Patents Represented by Attorney Stephen L. Nesbitt
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Patent number: 4508730Abstract: 1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(3H)-one derivatives of the formula ##STR1## wherein R is (C.sub.1-4)alkyl, R.sub.1 stands for hydrogen, methyl, ethyl, phenyl, bromo, chloro or nitro, R.sub.2 is hydrogen or (C.sub.1-4)alkyl, R.sub.3 represents hydrogen, chloro, fluoro, bromo, trifluoromethyl and methoxy, and X is ##STR2## wherein n is zero or 1, or --NH--R.sub.4 wherein R.sub.4 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, or phenyl group.The novel compounds are useful as anticonvulsant and anti-anxiety agents.Also encompassed by the present invention are the process for preparing the novel pyrrolodiazepines and the pharmaceutical compositions containing them.Type: GrantFiled: August 9, 1983Date of Patent: April 2, 1985Assignee: Gruppo Lepetit S.p.A.Inventors: Luigi Mariani, Giorgio Tarzia
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Patent number: 4501919Abstract: Serine derivatives are synthesized by the condensation of an alkali metal salt of a glycine derivative and a carbonyl compound in the presence of a phase transfer catalyst.Type: GrantFiled: May 22, 1980Date of Patent: February 26, 1985Assignee: Gruppo Lepetit S.p.A.Inventors: Melvin V. Koch, Ambrogio Magni
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Patent number: 4500525Abstract: The present invention is directed to new pyrazolo/4,3-c/pyridines, the process for their preparation, the pharmaceutical compositions containing them and their use as pharmocologically active substances. The compounds of the invention possess cardiotonic, antihypertensive, CNS depressant, neuroleptic, and analgesic activity.Type: GrantFiled: February 15, 1983Date of Patent: February 19, 1985Assignee: Gruppo Lepetit S.p.A.Inventors: Giorgio Winters, Alberto Sala, Domenico Barone
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Patent number: 4499072Abstract: This invention relates to the improvement of the polyamine depletion effects of ornithine decarboxylase inhibitors and/or S-adenosylmethionine decarboxylase inhibitors, the improvement being effected by the use of interferon in conjunctive therapy with said inhibitors.Type: GrantFiled: January 24, 1983Date of Patent: February 12, 1985Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Sai P. Sunkara, Nellikunja J. Prakash
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Patent number: 4496743Abstract: This invention relates to 1-[(2-acylthiocycloalkyl)carbonyl]-L-proline derivatives which are useful as antihypertensive agents and to a process for their preparation.Type: GrantFiled: January 26, 1983Date of Patent: January 29, 1985Assignee: Gruppo Lepetit S.p.A.Inventors: Romeo Ciabatti, Giovanna Padova
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Patent number: 4487721Abstract: The present invention is directed to a process for producing 2-amino-2-arylacetonitriles of general formula I: ##STR1## wherein R and R.sup.1 independently represent hydrogen, hydroxy, hydroxy(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.6)alkyl, 2-furyl, 2-thienyl, 4-pyridinyl, 1-pyrrolydinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-phenylpiperazinyl, or phenyl which can optionally be substituted with from 1 to 3 substituents independently selected from (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy, or R and R.sup.1 independently represent a phenyl(C.sub.1 -C.sub.4)alkyl or a phenyl(C.sub.1 -C.sub.4)alkoxy group wherein the phenyl group can be either unsubstituted or substituted as above.An arylaldehyde derivative of formula II ##STR2## is reacted with chloroform in base and in the presence of ammonia to give the 2-amino-2-arylacetonitrile derivative.Type: GrantFiled: June 7, 1983Date of Patent: December 11, 1984Assignee: Gruppo Lepetit S.p.A.Inventor: Romeo Ciabatti
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Patent number: 4479958Abstract: Methods and compositions for inhibiting herpes virus on living or non-living substrates by use of various pyridinyl ketones or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: September 13, 1978Date of Patent: October 30, 1984Assignee: The Dow Chemical CompanyInventor: Yulan C. Tong
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Patent number: 4476111Abstract: A new antibiotic, designated S/433, is disclosed which is produced in a microbiological fermentation under controlled conditions using a new strain of Streptomyces. This new antibiotic is active against gram-positive and gram-negative bacteria and is also active in inhibiting the growth of transplanted tumors.Type: GrantFiled: October 19, 1981Date of Patent: October 9, 1984Assignee: Gruppo Lepetit S.p.A.Inventors: Carolina Coronelli, Angelo Borghi, Giorgio Pirali, Giovanni Mistrello
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Patent number: 4461894Abstract: Naphth[1,2-d]imidazoles and naphth[2,1-d]oxazoles of formula ##STR1## wherein R and R.sub.1 are hydrogen, halogen, alkyl or alkoxy, R.sub.2 is hydrogen or halogen and A is one of the following moieties ##STR2## wherein R.sub.3 is alkyl, cycloalkyl, or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group in which n is 1, 2 or 3, R.sub.5 is hydrogen or alkyl, R.sub.6 is alkyl or R.sub.5 and R.sub.6 taken together with the adjacent nitrogen atom are a 4- to 7-membered saturated hetero ring which may contain a further hetero atom and optionally may be substituted, e.g., with phenyl or substituted phenyl, R.sub.4 is hydrogen, alkyl, cycloalkyl or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group, provided that one of R.sub.3 and R.sub.4 is a --(CH.sub.2).sub.n --NR.sub.5 R.sub.6 group, and R.sub.7 is --(CH.sub.2).sub.n --NR.sub.5 R.sub.6, or a pharmaceutically-acceptable acid addition salt thereof. They are made by contacting a corresponding naphth[1,2-d]imidazole or a naphth[2,1-d]oxazole wherein one of R.sub.3 and R.sub.Type: GrantFiled: April 26, 1982Date of Patent: July 24, 1984Assignee: Gruppo Lepetit S.p.A.Inventors: Amedeo Omodei-Sale, Emilio Toia
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Patent number: 4454158Abstract: Compounds of the formula ##STR1## wherein: R is phenyl, phenyl monosubstituted, disubstituted, or trisubstituted by (C.sub.1 -C.sub.8) alkyl, (C.sub.1 -C.sub.8)alkoxy, hydroxy, chlorine, bromine, iodine, fluorine, trifluoromethyl, nitro, (C.sub.1 -C.sub.6)alkylcarbonyl, benzoyl, or phenyl; 1-, or 2-naphthyl; 1-, 2-, or 3-indenyl; 1-, 2-, or 9-fluorenyl; 1-, 2-, or 3-piperidinyl; 2- or 3-pyrrolyl; 2- or 3-thienyl; 2- or 3-furanyl; 2- or 3- indolyl; 2- or 3-thianaphthenyl; or 2- or 3-benzofuranyl;R.sub.1 is hydrogen, (C.sub.1 -C.sub.8)alkyl, benzyl, or phenethyl;X and Y independently, are hydrogen, fluorine, chlorine, or bromine; andA is a divalent radical of the formula: ##STR2## wherein R.sub.2 is hydrogen, methyl, or ethyl, and m and n, independently, are an integer from 0 to 4, provided that m+n cannot be greater than 4; --(CH.sub.2).sub.p --D--(CH.sub.2).sub.Type: GrantFiled: June 1, 1981Date of Patent: June 12, 1984Assignee: Merrell Toraude et CompagnieInventor: Philippe Bey
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Patent number: 4447619Abstract: 4-alkanoylimidazol-2-ones of the following general structure which are useful as cardiotonics in the treatment of cardiac failure ##STR1## wherein Q and T are each an oxygen atom or a divalent sulfur atom; R is hydrogen, lower alkyl, lower alkylcarbonyl or benzoyl; R.sub.1 is hydrogen or lower alkyl; R.sub.2 is a lower aliphatic hydrocarbon radical, phenyl alkylene or heterocyclo alkylene; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: September 27, 1982Date of Patent: May 8, 1984Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: J. Martin Grisar, Richard A. Schnettler, Richard C. Dage
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Patent number: 4446151Abstract: Novel fluorinated diamine derivatives are inhibitors of ornithine decarboxylase enzyme and have the following general Formula I: ##STR1## wherein: R.sub.c represents hydrogen or carboxy;R.sub.1 represents hydrogen or C.sub.1 -C.sub.6 alkyl;Z represents methylene or oxygen;m and n each represent 0 or 1 but m+n=1; andp represents 1 or 2.Type: GrantFiled: August 11, 1982Date of Patent: May 1, 1984Assignee: Merrell Toraude et CompagnieInventors: Fritz Gerhart, Viviane Van Dorsselaer
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Patent number: 4439443Abstract: A method of reducing local hemorrhage and tissue necrosis resulting from the bite or sting of a venomous animal whereby an envenomated mammal is treated with a compound of the formula ##STR1## or a corresponding disulfide wherein n is 1, 2 or 3; Z is O, S or NH; R is H, a straight or branched chain lower alkyl group of from 1 to 4 carbon atoms, hydroxy, a straight or branched chain lower alkoxy group of from 1 to 4 carbon atoms, fluoro, chloro, bromo, iodo or trifluoromethyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 2, 1982Date of Patent: March 27, 1984Assignee: Richardson-Merrell Inc.Inventor: Eugene L. Giroux
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Patent number: 4437873Abstract: .alpha.-Substituted amines are described which are useful in controlling the growth of algae.Type: GrantFiled: April 15, 1982Date of Patent: March 20, 1984Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Albert Sjoerdsma
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Patent number: 4435417Abstract: 3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 stands for hydrogen, hydroxy, methoxy, ethoxy, or mono- or di-methylamino, and R.sub.4 represents hydrogen or (C.sub.1-4)alkyl.Also described and claimed are their use as antiinflammatory agents and the pharmaceutical compositions containing them.Type: GrantFiled: June 24, 1982Date of Patent: March 6, 1984Assignee: Gruppo Lepetit S.p.A.Inventors: Emilio Toja, Amedeo Omodei-Sale', Domenica Selva
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Patent number: 4418071Abstract: The use of novel imidazolecarboxylic acid derivatives of the following general structure which are useful as antihypertensives, cardiotonics and antithrombotics ##STR1## wherein Q and T are an oxygen or sulfur atom; R is hydrogen, lower alkyl, lower alkylcarbonyl or benzoyl; R.sub.1 is hydrogen or --CH(R.sub.3)R.sub.4 ; R2 is lower alkoxy, phenoxy or phenoxy substituted at the ortho, meta, or para position with lower alkyl, lower alkoxy, hydroxy, halogen, trifluoromethyl, lower alkylthio, lower alkylsulfone, or lower alkylsulfoxide; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, hydroxy, lower alkoxy, lower alkylcarbonyl, --ONO.sub.2 or halogen; and their pharmaceutically acceptable salts thereof.Type: GrantFiled: November 4, 1981Date of Patent: November 29, 1983Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Richard A. Schnettler, Richard C. Dage, J. Martin Grisar
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Patent number: 4410540Abstract: This invention relates to aroyl-2-imidazolidinones of the following general structure which are useful as cardiotonics and antihypertensive agents ##STR1## wherein Ar is furanyl, thienyl, 1H-pyrrolyl, or phenyl optionally substituted with one or two X groups; X is halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfoxide, lower alkylsulphone, trifluoromethyl, --SO.sub.2 N(R.sub.2).sub.2, NR.sub.3 R.sub.4, pyrrolidino, piperidino, morpholino, piperazino or N'-alkyl-piperazino; R is hydrogen, lower alkyl, lower alkylcarbonyl or benzoyl; each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is hydrogen or lower alkyl; T is an oxygen atom or a divalent sulfur atom; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: November 4, 1981Date of Patent: October 18, 1983Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Richard A. Schnettler, Richard C. Dage, J. Martin Grisar
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Patent number: 4405628Abstract: This invention relates to aroylimidazole-2-ones and their acid and base addition salts as well as their use as cardiotonics in the treatment of cardiac failure.Type: GrantFiled: October 23, 1981Date of Patent: September 20, 1983Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Richard C. Dage, Frank P. Palopoli, Richard A. Schnettler, J. Martin Grisar
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Patent number: 4405635Abstract: Novel 4-aroylimidazol-2-ones of the following general structure which are useful as antihypertensives, cardiotonics, antithrombotics, bronchodilators and uterospasmolytics ##STR1## wherein Ar is 2-furyl, 2-thienyl or phenyl, the latter of which may optionally be substituted with one or two X groups; X is halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, methylenedioxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfoxide, C.sub.1-4 alkylsulfone, CF.sub.3, --SO.sub.2 N(R.sub.2).sub.2, NR.sub.3 R.sub.4, pyrrolidino, piperidino, morpholino, piperazino or N'-alkyl-piperazino, R is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylcarbonyl or benzyl; each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen or C.sub.1-4 alkyl; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: September 13, 1982Date of Patent: September 20, 1983Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Richard A. Schnettler, Richard C. Dage, Johann M. Grisar
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Patent number: 4404286Abstract: An improved reagent and method for assay of total bilirubin in biological fluids utilizes diazo sulfanilic acid to convert bilirubin to azobilirubin which is then quantitatively measured. The improved reagent and method include the solvent accelerator tetramethylene sulfone. The use of tetramethylene sulfone as also allows the use of nonionic surfactants, obviating the need for serum blank correction in highly lipemic serum. Furthermore, the use of tetramethylene sulfone and nonionic surfactants renders the reagent mixture less viscous facilitating automated analysis.Type: GrantFiled: February 22, 1982Date of Patent: September 13, 1983Assignee: The Dow Chemical CompanyInventor: Bruce C. Shull