The Chalcogen Is In An -oh Or -om Group (m Is Group Ia Or Group Iia Light Metal) Patents (Class 546/240)
-
Patent number: 6153754Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: ##STR1## where Z is --CG.sup.1 G.sup.2 G.sup.3, ##STR2## and where m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR.sup.5 ; G.sup.1, G.sup.2, and G.sup.3 are the same or different and are selected from the group consisting of OR.sup.8, SR.sup.8, and NR.sup.8 R.sup.9 ; and R.sup.5, R.sup.8, and R.sup.9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety.Type: GrantFiled: December 21, 1995Date of Patent: November 28, 2000Assignee: Albany Molecular Research, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
-
Patent number: 6153755Type: GrantFiled: November 10, 1997Date of Patent: November 28, 2000Assignee: SmithKline Beecham plcInventors: David S. Ennis, David Charles Lathbury
-
Patent number: 6147217Abstract: Processes for preparing compounds having the general formula: ##STR1## wherein R.sup.1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula IV ##STR2## wherein R.sup.1 and R.sup.2 are as defined in the specification.Type: GrantFiled: May 24, 1999Date of Patent: November 14, 2000Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Qun Kevin Fang, Scott Harold Wilkinson
-
Patent number: 6147216Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula ##STR1## wherein W represents --C(.dbd.O)-- or --CH(OH)--;R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen;R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;m is an integer 0 or 1;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R.sub.1 and R.sub.2 are ta to form a second bond between the carbon R.sub.1 and R.sub.2 or where R.sub.1 represented hydroxy integer 0.Type: GrantFiled: June 2, 1995Date of Patent: November 14, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
-
Patent number: 6124323Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.Type: GrantFiled: September 16, 1998Date of Patent: September 26, 2000Assignees: Warner-Lambert Company, Cocensys, IncorporatedInventors: Christopher F. Bigge, Po-Wai Yuen, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F. W. Keana, Anthony P. Guzikowski
-
Patent number: 6110937Abstract: Compounds selected from the group of compounds represented by Formula I: ##STR1## as an individual isomer or as a racemic or non-racemic mixture of isomers, and their pharmaceutically acceptable salts and N-oxides thereof; are sodium channel blockers, and thus exhibit useful pharmacological properties, including utility for the treatment of neuropathic pain conditions.Type: GrantFiled: March 24, 1998Date of Patent: August 29, 2000Assignee: Syntex USA, Inc.Inventors: David Garrett Loughhead, Xiao-Fa Lin, Robert James Weikert, Lee Allen Flippin
-
Patent number: 6090824Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists Substance P and 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: November 14, 1996Date of Patent: July 18, 2000Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Bruce T. Dembofsky
-
Patent number: 6066737Abstract: The subject invention pertains to optically-enriched compounds of formula (1), wherein Ar is a C.sub.6-20 aryl group; and R.sup.1 and R.sup.2 are independently H, alkyl or aryl. The subject invention also pertains to method of preparing these compounds. The subject compounds can be prepared by reduction of the corresponding 1,4-dihydropyridine-3-aldehyde, e.g., using hydrogen an a catalyst. The aldehyde can be prepared by hydrolytic cleavage of an aminal obtainable by the reaction of 3-pyridinecarboxaldehyde and a chiral C-2 symmetric diamine, an then stereoselective introduction of the Ar and COOCHR.sup.1 R.sup.2 groups.Type: GrantFiled: June 29, 1998Date of Patent: May 23, 2000Assignee: Chirotech Technology, Ltd.Inventors: Brian Michael Adger, Gerard Andrew Potter, Martin Edward Fox
-
Patent number: 6015899Abstract: Products are described which can be obtained by reacting components a), b) and c), where component a) is a compound of the formula I or a mixture of compounds of the formula I, component b) is a compound of the formula II or a mixture of compounds of the formula II and component c) is a compound of the formula III or a mixture of compounds of the formula III, ##STR1## in which the general symbols are as defined in claim 1, the compound of the formula I being, for example, pentaerythritol, thiodiethylene glycol, 1,4-butanediol, 1,4-propanediol, diethylene glycol, triethylene glycol, diethanolamine or glycerol, the compound of the formula II being, for example, sunflower oil or coconut fat, and the compound of the formula III being, for example, methyl 3-(3',5'-di-tert-butyl-4'-hydroxyphenyl)propionate. The abovementioned products can be used as liquid antioxidants in polymers and lubricants.Type: GrantFiled: April 21, 1997Date of Patent: January 18, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Paul Dubs, Roger Martin, Samuel Evans
-
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: 5948914Abstract: A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R.sup.2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or --CO.sub.2 R.sup.7 group in which R.sup.7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group.Type: GrantFiled: April 2, 1998Date of Patent: September 7, 1999Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Kiyoshi Sugi, Nobushige Itaya, Tadashi Katsura, Masami Igi, Shigeya Yamazaki, Taro Ishibashi, Teiji Yamaoka, Yoshihiro Kawada, Yayoi Tagami
-
Patent number: 5935585Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: February 23, 1996Date of Patent: August 10, 1999Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Laurence Vigne
-
Patent number: 5936090Abstract: The present invention provides improved processes for the chemical reduction of imide esters to the corresponding amino alcohols with yields greater than 76%. A specific range of ethereal to hydrocarbon solvent ratio is used. The improved yield can be achieved using as a reducing agent lithium aluminum hydride or the less costly sodium aluminum hydride in combination with an additive such as lithium chloride.Type: GrantFiled: May 22, 1997Date of Patent: August 10, 1999Assignee: FMC CorporationInventors: Anne Pautard-Cooper, Philip Franklin Sims, James Anthony Schwindeman
-
Patent number: 5925761Abstract: Processes for preparing compounds having the general formula: ##STR1## wherein R.sup.1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula II ##STR2## and elaborate the product by reductive amination of an aldehyde of formula IVa ##STR3## with .alpha.,.alpha.-diphenyl-4-piperidinemethanol.Type: GrantFiled: February 4, 1997Date of Patent: July 20, 1999Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Qun Kevin Fang, Scott Harold Wilkinson
-
Patent number: 5872117Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: November 4, 1997Date of Patent: February 16, 1999Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
-
Patent number: 5863903Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.Type: GrantFiled: March 14, 1995Date of Patent: January 26, 1999Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Ole Kirk
-
Patent number: 5795901Abstract: Compounds of the following structure are disclosed as effective insecticides: ##STR1## in which Q is hydroxy; U is --(CH.sub.2).sub.n --, where n is 1; R is ##STR2## in which V, W, Y, and Z are each hydrogen; X is alkoxy, cycloalkylalkoxy, alkoxycarbonyl, alkoxycarbonylamino, or a five- or six-membered heteroaryl or heteroaryloxy, each heteroaryl optionally substituted with halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkoxyalkyl, or haloalkoxyalkyl; R.sup.1 and R.sup.2 are independently selected from haloalkyl; phenyl substituted with halogen, halothio, haloalkyl, or haloalkoxy; or a five- or six-membered heteroaryl substituted with halogen or haloalkyl; R.sup.Type: GrantFiled: May 6, 1997Date of Patent: August 18, 1998Assignee: FMC CorporationInventor: Steven W. Szczepanski
-
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
-
Patent number: 5750703Abstract: The present invention relates to a process for preparation of substantially pure piperidine derivative compounds of the formulae: ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;R.sub.3 is --COOH or --COOR.sub.4 ;R.sub.4 has 1 to 6 carbon atoms;A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents.Type: GrantFiled: February 2, 1995Date of Patent: May 12, 1998Assignee: Albany Molecular Research, Inc.Inventor: Thomas E. D'Ambra
-
Patent number: 5741910Abstract: A compound of formula: ##STR1## in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.Type: GrantFiled: February 29, 1996Date of Patent: April 21, 1998Assignee: SanofiInventors: Daniel Bichon, Patrick Gueule, Didier Van Broeck, Xavier Emonds-Alt, Vincenzo Proietto
-
Patent number: 5714500Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 is hydrogen, R.sub.2 is hydrogen or C.sub.1-6 alkyl, R.sub.3 and R.sub.4 independently represent one or more radicals selected from hydrogen, NH.sub.2, NO.sub.2, halogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl, X represents S or --CH.dbd.CH-- group and pharmaceutically acceptable salts are NMDA receptor antagonists.Type: GrantFiled: March 4, 1994Date of Patent: February 3, 1998Assignee: Astra ABInventors: Ronald Conrad Griffith, Richard Jon Schmiesing, Robert John Murray
-
Patent number: 5693639Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: February 20, 1996Date of Patent: December 2, 1997Assignee: Zeneca LimitedInventors: James Roy Empfield, Daniel Ray Mayhugh, Keith Russell
-
Patent number: 5686464Abstract: A 3,3-diphenylpropylamine of the formula I, or its physiologically acceptable acid salt thereof: ##STR1## wherein R.sup.1 represents hydrogen or methyl, R.sup.2 and R.sup.3 independently represent hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula II ##STR2## wherein R.sup.4 and R.sup.5 independently represent a hydroxy substituted or unsubstituted non-aromatic hydrocarbyl group which can join together to form a ring and which together contain at least three carbon atoms, wherein at least one of R.sup.4 and R.sup.5 is hydroxy substituted, is useful in treating acetylcholine-mediated disorders such as urinary incontinence.Type: GrantFiled: July 22, 1996Date of Patent: November 11, 1997Assignee: Pharmacia ABInventors: Rolf Arne Johansson, Pinchas Moses, Lisbeth Nilvebrant, Bengt .ANG.ke Sparf
-
Patent number: 5681962Abstract: A process for the preparation of a compound of formula (I) ##STR1## in which R.sub.3 is hydrogen, C.sub.1-6 alkyl or C.sub.1-6 alkylaryl, by reduction using diborane, of a compound of Formula (II) in which R.sub.3 is as defined in relation to formula (I) and R.sup.4 is C.sub.1-6 alkyl.Type: GrantFiled: September 6, 1995Date of Patent: October 28, 1997Assignee: SmithKline Beecham plcInventor: Sidney Edward Callander
-
Patent number: 5675009Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 1, 1995Date of Patent: October 7, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
-
Patent number: 5663353Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 2, 1995Date of Patent: September 2, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
-
Patent number: 5663352Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein X represents a propylene or propenylene chain optionally substituted by one or more of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 ; m is 2, 3 or 4; n is 0, 1 or 2 when m is 2 or 3, and n is 0 or 1 when m is 4; R.sup.1 represents optionally substituted phenyl; R.sup.2 represents optionally substituted phenyl, heteroaryl, benzhydryl or benzyl; R.sup.3 represents H, COR.sup.9, CO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, COCO.sub.2 R.sup.10, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, hydroxy, cyano, COR.sup.9, NR.sup.10 R.sup.11, C(NOH)NR.sup.10 R.sup.11, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.10, COCONR.sup.10 R.sup.11, SO.sub.2 R.sup.15, CONR.sup.10 SO.sub.2 R.sup.15 and optionally substituted phenyl), Y--R.sup.8 or CO--Z--(CH.sub.2).sub.q --R.sup.12 ; R.sup.4 and R.sup.Type: GrantFiled: January 19, 1996Date of Patent: September 2, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Angus Murray MacLeod, Kevin John Merchant, Graeme Irvine Stevenson
-
Patent number: 5654433Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 3, 1995Date of Patent: August 5, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
-
Patent number: 5652370Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 2, 1995Date of Patent: July 29, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
-
Patent number: 5650516Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 3, 1995Date of Patent: July 22, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
-
Patent number: 5646149Abstract: Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the compounds and corresponding pharmaceutical compositions are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, George Barnes, Robert J. Collier, Jr.
-
Patent number: 5644061Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 1, 1995Date of Patent: July 1, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin Richard King, Michele A. Kaminski
-
Patent number: 5631375Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators, these piperidine derivatives can be described by the following formulas: ##STR1## wherein R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen; orR.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;R.sub.3 is --CH.sub.2 OH, --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched;each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts, hydrates and individual optical isomers thereof.Type: GrantFiled: January 6, 1995Date of Patent: May 20, 1997Assignee: Merrell Pharmaceuticals, Inc.Inventors: Chi-Hsin R. King, Michele A. Kaminski, Teng-Man Chen
-
Patent number: 5618940Abstract: The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.Type: GrantFiled: May 2, 1995Date of Patent: April 8, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Chi-Hsin R. King, Michele A. Kaminski
-
Patent number: 5589486Abstract: The invention relates to novel N-hydroxy-substituted 1,2,3,6-tetrahydropyridine and piperidine derivatives of the formula ##STR1## wherein A, B, D, E, G, I and R are as defined in the specification, m is 0, 1 or 2, with the proviso that:m is 0 or 2, or both G and I are hydrogen, when A is benzyl or halogen-monosubstituted benzyl group; andm is 1, when A is 2-picolyl, as well as their pharmaceutically acceptable acid addition salts. The compounds of formula (I) are useful for enhancing the tolerance of mammals (including man) against hypoxic and/or ischaemic states as well as for treating the degenerative and functional disturbances arising from hypoxic and/or ischaemic results.Type: GrantFiled: January 17, 1995Date of Patent: December 31, 1996Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Kalman Harsanyi, Tibor Gizur, Eva Agai-Csongor, Anna Kallai-Sohonyai, Marta Kapolnas-Pap, Eva Csizer, Bela Heged us, Laszlo Szporny, Bela Kiss, Egon Karpati, Eva Palosi, Zsolt Szombathelyi, Adam Sarkadi, Aniko Gere, Mihaly Bodo, Katalin Csomor, Judit Laszy, Zsolt Szentirmai, Erzsebet Lapis, Sandor Szabo, Peter Bod, Attila Csehi
-
Patent number: 5545645Abstract: Compounds of the formula: ##STR1## wherein: m is 0 or 1;R.sup.1 is hydrogen, hydroxy, or lower alkyl;R.sup.2 is hydrogen, or lower alkyl;R.sup.3 is ##STR2## or R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached represent a group of the formula: ##STR3## wherein: n is 0 or 1;p is 0, 1, 2 or 3;q is 0 or 1;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, or optionally substituted phenyl;R.sup.5 is optionally substituted phenyl;X is (CH.sub.2).sub.p, or 4-piperidin-1-yl;Y is CH, CH--O--, CH--S--, or nitrogen;Z is CH.sub.2, NH, sulfur, or oxygen; andA is a substituted furanyl group.Type: GrantFiled: March 9, 1995Date of Patent: August 13, 1996Assignee: Syntex Pharmaceuticals, LimitedInventors: Jean-Claude Pascal, Gary McCort, Dominique Blondet, Fran.cedilla.oise Gellibert
-
Patent number: 5523464Abstract: The present invention relates to benzenesulfonamide derivatives represented by Formula (I): ##STR1## in which R.sup.1 and R.sup.2 independently represent hydrogen or lower alkanoyl; and R.sup.3 and R.sup.4 independently represent hydrogen, lower alkyl, cycloalkyl, substituted or unsubstituted polycycloalkyl, substituted aryl, or a substituted or unsubstituted heterocyclic group, or R.sup.3 and R.sup.4 are combined together with the adjacent nitrogen atom to form a substituted or unsubstituted aliphatic heterocyclic group, or a pharmaceutically acceptable salt thereof. The derivatives are useful as therapeutic agents for osteoporosis.Type: GrantFiled: June 30, 1994Date of Patent: June 4, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Haruki Takai, Nobuo Kosaka, Katsura Sugawara, Akio Ishii, Hiroyuki Ishida, Katsushige Gomi
-
Patent number: 5512584Abstract: Compounds of the formula ##STR1## where A-B-D, R.sup.1, R.sup.2 and R.sup.3 have the meanings stated in the description, and their preparation are described. The compounds are suitable for controlling diseases.Type: GrantFiled: November 1, 1994Date of Patent: April 30, 1996Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Liliane Unger, Hans P. Hofmann, Hans-Juergen Teschendorf, Berthold Behl, Rudolf Binder
-
Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
-
Patent number: 5489599Type: GrantFiled: June 28, 1993Date of Patent: February 6, 1996Assignee: Shell Research LimitedInventors: Paul A. Carter, Steven J. Tapp, Nicholas J. Daniels
-
Patent number: 5486609Abstract: A process for preparing carbocyclic m-aminohydroxyaromatics comprises reacting the corresponding o-- or m-halohydroxyaromatics or metal salts thereof with primary or secondary amines in the presence of a base and in the presence or absence of a diluent.Type: GrantFiled: March 24, 1995Date of Patent: January 23, 1996Assignee: BASF AktiengesellschaftInventors: Robert Reinhardt, Helmut Reichelt, Roland Merger
-
Patent number: 5478828Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols are useful as anxiolytic agents and have other psychotropic properties.Type: GrantFiled: January 24, 1995Date of Patent: December 26, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, John D. Catt
-
Patent number: 5462947Abstract: A compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2-- or 4--CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub. 2 -C.sub.8 alkenyl, C.sub.2 -C.sub.Type: GrantFiled: October 12, 1993Date of Patent: October 31, 1995Assignee: The Upjohn CompanyInventors: Kjell A. I. Svensson, Hakan V. Wikstrom, Per A. E. Carlsson, Anna M. P. Boije, R. Nicholas Waters, Clas A. Sonesson, Nils P. Stjernlof, Bengt R. Andersson, Lars O. Hansson
-
Patent number: 5457207Abstract: The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein "spirovesamicols" which are spirofused piperidines. The compounds bind to the vesamicol receptor, a site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.Type: GrantFiled: October 5, 1993Date of Patent: October 10, 1995Assignee: Regents of the University of MinnesotaInventors: Simon M. N. Efange, Stanley M. Parsons
-
Patent number: 5438142Abstract: Compounds useful as polymer stabilizers which are polymerizable into condensation polymer systems are disclosed and claimed. A particularly preferred embodiment is 1-(3'-(benzotriazol-2"-yl)-4'-hydroxyphenyl)-1,1-bis(4-hydroxyphenyl)ethan e.Type: GrantFiled: August 10, 1993Date of Patent: August 1, 1995Assignee: Hoechst Celanese Corp.Inventors: John R. Fritsch, Olan S. Fruchey, Debasish Kuila, George Kvakovszky, Mark A. Murphy, Michael T. Sheehan, James R Sounik, Richard Vicari
-
Patent number: 5434171Abstract: This invention relates to a process for preparing certain 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates, intermediates, and congeners. Finally, the invention provides new 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates with formulations and methods for using the compounds.Type: GrantFiled: December 8, 1993Date of Patent: July 18, 1995Assignee: Eli Lilly and CompanyInventors: Scott A. Frank, Douglas E. Prather, Jeffrey A. Ward, John A. Werner
-
Patent number: 5422356Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.Type: GrantFiled: June 1, 1994Date of Patent: June 6, 1995Assignee: Eli Lilly and CompanyInventors: Dennis M. Zimmerman, Charles H. Mitch
-
Patent number: 5387593Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##Type: GrantFiled: February 17, 1994Date of Patent: February 7, 1995Assignee: Briston-Myers SquibbInventors: Ronald J. Mattson, John D. Catt
-
Patent number: 5364867Abstract: 4-Phenylpiperidines of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy or lower-alkoxy;R.sub.2 is hydrogen, hydroxy, lower-alkanoyl, aroyl, lower-alkoxycarbonyl, lower-alkanoyloxy, lower-alkoxycarbonyl, or CONR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are the same or different lower-alkyl or R.sub.3 and R.sub.4 together represent a lower-alkylene chain;X is methylene or carbonyl;Y is methylene, C.dbd.NOH, hydroxymethylene or carbonyl;or pharmaceutically acceptable acid addition salts thereof, are useful in the treatment of psychoses and other ailments of the central nervous system.Type: GrantFiled: November 30, 1992Date of Patent: November 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne
-
Patent number: 5319087Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.Type: GrantFiled: September 3, 1992Date of Patent: June 7, 1994Assignee: Eli Lilly and CompanyInventors: Dennis M. Zimmerman, Charles H. Mitch