Patents Examined by Barbara Cassatt
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Patent number: 4734418Abstract: Disclosed herein is an antihypertensive preparation containing, as an active component, a novel quinazoline derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.100 means a hydrogen atom or methoxy group, R.sup.200 and R.sup.300 denote individually a hydrogen atom or lower alkoxy group, R.sup.400 is a hydrogen atom or amino group, l stands for 2 or 3, and Het is a specific hetero ring group.Type: GrantFiled: December 6, 1985Date of Patent: March 29, 1988Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Keiichi Yokoyama, Koji Kato, Takumi Kitahara, Hiroyasu Ohno, Takashi Nishina, Mikio Kumakura, Akira Awaya, Takuo Nakano, Kazuyuki Watanabe, Sakae Saruta
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Patent number: 4731361Abstract: An oral antibacterial, 7beta-[(Z)-2-(2-aminothiazol-4-yl)-2-alkenoylamino]-3-cephem-4-carboxylic acid pharmaceutically acceptable ester represented by the following formula: ##STR1## (wherein R is amino or protected amino,R.sup.1 is straight, branched, or cyclic alkyl optionally substituted by alkoxy,R.sup.2 is hydrogen or a 3-substitutent of cephalosporins,R.sup.3 is a pharmaceutically acceptable ester group, andX is sulfur or sulfinyl).Type: GrantFiled: March 27, 1986Date of Patent: March 15, 1988Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hamashima, Koji Ishikura, Kyoji Minami, Tadatoshi Kubota, Tadashi Yoshida
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Patent number: 4731362Abstract: An antibacterial 3-(alkylcarbamoyloxymethyl)-3-cephem-4-carboxylic acid or its derivatives represented by the following formula ##STR1## (wherein R is hydrogen or an amino-protecting group,R.sup.1 and R.sup.2 each is the same or different 1C to 8C alkyl,R.sup.3 is hydrogen, a salt or ester forming atom or group, andX is sulfur or sulfinyl),a pharmaceutical composition containing the same, a method for treating a bacterial infection with the same, and a method for preparing the same are disclosed.Type: GrantFiled: July 23, 1986Date of Patent: March 15, 1988Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hamashima, Teruji Tsuji, Tetsuo Okada, Kyoji Minami, Hiroyuki Ishitobi, Koji Ishikura
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Patent number: 4730001Abstract: There are disclosed compounds represented by Formulas I-III: ##STR1## wherein X is an azido group or an amino group and R is hydrogen or an acyl group. These compounds are useful for the treatment of viral infections and/or as intermediates in the production of compounds which are useful in the treatment of viral infections.Type: GrantFiled: January 22, 1986Date of Patent: March 8, 1988Assignee: Southern Research InstituteInventors: Y. Fulmer Shealy, C. Allen O'Dell
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Patent number: 4728740Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.Type: GrantFiled: September 15, 1986Date of Patent: March 1, 1988Assignee: Bristol-Myers CompanyInventors: Dolatrai M. Vyas, Paul M. Skonezny
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Patent number: 4727070Abstract: The antibiotic 7-[D-2-amino-2-(4-hydroxyphenyl)acetamido]-3-[(Z)-1-propenyl]ceph-3-em-4-c arboxylic acid (BMY-28100) forms imidazolidinone derivatives on reaction with ketones. These derivatives are useful in pharmaceutical dosage forms and as intermediates for separation thereof from mixtures containing the [(E)-1-propenyl]isomer of the antibiotic.Type: GrantFiled: November 25, 1985Date of Patent: February 23, 1988Assignee: Bristol-Myers CompanyInventors: Murray A. Kaplan, Michael W. Lovell, Joseph B. Bogardus
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Patent number: 4727156Abstract: 3-(Substituting phenyl)-3-(1H-imidazol-1-ylmethyl)-2-methyl-5-{[(substituted phenyl)thio]m ethyl}isoxazolidines in which hydrogens of their phenyl rings may be replaced by halogen, lower alkoxy, lower alkyl or nitro groups, and the sulfur atom may be oxidized, are useful as antifungal agents.Type: GrantFiled: August 27, 1986Date of Patent: February 23, 1988Assignee: Pennwalt CorporationInventors: Vassil St. Georgiev, George B. Mullen
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Patent number: 4727157Abstract: 3-(substituted phenyl)-3-(1H-1,2,4-triazol-1-yl)methyl-2-methyl-5-[(substituted phenoxy)methyl]isoxazolidine derivatives in which hydrogens of their phenyl rings may be replaced by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, alkanoylamino or nitro groups are useful as antifungal agents.Type: GrantFiled: August 27, 1986Date of Patent: February 23, 1988Assignee: Pennwalt CorporationInventors: Vassil St. Georgiev, George B. Mullen
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Patent number: 4725599Abstract: Certain trans-3-[3-(3-hydroxy-2-piperidyl)-2-oxopropyl]thieno[3,2-d]pyrimidin-4(3H )-one and furo[3,2-d]pyrimidin-4(3H)-one derivatives, a method of using same as anticoccidial agents, intermediates therefor, and a process for certain intermediates therefor.Type: GrantFiled: September 8, 1986Date of Patent: February 16, 1988Assignee: Pfizer Inc.Inventors: Edward A. Glazer, James W. McFarland
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Patent number: 4725687Abstract: It is disclosed that 5-methyl-5-deazamethotrexate and 5-methyl-5-deaza-10-ethylaminopterin are more than 10 times as potent as 5-deazamethotrexate in the L1210 cell growth inhibition test.Type: GrantFiled: April 28, 1986Date of Patent: February 16, 1988Assignees: Southern Research Institute, Sloan-Kettering Institute for Cancer ResearchInventors: James R. Piper, John A. Montgomery, Francis M. Sirotnak
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Patent number: 4723021Abstract: Substituted 5-(phenoxyalkyl)-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolidine s, in which hydrogens of their benzene rings may be replaced by halogen, lower alkoxy, lower alkyl, nitro, acetamido and/or trifluoromethyl groups, are useful as antifungal agents.Type: GrantFiled: August 27, 1986Date of Patent: February 2, 1988Assignee: Pennwalt CorporationInventors: Vassil St. Georgiev, George B. Mullen
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Patent number: 4719306Abstract: Substituted 3,5-diphenyl-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolidines in which hydrogens of their phenyl rings may be replaced by halogen, lower alkoxy or lower alkyl groups are useful as antifungal agents.Type: GrantFiled: August 27, 1986Date of Patent: January 12, 1988Assignee: Pennwalt CorporationInventors: Vassil St. Georgiev, George B. Mullen
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Patent number: 4719214Abstract: There are disclosed compounds having the formula: ##STR1## wherein R is a group having the formula --C.tbd.CSi(CH.sub.3).sub.3, --C.tbd.CH, --CH.dbd.CH.sub.2, --CH.sub.2 CH.sub.2 Si(CH.sub.3).sub.3 or --CH.sub.2 X; X is bromo, chloro or iodo; and R' is hydrogen or an acyl group, with the proviso that when R is --CH.sub.2 X, R' is an acyl group. Certain of these compounds are active in inhibiting the replication of DNA viruses. Other of these compounds are useful as intermediates in the production of compounds which are active in inhibiting the replication of DNA viruses.Type: GrantFiled: July 25, 1985Date of Patent: January 12, 1988Assignee: Southern Research InstituteInventors: Y. Fulmer Shealy, C. Allen O'Dell
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Patent number: 4717767Abstract: This invention relates to a 7-amino-3-(pyrazinylmethyl)- or (pyridazinylmethyl)-cephalosporins of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents a group of the formula: ##STR2## in which R.sup.6 represents a hydrogen atom, a C.sub.1-5 alkyl group or a di-C.sub.1-5 alkylamino group; R.sup.13 represents a C.sub.1-5 alkyl group; and R.sup.28 represents an amino group.Type: GrantFiled: July 22, 1986Date of Patent: January 5, 1988Assignee: Toyama Chemical Co., Ltd.Inventors: Hiroshi Sadaki, Hiroyuki Imaizumi, Takashi Nagai, Kenji Takeda, Isao Myokan, Takihiro Inaba, Yasuo Watanabe, Yoshikazu Fukuoka, Shinzaburo Minami, Isamu Saikawa
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Patent number: 4707180Abstract: The invention relates to certain 3-isoxazolyl-2-imidazolidinone derivatives, namely 3-[5- or 3-substituted-3- or -5-isoxazolyl]-1-substituted-4- or 5-substituted amino-2-imidazolidinones and the use thereof for preemergence or postemergence control of noxious plants, i.e., weeds.Type: GrantFiled: June 14, 1985Date of Patent: November 17, 1987Assignee: PPG Industries, Inc.Inventor: James A. Schwindeman
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Patent number: 4703049Abstract: Novel compounds selected from the group consisting of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of 1,2,4-oxadiazol-5-yl and 1,3,4-thiadiazol-2-yl, both optionally substituted with alkyl of 1 to 3 carbon atoms or alkenyl of 2 to 5 carbon atoms and 1,2,4-oxadiazol-3-yl and 1,3,4-oxadiazol-2-yl, both optionally substituted with alkenyl of 2 to 5 carbon atoms, alkyl of 1 to 3 carbon atoms or alkyl of 1 to 3 carbon atoms substituted with at least one fluorine, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and alkenyl of 2 to 5 carbon atoms or together form alkylene of 3 to 5 carbon atoms, X is selected from the group consisting of --O-- and --S--, R.sub.4 is alkyl of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic sedative and hypnotic activity and a novel process and novel intermediates therefor.Type: GrantFiled: December 12, 1985Date of Patent: October 27, 1987Assignee: Roussel UclafInventors: Roger J. Gillespie, Wilfred R. Tully
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Patent number: 4703120Abstract: The synthesis of furo[3,4-d]pyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and furo[3,4-d]pyrimidine-2,4-dione derivatives are general vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.Type: GrantFiled: April 28, 1986Date of Patent: October 27, 1987Assignee: Ortho Pharmaceutical CorporationInventor: Jeffery B. Press
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Patent number: 4701528Abstract: There are disclosed compounds of Formulas I and II: ##STR1## wherein R.sup.1 and R.sup.2 may be hydrogen, lower alkyl having from 1 to 8 carbon atoms, lower alkenyl having from 3 to 6 carbon atoms, lower alkoxy having from 1 to 6 carbon atoms, hydroxy, nitro, amino, halo including chlorine, bromine, iodine, and fluorine, phenyl, alkanoyl having from 2 to 6 carbon atoms or they are bonded to one another to form a cycloalkene ring fused to the thiophene ring and having a total of from 5 to 7 annular ring carbon atoms, and R.sup.3 is an aliphatic or an aromatic group such as lower alkyl, e.g., methyl or ethyl. Such compounds are useful as intermediates in the production of tiprinast and related compounds.There is also disclosed a process for the regioselective synthesis of a compound of Formula I wherein R.sup.1 is CH.sub.3 and R.sup.2 is (CH.sub.3).sub.2 CHCH.sub.2 which comprises reacting a mixture of compounds of the following formulas: ##STR2## and ##STR3## with trichloroacetonitrile under acidic conditions.Type: GrantFiled: December 23, 1985Date of Patent: October 20, 1987Assignee: Bristol-Myers CompanyInventors: Michael D. Thompson, Gary D. Madding
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Patent number: 4698358Abstract: The use in pest control of 3-acrylaminobenzisothiazoles of the formula I ##STR1## wherein R.sub.1 is unsubstituted or substituted alkyl or phenyl, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, trifluoromethyl, amino or nitro, and R.sub.6 is hydrogen or --COR.sub.1.There are also described the novel compounds of the formula Ia ##STR2## wherein R.sub.1 ' is C.sub.1 -C.sub.10 -alkyl substituted by halogen or by C.sub.1 -C.sub.5 -alkoxy, or is unsubstituted C.sub.2 -C.sub.10 -alkyl or phenyl,R.sub.2 ', R.sub.3 ', R.sub.4 ' and R.sub.5 ' independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, trifluoromethyl, amino or nitro, andR.sub.6 ' is hydrogen or --COR.sub.1 '; orR.sub.1 ' is methyl,R.sub.2 ', R.sub.3 ', R.sub.4 ' and R.sub.5 ' independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.Type: GrantFiled: August 13, 1986Date of Patent: October 6, 1987Assignee: Ciba-Geigy CorporationInventor: Jozef Drabek
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Patent number: 4698338Abstract: O-Substituted oximinocephalosporins represented by the formula ##STR1## wherein R is a 5-membered or 6-membered heterocycle, preferably amino-substituted, e.g., 2-aminothiazol-4-yl, R.sub.1 is an arylalkyl, aryloxyalkyl, or arylthioalkyl group, especially substituted benzyl; R.sub.2 is a 1,2,4-triazin-3-yl thio group; and M is a salt or a biologically labile ester group; are potent antibacterial agents. Also provided are antibiotic formulations of said compounds and a method for treating infectious diseases in man or animals comprising the administration of said compounds.Type: GrantFiled: February 19, 1986Date of Patent: October 6, 1987Assignee: Eli Lilly and CompanyInventor: Allen S. Katner