Carbon To Carbon Unsaturation, Chalcogen, Or Additional Nitrogen In The Chain Patents (Class 558/393)
  • Patent number: 5175170
    Abstract: 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: Grant
    Filed: July 29, 1991
    Date of Patent: December 29, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
  • Patent number: 5130456
    Abstract: 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: Grant
    Filed: April 15, 1991
    Date of Patent: July 14, 1992
    Assignee: Virginia Tech Intellectual Properties, Inc.
    Inventors: Harry W. Gibson, Yajnanarayana H. R. Jois
  • Patent number: 5066657
    Abstract: 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: Grant
    Filed: May 8, 1990
    Date of Patent: November 19, 1991
    Assignee: SDS Biotech K.K.
    Inventors: Shunji Hayashi, Satoshi Yamanaka, Sayoko Kawaguchi, Teruhiko Ishii, Toshiya Kimata, Naoaki Misu
  • Patent number: 5041663
    Abstract: 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: Grant
    Filed: December 11, 1990
    Date of Patent: August 20, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Henry Martin, Urs Fricker
  • Patent number: 4990683
    Abstract: 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: Grant
    Filed: January 11, 1988
    Date of Patent: February 5, 1991
    Assignee: A. H. Robins Company, Incorporated
    Inventor: Young S. Lo
  • Patent number: 4977148
    Abstract: 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: Grant
    Filed: March 8, 1990
    Date of Patent: December 11, 1990
    Assignee: Imperial Chemical Industries
    Inventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao, Donald Stribling
  • Patent number: 4927809
    Abstract: 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: Grant
    Filed: February 26, 1987
    Date of Patent: May 22, 1990
    Assignee: Behringwerke Aktiengesellschaft
    Inventor: Werner Stuber
  • Patent number: 4873327
    Abstract: 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: Grant
    Filed: March 8, 1988
    Date of Patent: October 10, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Martin Anderson, Anthony G. Brinnand
  • Patent number: 4863966
    Abstract: 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: Grant
    Filed: February 17, 1981
    Date of Patent: September 5, 1989
    Assignee: Burroughs Wellcome Co.
    Inventors: Malcolm H. Black, Alexander D. Frenkel, Peter T. Roberts
  • Patent number: 4741846
    Abstract: 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: Grant
    Filed: July 24, 1985
    Date of Patent: May 3, 1988
    Assignee: CIBA-GEIGY Corporation
    Inventor: Samuel Evans
  • Patent number: 4637902
    Abstract: 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: Grant
    Filed: March 14, 1984
    Date of Patent: January 20, 1987
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hiroyuki Hirai, Ken Kawata
  • Patent number: 4633014
    Abstract: 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: Grant
    Filed: July 6, 1984
    Date of Patent: December 30, 1986
    Assignee: Institut Organicheskogo Sinteza Akademii Nauk Latviiskoi Ssr
    Inventors: Gunar A. Bremanis, Ivars Y. Kalvinsh, Irene B. Antsena, Edmund Y. Lukevits, Maris M. Veveris, Valeryans Y. Kauss, Peter T. Trapentsier, Edvards E. Liepinsh
  • Patent number: 4608385
    Abstract: 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: Grant
    Filed: October 22, 1982
    Date of Patent: August 26, 1986
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Noguchi, Toshiro Kato, Junya Takahashi, Yukio Ishiguri, Shigeo Yamamoto, Katsuzo Kamoshita