Abstract: The invention provides N,N?-disubstituted monothiourea or bis-thiourea-Pd(0) complexes that are useful as catalysts for palladium-catalyzed Heck reaction of aryl iodides and bromides with olefins, and as catalysts for palladium catalyzed Suzuki reactions of organoboric compounds and aryl halides.
Abstract: Pyrrolopyrimidine derivatives of the formula I in which R3, R4, R5, R6 and X are as defined in claim 1, act as phosphodiesterase VII inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.
Abstract: The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, and their use in the preparation of medicaments for the treatment of neoplastic conditions
Abstract: The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.
Type:
Application
Filed:
November 28, 2006
Publication date:
December 25, 2008
Inventors:
Melanie Schultz, Lars Thore Burgdorf, Dirk Finsinger, Andree Blaukat, Hartmut Greiner, Christina Esdar
Abstract: Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single agent or in combination with an anti-neoplastic agent or therapeutic radiation having an anti-neoplastic effect for treating diseases or conditions such as cancers. The current invention relates to the making and using of such compounds.
Type:
Grant
Filed:
June 23, 2006
Date of Patent:
December 9, 2008
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Suzanne Benedict, Michael Bennett, Sacha Ninkovic, Min Teng, Eugene Rui, Fen Wang, Yong Wang, Jinjiang Zhu
Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Type:
Grant
Filed:
August 23, 2006
Date of Patent:
November 25, 2008
Assignee:
Abbott Laboratories Inc.
Inventors:
Lisa A. Hasvold, Laura Hexamer, Gaoquan Li, Nan-Horng Lin, Hing Sham, Thomas J. Sowin, Gerard M. Sullivan, Le Wang, Ping Xia
Abstract: Disclosed herein are non-nucleoside reverse transcriptase inhibitors having structural Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and the methods of their use thereof.
Abstract: The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
Type:
Application
Filed:
December 21, 2007
Publication date:
July 3, 2008
Inventors:
James B. McAlpine, Arjun H. Banskota, Mustapha Aouidate
Abstract: This invention relates to phosphate prodrugs of a farnesylated dibenzodiazepinone, to processes of their manufacture, to pharmaceutical compositions comprising the prodrugs, and to their use in the treatment of neoplasms.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
June 10, 2008
Assignee:
Thallion Pharmaceuticals, Inc.
Inventors:
Mustapha Aouidate, James B. McAlpine, Faustinus Yeboah, Ashraf Ibrahim, Arjun H. Banskota, Maxime Ranger, Gregory L. White
Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
Type:
Application
Filed:
February 1, 2008
Publication date:
June 5, 2008
Applicant:
Bristol-Myers Squibb Pharma Company
Inventors:
Richard E. Olson, Hong Liu, Lorin A. Thompson
Abstract: The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
Type:
Grant
Filed:
September 27, 2005
Date of Patent:
December 4, 2007
Assignee:
Thallion Pharmaceuticals Inc.
Inventors:
James B. McAlpine, Arjun H. Banskota, Mustapha Aouidate
Abstract: An improved process for making 5,11-dihydro-11-ethyl-5-methyl-8-{2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-di pyrido[3,2-b:2?,3?-e][1,4]diazepin-6-one.
Type:
Grant
Filed:
November 16, 2006
Date of Patent:
October 16, 2007
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Saeed Ahmad, Robert Frederick Boswell, Jr., Jack Delbert Brown, Cary Mark Davis, Kai Oliver Donsbach, Bernard Franklin Gupton, Christopher Peter Johnson, III, Ahmad Khodabocus, Vithalanand R. Kulkarni, Young S. Lo
Abstract: The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
Abstract: Compounds of the Formula I: wherein m, n, k, A, X, Y, Z, Ar, R1, R2, R3, and R4 are as defined herein. The compounds are useful as 5-HT6 receptor antagonists. Also provided are compositions comprising, methods of using, and methods of making the subject compounds.
Type:
Grant
Filed:
December 9, 2005
Date of Patent:
June 12, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
Abstract: The invention provides a process for making compounds of the general formula I: wherein R2, R4, R5, R11 and Q are defined as in claim 1. The compounds of the general formula I are effective inhibitors of HIV reverse transcriptase.
Type:
Grant
Filed:
November 1, 2005
Date of Patent:
December 19, 2006
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Oliver Meyer, Ingo Heddesheimer, Georg Zerban
Abstract: Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single agent or in combination with an anti-neoplastic agent or therapeutic radiation having an anti-neoplastic effect for treating diseases or conditions such as cancers.
Type:
Grant
Filed:
July 22, 2005
Date of Patent:
November 7, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Suzanne Benedict, Michael Bennett, Sacha Ninkovic, Min Teng, Eugene Rui, Fen Wang, Yong Wang, Jinjiang Zhu
Abstract: Compounds represented by formula I: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or (C1-4)alkyl; R3 is H or (C1-4)alkyl; R4 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C1-4)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C1-4)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.
Abstract: This invention relates to a novel farnesylated dibenzodiazepinone, named ECO-04601, its pharmaceutically acceptable salts and derivatives, and to methods for obtaining such compounds. One method of obtaining the ECO-04601 compound is by cultivation of a novel strain of Micromonospora sp., 046-ECO11; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to Micromonospora sp. strain 046-ECO11, to the use of ECO-04601 and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of cancer cell growth, bacterial cell growth, mammalian lipoxygenase, and to pharmaceutical compositions comprising ECO-04601 or a pharmaceutically acceptable salt or derivative thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of ECO-04601.
Type:
Grant
Filed:
January 21, 2004
Date of Patent:
September 5, 2006
Assignee:
Ecopia BioSciences, Inc.
Inventors:
Brian O. Bachmann, James B. McAlpine, Emmanuel Zazopoulos, Chris M. Farnet, Mahmood Piraee
Abstract: Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single agent or in combination with an anti-neoplastic agent or therapeutic radiation having an anti-neoplastic effect for treating diseases or conditions such as cancers.
Type:
Grant
Filed:
January 9, 2004
Date of Patent:
November 22, 2005
Assignee:
Agouron Pharmaceuticals Inc.
Inventors:
Suzanne Benedict, Michael Bennett, Sacha Ninkovic, Min Teng, Yuanjin Rui, Fen Wang, Yong Wang, Jinjiang Zhu
Abstract: The present invention relates to substituted piperidines of general formula wherein A1, A2, R, R1 and R2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
Type:
Grant
Filed:
December 22, 2000
Date of Patent:
September 27, 2005
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Klaus Rudolf, Henri Doods, Eckhart Bauer, Rudolf Hurnaus, Wolfgang Eberlein, Alexander Dreyer, Stephan Georg Mueller
Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.
Abstract: The present invention provides novel tricyclic compounds, compositions comprising these compounds and methods of using these compounds as neuroprotectants. In particular, the compounds of the invention are useful for treating stroke.
Abstract: Compounds represented by formula I:
wherein
R2 is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H or Me; R5 is H or Me; R11 is H, (C1-4)alkyl, (C3-4)cycloalkyl and (C1-4)alkyl-(C3-4)cycloalkyl; A is a connecting chain of (C1-3)alkyl; B is O or S; n is 0 or 1; wherein when n is 0:
Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted;
and E is CONR12R13; CONHNR14R15; NR16COR17; NR18SO2(C1-6)alkyl; SO2NR19R20; or SO2R21; or
when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and
Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents;
or a salt or
Type:
Grant
Filed:
May 6, 2003
Date of Patent:
October 19, 2004
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Bruno Simoneau, Serge Landry, Eric Malenfant, Julie Naud, Jeffrey O'Meara, Bounkham Thavonekham, Christiane Yoakim
Abstract: The present invention relates to novel pyrido-thieno-diazepines, their preparation process and the pharmaceutical compositions containing them.
Type:
Grant
Filed:
October 4, 2001
Date of Patent:
August 17, 2004
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Abstract: A process and novel intermediates for making compounds of the formula I:
wherein:
R2 is selected from the group consisting of H, F, Cl, C1-4 alkyl, C3-4 cycloalkyl and CF3;
R4 is H or Me;
R5 is H, Me or Et, with the proviso that R4 and R5 are not both Me, and if R4 is Me then R5 cannot be Et;
R11 is Me, Et, cyclopropyl, propyl, isopropyl, or cyclobutyl; and
Q is selected from the group consisting of:
Type:
Grant
Filed:
June 19, 2003
Date of Patent:
July 6, 2004
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Carl A. Busacca, Magnus C. Eriksson, Ji-Young Kim
Abstract: Activated haptens useful for generating immunogens to HIV protease inhibitors, immunogens useful for producing antibodies to HIV protease inhibitors, and antibodies and labeled conjugates useful in immunoassays for HIV protease inhibitors. The novel haptens feature an activated functionality at the central, non-terminal hydroxyl group common to all HIV protease inhibitors, e.g., saquinavir, nelfinavir, indinavir, amprenavir, ritonavir, lopinavir, and atazanavir.
Type:
Application
Filed:
September 24, 2003
Publication date:
July 1, 2004
Inventors:
Gerald F. Sigler, Raymond A. Hui, Ina Deras, Richard Terry Root, Mitali Ghoshal, Erasmus Huber, Herbert W. Von Der Eltz, Sigrun Metz, Peter Kern
Abstract: A compound of formula I:
wherein
A is a connecting chain of (C1-3) alkyl; B is O or S; R1 is H, (C1-6) alkyl, halo, CF3, or OR1a wherein R1a is H or (C1-6)alkyl; R2 is H or Me; R3 is H or Me; R4 is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl;
W is selected from
wherein,
a) one of Y is SO2 and the other Y is NR5, provided that both are not the same, wherein R5 is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR5o, COOR5p or CONR5pPR5q; and each R8 is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR8aR8b wherein R8a and R8b is H, or alkyl and J is CH2; or J is CR8aR8b and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR8aR8b or J is C(O) and E is CR8aR8b and the dotted line represents a single bond; or d) E and J are CR8aR8b and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.
Abstract: A pharmaceutical agent containing an NK-1 receptor antagonist, an NK-2 receptor antagonist and/or an anti-cholinergic drug in combination is provided, which is useful as a prophylactic or therapeutic agent of urinary frequency, urinary incontinence, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, osteoarthritis, pain, cough, irritable bowel syndrome, emesis, depression, anxiety, manic depressive psychosis or schizophrenia.
Abstract: Disclosed are compounds of formula I:
wherein
R2 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, NH(C1-4alkyl) or N(C1-4alkyl)2;
R4 is H or CH3;
R5 is H or CH3;
R12 is H, halogen, (C1-4)alkyl, CF3, or NO2;
R13 is H, (C1-4)alkyl, halogen, OH, or NH2, with the proviso that R12 and R13 are not both H; and
R14 is COOR14a wherein R14a is H or (C1-6)alkyl; or R14 is (C2-4)alkenyl-COOR14a
wherein R14a is as defined herein; or R14 is (C1-4)alkyl-COOR14a wherein R14a is as defined above;
or a salt or a prodrug thereof, useful as inhibitors of HIV reverse transcriptase.
Abstract: The invention relates to pharmaceutically active substances from the group comprising midazolam and compounds with a methyl-substituted nitrogen atom that is the ring atom of a nitrogenous heterocycle. These substances are used to reduce the oxygen consumption during a physical activity. They can be administered together with an effective amount of D-glucose, D-maltose, ethanol, a glucogenic amine, a glucogenic amino acid or an amino acid metabolizable via glyoxylate or a dipeptide or a pharmaceutically acceptable salt of such an amino acid and an effective amount of thiamine, of a pharmaceutically acceptable thiamine salt or of a combination of folic acid and cyanocobalamine, with the proviso that the third component is thiamine or a pharmaceutically acceptable thiamine salt if the second component is D-glucose, D-maltose, a glucogenic amine, a glucogenic amino acid non-metabolizable via glyoxylate, or a dipeptide or a pharmaceutically acceptable salt of such an amino acid.
Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I)
effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
Abstract: A process for making nevirapine, comprising the following steps:
(a) reacting a 2-halo-3-pyridinecarbonitrile of the formula
wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, with cyclopropylamine, to yield 2-(cyclopropylamino)-3-pyridinecarbonitrile;
(b) hydrolyzing the 2-(cyclopropylamino)-3-pyridinecarbonitrile to yield 2-(cyclopropylamino)-3-pyridine carboxylic acid;
(c) isolating the 2-(cyclopropylamino)-3-pyridine carboxylic acid from the reaction medium;
(e) treating the 2-(cyclopropylamino)-3-pyridine carboxylic acid with a chlorinating agent, to yield 2-(cyclopropylamino)-3-pyridinecarbonyl chloride;
(f) reacting the 2-(cyclopropylamino)-3-pyridine carbonyl chloride with a 2-halo-4-methyl-3-pyridinamine of the formula
wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, to produce an N-(2-halo-4-methyl-3-pyridinyl)-2-(cyclopropylamino)-3-pyridinecarboxamide; and (g) cyclizing the N-
Type:
Grant
Filed:
June 5, 2003
Date of Patent:
January 20, 2004
Assignee:
Boehringer Ingelheim Chemicals, Inc.
Inventors:
Robert Frederick Boswell, Bernard Franklin Gupton, Young Sek Lo
Abstract: Compounds represented by formula I:
wherein R2 is H, halogen, NHNH2, (C1-4)alkyl, O(C1-6)alkyl, and haloalkyl; R4 is H or Me; R5 is H or (C1-4)alkyl; R11 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is naphthyl, fused phenyl(C4-7)cycloalkyl and fused phenyl-5, 6, or 7-membered saturated heterocycle having one to two heteroatom selected from O, N, or S, said Q being substituted with from 1 to 4 R12 substituents selected from: R13, (C1-6)alkyl, (C3-7)cycloalkyl, or (C2-6)alkenyl, said alkyl, cycloalkyl, or alkenyl being optionally substituted with R13; or a salt thereof. Compounds represented by formula I have inhibitory activity against Wild Type, single and double mutant strains of HIV.
Abstract: The invention relates to a substituted 4-trifluoromethyl carbostyril according to formula (I) and is characterised in that the 4-trifluoromethyl carbostyril is provided with an absorption maximum between 350 and 420 nm and a luminescence maximum between 430 and 900 nm. The molecule can be substituted with groups that are useful for complexing metal ions and/or for binding the molecule to relevant groups of a target molecule or a solid supporting material. The carbostyril as described above can inter alia serve as an antenna molecule of a lanthanide complex. Said complexes can be templates and can be brought into contact with a directly bound or free colour molecule which absorbs in the rant of 580-710 nm. Luminescence effects and decay periods can be measured after the contact with a relevant analyte.
Abstract: The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.
Type:
Application
Filed:
November 13, 2002
Publication date:
June 12, 2003
Inventors:
Tianbao Lu, Louis V. Lafrance, Daniel J. Parks, Karen L. Milkiewicz, Raul R. Calvo, Maxwell D. Cummings, Alexander J. Kim, Bruce L. Grasberger, Theodore E. Carver
Abstract: Pharmaceutical compositions containing Form III, Form IV, Form V olanzapine and/or pharmaceutically acceptable salts thereof. The pharmaceutical compositions are useful for the treatment of psychotic conditions, mild anxiety and gastrointestinal conditions. In particular, the compositions are useful for treating schizophrenia and related disorders, acute mania, Bipolar I Disorder, psychotic mood disorder and psychosis in patients with Alzheimer's disease.
Type:
Application
Filed:
December 27, 2001
Publication date:
November 7, 2002
Inventors:
Yusuf K. Hamied, Rajendra N. Kankan, Dharmaraj R. Rao
Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
Type:
Grant
Filed:
December 24, 1997
Date of Patent:
August 20, 2002
Assignee:
Vertex Pharmaceuticals, Incorporated
Inventors:
Michael R. Hale, Roger D. Tung, Christopher T. Baker, Andrew Spaltenstein
Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I:
or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Abstract: Provided are compounds of the general formula I:
wherein
R2 is selected from the group consisting of H, F, Cl, (C1-4) alkyl, (C3-4) cycloalkyl and CF3; R4 is H or Me; R5 is H, Me or Et, with the proviso that R4 and R5 are not both Me, and if R4 is Me then R5 cannot be Et; R11 is Et, cyclopropyl, propyl, isopropyl, or isobutyl; and
Q is selected from the group consisting of:
and pharmaceutically acceptable salts thereof, as inhibitors of HIV reverse transcriptase, wild-type and several mutant strains.
Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
Type:
Grant
Filed:
September 27, 2000
Date of Patent:
May 14, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
Abstract: An aqueous pharmaceutical suspension consisting essentially of nevirapine hemihydrate having a particle size between about 1 and 150 microns in diameter.
Type:
Grant
Filed:
March 2, 2000
Date of Patent:
July 3, 2001
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.