Plural Piperidine Rings Patents (Class 546/186)
  • Patent number: 5889024
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: April 23, 1996
    Date of Patent: March 30, 1999
    Assignee: Zeneca Limited
    Inventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
  • Patent number: 5886191
    Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: March 23, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
  • Patent number: 5883096
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds of formula I ##STR1## wherein one of Y and Z is N and the other is N, CH, or C-alkyl;X is --O--, --SO.sub.0-2 --, amino, substituted amino, --CO--, --CH.sub.2 --, mono or di-substituted methylene, --CS--, --CONR.sup.20 --, --NR.sup.20 --SO.sub.2 --, --NR.sup.20 CO--, --SO.sub.2 NR.sup.20 --, --CH.dbd.CH--, --C.tbd.C-- or --NHC(O)NH--;R is optionally substituted phenyl, aryl or cycloalkyl, or other substituents as defined in the specification;R.sup.1 and R.sup.21 are H, CN or optionally substituted alkyl, or other substituents as defined in the specification;R.sup.2 is optionally substituted cycloalkyl or piperidyl, or other substituents as defined in the specification; andR.sup.3, R.sup.4, R.sup.5, R.sup.20, R.sup.27 and R.sup.
    Type: Grant
    Filed: February 16, 1996
    Date of Patent: March 16, 1999
    Assignee: Schering Corporation
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Patent number: 5872294
    Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts and the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: February 16, 1999
    Assignee: General Electric Company
    Inventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
  • Patent number: 5869655
    Abstract: A diamine useful as a catalyst for the polymerization of urethane. A method of making the catalyst comprises reacting a spiro quaternary amine with a secondary amine. The spiro quaternary amine is also useful as an antimicrobial agent.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: February 9, 1999
    Assignee: Buckman Laboratories International, Inc.
    Inventors: Wallace E. Puckett, Mark L. Zollinger
  • Patent number: 5859250
    Abstract: A description is given, as an alternative to known processes, of a process for preparing 4-amino-2,2,6,6-tetramethylpiperidine (TAD) of the formula (I) ##STR1## which comprises the steps of reacting without catalysis, in a first step, 2,2,6,6-tetramethylpiperidine-4-one(TAA) of the formula II ##STR2## with TAD to form 2,2,6,6-tetramethyl4?(2,2,6,6tetramethyl-4-piperidylidene)- amino!piperidine (imine III) of the formula III below ##STR3## and of reacting, in a further step, the imine (III) with ammonia and hydrogen in the presence of a hydrogenation catalyst to give 2 mol equivalents of TAD.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: January 12, 1999
    Assignee: BASF Aktiengesellschaft
    Inventor: Manfred Julius
  • Patent number: 5846979
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters, amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: February 28, 1997
    Date of Patent: December 8, 1998
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
  • Patent number: 5837707
    Abstract: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (I), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, m being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 17, 1998
    Assignee: H. Lundbeck A/S
    Inventors: Jens Perregaard, John W. Stenberg, Ejner K. Moltzen
  • Patent number: 5834486
    Abstract: The invention relates to compounds of formula (I) ##STR1## wherein either R.sub.1 is hydrogen andR.sub.2 is lower alkyl lower alkenyl or lower alkynyl,m is 3 or 4 andn is 2 or 3;orR.sub.1 and R.sub.2 together are tetrainethylene,m is 3 or 4 andn is 2;or salts thereof.The compounds of formula (I) influence polyamine biosynthesis and have antiproliferative activity as well as an action against protozoans.
    Type: Grant
    Filed: September 15, 1997
    Date of Patent: November 10, 1998
    Assignee: Novartis AG
    Inventors: Jorg Frei, Jaroslav Stanek
  • Patent number: 5830905
    Abstract: Derivatives of piperidine are useful in prophylaxis and treatment of hepatitis C virus infections.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: November 3, 1998
    Assignee: Viropharma Incorporated
    Inventors: Guy D. Diana, Thomas R. Bailey, Theodore J. Nitz
  • Patent number: 5817822
    Abstract: The present invention relates to the alpha-(N-substituted pyrrolidinyl and piperidinyl) alpha-(arysulfonamido)-aceto-hydroxamic acids of formula I ##STR1## wherein R represents acyl derived from a carboxylic acid, from a carbonic acid or from a carbamic acid; or R represents (lower alkyl, aryl-lower alkyl or aryl)-sulfonyl, di-(aryl-lower alkyl or alkyl)-aminosulfonyl, or aryl-lower alkyl; Ar represents carbocyclic aryl, heterocyclic aryl or biaryl; R.sub.1 and R.sub.2 represent independently hydrogen, lower alkyl, lower alkoxy, halogen, hydroxy, acyloxy, lower alkoxy-lower alkoxy, trifluoromethyl or cyano; or R.sub.1 and R.sub.
    Type: Grant
    Filed: January 24, 1997
    Date of Patent: October 6, 1998
    Assignee: Novartis Corporation
    Inventors: Philippe G. Nantermet, David T. Parker, Lawrence J. MacPherson
  • Patent number: 5770600
    Abstract: This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 23, 1998
    Assignee: Corvas International, Inc.
    Inventors: Matthew Mark Abelman, Robert John Ardecky, Ruth Foelsche Nutt
  • Patent number: 5770735
    Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## and their enantiomers, useful as neurokinin receptor antagonists.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: June 23, 1998
    Assignee: Elf Sanofi
    Inventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased
  • Patent number: 5756730
    Abstract: A process for preparing a compound of the formula (I) ##STR1## in which, R.sup.1 and R.sup.2 are the same or different and each is 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 heterocyclic ring which is unsubstituted or substituted and is a 5-membered or 6-membered N-heterocycle which optionally has a further heteroatom which is oxygen, nitrogen or sulfur; E is methylene; ring A is a unsubstituted or unsubstituted aryl ring, or a substituted or an unsubstituted heteroaryl ring; R.sup.3 is a C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen, or R.sup.3 and R.sup.4 together are a group of the formula --(CR.sup.a R.sup.b).sub.m --C(.dbd.Y)-- (IV), wherein each of R.sup.a and R.sup.b is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: January 28, 1997
    Date of Patent: May 26, 1998
    Assignee: Sankyo Company, Limited
    Inventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
  • Patent number: 5756519
    Abstract: The following invention relates to compounds which are effective for inhbiting platelet aggregation, pharmaceutical compositions for effecting such activity and a method for inhibiting platelet aggregation.
    Type: Grant
    Filed: June 20, 1997
    Date of Patent: May 26, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, James M. Samanen
  • Patent number: 5756508
    Abstract: This invention is concerned with novel 1,3-dihydro-1-?1-(1-heteroarylpiperidin-4-yl)piperidin-4-yl!-2H-benzimidaz olones, derivatives thereof, their preparation, method of use and pharmaceutical compositions. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: May 26, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Wayne J. Thompson, Richard W. Ransom, Pierre Mallorga, Michael F. Sugrue
  • Patent number: 5750767
    Abstract: The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting groupAA is an amino acid residue andX is H or a protecting group useful,and the first amino and peptide have a free amino group and a blocked carboxy end.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 12, 1998
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Louis A. Carpino, Ayman Ahmed El-Faham
  • Patent number: 5712418
    Abstract: The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting groupAA is an amino acid residue andX is H or a protecting group useful,and the first amino and peptide have a free amino group and a blocked carboxy end.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: January 27, 1998
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Louis A. Carpino, Ayman Ahmed El-Faham
  • Patent number: 5710240
    Abstract: The invention relates to compounds of the formula I ##STR1## in which n is a number in the range from 1 to 100; X is --R.sup.7 --, --CO--, --CO--CO--, --CO--R.sup.2 --CO--, --CO--NH--R.sup.5 --NH--CO--, --CO--O--R.sup.6 --O--CO-- or ##STR2## where p is a number in the range from 0 to 6, X' is O or a direct bond, E is C.sub.1 -C.sub.12 alkyl, phenyl, C.sub.7 -C.sub.12 phenylalkyl or C.sub.5 -C.sub.12 cycloalkyl, and E' is hydrogen or is as defined for E;Z, when X is R.sup.7, is O or NR.sup.1 ; Z, when X is ##STR3## is O; and Z, in all other cases, is O, NH or NR.sup.1 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.7 -C.sub.9 phenylalkyl, C.sub.5 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.8 alkanoyl, benzoyl or C.sub.1 -C.sub.4 alkyl-substituted benzoyl;R.sup.2 and R.sup.7 are C.sub.1 -C.sub.18 alkylene; C.sub.2 -C.sub.18 alkylene which is interrupted by O or S; phenylene; a mixed aromatic/aliphatic radical containing 7 to 12 carbon atoms; naphthylene; or an --R.sup.4 --D--R.sup.4 -- radical;R.sup.
    Type: Grant
    Filed: February 26, 1996
    Date of Patent: January 20, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Alfred Steinmann
  • Patent number: 5698607
    Abstract: Tertiary diamines having two saturated heterocyclic rings joined by an aliphatic carbon chain, of the general formula ##STR1## in which each A is a two- to four-membered aliphatic carbon chain substituted if desired by one or more C.sub.1 -C.sub.4 -alkyl groups, are prepared in one stage by catalytic hydrogenation of the corresponding dinitriles of the general formulaN.tbd.C--A--C.tbd.N IIThe diamines preparable in accordance with the invention are particularly suitable as catalysts for the production of polyurethanes.
    Type: Grant
    Filed: January 30, 1997
    Date of Patent: December 16, 1997
    Assignee: Lonza AG
    Inventors: Josef Heveling, Andreas Gerhard, Ulrich Daum
  • Patent number: 5686609
    Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;Ar and Ar' independently are a thienyl group; a substituted or unsubstituted phenyl group; or an imidazolyl group; it also being possible for Ar' to be a benzothienyl group which is unsubstituted or substituted by a halogen; a naphthyl group which is unsubstituted or substituted by a halogen; a biphenyl group; or a substituted or unsubstituted indolyl;X is hydrogen;X' is hydrogen or a hydroxyl group or is joined to X" below to form a carbon-carbon bond, or X and X' together form an oxo group or a dialkylaminoalkoxyimino group of the formula .dbd.N--O--(CH.sub.2).sub.p --Am, in which p is 2 or 3 and Am is a dialkylamino group;Y is a nitrogen atom or a group C(X"), in which X" is hydrogen or forms a carbon-carbon bond with X';Q is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aminoalkyl group of the formula --(CH.sub.2).sub.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: November 11, 1997
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5679794
    Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a hydroxylamine moiety where the N-hydroxy group is not attached to a nitrogen atom in a piperidine ring are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 21, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Joseph Suhadolnik, Ramanathan Ravichandran, Valerio Borzatta, Graziano Vignali
  • Patent number: 5668198
    Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a hydroxylamine moiety where the N-hydroxy group is not attached to a nitrogen atom in a piperidine ring are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 16, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Joseph Suhadolnik, Ramanathan Ravichandran, Valerio Borzatta, Graziano Vignali
  • Patent number: 5665885
    Abstract: Esters or phenol ethers of the formula I or II ##STR1## in which m and n are each an integer from the range from 1 to 6; A.sup.1 is an m-valent hydrocarbon radical having 1 to 30 carbon atoms; or an m-valent hydrocarbon radical having 2 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and the free valencies of which are located on carbon atoms and in which A.sup.1, in the case where m=2, additionally is a direct bond;A.sup.2 is an n-valent aromatic or araliphatic hydrocarbon radical having 6 to 30 carbon atoms; or an n-valent aromatic or araliphatic hydrocarbon radical having 5 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and n free valencies of which are located on those carbon atoms which are a constituent of aromatic rings;R.sup.1 is hydrogen; a hydrocarbon or hydrocarbonoxy radical having 1 to 36 carbon atoms, which is unsubstituted or substituted by --CO--N(R.sup.3).sub.2 or interrupted by --CO--N(R.sup.3)-- or --N(R.sup.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 9, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: Alfred Steinmann
  • Patent number: 5658928
    Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'" and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: August 19, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler, Marcel Muller, Beat Steiner, Thomas Weller
  • Patent number: 5654299
    Abstract: The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided.
    Type: Grant
    Filed: April 18, 1994
    Date of Patent: August 5, 1997
    Assignee: Zeneca Limited
    Inventors: Ashokkumar Bhikkappa Shenvi, Robert Toms Jacobs
  • Patent number: 5637714
    Abstract: Esters or phenol ethers of the formula I or II ##STR1## in which m and n are each an integer from the range from 1 to 6; A.sup.1 is an m-valent hydrocarbon radical having 1 to 30 carbon atoms; or an m-valent hydrocarbon radical having 2 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and the free valencies of which are located on carbon atoms; and in which A.sup.1, in the case where m=2, additionally is a direct bond;A.sup.2 is an n-valent aromatic or araliphatic hydrocarbon radical having 6 to 30 carbon atoms; or an n-valent aromatic or araliphatic hydrocarbon radical having 5 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and n free valencies of which are located on those carbon atoms which are a constituent of aromatic rings;R.sup.1 is hydrogen; a hydrocarbon or hydrocarbonoxy radical having 1 to 36 carbon atoms, which is unsubstituted or substituted by --CO--N(R.sup.3).sub.2 or interrupted by --CON(R.sup.3)-- or --N(R.sup.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 10, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: Alfred Steinmann
  • Patent number: 5635510
    Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: June 3, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, George D. Maynard
  • Patent number: 5625060
    Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## and their enantiomers, useful as neurokinin receptor antagonists.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: April 29, 1997
    Assignee: Elf Sanofi
    Inventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, Marie Bousquet, legal representative, Catherine M. L. Goulaouic, legal representative
  • Patent number: 5621107
    Abstract: Azo dyes of the formula ##STR1## where D is the radical of a diazo component, andX is substituted or unsubstituted C.sub.2 -C.sub.8 -alkylene,in the form of the free acid or its salts, the use thereof for dyeing or printing natural or synthetic substrates, sulfopyridones as coupling components for these dyes, and a process for preparing them.
    Type: Grant
    Filed: December 28, 1995
    Date of Patent: April 15, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Gunther Lamm, Helmut Reichelt, Matthias Wiesenfeldt
  • Patent number: 5618938
    Abstract: Compounds of the formula ##STR1## and their salts with mineral or organic acids are useful as neurokinin receptor antagonists. Methods of preparing the compounds, especially pure STEREO ISOMERS thereof, are provided.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 8, 1997
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5614534
    Abstract: The present invention concerns .beta.,.beta.-dimethyl-4-piperidineethanamine compounds of the formula: ##STR1## (wherein groups R.sub.1 to R.sub.3 are defined as indicated in the description), and addition salts thereof.It also concerns a process for their preparation and their therapeutic use as inhibitors for the cholesterol biosynthesis, in particular as epoxysqualene cyclase inhibitors, for obtaining an as hypocholesterolemic, hypolipemic, antiatheromatic and/or antifungal drug.
    Type: Grant
    Filed: October 30, 1995
    Date of Patent: March 25, 1997
    Assignee: Fournier Industrie et Sante
    Inventors: Jean Binet, Soth Samreth, Daniel de Fornel
  • Patent number: 5610227
    Abstract: The present invention provides anionic polymerization initiators, comprising lithium amino magnesiate complexes, resulting in diene polymer and copolymer elastomers. The invention initiators have stable living ends at high polymerization temperatures and produce polymers containing a high level of tertiary amine functionality. Such polymers exhibit an increased efficiency in coupling termination reactions, and elastomers and products prepared from such polymers exhibit reduced hysteresis properties. Methods are also provided for preparing the initiators, the polymers and the elastomers.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 11, 1997
    Assignee: Bridgestone/Firestone, Inc.
    Inventors: Thomas A. Antkowiak, James E. Hall
  • Patent number: 5574162
    Abstract: 1-Hydrocarbyloxy substituted hindered amine compounds which also contain a reactive functional group such as hydroxy, amino, oxirane or carboxyl can be chemically attached to selected polymer substrates by condensation reactions to give polymers containing a chemically-bonded, non-migrating stabilizer having excellent stabilization efficacy for protecting said polymer substrate from the adverse effects of actinic light.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: November 12, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: James P. Galbo, Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
  • Patent number: 5504211
    Abstract: A polyalky-piperidinyl-containing .beta.-aminoacrylic ester derivative represented by the formula I ##STR1## is useful in stabilizing plastic and paints against light, oxygen and heat.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: April 2, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Alexander Aumueller, Alfred Krause, Hubert Trauth
  • 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: 5457204
    Abstract: Esters or phenol ethers of the formula I or II ##STR1## in which m and n are each an integer from the range from 1 to 6; A.sup.1 is an m-valent hydrocarbon radical having 1 to 30 carbon atoms; or an m-valent hydrocarbon radical having 2 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and the free valencies of which are located on carbon atoms; and in which A.sup.1, in the case where m=2, additionally is a direct bond;A.sup.2 is an n-valent aromatic or araliphatic hydrocarbon radical having 6 to 30 carbon atoms; or an n-valent aromatic or araliphatic hydrocarbon radical having 5 to 30 carbon atoms, which contains the heteroatoms oxygen, nitrogen and/or sulfur and n free valencies of which are located on those carbon atoms which are a constituent of aromatic rings;R.sup.1 is hydrogen; a hydrocarbon or hydrocarbonoxy radical having 1 to 36 carbon atoms, which is unsubstituted or substituted by --CO--N(R.sup.3).sub.2 or interrupted by --CO--N(R.sup.3)-- or --N(R.sup.
    Type: Grant
    Filed: July 7, 1994
    Date of Patent: October 10, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Alfred Steinmann
  • Patent number: 5455348
    Abstract: The invention relates to cyclic imino derivatives of general formulaB--X.sub.5 --X.sub.4 --X.sub.3 --X.sub.2 --X.sub.1 --A--Y--E(I)whereinA, B, E, X.sub.2 to X.sub.5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.
    Type: Grant
    Filed: December 23, 1993
    Date of Patent: October 3, 1995
    Assignee: Karl Thomae
    Inventors: Volkhard Austel, Wolfgang Eisert, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Helmut Pieper, Johannes Weisenberger
  • Patent number: 5416216
    Abstract: Novel piperidine compounds of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, n is e.g. 1 and A is e.g. --COR.sub.2 with R.sub.2 being C.sub.1 -C.sub.18 alkyl.The said compounds are effective as light stabilisers, heat stabilizers and oxidation stabilisers for organic materials.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: May 16, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Roberto Scrima, Graziano Zagnoni
  • Patent number: 5413997
    Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: May 9, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
  • Patent number: 5340822
    Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: August 23, 1994
    Assignee: Elf Sanofi
    Inventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
  • Patent number: 5322947
    Abstract: Crude N,N'-bis(2,2,6,6-tetramethyl-4-piperidyl)alkanediamine represented by the formula: ##STR1## wherein n is an integer of 2 to 10, is purified by crystallization from a ketone solvent of 3 to 9 carbon atoms. The purified product thus obtained has a purity of 98% by weight or more, a 2,2,6,6-tetramethyl-4-piperidone content of 150 ppm or less, and an initial APHA value of 30 or less. The purified product is also inhibited from discoloration with the passage of time.
    Type: Grant
    Filed: January 14, 1993
    Date of Patent: June 21, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shinya Tanaka, Manji Sasaki, Shinichi Yachigo, Hiroki Yamamoto, Eiiti Yoneyama
  • Patent number: 5317020
    Abstract: Aromatic amine derivatives of the general formula (I) ##STR1## or salts of the derivatives with mineral or organic acids are useful as neurokinin receptor antagonists.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: May 31, 1994
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5316553
    Abstract: Salts of ionic dyes with compounds which contain at least one ammonium, cycloammonium or immonium group and at least one aliphatic, cycloaliphatic or carbonyl radical-substituted aromatic group or containing a piperazine or piperidine group or a heteroaromatic group selected from those of the triazine, pyrimidine, quinazoline, quinoxaline, phthalazine or phthalimidine series or which contain at least two carboxylic acid groups, at least one amino group and at least one carboxylic acid group or at least one sulfonic acid group and one aliphatic, cycloaliphatic, monocyclic aromatic or heteroaromatic group are useful for dyeing synthetic materials, particularly synthetic polyamides in the mass. The obtained dyeings have exceptionally good wet fastness.
    Type: Grant
    Filed: July 26, 1991
    Date of Patent: May 31, 1994
    Assignee: Sandoz Ltd.
    Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas
  • Patent number: 5290932
    Abstract: Amines of the general formula I ##STR1## where R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.20 -alkyl, C.sub.3 -C.sub.20 -cycloalkyl, C.sub.4 -C.sub.20 -alkylcycloalkyl, C.sub.4 -C.sub.20 -cycloalkylalkyl, aryl, C.sub.7 -C.sub.20 -alkylaryl, C.sub.7 -C.sub.20 -aralkyl or a heterocyclic radical and n is an integer of from 3 to 7, are prepared by a process in which a ketone of the general formula II ##STR2## where R.sup.1 and R.sup.2 have the abovementioned meanings, is reacted with a cyclic amine of the general formula III ##STR3## where n has the abovementioned meanings, in the presence of a zeolite and/or SiO.sub.2 having a zeolite structure and/or a phosphate and/or a phosphate having a zeolite structure as catalysts at from 50.degree. to 500.degree. C. and from 0.01 to 50 bar.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: March 1, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Uwe Dingerdissen, Wolfgang Hoelderich
  • Patent number: 5290790
    Abstract: The compounds correspond to the general formula ##STR1## in which R.sub.1 represents a hydrogen atom or a group --COR.sub.2, in which R.sub.2 represents a benzene ring, cyclopentylmethyl, cyclohexylmethyl, cyclopentylethyl or cyclohexylethyl groups or cyclopentylamine, cyclohexylamine or phenylamine, chlorophenylamine or dichlorophenylamine groups; R represents a hydrogen atom or a group COR.sub.3, in which R.sub.3 represents an aliphatic group, a cyclane or benzene ring-system, a group a group (CH.sub.2).sup.m R.sub.4, a group --CH.dbd.CHR.sub.8 or a secondary amine group --NH(CH.sub.2).sub.n R.sub.
    Type: Grant
    Filed: December 30, 1991
    Date of Patent: March 1, 1994
    Assignees: National De La Sante et De La Recherche Medicale, Societe Civile Bioprojet, Universite De Caen - Esplanade De La Faix
    Inventors: Jean-Michel Arrang, Monigue Garborg, Jean-Charles M. Lancelot, Jeanne-Marie Lecomte, Max-Fernand Robba, Jean-Charles Schwartz
  • Patent number: 5290796
    Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl;R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl;n is zero or one;R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl;R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: March 1, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
  • Patent number: 5273982
    Abstract: Acetic acid derivatives of formulaH.sub.2 N(NH)C--X--Y--CO--Z--CH(Q.sup.1)COOQ.sup.2 Iand hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of adhesive proteins to blood platelets and also to inhibit blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: March 5, 1991
    Date of Patent: December 28, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • 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: 5248778
    Abstract: A polyalkylpiperidine derivative of formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.8 -alkyl, phenyl- or tolylalkyl with 1 to 4 carbon atoms in the alkyl, C.sub.1 -C.sub.6 -acyl, benzoyl, allyl, cyanomethyl, hydroxyethyl, aminoethyl, hydroxyl or oxyl free radical,R.sup.2 is a radical of the formula: ##STR2## R.sub.3 is hydrogen, C.sub.1 -C.sub.22 -alkyl, C.sub.3 -C.sub.22 -alkenyl, C.sub.7 -C.sub.22 -phenyl- and diphenylalkyl, where the phenyl can be unsubstituted or substituted one to three times by C.sub.1 -C.sub.12 -alkyl, C.sub.1 --C.sub.12 -alkoxy, fluorine, chlorine, bromine, C.sub.3 -C.sub.12 -alkylamino or C.sub.1 -C.sub.12 -dialkylamino, or is C.sub.3 -C.sub.12 -cycloalkyl or bicycloalkyl, C.sub.4 -C.sub.22 -alkyl which is interrupted by oxygen or nitrogen atoms and which can additionally carry hydroxyl groups, phenyl which can be substituted by one to three methyl or carbo-C.sub.1 -C.sub.12 -alkoxy groups, or is C.sub.1 -C.sub.
    Type: Grant
    Filed: October 15, 1991
    Date of Patent: September 28, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Alexander Aumueller, Hubert Trauth