaction of alcohol, for example C1-C3 alcohols, with urea is disclosed wherein the water and ammonium carbamates impurities in the feed are removed in a prereactor. The water is reacted with urea in the feed to produce ammonium carbamate which is decomposed along with the ammonium carbamates originally in the feed to ammonia and carbon dioxide. In addition some of the urea is reacted with the alcohol in the first reactor to produce alkyl carbamate which is a precursor to dialkyl carbonate. Dialkyl carbonates are produced in the second reaction zone. The undesired by-product N-alkyl alkyl carbamates are continuously distilled off from the second reaction zone along with ammonia, alcohol and dialkyl carbonates under the steady state reactor operation. N-alkyl alkyl carbamates can be converted to heterocyclic compounds in a third reaction zone to remove as solids from the system.
Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for making the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Type:
Grant
Filed:
March 22, 2006
Date of Patent:
January 1, 2008
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Alex Aronov, Upul K. Bandarage, David J. Lauffer, Pan Li, Ronald C. Tomlinson