A Ring Or Polycyclo Ring System In A Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 564/196)
  • Patent number: 6201153
    Abstract: Midodrine hydrochloride, ±1-(2′,5′-dimethoxyphenyl)-2-glycineamido-ethanol-(1)-HCl, is prepared from a novel intermediate, 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: March 13, 2001
    Assignee: Geneva Pharmaceuticals Inc.
    Inventors: Anup K. Ray, Hiren Patel, Mahendra R. Patel
  • Patent number: 6194611
    Abstract: &agr;-Amino acid amides of formula (I) wherein the substituents are defined as follows: n is the number zero or one; R1 to R7 are as herein defined; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9 is C3-C8cycloalkyl; a C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl group substituted by one or more halogen atoms; or a group (a) wherein p and q are identical or different and are each independently of the other the number zero or one; and R13, R14, R15 and R16 are identical or different and are each independently of the others hydrogen or C1-C4alkyl; and X is hydrogen, in which case p and q must have the value zero; phenyl unsubstituted or mono- or poly-substituted by halogen, nitro, cyano, carboxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C3-C6alkenyloxy, C3-C6alkynyloxy, C3-C7cycloalkyl, C1-C6haloalcoxy, C1-C6alkylthio, C1-C6alcoxycarbonyl, C3-C6alkenyloxycarbonyl, C3-C6alkynyloxycarbonyl, C1-C6alkyl or by C1-C6alkoxy; cyano; —COOR17; —COR18 or a group (b) wherein R17 and R21 are each independently
    Type: Grant
    Filed: April 16, 1998
    Date of Patent: February 27, 2001
    Assignee: Novartis Crop Protection, Inc.
    Inventor: Martin Zeller
  • Patent number: 6194612
    Abstract: This invention features a template for synthesizing combinatorial libraries, methods of synthesizing combiatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.
    Type: Grant
    Filed: April 7, 1998
    Date of Patent: February 27, 2001
    Assignees: The Scripps Research Institute, CombiChem, Inc.
    Inventors: Dale L. Boger, Soan Cheng, Peter L. Myers
  • Patent number: 6096925
    Abstract: Disclosed is a photo-curable antifogging composition which may be applied to substrates such as glass, various plastic materials and the like to give antifogging property on the surface of these substrates. The main ingredient of the composition is a quaternary ammonium salt of the following formula (1): wherein:R.sup.1 is CH.sub.3 (CH.sub.2).sub.n CH.sub.2 or CH.sub.3 (CH.sub.2).sub.n CH.sub.2 C.sub.6 H.sub.4 wherein n is an integer from 1 to 16 inclusive;R.sup.2 and R.sup.3 are the same or different from each other, and represent CH.sub.2 .dbd.C(CH.sub.3)COOCH.sub.2 CH(OH)CH.sub.2, CH.sub.2 .dbd.CHCOOCH.sub.2 CH(OH)CH.sub.2 or H, with the proviso that R.sup.2 and R.sup.3 may not be H at the same time;R.sup.4 is H, CH.sub.3, CH.sub.3 CH.sub.2 or CH.sub.3 CH.sub.2 CH.sub.2 ; andX is CH.sub.3 OSO.sub.3, CH.sub.3 CH.sub.2 OSO.sub.3, CH.sub.3 COO, CF.sub.3 COO, CH.sub.3 (CH.sub.2).sub.n COO wherein n is an integer from 1 to 16 inclusive, CH.sub.3 (CH.sub.2).sub.7 CH.dbd.CH(CH.sub.2).sub.7 COO, C.sub.6 H.sub.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: August 1, 2000
    Assignee: Ventree Co., Ltd.
    Inventors: Haeng-Woo Lee, Young-Hoon Park, Sang-Keun Kim, Eun-A Shin
  • Patent number: 6063962
    Abstract: This invention relates to an improved process for the production of known amine compounds which are useful as medicaments.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: May 16, 2000
    Assignee: Astra Pharmaceuticals Limited
    Inventor: Alan Richard Harris
  • Patent number: 6048899
    Abstract: The present invention is directed to N-benzyl-2-amino-3-methoxypropionamide and stereoisomers the use thereof anti-convulsant and an intermediate in the preparation of other anti-convulsants.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: April 11, 2000
    Assignee: Research Corporation Tech., Inc.
