At Least Five Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/254)
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Publication number: 20040063659Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.Type: ApplicationFiled: September 18, 2003Publication date: April 1, 2004Applicant: Merrell Pharmaceuticals Inc.Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
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Patent number: 6713483Abstract: The invention provides [1,2,3]-triazolo[4,5-d]pyrimidine analogue compounds of formula (I) The invention is also directed to pharmaceutical compositions containing the compounds, processes for the preparation of the compounds and methods of treatment employing the compounds.Type: GrantFiled: May 13, 2002Date of Patent: March 30, 2004Assignee: AstraZeneca ABInventors: Simon Guile, Brian Springthorpe
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Publication number: 20040029899Abstract: The invention provides novel substituted cyclopentane compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: April 21, 2003Publication date: February 12, 2004Inventors: Simon Guile, Barrie Martin
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Publication number: 20040023988Abstract: The invention provides novel 1,2,3-triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: April 24, 2003Publication date: February 5, 2004Inventors: Roger Brown, Simon Guile, Garry Pairaudeau, Brian Springthorpe
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Publication number: 20040014759Abstract: The present invention provides compounds of Formula (I) wherein Q1, Q2, Q3, Q4, Y1, Y2, and Z are as defined in the description, and pharmaceutically acceptable salts thereof, and C1-C8 alkyl esters thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of Formula (I) and their pharmaceuticalyl acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.Type: ApplicationFiled: February 21, 2003Publication date: January 22, 2004Inventors: Joseph Armand Picard, William Howard Roark, Drago Robert Sliskovic
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Publication number: 20040014773Abstract: The invention features 2,7-disubstituted purines and their isosteres such as the corresponding 3-deazapurines and 3-deaza-8-azapurines. The compounds disclosed herein have potent anti-microbial, e.g., anti-bacterial and anti-mycoplasmal properties. The compounds described herein inhibit DNA polymerase IIIC and DNA polymerase IIIE species; the compounds thus inhibit the growth of bacteria and mycoplasmata. The compounds can be administered to prevent or to treat Gram-positive or Gram-negative bacterial or mycoplasmal infections, e.g., in eukaryotic cell cultures, animals, or humans.Type: ApplicationFiled: February 10, 2003Publication date: January 22, 2004Inventors: George E. Wright, Wei-Chu Xu, Neal C. Brown
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Publication number: 20030225098Abstract: The present application is directed to pyrazolopyrirnidine and furopyrimidine analogs of the formula (I) 1Type: ApplicationFiled: March 21, 2003Publication date: December 4, 2003Inventors: Gavin C. Hirst, Lee D. Arnold, Andrew Burchat, Neil Wishart, David Calderwood, Carol K. Wada, Michael R. Michaelides, Zhiqin Ji, Melanie Muckey
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Patent number: 6645965Abstract: Nitric acid salts with medicines having an antihypertensive activity.Type: GrantFiled: December 12, 2000Date of Patent: November 11, 2003Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Publication number: 20030199526Abstract: The present invention provides a compound of formula (I): 1Type: ApplicationFiled: December 9, 2002Publication date: October 23, 2003Inventors: Deborah Choquette, Robert J. Davies, Marion W. Wannamaker
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Patent number: 6635647Abstract: The invention provides compounds of formula (I) wherein A, B and R are as defined herein and the preparation thereof. The compounds of formula (I) are useful as somatostatin antagonists.Type: GrantFiled: September 18, 2002Date of Patent: October 21, 2003Assignee: Novartis AGInventor: Thomas J. Troxler
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Publication number: 20030181469Abstract: The invention provides new forms of a chemical compound of formula (I). The invention relates to forms fo a chemical compound (I), in particular to crystalline and amorphous forms, more particularly four crystalline forms and an amorphous form. The invention further relates to processes for the preparation of such forms, to pharmaceutical compositions comprising the compound in crystalline and/or amorphous form and to therapeutic use of such forms.Type: ApplicationFiled: December 2, 2002Publication date: September 25, 2003Inventors: Martin Bohlin, Steve Cosgrove, Bo Lassen
