Abstract: 2,3-Dihydrobenzofuran derivatives of general formula (1):
wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or sulfur atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.
Abstract: A process for the preparation of 1,5-dideoxy -1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.
Type:
Grant
Filed:
October 4, 2001
Date of Patent:
January 27, 2004
Assignee:
Board of Trustees of Michigan State University
Inventors:
Rawle I. Hollingsworth, Gabriela Pistia-Brueggeman
Abstract: Ligands of formula (V);
bis-aryliminepyridine MXn complexes comprising a ligand of formula (V), wherein M is a metal selected from Fe and Co, n is 2 or 3, and X is halide, optionally substituted hydrocarbyl, alkoxide, amide, or hydride; [bis-aryliminepyridine MYp.Ln+] [NC31 ]q complexes, comprising a ligand of formula (V), wherein Y is a ligand which may insert an olefin, M is Fe or Co, NC− is a non-coordinating anion and p+q is 2 or 3, matching the formal oxidation of the metal atom M, L is a neutral Lewis donor molecule and n=0, 1, or 2; and processes for the production of alpha-olefins from ethylene, using said complexes.
Type:
Grant
Filed:
June 28, 2001
Date of Patent:
January 27, 2004
Assignee:
Shell Oil Company
Inventors:
Eric Johannes Maria De Boer, Harry Van Der Heijden, Nicolaas Meijboom, Arie van Zon
Abstract: The present invention provides processes for purifying 6-methoxy omeprazole, products using such processes, pharmaceutical formulations using such products, and methods of using such products for gastric acid inhibition.
Type:
Grant
Filed:
April 20, 2001
Date of Patent:
January 6, 2004
Inventors:
Linda B. Whittall, Grayson Walker Stowell, Robert R. Whittle
Abstract: This invention encompasses the Form V polymorph of Compound A of structural formula:
which is useful in the treatment of cyclooxygenase-2 mediated diseases. The invention encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising the Form V polymorph of Compound A. The invention also encompasses a process for synthesizing the Form V polymorph of Compound A.
Type:
Grant
Filed:
January 14, 2003
Date of Patent:
January 6, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Louis S. Crocker, Ian W. Davies, Richard G. Osifchin, Andrew Kotliar
Abstract: The present invention relates to processes for the preparation of a compound of the formula
wherein W is nitrogen or —CR3; R1 is halogen, haloalkyl, haloalkoxy, R4S(O)n— or —SF5; R2 is hydrogen; R3 is halogen; R4 is alkyl or haloalkyl; and n is 0, 1 or 2.
Abstract: Non-steroidal compounds and compositions which are agonists, partial agonists, and antagonists for androgen receptors and methods of preparation for the non-steroidal compounds and compositions.
Type:
Grant
Filed:
August 25, 2000
Date of Patent:
December 23, 2003
Assignee:
Ligand Pharmaceuticals Inc.
Inventors:
Lawrence G. Hamann, James Kong, James P. Edwards
Abstract: The present invention relates to a process for synthesizing an anhydroecgonine derivative without using cocaine as a starting material, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative as an intermediate for the synthesis. The present invention provides a process for synthesizing an anhydroecgonine derivative which comprises reacting a cycloheptatriene derivative represented by the formula (1):
with a primary amine, a salt thereof or ammonia in the presence of a base to obtain an anhydroecgonine derivative, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative. In the formula (1), n is an integer of 0 or 1; and R1 is a cyano group in the case of n being 0, and R1 is selected from an alkyl group and an aralkyl group in the case of n being 1.
Abstract: The present invention concerns pyridine derivatives having the formula
the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein L is hydrogen; C1-6alkyl; C1-6alkyl carbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidyl; substituted piperidyl; C1-6alkylsulfonyl or arylsulfonyl; —A—B— is —CR8═CR5— or—CHR4—CHR5—; D is O or NR6; R1 is a hydrogen or C1-4alkyl; R2 is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyl oxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or substituted C1-6alkyl; or R2 is —O—R9 or —NH—R10; R3 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R2 and R1, or R2 and R3 taken together may form a bivalent radical; Q is disubstituted pyridine; R7 and R8 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cyclo alkyl; a
Type:
Grant
Filed:
September 29, 2000
Date of Patent:
December 2, 2003
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Eddy Jean Freyne, Gaston Stanislas Diels, Maria Encarnacion Matesanz-Ballesteros, Adolfo Diaz-Martinez
Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.
Type:
Grant
Filed:
October 4, 2001
Date of Patent:
November 25, 2003
Assignee:
Board of Trustees of Michigan State University
Inventors:
Rawle I. Hollingsworth, Gabriela Pistia-Brueggeman
Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.
Type:
Grant
Filed:
October 4, 2001
Date of Patent:
November 18, 2003
Assignee:
Board of Trustees of Michigan State University
Inventors:
Rawle I. Hollingsworth, Gabriela Pistia-Brueggeman
Abstract: The present invention provides a novel bioactive substance having an antiangiogenic effect.
The chemical compound represented by the formula (1)
(wherein, R1 represents hydrogen atom, aldehyde group or a lower acyl group, R2 and R3 are the same as or different from each other and represent hydrogen atom or a lower alkoxy group or are combined to represent oxygen atom, R4 represents a lower alkyl group and R5 represents hydrogen atom or a lower alkyl group, provided that compounds in which R1 is aldehyde group, R2 and R3are different from each other and are hydrogen atom or methoxy group, R4 is ethyl group and R5 is hydrogen atom are excluded), a salt thereof or a hydrate thereof was isolated from the culture broth of genus Streptomyces and the structure thereof was analyzed.
Abstract: The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino[1,2-b]quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II.
Type:
Grant
Filed:
December 12, 2000
Date of Patent:
October 14, 2003
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Abstract: A method of production of 2,4′-dipyridyl derivatives by a cross coupling reaction of a 2-halopyridine derivative and a 4-halopyridine using a nickel complex catalyst and a method of separation of a 2,4′-dipyridyl derivative from a mixture of dipyridyl isomers containing a 2,2′-dipyridyl derivative, 2,4′-dipyridyl derivative, and 4,4′-dipyridyl by using a dilute aqueous copper sulfate solution to insolubilize and remove the 2,2′-dipyridyl derivative and 4,4′-dipyridyl are disclosed.
Abstract: Orally administrable acid stable anti-ulcer benzimidazole derivatives which are polymer based. The process of preparation comprises condensing a benzimidazole with a biocompatible partially orally biodegradable synthetic cross linked polymer in aqueous medium at 5-80° C. and pH 4-11 under inert atmosphere. The weight percentage of benzimidazole with respect to the polymeric benzimidazole is 1-50. The reaction mixture is cooled and the product is isolated and dried at 25-45° C. There is also provided a formulation of the polymeric benzimidazoles in combination with pharmaceutically acceptable excipients.
Type:
Grant
Filed:
September 28, 2001
Date of Patent:
September 9, 2003
Assignee:
Kopran Research Laboratories Limited
Inventors:
Subhash Mali, Rajan Gupte, Jayant Deshpande, Kamlesh Ranbhan
Abstract: The invention discloses certain N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.
Abstract: The present invention provides novel thienopyridines, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP,
wherein X, R1, R2, R3, and R4 are defined more fully in the description. The compounds are useful in the treatment of type 1 diabetes, type 2 diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
Type:
Grant
Filed:
July 9, 2001
Date of Patent:
September 2, 2003
Assignee:
Novo Nordisk A/S
Inventors:
Henrik Sune Andersen, Thomas Kruse Hansen, Jesper Lau, Niels Peter Hundahl Moller, Ole Hvilsted Olsen, Frank Urban Axe, Farid Bakir, Yu Ge, Daniel Dale Holsworth, Luke Milburn Judge, Michael James Newman, Roy Teruyuki Uyeda, Barry Zvi Shapira
Abstract: The present invention provides processes for purifying 6-methoxy omeprazole, products using such processes, pharmaceutical formulations using such products, and methods of using such products for gastric acid inhibition.
Type:
Grant
Filed:
April 20, 2001
Date of Patent:
August 19, 2003
Inventors:
Linda B. Whittall, Grayson Walker Stowell, Robert R. Whittle
Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.
Type:
Grant
Filed:
January 7, 2003
Date of Patent:
August 12, 2003
Assignee:
Board of Trustees operating Michigan State University
Inventors:
Rawle I. Hollingsworth, Gabriela Pistia-Brueggeman