Plural Piperidine Rings Patents (Class 546/186)
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Patent number: 5908934Abstract: A process for the preparation of compounds of formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, m, n and q are as defined herein; which comprises the steps of (a)reacting a compound of formula III ##STR2## with a chiral acid in an organic solvent to form a salt of a compound of formula I and (b) treating the salt of a compound of formula I with an aqueous base to obtain the compounds of formula I. Compounds of formula I are intermediates useful in the preparation of protein kinase inhibitors.Type: GrantFiled: September 12, 1997Date of Patent: June 1, 1999Assignee: Bristol-Myers Squibb CompanyInventor: Kyoung Soon Kim
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Patent number: 5889006Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.Type: GrantFiled: August 8, 1996Date of Patent: March 30, 1999Assignee: Schering CorporationInventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle
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Patent number: 5889024Abstract: 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: GrantFiled: April 23, 1996Date of Patent: March 30, 1999Assignee: Zeneca LimitedInventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
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Patent number: 5886191Abstract: 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: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
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Patent number: 5883096Abstract: 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: GrantFiled: February 16, 1996Date of Patent: March 16, 1999Assignee: Schering CorporationInventors: 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
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Patent number: 5872294Abstract: 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: GrantFiled: January 11, 1996Date of Patent: February 16, 1999Assignee: General Electric CompanyInventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
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Patent number: 5869655Abstract: 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: GrantFiled: November 5, 1993Date of Patent: February 9, 1999Assignee: Buckman Laboratories International, Inc.Inventors: Wallace E. Puckett, Mark L. Zollinger
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Patent number: 5859250Abstract: 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: GrantFiled: October 28, 1997Date of Patent: January 12, 1999Assignee: BASF AktiengesellschaftInventor: Manfred Julius
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Patent number: 5846979Abstract: 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: GrantFiled: February 28, 1997Date of Patent: December 8, 1998Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
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Patent number: 5837707Abstract: 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: GrantFiled: June 6, 1995Date of Patent: November 17, 1998Assignee: H. Lundbeck A/SInventors: Jens Perregaard, John W. Stenberg, Ejner K. Moltzen
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Patent number: 5834486Abstract: 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: GrantFiled: September 15, 1997Date of Patent: November 10, 1998Assignee: Novartis AGInventors: Jorg Frei, Jaroslav Stanek
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Patent number: 5830905Abstract: Derivatives of piperidine are useful in prophylaxis and treatment of hepatitis C virus infections.Type: GrantFiled: March 29, 1996Date of Patent: November 3, 1998Assignee: Viropharma IncorporatedInventors: Guy D. Diana, Thomas R. Bailey, Theodore J. Nitz
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Patent number: 5817822Abstract: 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: GrantFiled: January 24, 1997Date of Patent: October 6, 1998Assignee: Novartis CorporationInventors: Philippe G. Nantermet, David T. Parker, Lawrence J. MacPherson
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Patent number: 5770735Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## and their enantiomers, useful as neurokinin receptor antagonists.Type: GrantFiled: June 15, 1994Date of Patent: June 23, 1998Assignee: Elf SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased
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Patent number: 5770600Abstract: 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: GrantFiled: June 6, 1995Date of Patent: June 23, 1998Assignee: Corvas International, Inc.Inventors: Matthew Mark Abelman, Robert John Ardecky, Ruth Foelsche Nutt
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Patent number: 5756508Abstract: 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: GrantFiled: October 28, 1996Date of Patent: May 26, 1998Assignee: Merck & Co., Inc.Inventors: Wayne J. Thompson, Richard W. Ransom, Pierre Mallorga, Michael F. Sugrue
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Patent number: 5756519Abstract: 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: GrantFiled: June 20, 1997Date of Patent: May 26, 1998Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, James M. Samanen
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Patent number: 5756730Abstract: 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: GrantFiled: January 28, 1997Date of Patent: May 26, 1998Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
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Patent number: 5750767Abstract: 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: GrantFiled: June 6, 1995Date of Patent: May 12, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Louis A. Carpino, Ayman Ahmed El-Faham
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Patent number: 5712418Abstract: 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: GrantFiled: August 2, 1994Date of Patent: January 27, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Louis A. Carpino, Ayman Ahmed El-Faham
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Patent number: 5710240Abstract: 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: GrantFiled: February 26, 1996Date of Patent: January 20, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Alfred Steinmann
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Patent number: 5698607Abstract: 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: GrantFiled: January 30, 1997Date of Patent: December 16, 1997Assignee: Lonza AGInventors: Josef Heveling, Andreas Gerhard, Ulrich Daum
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Patent number: 5686609Abstract: 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: GrantFiled: March 11, 1994Date of Patent: November 11, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5679794Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 21, 1997Assignee: Ciba-Geigy CorporationInventors: Joseph Suhadolnik, Ramanathan Ravichandran, Valerio Borzatta, Graziano Vignali
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Patent number: 5668198Abstract: 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: GrantFiled: June 6, 1995Date of Patent: September 16, 1997Assignee: Ciba-Geigy CorporationInventors: Joseph Suhadolnik, Ramanathan Ravichandran, Valerio Borzatta, Graziano Vignali
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Patent number: 5665885Abstract: 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: GrantFiled: June 7, 1995Date of Patent: September 9, 1997Assignee: Ciba-Geigy CorporationInventor: Alfred Steinmann
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Patent number: 5658928Abstract: 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: GrantFiled: September 21, 1994Date of Patent: August 19, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler, Marcel Muller, Beat Steiner, Thomas Weller
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Patent number: 5654299Abstract: 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: GrantFiled: April 18, 1994Date of Patent: August 5, 1997Assignee: Zeneca LimitedInventors: Ashokkumar Bhikkappa Shenvi, Robert Toms Jacobs
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Patent number: 5637714Abstract: 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: GrantFiled: June 7, 1995Date of Patent: June 10, 1997Assignee: Ciba-Geigy CorporationInventor: Alfred Steinmann
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Patent number: 5635510Abstract: 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: GrantFiled: October 31, 1994Date of Patent: June 3, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, George D. Maynard
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Patent number: 5625060Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## and their enantiomers, useful as neurokinin receptor antagonists.Type: GrantFiled: June 5, 1995Date of Patent: April 29, 1997Assignee: Elf SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, Marie Bousquet, legal representative, Catherine M. L. Goulaouic, legal representative
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Patent number: 5621107Abstract: 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: GrantFiled: December 28, 1995Date of Patent: April 15, 1997Assignee: BASF AktiengesellschaftInventors: Gunther Lamm, Helmut Reichelt, Matthias Wiesenfeldt
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Patent number: 5618938Abstract: 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: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5614534Abstract: 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: GrantFiled: October 30, 1995Date of Patent: March 25, 1997Assignee: Fournier Industrie et SanteInventors: Jean Binet, Soth Samreth, Daniel de Fornel
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Patent number: 5610227Abstract: 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: GrantFiled: June 7, 1995Date of Patent: March 11, 1997Assignee: Bridgestone/Firestone, Inc.Inventors: Thomas A. Antkowiak, James E. Hall
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Patent number: 5574162Abstract: 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: GrantFiled: May 31, 1995Date of Patent: November 12, 1996Assignee: Ciba-Geigy CorporationInventors: James P. Galbo, Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
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Patent number: 5504211Abstract: 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: GrantFiled: May 31, 1994Date of Patent: April 2, 1996Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Alfred Krause, Hubert Trauth
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Patent number: 5488119Abstract: 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: GrantFiled: October 12, 1993Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventors: Evelyn Fischer-Reimann, Walter Fischer
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Patent number: 5457204Abstract: 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: GrantFiled: July 7, 1994Date of Patent: October 10, 1995Assignee: Ciba-Geigy CorporationInventor: Alfred Steinmann
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Patent number: 5455348Abstract: 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: GrantFiled: December 23, 1993Date of Patent: October 3, 1995Assignee: Karl ThomaeInventors: Volkhard Austel, Wolfgang Eisert, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Helmut Pieper, Johannes Weisenberger
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Patent number: 5416216Abstract: 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: GrantFiled: February 18, 1994Date of Patent: May 16, 1995Assignee: Ciba-Geigy CorporationInventors: Roberto Scrima, Graziano Zagnoni
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Patent number: 5413997Abstract: 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: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5340822Abstract: 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: GrantFiled: May 4, 1992Date of Patent: August 23, 1994Assignee: Elf SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
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Patent number: 5322947Abstract: 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: GrantFiled: January 14, 1993Date of Patent: June 21, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Shinya Tanaka, Manji Sasaki, Shinichi Yachigo, Hiroki Yamamoto, Eiiti Yoneyama
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Patent number: 5316553Abstract: 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: GrantFiled: July 26, 1991Date of Patent: May 31, 1994Assignee: Sandoz Ltd.Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas
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Patent number: 5317020Abstract: 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: GrantFiled: November 5, 1990Date of Patent: May 31, 1994Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5290796Abstract: 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: GrantFiled: November 20, 1992Date of Patent: March 1, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5290932Abstract: 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: GrantFiled: October 30, 1992Date of Patent: March 1, 1994Assignee: BASF AktiengesellschaftInventors: Uwe Dingerdissen, Wolfgang Hoelderich
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Patent number: 5290790Abstract: 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: GrantFiled: December 30, 1991Date of Patent: March 1, 1994Assignees: National De La Sante et De La Recherche Medicale, Societe Civile Bioprojet, Universite De Caen - Esplanade De La FaixInventors: Jean-Michel Arrang, Monigue Garborg, Jean-Charles M. Lancelot, Jeanne-Marie Lecomte, Max-Fernand Robba, Jean-Charles Schwartz
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Patent number: 5273982Abstract: 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: GrantFiled: March 5, 1991Date of Patent: December 28, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller