Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
Abstract: Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.
Type:
Grant
Filed:
April 20, 2009
Date of Patent:
June 5, 2012
Assignee:
Lexicon Pharmaceuticals, Inc.
Inventors:
Hugh Alfred Burgoon, Nicole Cathleen Goodwin, Bryce Alden Harrison, Jason Patrick Healy, Ying Liu, Ross Mabon, Brett Marinelli, David Brent Rawlins, Dennis Stewart Rice, Norris Andrew Whitlock
Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders based on pathological cell proliferations.
Abstract: Disclosed are pyridodihydropyrazinone compounds, processes for preparing them and their use as pharmaceutical compositions. The compounds according to the invention correspond to general formula (I), while the groups L, R1, R2, R3, R4 and R5 may have the meanings given in the claims and specification.
Type:
Grant
Filed:
October 14, 2009
Date of Patent:
June 5, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Hoffmann, Matthias Grauert, Trixi Brandl, Martin Steegmaier, Rudolf Hauptmann
Abstract: The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.
Type:
Grant
Filed:
May 5, 2011
Date of Patent:
May 29, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Juergen Schroeder, Georg Dziewas, Thomas Fachinger, Burkhard Jaeger, Cartsen Reichel, Svenja Renner
Abstract: The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc. Q is single bond, a methylene group or a group of the formula: —N(RQ)—, RQ is an alkyl group, Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), R3 and R4 are the same or different and a hydrogen atom, a cyano group etc. E is one of the following groups (i) to (v): R00 is an alkyl group, Q1 is a single bond etc., Q2 is a single bond or an alkylene group, one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., one of R50 and R60 is a hydrogen atom or an alkyl group and the other is a hydrogen atom, an alkyl group etc., R51 is an alkyl group or an optionally substituted arylsulfonyl group, R61 is an alkylamino group or an azido group, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 20, 2006
Date of Patent:
May 29, 2012
Assignee:
Mitsubishi Tanabe Pharma Corporation
Inventors:
Yasunori Moritani, Kimihiro Shirai, Mariko Oi
Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.
Type:
Grant
Filed:
April 13, 2009
Date of Patent:
May 29, 2012
Assignee:
Hoffman-La Roche Inc.
Inventors:
Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Type:
Grant
Filed:
May 1, 2009
Date of Patent:
May 29, 2012
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Shawn David Erickson, Paul Gillespie, Kevin Richard Guertin, Prabha Saba Karnachi, Kyungjin Kim, Chun Ma, Warren William McComas, Sherrie Lynn Pietranico-Cole, Lida Qi, Jefferson Wright Tilley, Qiang Zhang
Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Type:
Grant
Filed:
May 31, 2006
Date of Patent:
May 22, 2012
Assignee:
UCB Pharma, S.A.
Inventors:
Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
Abstract: The invention provides heteroaryl substituted thiazolo compounds of Formula I and II and pharmaceutically acceptable salts thereof. The variables A and R3 to R7 are defined herein. The invention also includes methods for preparing compounds and salts of Formula I and II. The present invention also includes pharmaceutical compositions containing heteroaryl substituted thiazolo compounds and methods for using heteroaryl substituted thiazolo compounds, including methods for using the compounds in the treatment of hepatitis C virus.
Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Type:
Grant
Filed:
May 31, 2006
Date of Patent:
May 15, 2012
Assignee:
UCB Pharma, S.A.
Inventors:
Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
Abstract: A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II to produce the bacteriochlorin, wherein R is an acetal or aldehyde group. The condensing may be carried out in an organic solvent, preferably in the presence of an acid. The bacteriochlorins are useful for a variety of purposes such as active agents in photodynamic therapy, luminescent compounds in flow cytometry, solar cells, light harvesting arrays, and molecular memory devices.
Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention also relates to methods for screening compounds and compositions useful for inhibiting or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.
Abstract: The invention relates to 4-cyanophenyl, 2-sulfanyl, 1-phenyl pyrimidine derivatives, processes for their preparation, and pharmaceutical compositions of the same. Compounds and compositions of the invention are useful in the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction, and heart failure development.
Type:
Grant
Filed:
July 27, 2009
Date of Patent:
May 8, 2012
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenieh, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
Abstract: A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II to produce the bacteriochlorin, wherein R is an acetal or aldehyde group. The condensing may be carried out in an organic solvent, preferably in the presence of an acid. The bacteriochlorins are useful for a variety of purposes such as active agents in photodynamic therapy, luminescent compounds in flow cytometry, solar cells, light harvesting arrays, and molecular memory devices.
Abstract: The present invention provides a class of modified pyrimidine compounds, compositions and methods of using the compounds as glucocorticoid receptor modulators.
Type:
Grant
Filed:
July 8, 2009
Date of Patent:
May 8, 2012
Assignee:
Corcept Therapeutics, Inc.
Inventors:
Robin D. Clark, Nicolas C. Ray, Karen Williams, Peter H. Crackett, Gwen Hickin, David A. Clark
Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
Type:
Grant
Filed:
April 26, 2010
Date of Patent:
May 1, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yasutsugu Ueda, Timothy P. Connolly, John F. Kadow, Nicholas A. Meanwell, Tao Wang, Chung-Pin H. Chen, Kap-Sun Yeung, Zhongxing Zhang, David Kenneth Leahy, Shawn K. Pack, Nachimuthu Soundararajan, Pierre Sirard, Kathia Levesque, Dominique Thoraval
Abstract: The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: —C(?O)— or —SO2—, R is a group of the following formula [i], [ii]or [iii] etc: Ring A is (a) a C3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.
Abstract: The invention provides novel pyrazolo[1,5-a]pyrimidines which are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation.
Type:
Grant
Filed:
August 2, 2007
Date of Patent:
April 17, 2012
Assignee:
Ferrer Internacional, S.A.
Inventors:
Luis Anglada, Albert Palomer, Antonio Guglietta