    Inventors: Harold Kohn, Shridhar V. Andurkar
  • Patent number: 5981600
    Abstract: A compound selected from the group having the general formula ##STR1## wherein Z is a divalent moiety selected from linear or branched, saturated or unsaturated alkylene group, and the O.dbd.C(R) group contains one of a quaternary ammonium group and a sugar moiety, or the O.dbd.C(R) group is part of a neuraminic acid moiety, and their pharmacologically acceptable acid addition salts. Also a medical preparate with antineoplastic effects utilizing such a compound.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: November 9, 1999
    Inventor: Fikret Baykut
  • Patent number: 5922771
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 5880158
    Abstract: The present invention is directed to a compound of the following formula: ##STR1## pharmaceutical compositions containing the same and the use thereof as an anticonvulsant.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: March 9, 1999
    Assignee: Research Corporation Tech., Inc.
    Inventor: Harold Kohn
  • Patent number: 5856479
    Abstract: Using the fluorescent group-containing carbodiimide compound represented-by the following formula (I) as the label and the like in the nucleic acid detection method, immunoassay, or chemiluminescence assay, labeling can be made efficiently for a short time, a nucleic acid derived from nature can be labelled, and highly sensitive assay is enabled.B--Y.sup.3 --N.dbd.C.dbd.N--Y.sup.2 --W--Y.sup.1 --?A!.sub.n --F(I)wherein F represents a fluorescent group;A represents a moiety selected from the group consisting of --CH.sub.2 --, --NHCO--, --CONH--, --O--, --S--, --NR-- wherein R is an alkyl group, --COO--, --OCO--, --NHSO.sub.2 --, and --SO.sub.2 NH--;n is 0 or 1;W represents a direct bond or a quaternary ammonium group;Y.sup.1, Y.sup.2 and Y.sup.3 each represents an alkylene group which may have a functional group in its main chain; andB represents H or a monovalent organic group which may be the same as or different from that represented by --W--Y.sup.1 --?A!.sub.n --F.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: January 5, 1999
    Assignee: Nisshinbo Industries, Inc.
    Inventors: Osamu Suzuki, Gen Masuda, Namiko Shiohata, Kazuko Matsumoto
  • Patent number: 5814669
    Abstract: The invention relates to novel amino acid derivatives, to a process for their preparation and to their use as pesticides, in particular as fungicides, and as intermediates for preparing known substituted amino acid derivatives with fungicidal activity.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: September 29, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Stelzer, Carl Casser, Thomas Seitz
  • Patent number: 5808003
    Abstract: A compound according to the formula: ##STR1## and conjugates thereof.
    Type: Grant
    Filed: September 18, 1996
    Date of Patent: September 15, 1998
    Assignee: PerImmune Holdings, Inc.
    Inventors: Ramaswamy Subramanian, James Colony
  • Patent number: 5736578
    Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.
    Type: Grant
    Filed: May 10, 1996
    Date of Patent: April 7, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brett T. Watson, Katherine S. Takaki, Joseph P. Yevich, James R. Epperson, George N. Karageorge, Karen L. Leboulluec
  • Patent number: 5728875
    Abstract: .alpha.-Amino acid amides of the formula I ##STR1## in which n is the number zero or one;R.sub.1 is C.sub.1 -C.sub.12 alkyl, which is unsubstituted or can be substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.3 -C.sub.8 cycloalkyl, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.3 -C.sub.6 alkenyloxycarbonyl or C.sub.3 -C.sub.6 alkynyloxycarbonyl; C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.12 alkenyl;C.sub.2 -C.sub.12 alkynyl; C.sub.1 -C.sub.12 halogenoalkyl or a group NR.sub.13 R.sub.14 ; in which R.sub.13 and R.sub.14 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl or together are tetra- or pentamethylene;R.sub.2 and R.sub.3 independently of one another are hydrogen; C.sub.1 -C.sub.8 alkyl; C.sub.1 -C.sub.8 alkyl which is substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, mercapto or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.8 alkenyl;C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 cycloalkyl or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.
    Type: Grant
    Filed: August 26, 1996
    Date of Patent: March 17, 1998
    Assignee: Novartis Corporation
    Inventor: Martin Zeller
  • Patent number: 5679857
    Abstract: L-amino acid amides are converted to the corresponding D-amino acid amides. An amide formed from an L-amino acid and an optically active (S)-.alpha.-alkylbenzylamine is subjected to dehydration condensation with an aryl aldehyde to form a Schiff's base, which is racemized at the amino acid moiety in the presence of a base to yield an N-allylidene-D-amino acid-(S)-amide. The less-soluble diastereomer N-allylidene-D-amino acid-(S)-amide is crystallized from the reaction mixture and recovered by means of solid/liquid separation. The N-allylidene form is readily hydrolyzed into the amino acid-(S)-amide and the starting aldehyde.
    Type: Grant
    Filed: November 16, 1995
    Date of Patent: October 21, 1997
    Assignee: Ajinomoto Co., Inc.
    Inventors: Toyoto Hijiya, Chiaki Mochizuki, Tadashi Takemoto
  • Patent number: 5585519
    Abstract: .alpha.-Amino acid amides of the formula I ##STR1## in which n is the number zero or one;R.sub.1 is C.sub.1 -C.sub.12 alkyl, which is unsubstituted or can be substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.3 -C.sub.8 cycloalkyl, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.3 -C.sub.6 alkenyloxycarbonyl or C.sub.3 -C.sub.6 alkynyloxycarbonyl; C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.12 alkenyl; C.sub.2 -C.sub.12 alkynyl; C.sub.1 -C.sub.12 halogenoalkyl or a group NR.sub.13 R.sub.14 ; in whichR.sub.13 and R.sub.14 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl or together are tetra- or pentamethylene;R.sub.2 and R.sub.3 independently of one another are hydrogen; C.sub.1 -C.sub.8 alkyl; C.sub.1 -C.sub.8 alkyl which is substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, mercapto or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.8 alkenyl; C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 cycloalkyl or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: December 17, 1996
    Assignee: Ciba-Geigy Corporation
    Inventor: Martin Zeller
  • Patent number: 5532259
    Abstract: Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their useIsoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 2, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Robert R. Bartlett, Friedrich-Johannes Kammerer
  • Patent number: 5504115
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: April 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Patent number: 5494911
    Abstract: Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: February 27, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Robert R. Bartlett, Friedrich-Johannes Kammerer
  • Patent number: 5383942
    Abstract: An amido alkanolamine composition obtained by reacting, at a temperature of 10.degree. C.-200.degree. C.:(a) a 4-alkyl-2-morpholinone represented by the formula: ##STR1## in which R represents a monovalent aliphatic radical having from 1 to 10 carbon atoms; and(b) a hydrocarbyl oxypolyoxyalkylene amine represented by the formula ##STR2## in which R' represents an alkyl, an alicyclic or an alkyl-alicyclic radical having from 12 to 30 carbon atoms or ##STR3## wherein R" represents a hydrocarbyl radical having from 4 to 30 carbon atoms, x has a value of from about 5 to 50, and R'" is an ethyl radical or a mixture of methyl and ethyl radicals.
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: January 24, 1995
    Assignee: Texaco Inc.
    Inventors: Wei-Yang Su, Sheldon Herbstman, Joseph M. Russo, Robert L. Zimmerman, Michael Cuscurida
  • Patent number: 5382683
    Abstract: Compounds are provided of the following general structure: ##STR1## wherein B is hydrogen or lower alkyl (C.sub.1 -C.sub.4), R.sub.1 is hydrogen or methyl, R.sub.2 is lower alkyl (C.sub.1 -C.sub.4), phenylmethyl or 2-(aminocarbonyl)ethyl, R.sub.3 is H or lower alkyl (C.sub.1 -C.sub.4) and where W and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.
    Type: Grant
    Filed: April 8, 1992
    Date of Patent: January 17, 1995
    Assignee: Fisons Corporation
    Inventor: Ronald C. Griffith
  • Patent number: 5352705
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Patent number: 5331007
    Abstract: There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: July 19, 1994
    Assignee: Fisons Corporation
    Inventors: Ronald C. Griffith, James J. Napier
  • Patent number: 5318994
    Abstract: Compounds of the formula: ##STR1## in which: A represents ##STR2## R represents linear or branched lower alkyl, R.sub.1 represents hydrogen or linear or branched lower alkyl, andR.sub.2 represents aryl or lower arylalkyl or aryl or lower arylalkyl substituted by lower alkyl, lower alkoxy, trifluoromethyl, or halogen, aryl means phenyl or naphthyl, as well as optical isomers, epimers and diastereoisomers and addition salts thereof with a pharmaceutically-acceptable acid, lower alkyl and lower alkoxy having 1 to 6 carbon atoms inclusive, andmedicaments containing the same which are useful for the treatment of disorders of the melatoninergic system.
    Type: Grant
    Filed: November 3, 1992
    Date of Patent: June 7, 1994
    Assignee: Adir et Compagnie
    Inventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
  • Patent number: 5286264
    Abstract: A gasoline detergent additive composition comprising a) the reaction product of a 4-alkyl-2-morpholinone and an alkylphenoxypolyoxyalkylene amine; b) the reaction product of a polyalkenyl succinic acid anhydride and a polyethylene polyamine; and c) a polyalphaolefin. A motor fuel composition is also provided.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: February 15, 1994
    Assignee: Texaco Inc.
    Inventors: Joseph M. Russo, Sheldon Herbstman, Jefrey B. Furman
  • Patent number: 5278148
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: January 11, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Quirico Branca, Hans P. Marki, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
  • Patent number: 5234946
    Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: August 10, 1993
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
  • Patent number: 5234478
    Abstract: An amido alkanolamine composition obtained by reacting, at a temperature of 10.degree. C.-200.degree. C.:(a) a 4-alkyl-2-morpholinone represented by the formula: ##STR1## in which R represents a monovalent aliphatic radical having from 1 to 10 carbon atoms, and(b) an alkylphenoxypolyoxyalkylene amine represented by the formula: ##STR2## in which R' represents a hydrocarbyl radical having from 4 to 30 carbon atoms, x has a value from 5 to 50, and R" represents a methyl radical or a mixture of hydrogen and methyl radicals is provided.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: August 10, 1993
    Assignees: Texaco Inc., Texaco Chemical Co.
    Inventors: Wei-Yang Su, Sheldon Herbstman, Robert L. Zimmerman, Michael Cuscurida, Wheeler C. Crawford, Daniel T. Daly
  • Patent number: 5190974
    Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein n, R.sub.1, R.sub.2, X, A, R.sub.3A and R.sub.4A are set forth in the claims and their non-toxic, pharmaceutically acceptable acid addition salts having excellent analgesic, psychotropic and enkephalinase inhibiting properties.
    Type: Grant
    Filed: July 5, 1991
    Date of Patent: March 2, 1993
    Assignee: Roussel Uclaf
    Inventors: Francoise Clemence, Odile Le Martret, Francis Petit
  • Patent number: 5093524
    Abstract: Compounds are provided of the following general structure: ##STR1## wherein R.sub.4 is lower alkyl (C.sub.1 -C.sub.4); R.sub.1 is hydrogen or methyl, R.sub.2 is hydrogen or methyl, R.sub.3 is lower alkyl (C.sub.1 -C.sub.6) or cyclopropyl, and where R.sub.5 and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: March 3, 1992
    Assignee: Fisons Corporation
    Inventor: Ronald C. Griffith
  • Patent number: 5055594
    Abstract: A fluorogenic substrate for tryptophanase useful for identifying an unknown microorganism is a fluorescent dye linked to an amino acid by a carbamate or thiocarbamate group. In preferred substrates, the dye is fluorescein or 7-amino-4-methyl coumarin and the amino acid linked thereto is cysteine, threonine or serine.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: October 8, 1991
    Assignee: Becton, Dickinson and Company
    Inventor: Patrick D. Mize
  • Patent number: 4904661
    Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.
    Type: Grant
    Filed: December 16, 1987
    Date of Patent: February 27, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4863926
    Abstract: New nitro aliphatic compounds useful as antithrombotic and antihypertensing agents are disclosed.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: September 5, 1989
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Konsaka, Hiroshi Imanaka
  • Patent number: 4798687
    Abstract: Compounds are provided of the following general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen or methyl and A is amino, C.sub.1 -C.sub.4 monoalkylamino, C.sub.2 -C.sub.8 dialkylamino, cyclopropylamino, 1-pyrrolidinyl, 1-piperidinyl or 4-morpholinyl. They are useful for providing sedative and antiepileptic activity.
    Type: Grant
    Filed: February 6, 1987
    Date of Patent: January 17, 1989
    Assignee: Pennwalt Corporation
    Inventors: Ronald C. Griffith, James J. Napier
  • Patent number: 4778804
    Abstract: New nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.
    Type: Grant
    Filed: October 11, 1985
    Date of Patent: October 18, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
  • Patent number: 4767768
    Abstract: New Nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.
    Type: Grant
    Filed: December 8, 1983
    Date of Patent: August 30, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
  • Patent number: 4757137
    Abstract: Azo dyestuffs of the formula ##STR1## wherein R.sub.1 denotes acyl,R.sub.2 denotes hydrogen, fluorine, chlorine or trifluoromethyl,R.sub.3 denotes hydrogen, optionally substituted C.sub.1 -C.sub.4 -alkyl, cyclohexyl or optionally substituted phenyl andR.sub.4 denotes hydrogen or C.sub.1 -C.sub.4 -alkyl groupare suitable for dyeing natural and synthetic fibre materials, for example for dyeing wool or polyamide fibres, in level read to violet shades with very good fastnesses to light, wet processing and perspiration, the color yield being good.
    Type: Grant
    Filed: September 22, 1983
    Date of Patent: July 12, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Wolfrum, Erich Klauke, Hans-Gunter Otten
  • Patent number: 4739059
    Abstract: A novel amine amide of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are useful as thickening agents, disoxidation catalysts and monomers.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: April 19, 1988
    Assignee: Daikin Industries Ltd.
    Inventors: Yohnosuke Ohsaka, Yoshio Amimoto, Yoshio Negishi
  • Patent number: 4690950
    Abstract: The present invention relates to new derivatives selected from the group consisting of:(i) 1-[N-(.alpha.-alkylamino-.alpha.-methylacetyl)aminophenyl]-2-alkylaminopro panones of the general formula: ##STR1## in which R represents a C.sub.1 -C.sub.4 alkyl group and R' represents H or a C.sub.1 -C.sub.4 alkyl group; and(ii) addition salts thereof.These new derivatives are useful as CNS-active substances, in particular as stimulants and antidepressants.The invention also relates to the method for their preparation.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: September 1, 1987
    Assignee: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 4681898
    Abstract: Compounds of the formula ##STR1## where n is 0 or 1,R is alkyl, phenyl or R.sub.4 -substituted phenyl,R.sub.2 and R.sub.3 are, independently, alkyl orR.sub.2 and R.sub.3 together with N is ##STR2## m is 1, 2 or 3, R.sub.1 and R.sub.4 are, independently hydrogen, halo, alkyl or alkoxy, andR.sub.5 is hydrogen or alkyl of 1 to 6 carbon atomsor their pharmaceutically acceptable salts are useful as anti-diabetic agents, in particular, as hypoglycemic agents or inhibitors of post-prandial hypoglycemia.
    Type: Grant
    Filed: May 8, 1984
    Date of Patent: July 21, 1987
    Assignee: Sandoz Pharmaceuticals Corp.
    Inventor: Jeffrey Nadelson
  • Patent number: 4601839
    Abstract: Novel .alpha.-aminoacetamides are powerful stabilizers for organic materials subject to oxygen and heat degradation, and particularly for synthetic natural rubber, synthetic ester lubricants and synthetic resinous materials. A wide range of substituents on the amine and amide N atoms, at least one of which substituents is an alkylene imine (cyclic), and an even wider range of substituents on the saturated carbon atom, yields an array of stabilizers having a wide range of compatibility in compositions comprising various synthetic resinous compounds to be stabilized.Novel syntheses are provided utilizing at least one amine nucleophilic agent, a trichloromethide ion generating agent, and an alkoxide ion generating agent, which together in the presence of aqueous alkali and an onium salt, yield novel .alpha.-aminoacetamides in which a wide choice of substituents may be introduced. The nucleophilic agent may be a primary or secondary amine, or one of each. The trichloromethide ion generating agent is a haloform.
    Type: Grant
    Filed: November 13, 1981
    Date of Patent: July 22, 1986
    Assignee: The B. F. Goodrich Company
    Inventor: John T. Lai
  • Patent number: 4418077
    Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: November 29, 1983
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Fritz Gerhart, Michel Jung, Daniel Schirlin
  • Patent number: 4362877
    Abstract: 2,4-Disubstituted-1,2,5-thiadiazol-3(2H)-one antimicrobials have broad spectrum antibacterial and antifungal activity. They are found to be especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.
    Type: Grant
    Filed: April 21, 1980
    Date of Patent: December 7, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Richard A. Dybas, Bruce E. Witzel, Nathaniel Grier
  • Patent number: 4313956
    Abstract: Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.
    Type: Grant
    Filed: December 28, 1979
    Date of Patent: February 2, 1982
    Assignee: INTERx Research Corp.
    Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
  • Patent number: 4311706
    Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.
    Type: Grant
    Filed: January 22, 1980
    Date of Patent: January 19, 1982
    Assignee: INTERx Research Corporation
    Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
  • Patent number: 4293557
    Abstract: Phenoxypropylamine derivatives of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl or ethyl group, R.sub.2 and R.sub.3, independently from each other, represent a lower alkyl group, or together form a linear alkylene group having 4 to 7 carbon atoms which may be optionally substituted by a hydroxyl or hydroxymethyl group, and R.sub.4 represents a hydrogen atom or a group of the formula --R.sub.5 --Z in which R.sub.5 represents a lower alkylene group, and Z represents a hydrogen atom or an amino, mono- or di-(lower alkyl)-amino, hydrdoxy lower alkylamino, lower alkanoylamino, hydroxyl, lower alkoxy, lower alkanoyloxy, phenoxy, halophenoxy, benzoyloxy or halobenzoyloxy group, andthe salts thereof; to a process for production thereof; and to their medicinal use, particularly to antiulcer agents comprising these phenoxypropylamine derivatives or their salts.
    Type: Grant
    Filed: June 30, 1980
    Date of Patent: October 6, 1981
    Assignee: Teikoku Hormone Mfg. Co., Ltd.
    Inventors: Kenyu Shibata, Toshihisa Itaya, Nobuaki Yamakoshi, Shigeru Kurata, Naoyuki Koizumi, Masaaki Tarutani, Hideki Sakuma, Kunihiro Konishi
  • Patent number: 4235892
    Abstract: Described are D-(threo)-1-aryl-2-acylamido-3-fluoro-1-propanols, methods for their preparation, and methods for their use as antibacterial agents.Of particular interest are D-(threo)-1-p-nitrophenyl-2-dichloroacetamido-3-fluoro-1-propanol and D-(threo)-1-p-methylsulfonylphenyl-2-dichloroacetamido-3-fluoro-1-propanol and the corresponding 2-difluoroacetamido compounds which are the 3-fluoro-3-deoxy analogs of chloramphenicol, thiamphenicol, difluoroacetyl analog of chloramphenicol, and of fluorthiamphenicol, respectively, and which are active both against organisms sensitive to and resistant to the parent amphenicol antibiotics.Other particularly valuable antibacterial agents include the corresponding 2-(chlorofluoroacetamido)-, 2-dichlorodeuterioacetamido, 2-difluorodeuterioacetamido-, and the 2-(chlorofluorodeuterioacetamido)- derivatives of the foregoing 3-fluoro-3-deoxy amphenicols.
    Type: Grant
    Filed: February 5, 1979
    Date of Patent: November 25, 1980
    Assignee: Schering Corporation, Patent Dept.
    Inventor: Tattanahalli L. Nagabhushan