Patents Represented by Attorney John J. Killinger
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Patent number: 4282228Abstract: A process for increasing production in meat-producing, egg-laying or milk-producing animals comprising feeding a compound of the formula: ##STR1## wherein R is a member selected from the group consisting of hydrogen, R.sub.5, ##STR2## wherein R.sub.5 is alkyl of from 1 to 8 carbon atoms, inclusive, including isomeric forms thereof, alkenyl of from 2 to 8 carbon atoms, inclusive, including isomerici forms thereof, cycloalkyl of from 3 to 7 carabon atoms; or lower acyl wherein acyl is up to and including 5 carbon atoms; R.sub.1 is a member selected from the group consisting of R.sub.5 and ##STR3## wherein R.sub.6 is selected from the group consisting of hydrogen, ##STR4## or acyl wherein acyl is up to and including 5 carbon atoms; R.sub.2 is a member selected from the group consisting of hydrogen, R.sub.5, bromo of chloro; R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, provided that R.sub.3 and R.sub.4 are not both hydrogen, R.sub.Type: GrantFiled: June 23, 1980Date of Patent: August 4, 1981Assignee: The Upjohn CompanyInventors: Melvin J. DeGeeter, John M. McCall
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Patent number: 4279930Abstract: A process for treating inflammation locally or topically by administering a compound of the formula: ##STR1## wherein M and M' are hydrogen, hydroxy, halogen, lower alkyl of from 1 to 3 carbon atoms, lower alkoxy of from 1 to 3 carbon atoms; NH.sub.2, RNH, R'.sub.2 N where R is lower alkyl of from 1 to 3 carbon atoms or lower acyl of from 1 to 3 carbon atoms and R' is lower alkyl of from 1 to 3 carbon atoms; X, Y and Z are hydrogen, hydroxy, halogen, lower alkoxy of from 1 to 3 carbon atoms or lower acyloxy of from 1 to 6 carbon atoms, in association with appropriate pharmaceutical carriers.Type: GrantFiled: September 14, 1979Date of Patent: July 21, 1981Assignee: The Upjohn CompanyInventors: Charles M. Hall, Eldridge M. Glenn
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Patent number: 4264615Abstract: Pharmaceutical compositions comprising, in unit dosage form, from about 0.5 mg. to about 100 mg. of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, methyl or ethyl, and R.sub.3 is hydrogen, fluorine, chlorine, bromine, --CN, --NO.sub.2, --CF.sub.3, or alkylthio in which the alkyl is from one to three carbon atoms, inclusive; including the pharmacologically acceptable acid addition salts or H-oxides thereof, in association with a pharmaceutical carrier. The process is the administration of the above compositions to humans at a dose of from about 0.1 mg./kg./day to about 1 mg./kg./day for anti-depressant and anti-anxiety effects.Type: GrantFiled: October 4, 1979Date of Patent: April 28, 1981Assignee: The Upjohn CompanyInventor: Jackson B. Hester, Jr.
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Patent number: 4235887Abstract: This invention relates to a new method of therapy comprising the administration of a pro-drug to a human or animal, said pro-drug being a compound formed by a therapeutic compound chemically combined with another moiety by a photocleavable bond and irradiating the diseased area with ultraviolet radiation in an amount sufficient to cleave the bond and release the therapeutic compound in a therapeutically effective amount. Specifically disclosed are pro-drugs which are cleaved to therapeutically active medications which are anti-proliferative and anti-inflammatory compounds and the treatment of inflammatory and/or proliferative skin diseases therewith.Type: GrantFiled: April 13, 1977Date of Patent: November 25, 1980Assignee: The Upjohn CompanyInventors: John J. Voorhees, Wendell Wierenga
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Patent number: 4219569Abstract: A process for treating inflammation locally or topically by administering a compound of the formula: ##STR1## wherein M and M' are hydrogen, hydroxy, halogen, lower alkyl of from 1 to 3 carbon atoms, lower alkoxy of from 1 to 3 carbon atoms; NH.sub.2, RNH, R'.sub.2 N where R is lower alkyl of from 1 to 3 carbon atoms or lower acyl of from 1 to 3 carbon atoms and R' is lower alkyl of from 1 to 3 carbon atoms; X, Y and Z are hydrogen, hydroxy, halogen, lower alkoxy of from 1 to 3 carbon atoms or lower acyloxy of from 1 to 6 carbon atoms, in association with appropriate pharmaceutical carriers.Type: GrantFiled: October 10, 1978Date of Patent: August 26, 1980Assignee: The Upjohn CompanyInventor: Eldridge M. Glenn
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Patent number: 4211770Abstract: Pharmaceutical composition for treatment of proliferating skin diseases, primarily psoriasis. The compositions comprise a pharmaceutical carrier with a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of benzoyl, adamantane carboxylate or an acyl radical of an aliphatic carboxylic acid having from 2 to 18 carbon atoms inclusive including the pharmacologically acceptable acid addition salts thereof as the active compound.The compositions are administered to humans and animals systemically or topically.Type: GrantFiled: November 7, 1975Date of Patent: July 8, 1980Assignee: The Upjohn CompanyInventor: John J. Voorhees
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Patent number: 4180584Abstract: A class of new 4-amino-4-arylcyclohexanones, their ketals, and acid addition salts have been synthesized and found to be useful for relieving pain in animals. Their analgesic activity appears to be of high order, and in addition some exhibit narcotic antagonist activity that is useful in modifying the cardiovascular, respiratory, and behavioral depression caused by other analgesics. Several show mixed analgesic and narcotic antagonist activity. Preferred compounds of the class are 4-(m-hydroxyphenyl)-4-dimethylaminocyclohexanone ethylene ketal, and 4-(m-hydroxyphenyl)-4-(n-butylmethylamino)cyclohexanone ethylene ketal as free bases and as their hydrochloride salts.Processes for snythesis and intermediates are described. Unit dosage forms and therapeutic treatments are disclosed.Type: GrantFiled: October 11, 1977Date of Patent: December 25, 1979Assignee: The Upjohn CompanyInventor: Daniel Lednicer
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Patent number: 4168315Abstract: Novel compounds of Formula I: ##STR1## in association with a pharmaceutical carrier. The compositions are useful in vitro and in vivo for reduction of platelet adhesiveness and inhibition of platelet aggregation and preventing or treating disease conditions resulting from increased platelet adhesiveness or platelet aggregation.Type: GrantFiled: September 28, 1977Date of Patent: September 18, 1979Assignee: The Upjohn CompanyInventors: Ronald H. Rynbrandt, Edward E. Nishizawa
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Patent number: 4160827Abstract: This invention relates to novel compounds of the formula: ##STR1## wherein X.sup..sym. is a pharmacologically acceptable cation. The compounds are water soluble and are compounded with pharmaceutical carriers to form compositions which are useful as medical treatment for those conditions for which metronidazole is useful in treating.Type: GrantFiled: February 6, 1978Date of Patent: July 10, 1979Assignee: The Upjohn CompanyInventors: Moo J. Cho, John J. Biermacher
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Patent number: 4153707Abstract: A compound of the formula: ##STR1## wherein X is a member selected from the group consisting of hydrogen, alkyl of from 1 to 3 carbon atoms, inclusive, chlorine or bromine; Y is a member selected from the group consisting of hydrogen, chlorine or bromine and R is a member selected from the group consisting of hydrogen or lower alkyl of from 1 to 3 carbon atoms.The compounds can be applied to seeds, plants, animals, objects, or places for preventing damage due to fungi. General methods for preparing the active compounds, compositions and methods of use are shown.Type: GrantFiled: November 10, 1977Date of Patent: May 8, 1979Assignee: The Upjohn CompanyInventor: Malcolm W. Moon
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Patent number: 4139619Abstract: This invention relates to a process for stimulating the growth of mammalian hair comprising the application to mammalian skin of a compound of the formula: ##STR1## wherein R.sub.1 is a moiety selected from the group consisting of moieties of the formula ##STR2## wherein R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl, and lower cycloalkyl, and taken together R.sub.3 and R.sub.4 may be a heterocyclic moiety selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethylenimino, octamethylenimino, morpholino, and 4-lower-alkylpiperazinyl, each of said heterocyclic moieties having attached as substituents on the carbon atoms 0-3 lower alkyl groups, hydroxy or alkoxy wherein R.sub.Type: GrantFiled: August 19, 1977Date of Patent: February 13, 1979Assignee: The Upjohn CompanyInventor: Charles A. Chidsey, III
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Patent number: 4134913Abstract: Novel pesticidal compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl of from 1 to 4 carbon atoms; R.sub.2 is hydrogen, halogen or lower alkyl of from 1 to 4 carbon atoms; R.sub.3 and R.sub.4 are the same or different and are hydrogen, alkyl of 1 to 8 carbon atoms, inclusive; haloalkyl, arylalkyl and ##STR2## WHEREIN ALKYL IS FROM 1 TO 4 CARBON ATOMS, CYCLOALKYL OF FROM 3 TO 6 CARBON ATOMS, ARYL AND R.sub.3 and R.sub.4 taken together are a member selected from the group piperidine, morpholine, pyrazole, tribromopyrazole, N-methylpiperazine, pyrrole, pyrrolidine, pyrrolidone.The compounds are combined with carriers to prepare compositions and are useful in controlling insect pests either as an insecticide or behavioral modifier and are particularly effective as miticides.Type: GrantFiled: April 28, 1977Date of Patent: January 16, 1979Assignee: The Upjohn CompanyInventor: Victor L. Rizzo
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Patent number: 4132804Abstract: A process for the therapeutic and prophylactic treatment of allergy by the systemic administration of a compound of the formula: ##STR1## wherein Y is lower alkyl of 1 to 8 carbon atoms, cyclopropyl, ethinyl, --CF.sub.3, --F, --Cl, --OCH.sub.3, --OCHF.sub.3, --OCH.sub.2 OCH.sub.3, --SCH.sub.3, --SCHF.sub.2, --SCH.sub.2 OCH.sub.3, acetyl; R.sub.1 and R.sub.2 are H, CH.sub.3, CHF.sub.2, or taken together are .dbd.CH.sub.2 or .dbd.CF.sub.2 ; and X is hydrogen, lower alkyl of 1 to 8 carbon atoms or a pharmacologically acceptable cation in association with a pharmaceutical carrier.Type: GrantFiled: April 28, 1977Date of Patent: January 2, 1979Assignee: The Upjohn CompanyInventor: Margaret E. Greig
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Patent number: 4115649Abstract: The present invention discloses amides and thioamides substituted in the .alpha. or .beta. position with substituted pyrazoles which are useful as herbicides.Type: GrantFiled: October 27, 1977Date of Patent: September 19, 1978Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Gabriel Kornis
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Patent number: 4113866Abstract: Novel compounds of the formula: ##STR1## wherein R.sub.1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH.sub.2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R.sub.2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R.sub.5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.Type: GrantFiled: April 1, 1977Date of Patent: September 12, 1978Assignee: The Upjohn CompanyInventor: Daniel Lednicer
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Patent number: 4113956Abstract: The present invention discloses amides and thioamides substituted in the .alpha. or .beta. position with substituted pyrazoles which are useful as herbicides.Type: GrantFiled: October 27, 1977Date of Patent: September 12, 1978Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Gabriel Kornis
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Patent number: 4113955Abstract: The present invention discloses amides and thioamides substituted in the .alpha. or .beta. position with substituted pyrazoles which are useful as herbicides.Type: GrantFiled: October 27, 1977Date of Patent: September 12, 1978Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Gabriel Kornis
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Patent number: 4111941Abstract: The present invention discloses amides and thioamides substituted in the .alpha. or .beta. position with substituted pyrazoles which are useful as herbicides.Type: GrantFiled: October 27, 1977Date of Patent: September 5, 1978Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Gabriel Kornis
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Patent number: 4111939Abstract: The present invention discloses amides and thioamides substituted in the .alpha. or .beta. position with substituted pyrazoles which are useful as herbicides.Type: GrantFiled: October 27, 1977Date of Patent: September 5, 1978Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Gabriel Kornis
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Patent number: 4110161Abstract: A process for inhibiting platelet aggregation by the addition of a member selected from the group consisting of a compound of the formula: ##STR1## wherein Y is lower alkyl of 1 to 8 carbon atoms, cyclopropyl, ethinyl, -CF.sub.3, -F, -Cl, -OCH.sub.3, -OCHF.sub.3, -OCH.sub.2 OCH.sub.3, -SCH.sub.3, -SCHF.sub.2, -SCH.sub.2 OCH.sub.3, acetyl; R.sub.1 and R.sub.2 are H, CH.sub.3, CHF.sub.2, or taken together are .dbd.CH.sub.2 or .dbd.CF.sub.2 ; and X is hydrogen, lower alkyl of 1 to 8 carbon atoms or a pharmacologically acceptable cation, to in vivo and in vitro platelet systems. In vitro systems include whole blood as kept in blood banks, whole blood as used in heart-lung machines, and platelet rich concentrates. In vivo systems include human or animal bodies. The process provides a means for treating hemorrhage due to thrombocytopenia which in turn is caused by irradiation, cancer chemotherapy, or immunosuppressants as well as hemophilia due to congenital defects.Type: GrantFiled: March 7, 1977Date of Patent: August 29, 1978Assignee: The Upjohn CompanyInventor: Neel C. Sekhar