Carbon To Carbon Unsaturation, Chalcogen, Or Additional Nitrogen In The Chain Patents (Class 558/393)
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Patent number: 5175170Abstract: Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloakylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloakylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 29, 1991Date of Patent: December 29, 1992Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
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Patent number: 5130456Abstract: A bis Reissert can be formed by the initial reaction of an aliphatic or aromatic aldehyde (e.g., propionaldehyde) and primary amine (e.g., methylamine) to form a reaction product which is then reacted with a diacid chloride (e.g., adipoyl chloride).Type: GrantFiled: April 15, 1991Date of Patent: July 14, 1992Assignee: Virginia Tech Intellectual Properties, Inc.Inventors: Harry W. Gibson, Yajnanarayana H. R. Jois
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Patent number: 5066657Abstract: A crotonic acid amide derivative represented by formula (I): ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, X.sub.4, and X.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkyl group, a lower haloalkyl group, a lower haloalkoxy group, a nitro group, a substituted or unsubstituted lower alkanesulfonyl group, a substituted or unsubstituted alkanesulfonyloxy group, a substituted or unsubstituted benzenesulfonyl group, a substituted or unsubstituted benzenesulfonyloxy group, a substituted or unsubstituted phenoxy group, a substituted or unsubstituted benzyloxy group, a dialkylamino group, a mono- or di-lower alkanesulfonylamino group, a substituted or unsubstituted lower alkythio group, a --SO.sub.2 R.sub.1 wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group, a lower alkoxycarbonyloxy group, a substituted or unsubstituted alkoxycarbonyl group, a --CH.dbd.N--OR.sub.Type: GrantFiled: May 8, 1990Date of Patent: November 19, 1991Assignee: SDS Biotech K.K.Inventors: Shunji Hayashi, Satoshi Yamanaka, Sayoko Kawaguchi, Teruhiko Ishii, Toshiya Kimata, Naoaki Misu
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Patent number: 5041663Abstract: The invention relates to novel oxime ethers of the formula I ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkylthio, lower haloalkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower haloalkylsulfinyl, lower haloalkylsulfonyl or nitro, each of R.sub.2 and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or lower haloalkoxy, and Q is an unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl or cycloalkyl group, a lower alkanoyl radical, an aliphatic, cycloaliphatic, aromatic or heterocyclic acyl radical which may be substituted or unsubstituted, a carbonyl or thiocarbonyl radical, an aryl or aralkyl radical, an acylimidomethyl radical, a phthalimidomethyl radical or a heterocyclic radical.These compounds are able to act as antidotes or safeners for protecting cultivated plants from the phytotoxic action of aggressive herbicides.Type: GrantFiled: December 11, 1990Date of Patent: August 20, 1991Assignee: Ciba-Geigy CorporationInventors: Henry Martin, Urs Fricker
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Patent number: 4990683Abstract: A novel process is disclosed for the preparation of 3-pyrrolidinol compounds selected from the group having the formula: ##STR1## wherein: R is selected from hydrogen, loweralkyl, loweralkenyl, cycloalkyl, cycloalkyl-loweralkyl, phenyl-loweralkyl and substituted phenyl-loweralkyl; R.sup.1, R.sup.2, and R.sup.3 are selected from hydrogen, loweralkyl, and loweralkenyl; and the optical isomers thereof. In the process, 4-amino-3-hydroxybutyronitriles are reductively cyclized with Raney nickel to produce the 3-pyrrolidinol compound.Type: GrantFiled: January 11, 1988Date of Patent: February 5, 1991Assignee: A. H. Robins Company, IncorporatedInventor: Young S. Lo
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Patent number: 4977148Abstract: The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R.sup.1 is hydrogen or fluoro, R.sup.2 is phenyl, cycloalkyl, alkyl or alkenyl as defined herein, and R.sup.3 is hydrogen, methyl or ethyl, or R.sup.2 and R.sup.3 together form polymethylene as defined herein. The invention also includes pharmaceutical compositions containing the amide derivatives, means for the manufacture of the said derivatives and for their use in the treatment of obesity and related conditions and/or in the manufacture of novel medicaments.Type: GrantFiled: March 8, 1990Date of Patent: December 11, 1990Assignee: Imperial Chemical IndustriesInventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao, Donald Stribling
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Patent number: 4927809Abstract: Compounds of the formula IA--R--NH--CHR.sup.1 --(CH.sub.2).sub.a --NHC(.dbd.NH)NH.sub.2in whichR.sup.1 is the cyanide group,R is Pro or D--Phe--Pro,A is a hydrogen atom or a protective group customary in peptide chemistry, anda is an integer from 2 to 5, preferably 3 or 4,which are able to inhibit serine proteases, and a process for their preparation, are described.Agents containing compounds of this type can be used as anticoagulants.Type: GrantFiled: February 26, 1987Date of Patent: May 22, 1990Assignee: Behringwerke AktiengesellschaftInventor: Werner Stuber
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Patent number: 4873327Abstract: Compounds of the general formula ##STR1## in which each of A and B independently represents a halogen atom or an alkyl group; m is 0 or 1; Q represents a group of general formula ##STR2## in which R is as defined, or Q represents a group of general formula --CR.sup.2 R.sup.3 R.sup.4 in which R.sup.2, R.sup.3 and R.sup.4 are as defined; together with processes for the preparation of such compounds, pesticidal compositions containing them and their pesticidal use, and certain novel intermediates.Type: GrantFiled: March 8, 1988Date of Patent: October 10, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Martin Anderson, Anthony G. Brinnand
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Patent number: 4863966Abstract: Compounds of formula (I) are pesticides having activity against arthropods: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are H, alkyl, alkoxy, halo, cyano or trifluoromethyl, or two of R.sup.1, R.sup.2 and R.sup.3 are linked to form a 3 or 4 carbon atom group;X is O or NA where A is H or alkyl;R is H or alkyl; andR.sup.4 and R.sup.5 are H, alkenyl or haloalkenyl or optionally substituted alkyl, aryl or aralkyl, or NR.sup.4 R.sup.5 represents a heterocyclic ring; or an acid addition salt thereof.The invention further provides methods for the preparation of the compounds, pesticidal formulations containing them, and their use in controlling arthropod pests.Type: GrantFiled: February 17, 1981Date of Patent: September 5, 1989Assignee: Burroughs Wellcome Co.Inventors: Malcolm H. Black, Alexander D. Frenkel, Peter T. Roberts
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Patent number: 4741846Abstract: Novel compounds of the formula I ##STR1## are described. The radicals R.sup.1, R.sup.2 and R.sup.3 are hydroxyl-substituted alkyl, --C(R.sup.4 R.sup.5)--(CHR.sup.6).sub.m --W, --(CH.sub.2).sub.2 --OCOR.sup.10 or ##STR2## and W is --COR.sup.7, --COOR.sup.7, --CON(R.sup.9 R.sup.15) or CN. The other radicals are customary hydrocarbon radicals.The novel substances can be employed as stabilizers for organic polymers or for lubricants.Type: GrantFiled: July 24, 1985Date of Patent: May 3, 1988Assignee: CIBA-GEIGY CorporationInventor: Samuel Evans
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Patent number: 4637902Abstract: A base precursor represented by the following general formula (A) or (B): ##STR1## wherein A.sub.1, A.sub.2, A.sub.5, A.sub.6, A.sub.7, and A.sub.8 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, a substituted aryl group, an acyl group, or a heterocyclic group, and A.sub.1 and A.sub.2 can combine to form a ring and two of A.sub.5, A.sub.6, A.sub.7, and A.sub.8 can combine to form a ring, A.sub.3 and A.sub.4 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, or an aralkyl group, and A.sub.3 and A.sub.4 can combine to form a ring or A.sub.3 and A.sub.4 can be a double bond forming an imino group from ##STR2## and X represents a nucleophilic group.Type: GrantFiled: March 14, 1984Date of Patent: January 20, 1987Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroyuki Hirai, Ken Kawata
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Patent number: 4633014Abstract: Substituted 3-hydrazinopropionates comprising compounds of the general fola: ##STR1## wherein R.sup.1, R.sup.2 =H, an alkyl, a substituted alkyl, hydroxycarbonyl, alkoxycarbonyl, an aryl, an aralkyl, an unsaturated alkyl, a substituted aryl or a substituted aralkyl: ##STR2## wherein R.sup.7, R.sup.8 =H, an alkyl, an unsaturated alkyl, an aralkyl, an aryl, a substituted alkyl,R.sup.9 =OH, an alkoxy, an aralkoxy, an alkyl, an unsaturated alkyl, an aryl, a substituted aryl, an aralkyl;R.sup.4 is --C.tbd.N, --COR.sup.10, wherein R.sup.10 =OR.sup.11, NR.sup.12 R.sup.13, where R.sup.11 is H, an alkyl, an aralkyl and an alkali metal, R.sup.11 and R.sup.12 are each H, an alkyl, an aralkyl, an aryl;R.sup.5, R.sup.6 = an alkyl, an aryl, an aralkyl.Type: GrantFiled: July 6, 1984Date of Patent: December 30, 1986Assignee: Institut Organicheskogo Sinteza Akademii Nauk Latviiskoi SsrInventors: Gunar A. Bremanis, Ivars Y. Kalvinsh, Irene B. Antsena, Edmund Y. Lukevits, Maris M. Veveris, Valeryans Y. Kauss, Peter T. Trapentsier, Edvards E. Liepinsh
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Patent number: 4608385Abstract: Use of an N-phenylcarbamate of the formula: ##STR1## as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: October 22, 1982Date of Patent: August 26, 1986Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Noguchi, Toshiro Kato, Junya Takahashi, Yukio Ishiguri, Shigeo Yamamoto, Katsuzo Kamoshita