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Publication number: 20030148888Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.Type: ApplicationFiled: November 7, 2002Publication date: August 7, 2003Inventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
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Publication number: 20030144305Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: December 20, 2002Publication date: July 31, 2003Applicant: AstraZeneca ABInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
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Publication number: 20030144235Abstract: Compounds represented by the formula 1: 1Type: ApplicationFiled: September 9, 2002Publication date: July 31, 2003Inventors: John A. Secrist, Kamal N. Tiwari, John A. Montgomery
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Patent number: 6600038Abstract: Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.Type: GrantFiled: August 30, 2001Date of Patent: July 29, 2003Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Kazuyuki Tomisawa
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Publication number: 20030139427Abstract: This invention pertains to compounds which specifically bind to the adenosine A1, A2a, and A3 receptors and the use of these compounds to treat a disease associated with the A1, A2a, and A3 adenosine receptors in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.Type: ApplicationFiled: August 23, 2002Publication date: July 24, 2003Applicant: OSI Pharmaceuticals Inc.Inventors: Arlindo L. Castelhano, Bryan McKibben
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Publication number: 20030109484Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.Type: ApplicationFiled: June 6, 2002Publication date: June 12, 2003Inventors: James R. McCarthy, Michael L. Edwards, Donald P. Matthews
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Publication number: 20030092908Abstract: Fused heterocylic phosphodiesterase 7 (PDE 7) inhibitors of the following formula 1Type: ApplicationFiled: May 1, 2002Publication date: May 15, 2003Inventors: William J. Pitts, Joseph Barbosa, Junqing Guo
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Publication number: 20030078275Abstract: This invention describes novel pyrazole compounds of formula IIa: 1Type: ApplicationFiled: December 19, 2001Publication date: April 24, 2003Inventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M.C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
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Publication number: 20030069237Abstract: The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: ApplicationFiled: April 26, 2002Publication date: April 10, 2003Inventors: John M. Fevig, Joseph Cacciola, Charles G. Clark, Qi Han, Patrick Yuk Sun Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan, Karen A. Rossi
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Publication number: 20030064986Abstract: Process for the preparation of pyrimidone derivatives of formula I, which comprises reacting a compound of formula II with a compound of formula III in the presence of a base. The pyrimidone derivatives of formula I are useful as antifungal agents.Type: ApplicationFiled: September 9, 2002Publication date: April 3, 2003Inventors: Javier Bartroli Orpi, Manuel Anguita Lopez
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Publication number: 20030060431Abstract: Nucleoside analogues or base analogues having structure (1), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.Type: ApplicationFiled: September 3, 2002Publication date: March 27, 2003Applicant: NYCOMED AMERSHAM PLCInventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
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Patent number: 6525060Abstract: Triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation. The compounds of the invention have the formula (I) as follows: wherein R, X and R1 through R3 are as defined in the specification.Type: GrantFiled: March 8, 2000Date of Patent: February 25, 2003Assignee: Astrazeneca UK LimitedInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
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Patent number: 6525056Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.Type: GrantFiled: February 21, 2001Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
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Publication number: 20030028013Abstract: Conformationally restricted 2′, 4′-bridged nucleoside analogues are described herein. The compounds can be prepared by cyclization at C2′ and C4′ of nucleosides through a linker or linking molecule. These novel nucleosides have a desired, locked sugar pucker and are potentially useful as pharmaceutical ingredients, and especially for use in treatment of HCV.Type: ApplicationFiled: April 30, 2002Publication date: February 6, 2003Inventors: Guangyi Wang, Zhi Hong, Haoyun An
