Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/231)
-
Patent number: 6239151Abstract: The invention provides hydrazine derivatives of the formula wherein R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is an acyl group derived from an &agr;-, &bgr;-, &ggr;- or &dgr;-(amino, hydroxy or thiol)carboxylic acid in which the amino, hydroxy or thiol group is optionally lower alkylated or the amino group is optionally acylated, sulphonylated or amidated and in which any functional group present in a side-chain is optionally protected, or a group of the formula Het(CH2)mCO; R3 is hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl-lower alkenyl, aryl or heterocyclyl; R4 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a groupinType: GrantFiled: June 14, 1999Date of Patent: May 29, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
-
Patent number: 6239126Abstract: Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, migraine, obesity, cognitive disorders and neurodegenerative diseases.Type: GrantFiled: December 13, 1999Date of Patent: May 29, 2001Assignee: American Home Products CorporationInventors: Michael G. Kelly, Gan Zhang
-
Patent number: 6229047Abstract: A nonlinear optical material which is characterized as having a relatively high macroscopic dipole moment achieved through the generally parallel packing of dipolar molecules in a relative orientation to reinforce their dipole moments. The nonlinear optical material may be a crystalline azine or imine bridged di-arene in which the arenyl groups, which can be the same or different, are substituted with an electron donor group on the first arenyl group Ar1 and A is an electron acceptor group which is substituted on the second arenyl group Ar2. B is an azine or imine bridge which extends between and interconnects the first and second arenyl groups. The nonlinear optical material has a dipole alignment factor of at least 0.1, more preferably, at least 0.5.Type: GrantFiled: December 4, 1995Date of Patent: May 8, 2001Assignee: The Curators of the University of MissouriInventors: Ranier E. Glaser, Grace S. Chen
-
Patent number: 6225302Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: August 1, 2000Date of Patent: May 1, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
-
Patent number: 6221898Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: August 29, 1997Date of Patent: April 24, 2001Assignee: Astra AktiebolagInventor: Thomas Antonsson
-
Patent number: 6204384Abstract: The present invention provides peptide aldehydes having an 3-amino-2-hydro yenyl acetamide group as part of the peptide backbone d an arginine group or analog at P1. These compounds e potent and specific or inhibitors of thrombin. Ther pharmaceutically acceptable salts, pharmaceutic ly acceptable compositions thereof, and methods of using t as therapeutic agents for disease states in mammals charachterized by abnormal thrombosis are also described. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having in history activity towards proteases of the trypsin/chymotrypsin class.Type: GrantFiled: November 26, 1997Date of Patent: March 20, 2001Assignee: Corvas International, Inc.Inventors: Joseph Edward Semple, Marguerita S. Lim-Wilby, Terence K. Brunck
-
Patent number: 6147163Abstract: A durability enhancing agent comprising the reaction product of an acrylic oligomer or acrylic polymer and an ultraviolet light absorbing compound, a hindered amine light stabilizer or mixture thereof, said durability enhancing agent further comprising more than one carbamate functional group, or group convertible to a carbamate group, and optionally, including other reactive functionality capable of undergoing a crosslinking reaction. Also included is a curable coating composition comprising the durability enhancing agent, a method for obtaining a coated substrate and the coated article obtained thereby.Type: GrantFiled: December 18, 1996Date of Patent: November 14, 2000Assignee: BASF CorporationInventors: John E. Boisseau, Donald L. St. Aubin, Patricia K. Oberg, John W. Rehfuss
-
Patent number: 6124277Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 11, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
-
Patent number: 6093733Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.Type: GrantFiled: April 30, 1997Date of Patent: July 25, 2000Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
-
Patent number: 6063926Abstract: Compounds within the genus represented by the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein: T is substituted phenyl or substituted pyridyl; ##STR2## R.sup.4 is methyl or ethyl; and Z is substituted piperidinyl.Type: GrantFiled: November 18, 1998Date of Patent: May 16, 2000Assignee: Schering CorporationInventors: Gregory A. Reichard, Cheryl A. Alaimo, Neng-Yang Shih, Pauline C. Ting, Nicholas I. Carruthers, Brian J. Lavey
-
Patent number: 6057322Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.Type: GrantFiled: July 30, 1997Date of Patent: May 2, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
-
Patent number: 6020347Abstract: 4-Substituted-4-piperidinecarboxamides of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.Type: GrantFiled: November 13, 1998Date of Patent: February 1, 2000Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann
-
Patent number: 6011047Abstract: The present invention provides peptide aldehydes having a 3-amino-2-hydroxyphyenyl-acetamide group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or amidinophenyl tail. These compounds are potent and specific inhibitors of thrombin. Their pharmaceutically salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis are also described. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having inhibitory activity toward proteases of the trypsin/chymotrypsin class.Type: GrantFiled: November 26, 1997Date of Patent: January 4, 2000Assignee: Corvas International Inc.Inventors: Joseph Edward Semple, Marguerita S. Lim-Wilby, Terence K. Brunck
-
Patent number: 6008220Abstract: Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, arthrities, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.Type: GrantFiled: June 8, 1998Date of Patent: December 28, 1999Assignee: Warner Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Daniel Fred Ortwine, Claude Forsey Purchase, Jr., Andrew David White, Qi-Zhuang Ye
-
Patent number: 6002009Abstract: Pharmacologically active novel esters and amides of di-substituted 1,4 piperidine as 5-HT.sub.4 antagonists of formula (I) ##STR1## wherein A, X, Y and R have the meanings specified in the description, and a process for their preparation, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: December 14, 1999Assignee: Boehringer Ingelheim Italia, S.p.A.Inventors: Enzo Cereda, Maura Bignotti, Vincenzo Martino, Giovanni Battista Schiavi, Angelo Sagrada
-
Patent number: 5998399Abstract: Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.Type: GrantFiled: November 16, 1998Date of Patent: December 7, 1999Assignee: Astra AktiebolagInventors: James E. Macdonald, Robert Gentile, Robert J. Murray
-
Patent number: 5958952Abstract: The present invention relates to phenyl amidines of general formula (I), ##STR1## in which R.sup.1 to R.sup.5 are as defined in claim 1, their tautomers, their stereoisomers and their mixtures and their salts, especially their physiologically acceptable salts with inorganic or organic acids or bases also having valuable pharmacological properties, preferably aggregation-limiting effects, producing them.Type: GrantFiled: December 17, 1997Date of Patent: September 28, 1999Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Volkhard Austel, Gunther Linz, Helmut Pieper, Brian Guth, Johannes Weisenberger
-
Patent number: 5939438Abstract: It has now been found that certain novel oximino and hydrazono derivatives of N-benzyl-4-benzhydryl- and 4-benhydrolpiperidines, and their corresponding N-oxides and agriculturally acceptable salts are useful as insecticides. These compounds are represented by Formula I: where R is hydrogen, halogen, alkyl, alkoxy, dialkylamino; R.sup.1 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkylcarbonyl and alkylaminocarbonyl; X is oxygen, or NR.sup.2, Q is fluoro and hydroxy; Z is halogen, haloalkyl, haloalkoxy, pentahalothio, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, and --OCF.sub.2 O-- attached to two adjacent carbon atoms of the phenyl ring; n is 0 or 1; and, when X is NR.sup.2, R.sup.2 is hydrogen, alkyl, alkylcarbonyl, alkoxycarbonyl, or R.sup.1 and R.sup.2 taken together may be --C.sub.m H.sub.2.spsb.m, or --C.sub.2 H.sub.4 OC.sub.2 H.sub.4 --, where m is 3-9. Preferred compounds include those where R is hydrogen; R.sup.Type: GrantFiled: September 9, 1998Date of Patent: August 17, 1999Assignee: FMC CorporationInventors: Walter H. Yeager, Ian R. Silverman, Robert N. Henrie, II, Thomas G. Cullen, Clinton J. Peake
-
Patent number: 5922763Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: November 26, 1997Date of Patent: July 13, 1999Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
-
