Patents Examined by John F. Dolan
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Patent number: 6130238Abstract: The present invention relates to novel 3-(cyclohexanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: June 19, 1998Date of Patent: October 10, 2000Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6127550Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.Type: GrantFiled: March 11, 1999Date of Patent: October 3, 2000Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Luc Grondard, Jean-Paul Casimir, Patrick Leon, Michael K. O'Brien, Matthew R. Powers, Daniel Robin
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Patent number: 6096741Abstract: Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof ##STR1## wherein R.sup.1 represents an optionally substituted aryl, an optionally substituted alkl or the like; R.sup.2 represents an optionally substituted al,y an optionally substituted alkenyl, an optionally substituted alyyl, an optionally substituted aryl, an optionally substituted heterocyclic group or the like; R.sup.3 represents an optionally substituted alkl, an optionally substituted alkenyl, an optionally substituted alkynyl, an optionally substituted arylsulfonyl, an optionally substituted heterocyclic group or the like; R.sup.4 and R.sup.5, which may be the same or different, represent each a hydrogen atom, an optionally substituted al,y or an optionally substituted allkoxy, or R.sup.4 and R.sup.5 may form together with the adjacent nitrogen atom an optionally substituted monocycle or polycycle; X and Y, which may be the same or different, represents each an oxygen atom or NR.sup.Type: GrantFiled: April 14, 1999Date of Patent: August 1, 2000Assignee: Shionogi & Co., Ltd.Inventors: Moriyasu Masui, Norihiko Tanimoto, Kuniyoshi Nishida
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Patent number: 6083903Abstract: Disclosed herein are boronic ester and acid compounds, their synthesis and uses. More specifically, disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds.Type: GrantFiled: May 16, 1995Date of Patent: July 4, 2000Assignee: LeukoSite, Inc.Inventors: Julian Adams, Yu-Ting Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
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Patent number: 6063804Abstract: Compounds of formula (I): ##STR1## wherein: R represents hydrogen, alkyl, optionally-substituted amino, or linear or branched (C.sub.1 -C.sub.6)-acyl,R.sub.1 and R.sub.2, which may be identical or different, each represents independently of the other aryl, heteroaryl, or (C.sub.5 -C.sub.7)-cycloalkyl, or one of those groups optionally substituted,A, together with the atoms in common with the pyrrole, represents saturated or unsaturated, monocyclic or bicyclic (C.sub.3 -C.sub.12)-cycloalkyl, or a saturated heterocycle having 5 to 7 ring members and containing one or two nitrogen, or 7-oxabicyclo[2.2.1]heptane, or one of those groups optionally substituted,their isomers, and also addition salts thereof with a pharmaceutically-acceptable acid or base, pharmaceutical compositions thereof, and use thereof as medicaments.Type: GrantFiled: November 25, 1998Date of Patent: May 16, 2000Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Bernard Portevin, Jacqueline Bonnet, Charles Tordjman
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Patent number: 6060492Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.Type: GrantFiled: June 25, 1997Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Anthony John Shuker, Mark Alan Winter
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Patent number: 6037362Abstract: Compounds having a .beta.-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R.sup.1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R.sup.2 represents hydrogen, hydroxymethyl, NHR.sup.3, SO.sub.2 NR.sup.4 R.sup.4', or nitro; R.sup.6 represents hydrogen or lower alkyl; and X represents nitrogen, R.sup.9 represents hydrogen, one of R.sup.7 and R.sup.8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.Type: GrantFiled: August 5, 1998Date of Patent: March 14, 2000Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Shiro Miyoshi, Kohei Ogawa
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Patent number: 6025355Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: May 19, 1997Date of Patent: February 15, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: N. Laxma Reddy, Michael Maillard, David Berlove, Sharad Magar, Graham J. Durant
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Patent number: 6017945Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R.sup.1 and R.sup.2 are optional substituents and independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl [optionally substituted by CO.sub.2 H or CO.sub.2 (C.sub.1-6 alkyl)], C.sub.2-6 alkynyl, halogen, C.sub.1-3 perfluoroalkyl, (CH.sub.2).sub.m Ar.sup.1, (CH.sub.2).sub.m Het.sup.1, (CH.sub.2).sub.m CONR.sup.7 R.sup.8, (CH.sub.2).sub.m CO.sub.2 R.sup.8, O(CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.m COR.sup.8, (CH.sub.2).sub.m OR.sup.8, O(CH.sub.2).sub.p OR.sup.8, (CH.sub.2).sub.m NR.sup.7 R.sup.8, CO.sub.2 (CH.sub.2).sub.q NR.sup.7 R.sup.8, (CH.sub.2).sub.m CN, S(O).sub.n R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, CONH(CH.sub.2).sub.m Ar.sup.1 or CONH(CH.sub.2).sub.m Het.sup.1 ; R.sup.3 represents H, C.sub.1-6, alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, SO.sub.2 R.sup.10, SO.sub.2 NR.sup.9 R.sup.10, (CH.sub.2).sub.m COR.sup.10, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (CH.sub.2).sub.m CONR.sup.9 R.sup.10, (CH.sub.2).sub.Type: GrantFiled: October 5, 1998Date of Patent: January 25, 2000Assignee: Pfizer Inc.Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
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Patent number: 5994559Abstract: The high intensity natural sweetener monatin, an .alpha.-amino acid (1) is synthesized from readily available starting materials. Regiospecific ring opening of epoxide (9) with indole magnesium bromide yields lactone (11). Amination of (11) followed by saponification yields Monatin.Type: GrantFiled: August 6, 1998Date of Patent: November 30, 1999Assignee: The Board of Governors for Higher Education, State of Rhode Island and Providence PlantationsInventors: Elie Abushanab, Subramaniam Arumugam
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Patent number: 5990151Abstract: The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]: ##STR1## wherein A is a substituted or non-substituted phenyl or thienyl; X.sup.1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C.sub.1-5 alkoxy; R.sup.1 and R.sup.2 are equally or differently hydrogen, C.sub.1-7 alkyl, C.sub.3-7 alkenyl or C.sub.3-7 alkynyl; R.sup.3 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases.Type: GrantFiled: May 15, 1998Date of Patent: November 23, 1999Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Tomoki Miyazawa, Koumei Ohta, Yutaka Kawashima, Katsuo Hatayama, deceased
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Patent number: 5973178Abstract: A compound of the formula: ##STR1## wherein: A is hydrogen, a substituted or unsubstituted C.sub.1 to C.sub.4 alkyl, a substituted or unsubstituted C.sub.1 to C.sub.4 alkoxy or a substituted or unsubstituted phenyl;W is a substituted or unsubstituted phenylene or a substituted or unsubstituted naphthylene;Y is--CH.sub.2 --CH.sub.2 --Z wherein Z is selected from --OSO.sub.3 H, --SSO.sub.3 H, --OPO.sub.3 H, --OCOCH.sub.2 --Cll.sub.3, Cl, Br or F; andm is 1 or 2, e is 0 or 1,with the sum of e+m=2.Type: GrantFiled: May 20, 1998Date of Patent: October 26, 1999Assignee: DyStar L.P.Inventors: Thomas S. Phillips, Ronald P. Pedemonte
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Patent number: 5965753Abstract: A process for preparation of a glycidyl sulfonate derivative with high purity and in high yield, which is characterized in reacting glycidol which is prepared from treating 3-chloro-1,2-propanediol in an aqueous solvent in the basic condition, without isolating the resulting glycidol with a sulfonyl halide in a two phase solvent consisting of an organic solvent and water in the presence of an inorganic base and a tertiary amine or a pyridine derivative.Type: GrantFiled: July 20, 1998Date of Patent: October 12, 1999Assignee: Daiso Co., LTd.Inventors: Midori Masaki, Yoshiro Furukawa, Keishi Takenaka
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Patent number: 5939443Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.Type: GrantFiled: June 25, 1997Date of Patent: August 17, 1999Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Christine Ann Droste, Donald Paul Matthews, John Hampton McDonald, III, Christopher John Rito, Anthony John Shuker, Mark Alan Winter