Patents Examined by E. Brendan Magrab
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Patent number: 4894386Abstract: This invention provides a series of novel heterocyclic aliphatic carboxamides of formula I in which the group >Z--Y--X< is selected from >C.dbd.CH--N<, >N--CH.dbd.C<, >C.dbd.N--N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.Type: GrantFiled: October 11, 1988Date of Patent: January 16, 1990Assignee: ICI Americas Inc.Inventors: Frederick J. Brown, Victor G. Matassa
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Patent number: 4883877Abstract: Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, for example, H, alkyl, cycloalkyl, aryl or alkaryl are suitable as an ammonium salt-forming component for acid pharmaceutical active ingredients, and in particular for the preparation of azabicyclo[3.1.1.]heptane-substituted alkanediphosphonic acids for the treatment of diseases which can be attributed to disturbances in calcium metabolism.Type: GrantFiled: October 31, 1988Date of Patent: November 28, 1989Assignee: Ciba-Geigy CorporationInventor: Alex Alder
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Patent number: 4883807Abstract: Compounds of the formula (I): ##STR1## and stereoisomers and salts thereof, wherein R.sup.1 and R.sup.2, are optionally substituted alkyl; V is either oxygen or sulphur; Y is hydrogen, optionally substituted alkyl, cyano, nitro or halogen; X is ##STR2## Z is NOR.sup.5 or ##STR3## A is CO.sub.2 R.sup.6, COR.sup.7, cyano, nitro or acylamino; B is hydrogen, optionally substituted alkyl, optionally substituted aryl, CO.sub.2 R.sup.8, COR.sup.9, cyano, nitro or acylamino, or A and B together form a ring containing one or more heteroatoms; R.sup.4 is CO.sub.2 R.sup.3 or R.sup.17 ; R.sup.12 is OR.sup.13, SR.sup.14, NR.sup.15 R.sup.16 or R.sup.18 ; R.sup.3 is optionally substituted alkyl;and R.sup.5 to R.sup.11 and R.sup.13 to R.sub.Type: GrantFiled: December 1, 1987Date of Patent: November 28, 1989Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine, Brian K. Snell
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Patent number: 4866179Abstract: An improved method of catalytic gaseous chemical synthesis of pyridine by reaction of ammonia and a carbonyl compound, preferably with added hydrogen, is described herein. The process employs as the catalyst a crystalline aluminosilicate zeolite which has been ion exchanged with a Group VIII metal of the Periodic Table. The preferred metal is palladium. Suitably, the Group VIII metal is present in an amount of about 0.01% to 5% by weight of the catalyst, preferably 0.1% to 2%. The crystalline aluminosilicate zeolite catalyst suitably has a silica to alumina mole rate of at least 15, preferably 30 to 200, and optimally, about 120 to 150. The process of the invention provides a high and selective yield of pyridine over a prolonged reaction period, and affords facile restorability of the catalyst.Type: GrantFiled: June 6, 1988Date of Patent: September 12, 1989Assignee: Dairen Chemical CorporationInventors: Wan J. Cheng, Fu S. Lin, Yuh L. Jong, Fu J. Huang
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Patent number: 4851432Abstract: This invention relates to the therapeutic uses of oligomers of 15-dehydroprostaglandin B.sub.1 and oligomers of 16, 16'-dimethyl-15-dehydro PGB.sub.1 and oligomers or other 16 carbon substituted 15-dehydro PGB.sub.1 compounds (hereinafter referred to as oligomers of PGB.sub.1) in tissue ischemia, hyposix and anoxia, (hereinafter referred to collectively as tissue ischemia) and in protecting isolated organs (hearts, kidneys etc.) and cells (whole blood, erythrocytes, platelets, etc.) during in vitro transfer and storage; and as a phamacological agent in abnormal conditions in humans and animals in which alteration in cellular calcium is a mediator in the disease process.Type: GrantFiled: May 21, 1987Date of Patent: July 25, 1989Inventor: Thomas M. Devlin
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Patent number: 4849525Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts wherein Z completes a cycloalkyl ring, a substituted cycloalkyl ring, a cycloalkenyl ring, a substituted cycloalkenyl ring or a saturated heteroalkyl ring; R.sub.2 is lower alkyl, aralkyl or aminoalkyl and X is an amino or imino acid. The compounds possess angiotensin converting enzyme inhibition activity.Type: GrantFiled: September 21, 1987Date of Patent: July 18, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Eric M. Gordon
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Patent number: 4849414Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: May 20, 1987Date of Patent: July 18, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Melanie J. Loots, Donald S. Karanewsky
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Patent number: 4847288Abstract: The present invention relates to compounds which are allenyl amines, more specifically, .beta.-ethenylidene-(substituted)ethanamines, possessing antihypertensive activity. They are prepared by a noval reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.Type: GrantFiled: February 8, 1988Date of Patent: July 11, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: James R. McCarthy, Thomas M. Bargar, Charlotte L. Barney, Donald P. Matthews, Robert J. Broersma
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Patent number: 4847294Abstract: Derivatives of 2-(Substituted sulfamyl) 6-nitrobenzoic acids are disclosed, wherein at least one of the sulfamyl substituents is selected from amino-(lower alkyl), (lower alkyl)-amino-(lower alkyl), or di(lower alkyl)-amino-(lower alkyl), hydrogen, lower alkyl, hydroxy-(lower alkyl), allyl, or when taken together with the nitrogen of the sulfamyl moiety, form a heterocyclic ring. These compounds have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.Type: GrantFiled: June 1, 1987Date of Patent: July 11, 1989Assignee: Merck & Co., Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
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Patent number: 4843085Abstract: The present invention provides pyridine derivatives of following general formula (I) or a physiologically acceptable acid addition salt thereof: ##STR1## wherein R.sub.1 is a hydrogen atom or a hydroxy group, R.sub.2 and R.sub.3, which may be the same or different, each is a lower alkyl group, and n is an integer of 1 to 6. The invention also provides for producing the pyridine derivative and pharmaceutical compositions containing the same. The compounds (I) possess anti-arrhythmic activity.Type: GrantFiled: June 29, 1988Date of Patent: June 27, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Takashi Fujikura, Yuzo Matsumoto, Masharu Asano
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Patent number: 4841070Abstract: The novel 5,6-sulfinyl-L-ascorbic acid and its stereoisomers, their manufacture by sulfinylating L-ascorbic acid or corresponding stereoisomers, compositions having oxidation-inhibiting properties which contain 5,6-sulfinyl-L-ascorbic acid or a stereoisomer thereof as well as the use of 5,6-sulfinyl-L-ascorbic acid or a stereoisomer thereof as an antioxidant are described.Type: GrantFiled: June 24, 1988Date of Patent: June 20, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Horst Pauling, Christof Wehrli
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Patent number: 4837226Abstract: A method for the treatment of cerebrovascular disorders by administering a fluorenamine, dibenzofuranamine, or dibenzothiophenamine derivative.Type: GrantFiled: April 27, 1988Date of Patent: June 6, 1989Assignee: Warner-Lambert CompanyInventors: Linda L. Coughenour, Graham Johnson