Abstract: The present invention provides O2-substituted 1-[(2-carboxylato)pyrrolidin-1-yl]diazen-1-ium-1,2-diolates (1-[(2-carboxylato)pyrrolidin-1-yl]diazeniumdiolates) of the formula in which R and R22are as described herein. Also provided is a composition comprising such a compound and a carrier. The 1-[(2-carboxylato)pyrrolidin-1-yl]diazeniumdiolates compounds release nitric oxide under physiological conditions and are useful for treating biological disorders.
Type:
Grant
Filed:
April 12, 2005
Date of Patent:
July 25, 2006
Assignee:
The United States of America as represented by the Department of Health and Human Services
Abstract: A pyridopyrimidine or a naphthyridine derivative of the formula (I): wherein R1 is an optionally substituted nitrogen-containing heterocyclic group, etc.; R2 is H or a lower alkyl group; R3 is H or an optionally substituted lower alkyl group, etc.; R4 is H, a lower alkyl group, COOH, etc.; R5 is a lower alkyl group which may optionally be substituted by an optionally substituted aryl etc.; one of X and Y is CH and the other is nitrogen, or both of X and Y are nitrogen; or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent PDE V inhibitory activities, and being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.
Abstract: A compound of the formula: wherein R1 is an aliphatic hydrocarbon group optionally having substituent(s), an aromatic hydrocarbon group optionally having substituent(s), a heterocyclic group optionally having substituent(s), a group of the formula: OR1a wherein R1a is a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), or a group of the formula: wherein R1b and R1c are the same or different and each is a hydrogen atom or an aliphatic hydrocarbon group optionally having substituent(s), X is a methylene group, a nitrogen atom, a sulfur atom or an oxygen atom, Y is an optionally substituted methylene group or an optionally substituted nitrogen atom, ring A is a 5 to 8-membered ring optionally substituted further by 1 to 4 substituent(s) selected from (1) an aliphatic hydrocarbon group optionally having substituent(s), (2) an aromatic hydrocarbon group optionally having substituent(s), (3) a group of the formula: OR2 wherein R2 is a hydrogen atom, or an aliphatic hydrocarb
Type:
Grant
Filed:
August 3, 2000
Date of Patent:
July 18, 2006
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Norikazu Tamura, Takashi Ichikawa, Masayuki Ii
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
September 3, 2003
Date of Patent:
July 18, 2006
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, Inc.
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
Abstract: The invention provides novel soluble conazole crystalline forms (e.g. itraconazole, posaconazole and saperconazole) that include salts, co-crystals and related solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, these conazole crystalline forms. Methods of using such compositions for the treatment or prevention of systemic and local fungal, yeast, and dermatophyte infections are also provided.
Type:
Grant
Filed:
May 30, 2003
Date of Patent:
July 18, 2006
Assignee:
TransForm Pharmaceuticals, Inc.
Inventors:
Jules Remenar, Michael MacPhee, Matthew Lynn Peterson, Sherry Lynn Morissette, Orn Almarsson
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
September 3, 2003
Date of Patent:
July 11, 2006
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, Inc.
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
Abstract: 6-(2-Chloro-6-fluoro-phenyl)-triazolopyrimidines of formula (I), in which R1 and R2 independently denote hydrogen or alkyl, alkenyl, alkynyl, alkadienyl, or haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or where R1 and R2 radicals may be unsubstituted or partially or fully halogenated or may be substituted as defined in the description.
Type:
Grant
Filed:
April 6, 2002
Date of Patent:
July 4, 2006
Assignee:
BASF Aktiengesellschaft
Inventors:
Jordi Tormo i Blasco, Hubert Sauter, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
Abstract: A Compound of formula (wherein X is O or S and R1–R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (each being a “Piperazine Compound”), pharmaceutical compositions comprising a Piperazine Compound and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperazine Compound are disclosed.
Abstract: The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases associated with carboxypeptidase U. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds: to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
Abstract: The present invention provides for triazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, R4, and R5 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
Type:
Grant
Filed:
July 29, 2004
Date of Patent:
July 4, 2006
Assignee:
Bristol-Myers Squibb Company
Inventors:
Donald Combs, Charles M. Langevine, Yuping Qiu, Fred Christopher Zusi
Abstract: The invention describes the synthesis of a panel of novel carbon-carbon linked carboranyl-containing 5,10,15,20-tetraphenylporphyrins bearing 25–44% boron by weight. In certain embodiments, a phenyl porphyrin compound has a carboranyl group attached to the phenyl group by a carbon-carbon linkage, wherein the phenyl group corresponds to the following formula where R7 through R11 are hydrogen, a carboranyl group, or are selected from the group consisting of hydroxyl, NMe3+, PMePh2+, PO(OH)2, SO3H, COOH, and NH2. In this embodiment, the carboranyl group is attached to the phenyl group by a carbon-carbon linkage, either one or two of R7 through R11 are other than hydrogen; and the phenyl porphyrin compound contains at least one phenyl group having at least one of said carboranyl groups.
Type:
Grant
Filed:
May 9, 2001
Date of Patent:
June 27, 2006
Assignee:
The Regents of the University of California
Inventors:
Maria Da Graca H. Vicente, Shankar Jayaram Shetty, Laurent Jaquinod, Kevin M. Smith
Abstract: The present invention provides compounds of Formula I: wherein the variables A, B, Ar, R1, R2, and R3 are as defined herein. The compounds of Formula (I) can function as corticotropin releasing factor (CRF) receptor antagonists and can be useful, for example, in the treatment of disorders characterized by abnormal levels of CRF such as anxiety and depression.
Type:
Grant
Filed:
September 26, 2003
Date of Patent:
June 27, 2006
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thais Motria Sielecki-Dzurdz, Argyrios George Arvanitis, Carolyn Diane Dzierba
Abstract: A reactive oxygen generating enzyme inhibitor with NO donor bioactivity, e.g., nitrated allopurinol, e.g., 1,5-bis(3-nitrooxypropyyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one is useful to treat heart failure, stable angina, ischemic disorder, ischemic reperfusion injury, atherosclerosis, sickle cell disease, diabetes, Alzheimer's disease, Parkinson's disease, ALS and asthma and to obtain proper contraction of heart, skeletal and smooth muscle. Where the disorder is heart failure, administration of the enzyme inhibitor mediates amelioration of acute coronary symptoms and/or myocardial infarction.
Type:
Grant
Filed:
April 23, 2004
Date of Patent:
June 27, 2006
Assignees:
Duke University, Johns Hopkins University
Inventors:
Jonathan S. Stamler, Eric J. Toone, Joshua M. Hare
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
September 3, 2003
Date of Patent:
June 27, 2006
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, Inc.
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Carmen S. Alvarez, Tin-Yau Chan, Chad Knutson, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
Abstract: There is provided a process for the production a compound of general formula I: wherein A, R1, R2, R3 and R4 have meanings given in the description, which process comprises the dehydrogenation of a compound of general formula II,
Type:
Grant
Filed:
December 1, 2003
Date of Patent:
June 27, 2006
Assignee:
Pfizer Inc.
Inventors:
Mark Edward Bunnage, Philip Charles Levett, Nicholas Murray Thomson
Abstract: Provided herein is a compound having the formula (Ia): wherein said compounds are useful for the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease and pain.
Abstract: New compounds having a tricyclic pyrazolotriazolopyrimidine ring structure are provided and methods of using those compounds for a variety of therapeutic indications.
Type:
Grant
Filed:
May 30, 2003
Date of Patent:
June 20, 2006
Assignee:
King Pharmacueticals Reserch and Development, Inc.
Inventors:
Pier Giovanni Baraldi, Pier Andrea Borea
Abstract: The present invention relates to 5-aminomethylpyrazolo[4,3-d]pyrimidines of the general formula (I) in which the radicals R1 to R6 have the meaning indicated in the text. The compounds show phosphodiesterase V inhibition and can be employed for the treatment of conditions of the cardiovascular system and for the treatment of potency disorders.
Type:
Grant
Filed:
June 28, 2001
Date of Patent:
June 13, 2006
Assignee:
Merck Patent GmbH
Inventors:
Rochus Jonas, Pierre Schelling, Maria Christadler, Norbert Beier
Abstract: This invention relates to new therapeutically useful 8-(disubstituted)phenyl-6,9-dihydro-5H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-c]pyrimidine-5-one and 8-phenyl-6,9-dihydro-5H-pyrrolo[3,2-e][1,2,4]triazolo[4,3-c]pyrimidine-5-one derivatives of formula (I): wherein: —X—C—Y— represents (a) or (b) to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their medical uses as potent and selective inhibitors of phosphodiesterase 5 (PDE 5).
Type:
Grant
Filed:
August 1, 2001
Date of Patent:
June 13, 2006
Assignee:
Almirall Prodesfarma, S.A.
Inventors:
Bernat Vidal Juan, Cristina Esteve Trias, Jordi Gracia Ferrer, José Manuel Prieto Soto
Abstract: The present invention relates to methods for the synthesis of chiral non-racemic products, e.g., enantiomerically-enriched hemiesters, from prochiral starting materials, e.g., meso anhydrides. The present invention also relates to catalysts for the aforementioned methods, and methods for synthesizing these catalysts.