Patents Represented by Attorney Paul Thompson
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Patent number: 5321031Abstract: Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent =O;or a pharmaceutically acceptable salt thereof;useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.Type: GrantFiled: September 23, 1992Date of Patent: June 14, 1994Assignee: Schering CorporationInventor: Sundeep Dugar
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Patent number: 5306817Abstract: This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an trans-azetidinone represented by the formula ##STR1## from a carboxylic acid R.sup.2 -D-CH.sub.2 -COOH, an aldehyde R.sup.1 -A-CHO and an amine RNH.sub.2, by the steps of: (a1) converting a carboxylic acid to the corresponding acid chloride; (b1) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a1); (c1) enolizing the product of step (b1) and condensing with the aldehyde; (d1) hydrolyzing the product of step (c1); (e1) condensing the product of step (d1) with the amine; and (f1) cyclizing the product of step (e1).Alternatively, the process comprises (a2) enolizing the product of step (b1) and condensing, in the presence of a Lewis acid, with a Schiff's base prepared from the aldehyde and the amine; and (b2) cyclizing the product of step (a2).Type: GrantFiled: October 19, 1992Date of Patent: April 26, 1994Assignee: Schering CorporationInventors: Tiruvettipuram K. Thiruvengadam, Chou-Hong Tann, Junning Lee, Timothy McAllister, Anantha Sudhakar
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Patent number: 5298492Abstract: Novel diamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: Z is amino, lower alkylamino, di-(lower alkyl)amino R.sup.9 C(O)NH-- or an optionally substituted guanidino group;R.sup.1 is hydrogen or R.sup.7 R.sup.8 N--;R.sup.2 is hydrogen, lower alkyl, cyclolower alkyl, aryllower alkyl or heteroaryllower alkyl; and R.sup.3 is hydrogen, lower alkyl or cyclolower alkyl; or R.sup.2 and R.sup.3, together with the carbon to which they are attached, comprise a 3-7 membered carboxyclic ring;R.sup.4 is hydrogen, lower alkyl, aryl lower alkyl or heteroaryllower alkyl;R.sup.5 and R.sup.6 are independently hydroxy, lower alkoxy, amino, aryllower alkoxy, lower alkylamino and di-(lower alkyl)amino;R.sup.7 is R.sup.9 C(O)-- or R.sup.10 SO.sub.2 --; and R.sup.8 is hydrogen, lower alkyl, aryllower alkyl or aryl; or R.sup.7 and R.sup.8, together with the nitrogen to which they are attached, comprise a 5-7 membered ring;R.sup.Type: GrantFiled: August 4, 1992Date of Patent: March 29, 1994Assignee: Schering CorporationInventors: Bernard R. Neustadt, Elizabeth M. Smith, Deen Tulshian
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Patent number: 5288904Abstract: A process for the decomposition of trichloroacetic acid (TCAA) to form chlorides, carbonates and formates is disclosed. The process comprises treating TCAA with 6 or more equivalents of a metal hydroxide at a temperature above 60.degree. C.Type: GrantFiled: May 4, 1993Date of Patent: February 22, 1994Assignee: Schering CorporationInventors: Maurice Fitzgerald, Eithne Cantwell
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Patent number: 5256410Abstract: Human squamous cell carcinoma is successfully treated by intralesional administration of recombinant human interferon alpha-2b.Type: GrantFiled: May 20, 1991Date of Patent: October 26, 1993Assignee: Schering CorporationInventors: Daniel J. Tanner, Edwin A. Peets, Kenneth A. Smiles
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Patent number: 5247080Abstract: Disclosed herein are novel compounds of formula II ##STR1## and pharmaceutically acceptable salts thereof, wherein: Q represents H, halo or --OSO.sub.2 R" wherein R" is CH.sub.3, CF.sub.3, phenyl or tolyl;R.sup.3a represents H, alkyl, allyl, cyclopropylmethyl or COOR.sup.14 wherein R.sup.14 is alkyl, aryl, aralkyl or haloalkyl;R.sup.4 represents H, halo, alkyl, haloalkyl or alkoxy;R.sup.5a represents --OR.sup.10, --N(R.sup.9).sub.2, --O--C(R.sup.7).sub.2 .multidot.OCOR.sup.13, or alkoxy; wherein each R.sup.9 independently represents H, alkyl, alkoxy, alkoxyalkyl, aralkyl or aryl;R.sup.10 represents H, --COR.sup.9 or --CON(R.sup.9).sub.2 ; andR.sup.13 represents alkyl, aralkyl or aryl,with the proviso that R.sup.3a can not be hydrogen or alkyl when Q is hydrogen, R.sup.4 is hydrogen, and R.sup.5a is hydroxy.Compounds of formula II are useful intermediates for producing compounds having valuable pharmaceutical properties in treating psychosis, depression, pain and hypertension.Type: GrantFiled: February 21, 1991Date of Patent: September 21, 1993Assignee: Schering CorporationInventors: Joel G. Berger, Wei K. Chang, Marjorie Peters
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Patent number: 5238935Abstract: N-acyltetrahydroisoquinolines including novel compounds of the formula ##STR1## wherein R.sup.1 is a C10-C25 alkyl chain; a substituted C10-C25 alkyl chain; an interrupted C10-C25 alkyl chain; a substituted interrupted C10-C25 alkyl chain; diphenylamino; di-(R.sup.2 -substituted phenyl)amino; di-(heteroaryl)amino; di-(R.sup.2 -substituted heteroaryl)amino; diphenylmethyl; or di-(R.sup.2 -substituted phenyl)methyl;R.sup.2 is hydroxy, lower alkyl, lower alkoxy, halogeno, amino, lower alkylamino or di-(lower alkyl)amino;R.sup.3, R.sup.4 and R.sup.5 are independently H or --(CH.sub.2).sub.n --Ar;Ar is phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 - substituted heteroaryl;n=0,1 or 2;m=0,1 or 2;or a pharmaceutically acceptable salt thereof, useful in the treatment of atherosclerosis are disclosed.Type: GrantFiled: February 20, 1992Date of Patent: August 24, 1993Assignee: Schering CorporationInventors: Sundeep Dugar, Timothy Kogan
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Patent number: 5238950Abstract: A method of inhibiting the binding of PDGF using compounds of the formula I ##STR1## useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery is disclosed.Also disclosed are pharmaceutical compositions and novel PDGF inhibitory compounds of the formula ##STR2## or a pharmaceutically acceptable addition salt thereof, useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery.Type: GrantFiled: December 17, 1991Date of Patent: August 24, 1993Assignee: Schering CorporationInventors: John W. Clader, Harry R. Davis, Deborra Mullins, Stuart Rosenblum, Jay Weinstein
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Patent number: 5232920Abstract: Novel N-(mercaptoalkyl)amides of the formula ##STR1## wherein R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 is (COR.sub.3)-aryl, heteroaryl, substituted (COR.sub.3)-aryl or substituted heteroaryl, wherein the substituents are 1-3 substituents selected from the group consisting of carboxy, alkoxycarbonyl, lower alkyl, hydroxy, halo, lower alkoxy, cyclolower alkyl, cyano, trifluoromethyl, phenyl, phenoxy and phenylthio;R.sub.3 is --OR.sub.4 or --NR.sub.4 R.sub.5 ;R.sub.4 and R.sub.5 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;Q is hydrogen or R.sub.6 CO--;R.sub.Type: GrantFiled: December 21, 1990Date of Patent: August 3, 1993Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 5227494Abstract: A novel process for regioselectively preparing oxazoline compounds is disclosed. The process utilizes an amino alcohol, a cyano compound, a base and a dihydric alcohol solvent, a polyhydric alcohol solvent or mixtures thereof.Type: GrantFiled: June 29, 1992Date of Patent: July 13, 1993Assignee: Schering CorporationInventors: Doris P. Schumacher, Jon E. Clark, Bruce L. Murphy
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Patent number: 5208236Abstract: Novel glutarylamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: R.sup.1 and R.sup.3 are independently hydroxy, lower alkoxy, aryllower alkoxy, amino, lower alkylamino and di-(lower alkyl)amino;R.sup.2 is H or hydroxy;R.sup.4 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;R.sup.6 is H or R.sup.7 --(CH.sub.2).sub.3 --, wherein R.sup.7 is amino or (aryllower alkoxy)carbonylamino;Q is --C(O)-- or --SO.sub.2 --;Y is lower alkyl, lower alkoxy, aryllower alkoxy, amino, lower alkylamino, di-(lower alkyl)amino, or a group of the formula ##STR2## wherein A is a bond, --N(R.sup.5)--, or --O--; and R.sup.5 is H or lower alkyl;B is H or Z--(CH.sub.2).sub.m --Z is amino, lower alkylamino, di-(lower alkyl)amino, (aryllower alkoxy)carbonylamino, 1-pyrrolidino or 1-piperidino;m=1,2,3,4 or 5; and n=1,2 or 3; oror a pharmaceutically acceptable addition salt thereof; useful in the treatment of cardiovascular disorders, are disclosed.Type: GrantFiled: September 23, 1992Date of Patent: May 4, 1993Assignee: Schering CorporationInventor: Bernard R. Neustadt
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Patent number: 5182289Abstract: Heterobicyclic and heterocyclic intermediate compounds and their use in treating inflammation, hyperproliferative skin conditions such as psoriasis and allergy are disclosed.Type: GrantFiled: December 10, 1990Date of Patent: January 26, 1993Assignee: Schering CorporationInventors: Pauline C. Ting, Margaret H. Sherlock, Wing C. Tom, James J. Kaminski
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Patent number: 5149709Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.Type: GrantFiled: July 3, 1990Date of Patent: September 22, 1992Assignee: Schering CorporationInventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro