Abstract: Disclosed is a process for forming an N-acylamino pyrazole comprising contacting a N-acyl-3-oxo-imino ether compound either with a salt of hydrazine in the presence of a base or with hydrazine.
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
July 1, 2003
Assignee:
Pharmacia Corporation
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
Abstract: Disclosed is a process comprising reacting an N-allylimino nitrobenzene compound with a diaminodinucleophile to form an &agr;-amino-N-allylamidino nitrobenzene compound and the compound itself.
Abstract: Amino pyrazole derivatives of the formula:
which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active ingredient are described. The amino pyrazole derivatives are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
March 11, 2003
Inventors:
Cheryl P. Kordik, Scott L. Dax, Chi Luo, Allen B. Reitz, James J. McNally, Timothy W. Lovenberg
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
Type:
Grant
Filed:
November 23, 2001
Date of Patent:
October 1, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II:
wherein
R is
wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms;
R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and
X is O or S;
R1 is hydrogen or a lower alkyl of 1-6 carbon atoms;
R2, R3, and R4 are each, independently, hydrogen or halogen; and
R5 is a lower alkyl of 1-6 carbon atoms;
or a pharmaceutically acceptable salt thereof.
Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I):
wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.
Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
Type:
Grant
Filed:
March 14, 2001
Date of Patent:
August 13, 2002
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: The present invention relates to compounds of formula I,
and to their pharmaceutically acceptable salts. Compounds of formula I exhibit activity as serotonin, norepinephrine, and dopamine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.
Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
Type:
Application
Filed:
June 12, 2001
Publication date:
May 16, 2002
Inventors:
Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
Abstract: N-Phenylpyrazole derivatives of the formula:
wherein
R1 represents optionally halogenated alkyl;
R2 represents halogen, cyano, nitro, cycloalkyl, alkenyl, thiocyanato, optionally alkyl substituted sulphamoyl, optionally alkyl substituted carbamoyl, alkoxycarbonyl, alkanoyl or optionally halogenated alkyl; and R3 represents a hydrogen atom or a group N″R′″ or a variety of other groupings. These compounds possess arthropodicidal, plant nematocidal, anthelmintic and anti-protozoal properties; their preparation, compositions containing them and their use are described.
Type:
Grant
Filed:
July 16, 1999
Date of Patent:
April 16, 2002
Assignee:
Rhone-Poulenc Agriculture Ltd.
Inventors:
Leslie Roy Hatton, Ian George Buntain, David William Hawkins, Edgar William Parnell, Christopher John Pearson, David Alan Roberts
Abstract: Described are substituted cyanoenamines of formula I
wherein Z, R1, R2 and R3 are defined in the description, compositions thereof and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
March 26, 2002
Assignee:
Novo Nordisk A/S
Inventors:
John Bondo Hansen, Tina Moller Tagmose, John Patrick Mogensen, Florencio Zaragoza Dorwald, Anker Steen Jorgensen
Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
Type:
Grant
Filed:
February 16, 2000
Date of Patent:
March 19, 2002
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Proudfoot, John R. Regan, Alan D. Swinamer, Hidenori Takahashi
Abstract: The invention relates to new 3-thiocarbarnoylpyrazole derivatives of the formula (I)
in which
Ar represents in each case optionally substituted phenyl or pyridyl,
R1 represents H2N—CS— and
R2 and R3 are as defined in the description,
to a plurality of processes for their preparation and to their use as pesticides.
Type:
Grant
Filed:
May 6, 1999
Date of Patent:
July 24, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Bernd Alig, Achim Bertsch, Dietmar Bielefeldt, Norbert Lui, Albrecht Marhold, Christoph Erdelen, Wolfram Andersch, Andreas Turberg, Norbert Mencke
Abstract: The invention relates to new 3-thiocarbamoylpyrazole derivatives of the formula (I) 1
Type:
Application
Filed:
May 6, 1999
Publication date:
July 12, 2001
Inventors:
BERND ALIG, ACHIM BERTSCH, DIETMAR BIELEFELDT, NORBERT LUI, ALBRECHT MARHOLD, CHRISTOPH ERDELEN, WOLFRAM ANDERSCH, ANDREAS TURBERG, NORBERT MENCKE
Abstract: Parasiticidal pyrazole derivatives of formula (I) wherein: R1 represents CN, C1-6 alkoxycarbonyl, NO2, CHO, C1-6 alkanoyl, phenyl optionally substituted by one or more halogen, or C1-6 alkyl optionally substituted by one or more halogen; R2 represents a group of formula (II), (III) or (IV) in which: R7 represents H, halogen, carbamoyl, cyano, tri(C1-6 alkyl)silyl, C1-6 alkyl (optionally substituted by one or more halogen, OH or C1-6 alkoxy), C1-6 alkoxycarbonyl, phenyl, or a 5- or 6-membered ring heterocycle which is saturated or partially or fully unsaturated and contains up to 4 hetero-atoms independently selected from up to 4 N atoms, up to 2 O atoms and up to 2 S atoms and which is attached to the alkynyl moiety by an available C, S or N atom where the valence allows; and R8, R9 and R10 each independently represents H, halogen, phenyl optionally substituted by one or more halogen, CN or C1-6 alkyl optionally substituted by one or more halogen; R3 represents H, C1-6 alkyl, halogen, NH2, NH(C1-6 alkanoyl),
Abstract: Sildenafil, a known pharmaceutical chemical useful in treatment of male sexual dysfunction, is prepared by processes in which the final chemical intermediate is of significantly lower basicity than sildenafil itself, so that sildenafil can be extracted in substantially pure form from the organic reaction mixture in which it is made by adding an aqueous medium of appropriately chosen acidic pH and causing phase shift of the sildenafil to occur selectively into the aqueous phase.
Type:
Grant
Filed:
June 3, 1998
Date of Patent:
March 20, 2001
Assignee:
Torcan Chemical Ltd.
Inventors:
Yee-Fung Lu, Casimir Antczak, Jan Oudenes, Yong Tao