Patent number: 5872115Abstract: This invention is concerned with 2-ureido-benzamide compounds of the formula (1) ##STR1## in which R.sup.1 is H, halogen atom, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)dialkylamino and R.sup.2 is H, halogen atom, hydroxy, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.3 -C.sub.6) cycloalkylmethoxy, (C.sub.1 -C.sub.4) alkylthio, (C.sub.1 -C.sub.4) alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl or ##STR2## wherein j is an integer of from 0 to 2 and R.sup.3 and R.sup.4 are each independently H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkanoyl, (C.sub.1 -C.sub.4)alkylsulfonyl or (C.sub.1 -C.sub.4)alkylcarbamoyl, NR.sup.3 R.sup.4 can to form a pyrrolidine, piperidine, morpholine, imidazole or pyrazole ring;X is a (C.sub.3 -C.sub.15)alkyl, (C.sub.3 -C.sub.6) cycloalkyl, (C.sub.3 -C.sub.6) cycloalkylmethyl, .omega.-(C.sub.1 -C.sub.4) alkoxy-(C.sub.1 -C.sub.4) alkyl group or ##STR3## wherein k is an integer of from 1 to 4 and R.sup.5 and R.sup.Type: GrantFiled: December 30, 1996Date of Patent: February 16, 1999Assignees: Grelan Pharmaceutical Co. Ltd., Laboratoires Fournier S.C.A.Inventors: Jean Binet, Christian Guffroy, Hirotaka Kasai, Nagatoshi Wagatsuma
-
Patent number: 5792769Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 --R.sup.4, R.sup.7 --R.sup.8, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: August 15, 1996Date of Patent: August 11, 1998Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Carl R. Illig, Bruce E. Tomczuk, Richard M. Soll, Nalin L. Subasinghe, Roger F. Bone
-
Patent number: 5789422Abstract: Compounds represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, wherein: A.sup.1 is --CH.sub.2 R.sup.6, --OR.sup.6, --N(R.sup.6)(R.sup.7), --S(O).sub.e R.sup.13, --(C(R.sup.6)(R.sup.7)).sub.1-6 --OR.sup.6, --(C(R.sup.6)(R.sup.7).sub.1-6 --N(R.sup.6)(R.sup.7) or --(C(R.sup.6) (R.sup.7)).sub.1-6 --S(O).sub.e R.sup.13 and A.sup.2 is H, or A.sup.1 and A.sup.2 together are .dbd.O, .dbd.C(R.sup.6)(R.sup.7), .dbd.NOR.sup.6 or .dbd.S;Q is phenyl, naphthyl, --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6 or heteroaryl;T is H, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl;b is 0, 1 or 2;b.sub.1 is 1 or 2;X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O).sub.e --, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)--, --OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.6)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --, --N(R.sup.6)C(O)O-- or --OC(O)--;R.sup.6, R.sup.7, R.sup.8a, and R.sup.Type: GrantFiled: October 28, 1996Date of Patent: August 4, 1998Assignee: Schering CorporationInventors: Gregory A. Reichard, Robert G. Aslanian
-
Patent number: 5783576Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.Type: GrantFiled: August 9, 1996Date of Patent: July 21, 1998Assignee: Boehringer Ingelheim KGInventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
-
Patent number: 5739142Abstract: 4-Aminobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: January 26, 1996Date of Patent: April 14, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rolf Gericke, Manfred Haumgarth, Norbert Beier, Klaus-Otto Minck
-
Patent number: 5736559Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: August 1, 1996Date of Patent: April 7, 1998Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
-
Patent number: 5721247Abstract: There are provided novel compounds of formula I ##STR1## wherein D, R.sup.1, R.sup.2, R.sup.3, X and p are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy.Compounds of formula I are expected to be useful inter alia in the treatment of neurodegenerative disorders.Type: GrantFiled: November 14, 1995Date of Patent: February 24, 1998Assignee: Astra AktiebolagInventor: James Edwin Macdonald
-
Patent number: 5597825Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: May 16, 1994Date of Patent: January 28, 1997Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
-
Patent number: 5578594Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.Type: GrantFiled: December 21, 1994Date of Patent: November 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, G erard Schmid
-
Patent number: 5576334Abstract: The invention concerns chemical compounds of formula IR.sup.1 --CON(R.sup.2)--CON(R.sup.3)--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention concerns processes for the preparation of the chemical compounds of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: November 19, 1996Assignee: Zeneca LimitedInventors: George R. Brown, Richard E. Shute
-
Patent number: 5559232Abstract: The novel carboxamides of the formula ##STR1## wherein A, E, G, L, M, R and Q have the significance given in the description, as well as hydrates or solvates thereof inhibit thrombin-induced platelet aggregation and fibrinogen coagulation in plasma. They can be manufactured starting from the corresponding acid and the corresponding amine H.sub.2 NCH.sub.2 Q.Type: GrantFiled: September 2, 1994Date of Patent: September 24, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, G erard Schmid
-
Patent number: 5532232Abstract: 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: GrantFiled: November 22, 1994Date of Patent: July 2, 1996Assignee: 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: 5523325Abstract: This invention relates to amidrazones, insecticidal amidrazone compositions, and methods of using such compositions.Type: GrantFiled: September 9, 1993Date of Patent: June 4, 1996Inventor: Richard M. Jacobson
-
Patent number: 5489603Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.Type: GrantFiled: July 15, 1993Date of Patent: February 6, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
-
Patent number: 5476850Abstract: There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for those cases in which arrhythmias are a result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.Type: GrantFiled: December 5, 1994Date of Patent: December 19, 1995Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser
-
Patent number: 5470921Abstract: A synthetic polyamide of formula I and its salts ##STR1## in which each R.sub.1 independently is selected from hydrogen, carboxyl, amino or a group of formula .alpha.-A.sub.1 -R.sub.10 (.alpha.)where A, is a bridging group and R.sub.10 is a sterically hindered amine group;each R.sub.2 independently is hydrogen or a group of formula .alpha.A is a bridging group of the formula ##STR2## is 0 or 1; R.sub.3 is hydrogen, C.sub.1-12 alkyl or is a significance of R.sub.10 ;R.sub.5 is hydrogen or C.sub.1-12 alkylR.sub.4 is a significance of R.sub.10 or a group of formula .alpha.; andp is an integer from 5 to 200;with the proviso that the compound of formula I contains 1-400 sterically hindered amine groups.Type: GrantFiled: May 20, 1994Date of Patent: November 28, 1995Assignee: Sandoz Ltd.Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas, Jurgen Goldmann
-
Patent number: 5432178Abstract: Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)-- (in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which ##STR3## is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R.sup.10 is H, C7-10 phenylalkyl or COOR.sup.13 (in which R.sup.13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R.sup.7 and R.sup.8 do not represent hydrogen at the same time, and (ii) when at least one group in R.sup.7, R.sup.8 and R.sup.9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA.sub.Type: GrantFiled: September 16, 1993Date of Patent: July 11, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Masanori Kawamura, Tsumoru Miyamoto
-
Patent number: 5405854Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.Type: GrantFiled: February 24, 1993Date of Patent: April 11, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid
-
Patent number: 5399570Abstract: Aspartic acid derivatives of the formula ##STR1## in which X denotes, for example, ##STR2## and R denotes, for example, cyclohexylamino, have useful pharmacological properties.Type: GrantFiled: March 25, 1993Date of Patent: March 21, 1995Assignee: Cassella AktiengesellschaftInventors: Otmar Klingler, Gerhard Zoller, Melitta Just, Bernd Jablonka
-
Patent number: 5364868Abstract: Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing themBenzoylguanidines of the formula I ##STR1## are described in which R(1) or R(2) is an amino group --NR(3)R(4), where R(3) and R(4) are H or (cyclo)alkyl or R(3) is phenyl-(CH.sub.2).sub.p -- where p=0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) can also together be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF.sub.3, C.sub.m F.sub.2m+1 --CH.sub.2 --, benzyl or phenoxy, and their pharmaceutically tolerable salts.The compounds according to the invention have very good antiarrhythmic properties, as occur, for example, in the case of oxygen deficiency symptoms.Type: GrantFiled: February 11, 1993Date of Patent: November 15, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Hans-Jochen Lang, Wolfgang Scholz, Wolfgang Linz, Udo Albus
-
Patent number: 5364864Abstract: 1,4-disubstituted piperidines of formula 1: ##STR1## as well as the therapeutically acceptable salts of these molecules. The invention also relates to the application in therapy of the compounds of the general formula 1.Type: GrantFiled: May 26, 1992Date of Patent: November 15, 1994Assignee: Pierre Fabre MedicamentInventors: Denis Bigg, Jean-Louis Vidaluc, Francis Calmel
-
Patent number: 5350852Abstract: The invention relates to a process for making compounds of formula: ##STR1##Type: GrantFiled: August 13, 1993Date of Patent: September 27, 1994Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
-
Patent number: 5322858Abstract: There are provided compounds of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and arlkyl, R.sup.3 is selected from the group consisting of same group of values as R.sup.5, R.sup.5 is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl loweralkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R.sup.6 and R.sup.7 may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R.sup.7 may also have the same value as R.sup.Type: GrantFiled: February 14, 1992Date of Patent: June 21, 1994Assignee: Jacobus Pharmaceutical Co. Inc.Inventors: Craig Canfield, David P. Jacobus, Neil J. Lewis
-
Patent number: 5302720Abstract: Compounds of formula I ##STR1## and their salts in which R.sub.1 is optionally substituted phenyl, R.sub.2 is alkyl, cycloalkyl or optionally substituted amino, or R.sub.2 and R.sub.3 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring and R.sub.5 is H, halo, alkyl, alkoxy, trifluoromethyl or a group of formula S(O).sub.m R.sub.8 in which m is 0, 1 or 2 and R.sub.8 is alkyl have utility in the treatment of diabetes particularly in the treatment of hyperglycaemia.Type: GrantFiled: June 17, 1992Date of Patent: April 12, 1994Assignee: The Boots CompanyInventor: Balasubramanian Gopalan
-
Patent number: 5294708Abstract: This invention relates to new heterocyclic derivatives of guanidine and more particularly to such derivatives which have hypoglycemic activity, their methods of use for treating hyperglycemia and novel intermediate compounds for their preparation.Type: GrantFiled: July 20, 1993Date of Patent: March 15, 1994Assignee: McNeilab, Inc.Inventors: Henry J. Breslin, Michael J. Kukla, Chris R. Rasmussen, Robert W. Tuman
-
Patent number: 5292755Abstract: Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylalkyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 --C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(4) are together an alkylene chain,and where n is equal to zero, 1 or 2and their pharmaceutically tolerable salts are outstanding antiarrhythmics.Type: GrantFiled: January 31, 1992Date of Patent: March 8, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich C. Englert, Hans-Jochen Lang, Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz
-
Patent number: 5281625Abstract: Guanidines I ##STR1## (A=C.sub.5 -C.sub.12 -cycloalkyl which may bear up to three further substituents; benzyl substituted in the para-position; R.sup.1, R.sup.2, R.sup.3 =H, C.sub.1 -C.sub.4 -alkyl; R.sup.4 =C.sub.5 -C.sub.18 -alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.18 -alkenyl, C.sub.4 -C.sub.18 -alkynyl or phenyl-C.sub.1 -C.sub.6 -alkyl, and these groups may bear up to three further substituents and the phenyl moiety of the phenylalkyl may additionally bear a phenoxy group or up to three C.sub.2 -C.sub.4 -alkenyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkyl or haloalkyl groups, C.sub.5 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.8 -alkyl, where the ring may bear up to three further substituents; A=benzyl and R.sup.4 =C.sub.3 -C.sub.4 -alkyl which may be interrupted by oxygen, or C.sub.4 -alkenyl, both of which may bear up to three further substituents; R.sup.3 +R.sup.4 =C.sub.5 -C.sub.Type: GrantFiled: December 4, 1991Date of Patent: January 25, 1994Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 5270328Abstract: N-alkylamino-3,4,4-substituted piperidines are provided which are useful as peripheral opioid antagonists.Type: GrantFiled: June 29, 1992Date of Patent: December 14, 1993Assignee: Eli Lilly and CompanyInventors: Buddy E. Cantrell, Dennis M. Zimmerman
-
Patent number: 5260307Abstract: 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: GrantFiled: June 24, 1991Date of Patent: November 9, 1993Assignee: 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: 5250542Abstract: 3,4,4-trisubstitutedpiperidinyl-N-alkylcarboxylates and intermediates for their preparation are provided. These piperidine-N-alkylcarboxylates are useful as peripheral opioid antagonists.Type: GrantFiled: July 17, 1992Date of Patent: October 5, 1993Assignee: Eli Lilly and CompanyInventors: Buddy E. Cantrell, Dennis M. Zimmerman
-
Patent number: 5236921Abstract: The invention relates to compounds of formula: ##STR1## in which Y represents--either a group Cy--N in whichCy represents a phenyl, optionally substituted; a C.sub.3 -C.sub.7 cycloalkyl group; a pyrimidinyl group or a pyridyl group;or a group ##STR2## in which Ar represents a phenyl, optionally substituted, a pyridyl group; a thienyl group;x is zero or one;X represents a hydroxyl, a C.sub.1 -C.sub.4 alkoxy; a hydroxyalkyl; a C.sub.1 -C.sub.4 acyloxy; a phenacyloxy; a carboxyl; a C.sub.1 -C.sub.4 carbalkoxy; a cyano; an aminoalkylene; a group --N--(X.sub.1).sub.2 in which the groups X.sub.1 independently represent hydrogen, a C.sub.1 -C.sub.4 alkyl; a group ##STR3## in which Alk represents a C.sub.1 -C.sub.6 alkyl; a group ##STR4## in which the Alk.sub.1 is a C.sub.1 -C.sub.3 alkylene and Alk'.sub.1 is a C.sub.1 -C.sub.3 alkyl; a C.sub.1 -C.sub.4 acyl; a group --S--X.sub.2 in which X.sub.2 represents hydrogen or a C.sub.1 -C.sub.Type: GrantFiled: September 5, 1991Date of Patent: August 17, 1993Assignee: SanofiInventors: Xavier Emonds-Ai, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck