Double Bonded Divalent Chalcogen Containing Patents (Class 544/130)
  • Patent number: 5686447
    Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: November 11, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5686588
    Abstract: A stoichiometric acid moiety transfer reaction for the preparation of an acid salt of an amine compound is disclosed. The acid moiety transfer reaction provides amine acid salts of high purity and having crystalline structure of uniform size and shape.
    Type: Grant
    Filed: August 16, 1995
    Date of Patent: November 11, 1997
    Inventor: Seo Hong Yoo
  • Patent number: 5684021
    Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: November 4, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5672615
    Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: September 30, 1997
    Assignee: Novartis Corporation
    Inventors: Lawrence J. MacPherson, David Thomas Parker
  • Patent number: 5665756
    Abstract: Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.
    Type: Grant
    Filed: August 3, 1994
    Date of Patent: September 9, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
  • Patent number: 5643854
    Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR.sub.2 moiety where R.sub.2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as well as herbicidal compositions and herbicidal use of these compounds.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 1, 1997
    Assignee: Rohm and Haas Company
    Inventors: Donald Edwin Korte, Len Fang Lee
  • Patent number: 5641777
    Abstract: The invention relates to neurokinin receptor antagonist compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycleAPPLICATION: Neurokinin receptor antagonists.
    Type: Grant
    Filed: January 30, 1996
    Date of Patent: June 24, 1997
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5633248
    Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.
    Type: Grant
    Filed: November 21, 1995
    Date of Patent: May 27, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
  • Patent number: 5620971
    Abstract: The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: April 15, 1997
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David M. Armistead, Jeffrey O. Saunders, Joshua S. Boger
  • Patent number: 5612337
    Abstract: The present invention relates to compounds of formula (I), wherein R.sup.1 is hydrogen, halogen, C.sub.1-6 C alkyl, C.sub.1-6 alkoxy, CF.sub.3, NO.sub.2, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.1-4 alkyl substituted by C.sub.1-4 alkoxy, where R.sup.a and R.sup.b are hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halogen, C .sub.1-6 alkyl, C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.3 is hydrogen, halogen or CF.sub.3 ; R.sup.4 is selected from the definitions of R.sup.1 ; R.sup.5 is selected from the definitions of R.sup.2 ; R.sup.6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by .dbd.O, .dbd.S or a C.sub.1-4 alkyl group, and optionally substituted by an aminoalkyl group; R.sup.9a and R.sup.9b are hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined to form a C.sub.5-7 ring; X is C.sub.
    Type: Grant
    Filed: June 13, 1996
    Date of Patent: March 18, 1997
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Timothy Harrison, Angus M. MacLeod, Andrew P. Owens, Eileen M. Seward, Christopher J. Swain, Martin R. Teall
  • Patent number: 5606065
    Abstract: The invention relates to N-alkylenepiperidino compounds of formula ##STR1## as well as their enantiomers, a process for preparing them and pharmaceutical compositions containing them.These compounds are useful as antagonists of neurokinin receptors in the treatment of substance P- and/or neurokinin-dependent pathologies.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: February 25, 1997
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Serge Martinez, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5597390
    Abstract: A di- or tri-ester polyether unsaturated acid amine reaction product effective as a fuel additive for reducing intake valve deposits and octane requirement increase, as well as controlling combustion chamber deposits, in gasoline engines is disclosed together with fuel compositions and methods of making and using the same. Also disclosed are compositions and methods for dispersing deposits in lubricating oil products.
    Type: Grant
    Filed: September 25, 1995
    Date of Patent: January 28, 1997
    Assignee: Ethyl Corporation
    Inventor: John T. Loper
  • Patent number: 5597917
    Abstract: A process for the dissolution of chemical compounds by use of ureas in which at least one of the urea's two nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom as a chemical solvent, and a method of producing tri- or tetraalkylated ureas or bis ureas wherein at least one of the urea's nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom by means of dialkylating the --NH.sub.2 group of a urea with an alkene or alkene arylene alkene dihalogenide, disulphonate or dihydrogen sulphonate in the presence of a solid base and a phase-transfer catalyst.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: January 28, 1997
    Assignee: DSM Chemie Linz GmbH
    Inventors: Kurt A. Hackl, Markus R ossler, Martin M ullner, Gerhard Stern
  • Patent number: 5585374
    Abstract: Amide derivatives of formula (I) and their pharmaceutically acceptable salts (where a and b each represent 0, 1, 2 or 3 such that a+b=0, 1, 2 or 3, the dotted line represents an optional double bond, A is an optionally substituted C.sub.1-2 -alkylene chain, R is mono or bicyclic aryl or heteroaryl radical, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an aryl, aralkyl, heteroaryl or heteroarylalkyl and --CONR.sup.3 R.sup.4 represents a specified amide group) are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: December 17, 1996
    Assignee: John Wyeth Brother, Limited
    Inventors: Ian A. Cliffe, Alan C. White
  • Patent number: 5583146
    Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: December 10, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: Spencer D. Kimball, Jagabandhu Das, Wan F. Lau, Steven E. Hall, Wen-Ching Han
  • Patent number: 5563142
    Abstract: The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: October 8, 1996
    Assignee: The Upjohn Company
    Inventors: John R. Palmer, Donna L. Romero, Paul A. Aristoff, Richard C. Thomas, Herman W. Smith
  • Patent number: 5561130
    Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein n is 1, 2 or 3; X represents O or S; R.sup.1 is optionally substituted phenyl; R.sup.2 is aryl or heteroaryl; R.sup.4 and R.sup.5 are independently H, halo, C.sub.1-6 alkyl, oxo, CH.sub.2 OR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.8 represents C(COOR.sup.a).sub.2, C(CONR.sup.a R.sup.b).sub.2 or C.sub.1-6 alkyl substituted by C(.dbd.NR.sup.a)NR.sup.b NR.sup.c CO.sub.2 R.sup.d, CONHNR.sup.a R.sup.b, C(S)NR.sup.a R.sup.b, CONR.sup.a C.sub.1-6 alkylR.sup.12, CONR.sup.13 C.sub.2-6 alkynyl, CONR.sup.13 C.sub.2-6 alkenyl, COCONR.sup.a R.sup.b, CONR.sup.a C(NR.sup.b)NR.sup.c R.sup.d, CONR.sup.13 SO.sub.2 R.sup.a, SO.sub.2 NR.sup.13 COR.sup.a, CONR.sup.a heteroaryl or COR.sup.q ; R.sup.a, R.sup.b, R.sup.c and R.sup.d are each H, C.sub.1-6 alkyl, phenyl or trifluoromethyl. R.sup.12 represents OR.sup.a, CONR.sup.a R.sup.b or heteroaryl; R.sup.13 represents H or C.sub.1-6 alkyl; and R.sup.
    Type: Grant
    Filed: January 24, 1995
    Date of Patent: October 1, 1996
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Eileen M. Seward, Christopher J. Swain
  • Patent number: 5561146
    Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: October 1, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kyoung S. Kim, Spencer D. Kimball, Jagabandhu Das, Edwin J. Iwanowicz, Wen-Ching Han
  • Patent number: 5552419
    Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: September 3, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5532232
    Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: July 2, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
  • Patent number: 5512567
    Abstract: Analgesic compounds of the formula (I); ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents oxygen or an imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is an aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen; provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: April 30, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
  • Patent number: 5500424
    Abstract: The present invention relates to a compound represented by the general formula (I): ##STR1## [wherein R.sup.1 is a lower alkyl group or the like, R.sup.2 is a lower alkyl group or the like, R.sup.3 and R.sup.4, which may be the same or different, are halogen atoms or the like, R.sup.5, R.sup.6 and R.sup.7, which may be the same or different, are halogen atoms or the like, and X is .dbd.N-- or .dbd.CH--] or a pharmacologically acceptable salt thereof, which has inhibitory effect on acyl-CoA:cholesterol O-acyltransferase (ACAT), a process for producing said compound, and uses of said compound.
    Type: Grant
    Filed: August 12, 1994
    Date of Patent: March 19, 1996
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masashi Nagamine, Kenji Yamamoto, Kenji Horiuchi, Yoshimitsu Matsui, Masanori Yoshida
  • Patent number: 5496943
    Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: March 5, 1996
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
  • Patent number: 5488119
    Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: January 30, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Evelyn Fischer-Reimann, Walter Fischer
  • Patent number: 5428036
    Abstract: Reaction products of sertindole with an acid or an activated acid, with formaldehyde alone, formaldehyde in the presence of an alcohol or an amine, or with an acyloxymethylene halide, and having general formula (1) wherein X is CO, CS, or CH.sub.2, and if X is CO or CS, R is (i) hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl or cycloalk(en)ylalk(en)yl optionally substituted with hydroxy, or optionally substituted phenyl; or (ii) YR.sup.1, wherein Y is O or S and R.sup.1 is one of the substituents defined for R under (i) above; or (iii) NR.sup.2 R.sup.3, wherein R.sup.2 and R.sup.3 independently are selected from the substituents defined for R under (i) above or R.sup.2 and R.sup.3 are combined to form a heterocyclic ring; or if X is CH.sub.2, R is: (iv) a group YR.sup.1 as defined in (ii); (v) a group NR.sup.2 R.sup.3 as defined in (iii); or (vi) a group OC(O)R.sup.4, wherein R.sup.4 is as defined for R.sup.
    Type: Grant
    Filed: March 30, 1993
    Date of Patent: June 27, 1995
    Assignee: H. Lundbeck A/S
    Inventors: Jens K. Perregaard, Henrik Pederson
  • Patent number: 5414083
    Abstract: A process for the dissolution of chemical compounds by use of ureas in which at least one of the urea's two nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom as a chemical solvent, and a method of producing tri- or tetraalkylated ureas or bis ureas wherein at least one of the urea's nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom by means of dialkylating the --NH.sub.2 group of a urea with an alkene or alkene arylene alkene dihalogenide, disulphonate or dihydrogen sulphonate in the presence of a solid base and a phase-transfer catalyst.
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: May 9, 1995
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Kurt A. Hackl, Markus Rossler, Martin Mullner, Gerhard Stern
  • Patent number: 5411971
    Abstract: The invention relates to N-alkylenepiperidino compounds of formula ##STR1## as well as their enantiomers, and pharmaceutical compositions containing them that are useful as antagonists of neurokinin receptors in the treatment of substance P- and/or neurokinin-independent pathologies.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: May 2, 1995
    Assignee: Elf Sanofi
    Inventors: Xavier Edmonds-Alt, Serge Martinez, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5393760
    Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
    Type: Grant
    Filed: June 15, 1993
    Date of Patent: February 28, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
  • Patent number: 5389647
    Abstract: A renin inhibiting compound of the formula: ##STR1## wherein X is O, NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-Morpholino)propyl)-5(S)-(2(S)-(1(S)-(4-methoxymethoxy)piperidin-1- yl)carbonyl-2-phenyl)ethoxyhexanamido)-6-cyclohexyl-4(S)-hydroxy-2(S)-isopr opylhexanamide.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: February 14, 1995
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, Steven A. Boyd, Anthony K. L. Fung, Herman H. Stein, Jon F. Denissen, Charles W. Hutchins
  • Patent number: 5387586
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein Ar, n, B and A are as defined in the description, to their optical isomers, and to their addition salts there of with a pharmaceutically-acceptable acid or base.Medicinal product which is useful for treating pain and treating or preventing pathologies which require psychotropic agents.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: February 7, 1995
    Assignee: Adir et Compagnie
    Inventors: Ousmane Diouf, Daniel Lesieur, Patrick Depreux, Beatrice Guardiola-Lemaitre, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
  • Patent number: 5374634
    Abstract: There is provided a pyridine derivative represented by the formula (I) ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or lower alkyl and each of R.sup.3 and R.sup.4 independently represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted polycyclic alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic group, or R.sup.3 and R.sup.4 are combined with nitrogen atom adjacent thereto to form a substituted or unsubstituted alicyclic heterocyclic group, or pharmaceutically acceptable salt thereof. The pyridine derivative exhibits bone resorption inhibiting effect and is useful as a medicament for treating osteoporosis.
    Type: Grant
    Filed: July 1, 1993
    Date of Patent: December 20, 1994
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Akio Ishii, Joji Nakamura, Hiroyuki Ishida, Katsushige Gomi
  • Patent number: 5356907
    Abstract: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## wherein, A is a cycloalkyl of 3-6 carbon optionally substituted, R, R.sub.1, R.sub.2 and Y are defined in the specification.
    Type: Grant
    Filed: October 1, 1992
    Date of Patent: October 18, 1994
    Assignee: Roussel UCLAF
    Inventors: Francois Clemence, Michel Fortin, Odile Le Martret
  • Patent number: 5348954
    Abstract: Heterocylic chelating agents and salts thereof of formula I: ##STR1## wherein X represents a bond, O or S, or a group CHR.sup.1 or NR.sup.3 ; R.sup.1 represents H, a group OR.sup.3 or NR.sup.3 R.sup.3, or an alkyl or alkoxyalkyl group optionally substituted by a hydroxyl group or by a group NR.sup.3 R.sup.3 or CON.sup.3 R.sup.3 ;each R.sup.2 represents H, or an alkyl or alkoxy group optionally substituted by a hydroxyl or alkoxy group;each R.sup.3 represents H, an optionally hydroxylated alkyl group or a group CH.sub.2 Y;Y represents a group COZ, CON(OH)R.sup.4, POZ.sub.2 or SO.sub.2 Z;Z represents a group OR.sup.4, NR.sup.4 R.sup.4 or ##STR2## where each R.sup.11 is H, a hydroxyl group or an optionally hydroxylated alkyl group, s is 0, 1 or 2, and W is CHR.sup.11, NR.sup.11 or an oxygen atom; andeach R.sup.4 represents H, or an optionally mono- or poly-hydroxylated alkyl, alkoxyalkyl or polyalkoxyalkyl group;with the provisos that where s is 0 then W is CHR.sup.11 and that where X represents a bond or CHR.
    Type: Grant
    Filed: July 24, 1991
    Date of Patent: September 20, 1994
    Assignee: Nycomed Imaging AS
    Inventors: Torsten Almen, Arne Berg, Harald Dugstad, Jo Klaveness, Klaus D. Krautwurst, Pal Rongved
  • Patent number: 5342838
    Abstract: The present invention relates to phenolic thioetheramides of the formula ##STR1## wherein R.sup.1 and R.sup.2 are tert-alkyl or phenyl, Alk.sup.1 and Alk.sup.2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen or alkyl and Alk.sup.3 is alkylene; or ##STR3## wherein Y is CH, N, O, or S; R.sup.6 is hydrogen, alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl or a heterocyclic amine; and R.sup.7 is hydrogen or alkyl. The compounds inhibit 5-lipoxygenase and are useful in the treatment of inflammation and allergic conditions.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: August 30, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5314889
    Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5304549
    Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: April 19, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
  • Patent number: 5276030
    Abstract: The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: January 4, 1994
    Assignee: Egis Gyogyszergyat
    Inventors: Josef Barkoczy, Josef Reiter, Laszlo Pongo, Lujza Petocz, Marton Fekete, Frigyes Gorgenyi, Gabor Gigler, Istvan Gacsalyi, Istvan Gyertyan
  • Patent number: 5270327
    Abstract: Analgesic compounds of the formula (I): ##STR1## in which, R.sup.1 R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a 5-6-membered N-heterocyclic ring optionally having a further O, N, or S heteroatom; E represents methylene; ring A is an unsubstituted or substituted benzene or naphthalene; R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(=Y)-- (IV)wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen with up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygens.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: December 14, 1993
    Assignee: Sankyo Company, Limited
    Inventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
  • Patent number: 5268374
    Abstract: The present invention relates to renin inhibiting compounds of the formula: ##STR1##
    Type: Grant
    Filed: May 22, 1991
    Date of Patent: December 7, 1993
    Assignee: Abbott Laboratories
    Inventors: Anthony K. L. Fung, William R. Baker, Yoek-Lin Armiger, Saul H. Rosenberg, Biswanath De, Jacob J. Plattner, Steven A. Boyd, Dale J. Kempf, Hing L. Sham, Hollis D. Kleinert, Robert A. Mantei
  • Patent number: 5266570
    Abstract: Compounds of formula I, Ia or Ib and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof; ##STR1##
    Type: Grant
    Filed: August 6, 1992
    Date of Patent: November 30, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Ying K. Yee, Cyrus J. Ohnmacht, Diane A. Trainor, Joseph J. Lewis
  • Patent number: 5260307
    Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
    Type: Grant
    Filed: June 24, 1991
    Date of Patent: November 9, 1993
    Assignee: Hofmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
  • Patent number: 5252735
    Abstract: This invention relates to compounds of Formula I ##STR1## which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: October 12, 1993
    Assignee: The Upjohn Company
    Inventor: Joel Morris
  • Patent number: 5245034
    Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: September 14, 1993
    Assignee: Kiroyoshi Hidaka
    Inventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
  • Patent number: 5244910
    Abstract: A renin inhibiting compound of the formula: ##STR1## wherein X is O NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-Morpholino)propyl)-5(S)-(2(S)-(1(S)-(4-(methoxymethoxy)piperidin-1 -yl)carbonyl-2- phenyl)ethoxyhexanamido)-6-cyclohexyl-4(S)-hydroxy-2(S)-isopropylhexanamid e.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: September 14, 1993
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, Steven A. Boyd, Anthony K. L. Fung, Herman H. Stein, Jon F. Denissen, Charles W. Hutchins
  • Patent number: 5241067
    Abstract: Hindered amine light stabilizers are provided in which the hindered amine is contained in a unit of formula ##STR1## and R.sup.1, R.sup.2, R.sup.3, and A are as defined as in the Summary of the Invention. Unique polymeric and non-polymeric compounds containing this unit are useful as additives for the stabilization of polymeric compositions which are normally subject to thermal, oxidative or actinic light degradation.
    Type: Grant
    Filed: March 1, 1989
    Date of Patent: August 31, 1993
    Assignee: Elf Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 5224980
    Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together, and R.sup.3 and R.sup.4 taken together, independently represent a polymethylene chain having 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having from 1 to 4 carbon atoms, and R.sup.5 to R.sup.8 are independently hydrogen, hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 complete a trimethylene ring, R.sup.5 and R.sup.7 are each hydrogen and R.sup.6 and R.sup.8 are alkyl such as methyl. The compounds have microbiological activity.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: July 6, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Peter W. Austin, Neville Tyreman
  • Patent number: 5223018
    Abstract: The invention relates to new 1-phenyl-piperidine-2,6-diones of the formula I ##STR1## wherein R is C.sub.3 -C.sub.7 -cycloalkyl,R.sub.1 is hydrogen or halogen;R.sub.2 is hydrogen, cyano, nitro or halogen; andA is hydrogen, cyano, nitro or is an ether or carboxylic acid radical as defined in the description. The salts, complexes as well as the stereoisomeric forms of these compounds, their preparations, use and agrochemical compositions which contains them form also part of this invention.
    Type: Grant
    Filed: March 26, 1992
    Date of Patent: June 29, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Moser, Georg Pissiotas, Hans-Georg Brunner
  • Patent number: 5216150
    Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.
    Type: Grant
    Filed: September 12, 1991
    Date of Patent: June 1, 1993
    Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki Kaisha
    Inventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
  • Patent number: 5216001
    Abstract: Specific 6-substituted or 2-alkyl substituted indole or 2,3-dihydroindole compounds are provided, having long lasting serotonin activity with specific binding to 5-HT.sub.2 receptors of the central nervous system. These compounds are suitable for therapeutic treatment of CNS disorders, such as anxiety, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, and Parkinson's disease.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: June 1, 1993
    Assignee: H. Lunbeck A/S
    Inventors: Jens K. Perregaard, Kim Andersen, Klaus P. Boegesoe, Henrik Pedersen
  • Patent number: 5216171
    Abstract: 2-Amino-4-trichloromethylpyridines of the general formula I ##STR1## where R.sup.1 is hydrogen or C.sub.1 -C.sub.8 -alkyl,R.sup.2 is C.sub.1 -C.sub.8 -alkyl, C.sub.5 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.4 -alkenyl or phenyl, benzyl or phenylsulfonyl,--CX--R.sup.3, --SO.sub.2 R.sup.3 or --PX(OR.sup.4).sub.2 orR.sup.1 and R.sup.2 together form .dbd.CR.sup.5 R.sup.6 or --CO--Z--CO--,X is oxygen or sulfur,R.sup.3 is C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.6 -alkenyl, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, morpholino, piperidino, pyrazolidino or C.sub.1 -C.sub.8 -alkylcarbonylamino, substituted or unsubstituted phenylamino or benzylamino,R.sup.4 is C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -haloalkyl or substituted or unsubstituted phenyl,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl, or substituted or unsubstituted phenyl,R.sup.
    Type: Grant
    Filed: April 8, 1991
    Date of Patent: June 1, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Hagen, Hans Ziegler, Juergen Pfister, Gerhard Nilz, Gisela Lorenz, Juergen Dressel