Larry K. Truesdale - San Diego CA James P. Sherbine - Voorhees NJ Benoit J. Vanasse - Collegeville PA
Assignee:
Aventis Pharmaceuticals Inc. - Bridgewater NJ
International Classification:
C07D21373
US Classification:
546296, 546297
Abstract:
The present invention is directed to a process for preparing 2,4-dihydroypyridine comprising heating a compound of the formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroy-3-nitropyridine comprising reacting 2,4-dihydroypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischeria, ameliorating ischemic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.
Stable Non-Hygroscopic Crystalline Form Of N-[N-[N-(4-(Piperidin-4-Yl)Butanoyl)-N-Ethylglycyl]Aspartyl]-L--Cyclohexyl Alanine Amide, Intermediates Thereof, And Preparation Thereof And Of Antithrombotic Azacycloalkylalkanoyl Peptides And Pseudopeptides
Zofia J. Chrzan - Sellersville PA James J. Mencel - Lansdale PA Vincent Windisch - Green Lane PA Rick G. Woodward - Harleysville PA Diane C. Salazar - late of Wayne PA Narasimha M. Vemuri - Phoenixville PA Anthony J. Gardetto - Oley PA Matthew R. Powers - Barto PA Gregory G. Kubiak - Wilmington DE Robert C. Liu - Walnut Creek CA Benoit J. Vanasse - Collegeville PA James P. Sherbine - Voorhees NJ Walter Rodriguez - Douglasville PA Adam W. Sledeski - Collegeville PA
Assignee:
Aventis Pharmaceuticals Inc. - Bridgewater NJ
International Classification:
C07K 508
US Classification:
530331, 530333, 514 19
Abstract:
The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)--cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula wherein: A, B, Z, E , E , G, R, m, n, and p are as defined herein.
Processes For The Preparation Of Pyrazolo[1,5-A]-1,3,5-Triazines And Intermediates Thereof
James P. Sherbine - Voorhees NJ, US Shawn K. Pack - Plainsboro NJ, US Jaan A. Pesti - Yardley PA, US Robert E. Yule - Green Oaks IL, US Kenneth C. McNulty - West Chester PA, US
Assignee:
Bristol-Myers Squibb Pharma Company - Princeton NJ
The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression.
Process For The Preparation Of Pyrazolo[1,5-A]-1,3,5-Triazines And Intermediates Thereof
James P. Sherbine - Voorhees NJ, US Shawn K. Pack - Plainsboro NJ, US Jaan A. Pesti - Yardley PA, US Robert E. Yule - Green Oaks IL, US Kenneth C. McNulty - West Chester PA, US
Assignee:
Bristol-Myers Squibb Pharma Company - Princeton NJ
The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression.
Process For Preparing N6-Substituted Adenosine Derivatives
Diane C. Salazar - late of Wayne PA Walter Rodriguez - Douglasville PA James P. Sherbine - Voorhees NJ Rick G. Woodward - Harleysville PA Adam W. Sledeski - Collegeville PA Matthew R. Powers - Barto PA Michael K. O'Brien - Berwyn PA
Assignee:
Aventis Pharmaceuticals Products Inc. - Collegeville PA
International Classification:
C07D40912
US Classification:
5462814
Abstract:
The invention is directed to improved methods for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.
Process For Preparing 2,4- Dihydroxypyridine And 2,4- Dihydroxy-3-Nitropyridine
Larry K. Truesdale - San Diego CA James P. Sherbine - Voorhees NJ Benoit J. Vanasse - Collegeville PA
Assignee:
Aventis Pharmaceuticals Products Inc. - Bridgewater NJ
International Classification:
C07D21369 C07D21373 C07D21378
US Classification:
546296
Abstract:
The present invention is directed to a process for preparing 2,4-dihydroxy-pyridine comprising heating a compound of the formula A ##STR1## wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroxy-3-nitropyridine comprising reacting 2,4-dihydroxypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischemia, ameliorating ischenic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.
Stable Non-Hygroscopic Crystalline Form Of N-[N-[N-4-(Piperidin-4-Yl)Butanoyl)-N-Ethylglycyl] Aspartyl]-L-.Beta.-Cyclohexyl Alanine Amide
Zofia J. Chrzan - Sellersville PA James J. Mencel - Lansdale PA Vincent Windisch - Green Lane PA Rick G. Woodward - Harleysville PA Diane C. Salazar - late of Wayne PA Narasimha M. Vemuri - Phoenixville PA Anthony J. Gardetto - Oley PA Matthew R. Powers - Barto PA Gregory G. Kubiak - Wilmington DE Robert C. Liu - Walnut Creek CA Benoit J. Vanasse - Collegeville PA James P. Sherbine - Voorhees NJ Walter Rodriguez - Douglasville PA Adam W. Sledeski - Collegeville PA
Assignee:
Aventis Pharmaceuticals Products Inc. - Collegeville PA
International Classification:
A61K 3806 C07K 500
US Classification:
514 18
Abstract:
The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)-. beta. -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E. sup. 1, E. sup. 2, G, R, m, n, and p are as defined herein.