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Patent number: 6506762Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV.Type: GrantFiled: September 29, 2000Date of Patent: January 14, 2003Assignees: Neurogen Corporation, Pfizer Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Publication number: 20020165202Abstract: Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-&agr; and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses in stimuli in vivo (particularly TN-&agr;) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression. Compounds having enhanced water solubility are also described.Type: ApplicationFiled: September 13, 2001Publication date: November 7, 2002Applicant: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Howard Cottam
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Patent number: 6462044Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: August 30, 2001Date of Patent: October 8, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Patent number: 6458950Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):Type: GrantFiled: August 3, 2000Date of Patent: October 1, 2002Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Patent number: 6458796Abstract: The present invention relates to novel dihydro-[1,2,3]triazolo-[4,5-d]pyrimidin-7-one, to processes for their preparation and to their use as medicaments, in particular as inhibitors of cGMP-metabolizing phosphodiesterases.Type: GrantFiled: February 26, 2001Date of Patent: October 1, 2002Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Ulrich Niewöhner, Ulrich Rosentreter, Thomas Schenke, Erwin Bischoff, Karl-Heinz Schlemmer
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Patent number: 6455322Abstract: The invention provides a competition binding assay for detecting P2YADP receptor ligands.Type: GrantFiled: January 6, 2000Date of Patent: September 24, 2002Assignee: AstraZeneca ABInventor: Ian P. Kirk
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Publication number: 20020123629Abstract: The invention provides a compound of formula I 1Type: ApplicationFiled: February 15, 2002Publication date: September 5, 2002Inventor: Bernhard Peter Neumann
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Patent number: 6436945Abstract: The present invention provides AGT inactivating compounds, for example, substituted O6-benzyl-8-aza-guanines of the formula wherein R, for example, is pivaloyloxymethyl as well as pharmaceutical compositions comprising such compounds along with a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O6-position of guanine, by administering to a mammal an effective amount of one of the aforesaid compounds, and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O6-position of guanine.Type: GrantFiled: August 14, 2001Date of Patent: August 20, 2002Assignees: The United States of America as represented by the of Health and Human Services, The Penn State Research Foundation, Arch Development CorporationInventors: Robert C. Moschel, Anthony E. Pegg, M. Eileen Dolan, Mi-Young Chae
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Patent number: 6423716Abstract: The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and R2 represents a hydrogen atom, etc. ), OR4, or SR5; V represents an oxygen atom, a sulfur atom, N—R6, or CR7R8, at least one of X, Y and Z represents a nitrogen atom, and the others are the same or different, and each represents a nitrogen atom or C—RA; and D1, D2, D3 and D4 each independently represent C—RB, a nitrogen atom, an oxygen atom, a sulfur atom, etc., optional adjoining two among D1 to D4 are combined to represent a nitrogen atom, N—R2A, an oxygen atom, a sulfur atom, etc.Type: GrantFiled: September 29, 2000Date of Patent: July 23, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Kenji Matsuno, Yuji Nomoto, Michio Ichimura, Shin-ichi Ide, Shoji Oda
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Publication number: 20020068744Abstract: The invention provides a method of treating or inhibiting the growth of cancerous tumour cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof and further provides a method of treating or inhibiting the growth of cancerous tumour cells and associated diseases in a mammal in need thereof by interacting with tubulin and microtubules and promoting microtubule polymerization which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 29, 2001Publication date: June 6, 2002Applicant: American Home Products CorporationInventors: Mark R. Schmitt, Donald R. Kirsch, Jane E. Harris, Carl F. Beyer, Klaus-Juergen Pees, Paul A. Carter, Waldemar Pfrengle, Guido Albert
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Publication number: 20020061882Abstract: 6-(2-Trifluoromethyl-phenyl)-triazolopyrimidines of formula I 1Type: ApplicationFiled: December 12, 2000Publication date: May 23, 2002Applicant: BASF CorporationInventors: Klaus-Juergen Pees, Frank Schieweck, Jordi Tormo I Blasco, Hubert Sauter, Oliver Cullman, Bernd Muller, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Eberhard Ammermann, Siegried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20020058635Abstract: Novel purine L-nucleoside compounds are disclosed, in which both the purine rings and the sugar are either modified, functionalized, or both. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Th1 and Th2.Type: ApplicationFiled: October 30, 2001Publication date: May 16, 2002Inventor: Devron R. Averett
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Publication number: 20020055508Abstract: Compounds of general structural formula (1) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior.Type: ApplicationFiled: April 27, 2001Publication date: May 9, 2002Applicant: Cortex Pharmaceuticals, Inc.Inventors: Gary A. Rogers, Christopher M. Marrs
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Patent number: 6376667Abstract: Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.Type: GrantFiled: November 24, 1998Date of Patent: April 23, 2002Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo L. Castelhano, Hui Shao
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Patent number: 6369064Abstract: Triazolo[4,5-d]pyrimidine compounds are provided of the formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification. Compositions containing the compounds are also provided, together with processes for their preparation and methods of use in the treatment of diseases, including myocardial infarction and unstable angina.Type: GrantFiled: March 25, 1999Date of Patent: April 9, 2002Assignee: AstraZeneca ABInventors: Roger Brown, Garry Pairaudeau, Brian Springthorpe, Stephen Thom, Paul Willis
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Publication number: 20020038028Abstract: Compounds of the formula 1Type: ApplicationFiled: November 21, 2001Publication date: March 28, 2002Inventors: Daniel Yohannes, Mark W. Bundesmann
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Publication number: 20020035262Abstract: Compounds of the formula 1Type: ApplicationFiled: November 21, 2001Publication date: March 21, 2002Inventors: Daniel Yohannes, Mark W. Bundesmann
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Patent number: 6297232Abstract: The invention relates to triazolo[4,5-d]pyrimidin-3-yl derivatives which are useful in the treatment of platelet aggregation disorders.Type: GrantFiled: February 19, 1999Date of Patent: October 2, 2001Assignee: AstraZeneca ABInventors: Roger Victor Bonnert, Anthony Howard Ingall, Brian Springthorpe, Paul Andrew Willis
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Publication number: 20010025042Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): 1Type: ApplicationFiled: February 21, 2001Publication date: September 27, 2001Inventors: Argyrios Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
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Patent number: 6251910Abstract: Compounds of formula having the following stereochemistry wherein R, R1, R2, R3 and R4 are as defined in the specification. The compounds are useful as P2T receptor antagonists.Type: GrantFiled: September 21, 1998Date of Patent: June 26, 2001Assignee: AstraZeneca UK LimitedInventors: Simon Guile, Anthony Ingall, Brian Springthorpe, Paul Willis
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Patent number: 6245769Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.Type: GrantFiled: September 1, 1998Date of Patent: June 12, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
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Patent number: 6211179Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i. e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: July 6, 1999Date of Patent: April 3, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6166022Abstract: Triazolo[4,5-d]pyrimidine compounds of the formula ##STR1## where R.sup.1 through R.sup.4 and X are as defined in the specification are provided, together with compositions containing them, a process for their preparation and methods of use. The compounds are useful in the treatment of platelet aggregation disorders and angina.Type: GrantFiled: September 30, 1999Date of Patent: December 26, 2000Assignee: AstraZeneca UK LimitedInventors: Roger Brown, Garry Pairaudeau
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Patent number: 6165942Abstract: A compound represented by the general formula (I) and a salt thereof: ##STR1## wherein: Rf represents a (C.sub.1 -C.sub.4)haloalkyl group; X.about.Y represents N.dbd.N or CH.dbd.N or the like; A represents a nitrogen atom or CH; Z represents an oxygen or sulfur atom; Rg represents a hydrogen or halogen atom and the like; R1, R2, R3, R4 and R5 are each independently represent a hydrogen or halogen atom or a nitro or cyano group or the like.Type: GrantFiled: April 1, 1999Date of Patent: December 26, 2000Assignee: Nissan Chemical Industries, Ltd.Inventors: Jun Satow, Yoshihiro Kudo, Eitatsu Ikeda, Tsutomu Nawamaki, Chiaki Kawaguchi
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Patent number: RE37234Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: December 16, 1999Date of Patent: June 19, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada