Amino Nitrogen Attached To The Carbon By An Acyclic Carbon Or Chain Patents (Class 564/316)
-
Patent number: 6310248Abstract: The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprises the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II): wherein R1, R2 and R3 independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb): wherein R1, R2 and R3 are as defined above; b) subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb): wherein R1, R2 and R3 are as defined above; c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Virliger oxidation to form a corresponding enantiomerically enriched compound of the general formula (Va) or (Vb): wherein R1, R2 and R3 are as defined above; d) converting the compoType: GrantFiled: December 22, 2000Date of Patent: October 30, 2001Assignee: Pharmacia ABInventors: Pher G. Andersson, Christian Hedberg
-
Patent number: 6306912Abstract: Method for identifying a compound useful for the therapeutic treatment of a neurological disease or disorder such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease or Parkinson's Disease, or useful as a muscle relaxant, analgesic, or adjuvant to general anesthetics. The compound is active on a receptor-operated calcium channel, including, but not limited to, that present as part of an NMDA receptor-ionophore complex, a calcium-permeable AMPA receptor, or a nicotinic cholinergic receptor, as a noncompetitive antagonist. The method includes identifying a compound which binds to the receptor-operated calcium channel at the site bound by the arylalkylamines Compound 1, Compound 2 or Compound 3.Type: GrantFiled: June 7, 1995Date of Patent: October 23, 2001Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Bradford C. VanWagenen, Eric G. DelMar, Manuel F. Balandrin, Scott T. Moe, Linda D. Artman
-
Publication number: 20010016669Abstract: The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprises the steps of:Type: ApplicationFiled: December 22, 2000Publication date: August 23, 2001Inventors: Pher G. Andersson, Christian Hedberg
-
Patent number: 6258842Abstract: A method for the preparation of citalopram is described comprising reaction of a compound of Formula (IV) wherein R1 is H or C1-6alkylcarbonyl successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3-halogen-N,N-dimethylpropylamine, effecting ring closure of the resulting compound of Formula (IV) and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram.Type: GrantFiled: April 28, 2000Date of Patent: July 10, 2001Assignee: H. Lundbeck, A/SInventors: Hans Petersen, Peter Bregnedal, Klaus Peter Bogeso
-
Patent number: 6191165Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 30, 1997Date of Patent: February 20, 2001Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
-
Patent number: 6136863Abstract: This invention relates to compounds represented by the following formula (1): ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a substituted or unsubstituted phenylene group, R.sup.3 represents a substituted or unsubstituted phenyl group or an aliphatic hydrocarbon group containing at least four .pi. electrons, R.sup.4 represents an alkyl group having 1 to 4 carbon atoms, and m and n individually represent integers of from 1 to 4, or salts thereof, and also to compositions containing the same. These compounds have antifungal activities and are useful as drugs.Type: GrantFiled: August 7, 1998Date of Patent: October 24, 2000Assignee: Pola Chemical Industries, Inc.Inventors: Yukio Kawazu, Masayuki Yuasa, Toshimitsu Suzuki, Takuji Nakashima, Takao Itoh, Toshiro Majima
-
Patent number: 6096874Abstract: The synthesis of tamoxifen derivatives, most particularly halo, halo alkyl, hydroxy, and amino tamoxifen derivatives is disclosed. The native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule. Particular tamoxifen derivatives of the invention include chloro, bromo, iodo, fluoro, amino and DTPA tamoxifen derivatives, and corresponding lower alkyl halogenated forms. The halogenated tamoxifen derivatives possess superior binding affinities for estrogen receptor rich tissues, such as uterine tissue and breast tissue, relative to unsubstituted native tamoxifen. Radiolabeled forms of the tamoxifen derivatives may be used as highly specific imaging agents for estrogen receptor rich tissues. The fluoro and bromo tamoxifen derivatives are particularly useful for imaging estrogen receptors by PET whereas the iodinated tamoxifens are particularly useful in imaging estrogen receptors by SPECT.Type: GrantFiled: June 7, 1995Date of Patent: August 1, 2000Assignee: Board of Regents, the University of Texas SystemInventors: Sidney Wallace, David Yang, E. Delpassand, A. Cherif, S. Quadri
-
Patent number: 6071970Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: GrantFiled: June 7, 1995Date of Patent: June 6, 2000Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Manuel F. Balandrin, Bradford C. VanWagenen, Eric G. DelMar, Scott T. Moe, Linda D. Artman, Robert M. Barmore
-
Patent number: 6028103Abstract: The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. The compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.Type: GrantFiled: March 19, 1997Date of Patent: February 22, 2000Assignees: Children's Medical Center Corporation, Ion Pharmaceuticals, Inc.Inventors: Carlo Brugnara, Jose Halperin, Emile M. Bellot, Jr., Mark Froimowitz, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Falguni M. Kher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
-
Patent number: 6022895Abstract: Substituted amino compounds of general formula (I) ##STR1## are described, as are a method of preparing them and their use as drugs, especially as analgesics.Type: GrantFiled: March 11, 1998Date of Patent: February 8, 2000Assignee: Gruenenthal GmbHInventors: Oswald Zimmer, Wolfgang Werner Alfred Strassburger, Helmut Heinrich Buschmann, Werner Englberger, Elmar Josef Friderichs
-
Patent number: 6015925Abstract: This invention relates to compounds represented by the following formula (1): ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aromatic hydrocarbon group having 6 to 18 carbon atoms, R.sup.2 represents a hydrogen atom or a substituted or unsubstituted aromatic hydrocarbon group having 6 to 18 carbon atoms, R.sup.3 represents an alkyl group having 1 to 4 carbon atoms, R.sup.4 represents a substituted or unsubstituted phenyl group or an aliphatic hydrocarbon group containing at least four .pi. electrons, and m and n individually represent integers of from 1 to 4, or salts thereof, and also to compositions containing the same. These compounds have antifungal activities and are useful as drugs and the like.Type: GrantFiled: September 22, 1998Date of Patent: January 18, 2000Assignee: Pola Chemical Industries, Inc.Inventors: Yukio Kawazu, Toshimitsu Suzuki, Masayuki Yuasa, Yuichi Yokomizo, Toshiro Majima, Takao Ito, Takuji Nakashima, Akira Nozawa
-
Patent number: 5910610Abstract: A triphenylamine derivative, represented by the following general formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each represents a hydrogen atom, a lower alkyl group, an alkoxy group, a halogen atom or an aryl group which may have a substituent group; and m and n each represents 0 or 1.Type: GrantFiled: September 2, 1997Date of Patent: June 8, 1999Assignee: Takasago International CorporationInventors: Tohru Kobayashi, Yoshimasa Matsushima, Hiroshi Sugiyama, Toshimitsu Hagiwara
-
Patent number: 5773469Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.Type: GrantFiled: June 18, 1996Date of Patent: June 30, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
-
Patent number: 5739405Abstract: A process for the preparation of amines of the general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 denote hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 alkynyl, 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, or C.sub.7 -C.sub.20 aralkyl,R.sup.1 and R.sup.2 together denote a saturated or unsaturated C.sub.3 -C.sub.9 alkylene dichain andR.sup.3 or R.sup.5 denotes C.sub.21 -C.sub.200 alkyl, C.sub.21 -C.sub.200 alkenyl or they together form a C.sub.2 -C.sub.12 alkylene dichain,by the reaction of olefins of the general formula II ##STR2## in which R.sup.3, R.sup.4, R.sup.5, and R.sup.6 have the above meanings, with ammonia or primary or secondary amines of the general formula III ##STR3## in which R.sup.1 and R.sup.2 have the above meanings, at temperatures ranging from 200.degree. to 350.degree. C.Type: GrantFiled: December 4, 1996Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Karsten Eller, Rudolf Kummer, Peter Stops
-
Patent number: 5643950Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: June 2, 1995Date of Patent: July 1, 1997Assignee: Ortho Pharmaceutical CorporationInventors: James P. Demers, Sigmond Johnson, Michele Ann Weidner-Wells, Ramesh M. Kanojia, Stephanie A. Fraga, Dieter Klaubert
-
Patent number: 5561135Abstract: The invention relates to new N,N,N'N'-tetra-substituted-1,2-ethanediamine compounds of the general formula (I): ##STR1## wherein X is a carbonyl (CO), hydroxymethylen (CHOH) or p-fluorophenyl-methylen (p--F--C.sub.6 H.sub.4 --CH) group and R is a benzyl group optionally substituted in p-- with an halogen, or R is a 2-pyrimidinyl group with the proviso that simultaneously X may not be p-fluorophenyl-methylen (p--F--C.sub.6 H.sub.4 --CH) and R may not be an unsubstituted benzyl group, as well as their pharmaceutically acceptable additions salts.The compounds are potentially useful in the treatment of sigma receptor-related nervous system diseases.Type: GrantFiled: April 21, 1995Date of Patent: October 1, 1996Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Santiago Gubert, Jos e Ortiz, Aurelio Sacrist an, Josep M. Castell o
-
Patent number: 5530125Abstract: A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.Type: GrantFiled: August 19, 1994Date of Patent: June 25, 1996Assignee: Schering CorportionInventors: Joel G. Berger, Wei K. Chang, Joseph A. Kozlowski, Guowei Zhou
-
Patent number: 5438056Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.Type: GrantFiled: October 5, 1993Date of Patent: August 1, 1995Assignee: American Home Products CorporationInventors: Steven W. Felman, Kevin A. Memoli, Ivo Jirkovsky
-
Patent number: 5420130Abstract: Compounds corresponding to the general formula (I) ##STR1## in which n represents 0 or 1, R.sub.1 represents a methyl group, in which case R.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group is optionally substituted), or else R.sub.1 and R.sub.2 together form, and with the nitrogen atom which carries them, a 4-(phenoxymethyl)piperid-1-yl group (in which the phenoxy group is optionally substituted) or a 4-phenylpiperazin-1-yl group (in which the phenyl group is optionally substituted), R.sub.3 represents a hydrogen atom or a methyl group, R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydrogen atom or a group of general formula -CH.sub.2 -CH.sub.2 -NH-R.sub.6, R.sub.6 being a hydrogen atom or a tert-butyloxycarbonyl, 4-carbamoylpyrimidin-2-yl or 5-carbamoylpyrazin-2-yl group, are useful in the treatment of diseases and complaints involving hyperactivity of the .alpha.-adrenergic system at the level of the lower urinary apparatus.Type: GrantFiled: May 16, 1994Date of Patent: May 30, 1995Assignee: SynthelaboInventors: Pascal George, Benoit Marabout, Jacques Froissant
-
Patent number: 5382600Type: GrantFiled: December 19, 1991Date of Patent: January 17, 1995Assignee: Pharmacia AktiebolagInventors: Nils A. Jonsson, Bengt A. Sparf, Lembit Mikiver, Pinchas Moses, Lisbet Nilvebrant, Gunilla Glas
-
Patent number: 5233089Abstract: A novel enamine derivative is effective as a charge transport material and can provide an electrophotographic plate excellent in sensitivity, photoresponse and durability.Type: GrantFiled: December 30, 1987Date of Patent: August 3, 1993Assignee: Hitachi, Ltd.Inventors: Yasuo Katsuya, Takayuki Akimoto, Yoshii Morishita, Yasushi Shinbo, Akira Kageyama, Shigeru Hayashida
-
Patent number: 5091574Abstract: Tetrafunctional amine derivatives of digyclidyl ethers of Bisphenol A that are liquid at ambient temperatures and that are useful as curing agents for epoxy resins are disclosed together with the method by which they are prepared which comprises the steps of:dissolving the diglycidyl ether in a solvent (acetone or methyl ethyl ketone) and adding a polyoxyalkylene diamine in the mole ratio of about 4 to about 5 moles of the diglycidyl ether per mole of said polyoxyalkylene diamine to provide an initial reaction mixture,heating the initial reaction mixture with agitation at a temperature of about 80.degree. to about 160.degree. C.Type: GrantFiled: February 25, 1991Date of Patent: February 25, 1992Assignee: Texaco Chemical CompanyInventors: Jiang-Jen Lin, George P. Speranza
-
Patent number: 5086074Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sup.2 is selected from hydroxy and lower alkoxy, R.sup.5 is lower alkyl, and R.sup.11 and R.sup.12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective .alpha..sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.Type: GrantFiled: March 26, 1990Date of Patent: February 4, 1992Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Robert E. Zelle, Fatima Z. Basha
-
Patent number: 4996235Abstract: The present invention provides 3,4-diphenylbutanamines capable of selectively inhibiting the uptake of serotonin and norepinephrine.Type: GrantFiled: November 25, 1987Date of Patent: February 26, 1991Assignee: Eli Lilly and CompanyInventors: David W. Robertson, David T. Wong
-
Patent number: 4988730Abstract: The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group;orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.Type: GrantFiled: July 21, 1989Date of Patent: January 29, 1991Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyar RTInventors: Dezso Korbonits, Pal Kiss, Laszlo Szekeres, Gyula Papp, Gabor Kovacs, Andrea Santane Csutor, Sandor Virag, Eva Udvari, Imre Bata, Katalin Marmarosi nee Kellner, Laszlo Tardos, Peter Kormoczy, Vera Gergely, Zoltan Vargai
-
Patent number: 4988735Abstract: The compound N,N'-dimethyl-N-(3,4,5-trimethoxybenzyl)-N'-[3,3-di-(4-fluorophenyl)-propy l]-ethylenediamine and its salts are described.This compound is useful in the treatment of several cardiovascular pathologies.Type: GrantFiled: May 24, 1988Date of Patent: January 29, 1991Assignee: SimesInventors: Cesare Casagrande, Francesco Santangelo, Maria L. Calabi
-
Patent number: 4788010Abstract: Hypotensive activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is hydrogen or alkyl;R.sub.2 and R.sub.3 are each independently phenyl, substituted phenyl, cycloalkyl, or R.sub.2 is hydrogen and R.sub.3 is heteroaryl;R.sub.4 and R.sub.5 are the same or different and each is hydrogen, hydroxy, alkoxy, alkanoyl or alkyl;R.sub.6 is hydrogen or alkyl; andn is 1, 2, 3 or 4; with the proviso that if R.sub.2 and R.sub.3 are each phenyl, at least one of R.sub.1, R.sub.4, R.sub.5 and R.sub.6 is other than hydrogen.Type: GrantFiled: April 24, 1985Date of Patent: November 29, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: David M. Floyd, Spencer D. Kimball, Steven Brandt
-
Patent number: 4767555Abstract: Aqueous fluids are thickened with epoxide modified polyoxyalkylene diamines. The polyoxyalkylene diamines are of the formula:H.sub.2 NCH(CH.sub.3)CH.sub.2 O(CH.sub.2 CH(R)O).sub.x CH.sub.2 CH(CH.sub.3)NH.sub.2wherein:R is methyl or hydrogen andx is a number selected to give the diamine a molecular weight of 3000 to 9000.The epoxide is a hydrophobic monoepoxide, diepoxide or mixture thereof.The aqueous fluid optionally incorporate ethylene glycol. They are useful for water/glycol base hydraulic fluids, cosmetics and surfactants.Type: GrantFiled: April 10, 1987Date of Patent: August 30, 1988Assignee: Texaco Inc.Inventor: Edward C. Y. Nieh
-
Patent number: 4690933Abstract: The invention provides compounds of the formula (I) ##STR1## or salts, esters, or amides or other protected forms thereof; wherein R.sub.1 is a C.sub.1-7 bivalent aliphatic hydrocarbon group or a single bond;R.sub.2 and R.sub.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members;X is --N.dbd. or --CH.dbd.;A and B each represent hydrogen atoms or --CA--CB-- represents --C.dbd.C--; and D is an acidic group other than a carboxylic acid group.Also provided are pharmaceutical compositions of compounds of the formula (I), methods for the preparation of the compounds and intermediates in their preparation.The compounds of the formula (I) have antihistamic activity.Type: GrantFiled: July 27, 1984Date of Patent: September 1, 1987Assignee: Burroughs Wellcome Co.Inventors: Geoffrey G. Coker, John W. A. Findlay
-
Patent number: 4649204Abstract: Dialkanolamines and nontoxic pharmaceutically-acceptable acid-addition salts of the compounds of the following formula ##STR1## wherein R.sub.1 is hydrogen lower alkyl, or fluoro; R.sub.2 is hydrogen or lower alkyl; R.sub.3 and R.sub.4 are the same or different and selected from the group consisting of hydrogen or lower alkyl or R.sub.3 and R.sub.4 together define a chemical bond directly linking the two alkanol chains so as to form a pyrrolidine ring; Ar, is phenyl or thienyl or phenyl substituted with one to three substituents selected from the group consisting of lower alkyl and halo; and Ar.sub.2 is phenyl and phenyl substituted with one to three substituents selected from the group consisting of lower alkyl and halo which have antidepressant activity.Type: GrantFiled: September 30, 1985Date of Patent: March 10, 1987Assignee: McNeilab, Inc.Inventor: Bruce E. Maryanoff
-
Patent number: 4638003Abstract: N-substituted derivatives of 1-(4'-alkylthiophenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with calcium antagonist activity and are useful as antiarrhythmic and vasodilating agents.Type: GrantFiled: August 1, 1984Date of Patent: January 20, 1987Assignee: Zambon S.p.A.Inventors: Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
-
Patent number: 4632940Abstract: N-substituted derivatives of 1-(4'-alkylsulfonylphenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with local anesthetic activity.Type: GrantFiled: August 3, 1984Date of Patent: December 30, 1986Assignee: Zambon S.p.A.Inventors: Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
-
Patent number: 4602035Abstract: There are described compounds of the formula ##STR1## where n is 2 or 3, X and Y are each independently hydrogen, loweralkyl, or halogen, and R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, cyano, beta,beta,beta-trichloroethyoxycarbonyl, cyclopropylmethyl, phenethyl, or cyanoethyl, but at least one of the two is loweralkyl, which are useful as antidepressant and analgesic agents; novel intermediate compounds for preparing said compounds; and methods for synthesizing the foregoing compounds.Type: GrantFiled: December 7, 1983Date of Patent: July 22, 1986Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Craig J. Diamond, Grover C. Helsley
-
Patent number: 4506099Abstract: Diamines of the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meanings defined in claim 1, can be produced by a simple process comprising reacting 1-aza-1,5,9-cyclododecatrienes, correspondingly substituted in the 3- and/or 12-position, with ammonia and hydrogen, in the presence of a hydrogenation catalyst, to obtain compounds (I). The compounds (I) are used for example as curing agents for epoxide resins, or for producing polyamides.Type: GrantFiled: September 30, 1982Date of Patent: March 19, 1985Assignee: Ciba-Geigy CorporationInventors: Peter Baumeister, Dieter Reinehr, Eckehard Rosenegger
-
Patent number: 4486602Abstract: A compound of the formula: ##STR1## wherein A is a chain hydrocarbon group having 1 to 10 carbon atoms optionally substituted by hydroxyl, phenoxy, thienyl, furyl, pyridyl, cyclohexyl or an optionally substituted phenyl group; or a cyclic hydrocarbon group having 3 to 7 carbon atoms optionally substituted by hydroxyl, and their production and use.These compounds exhibit excellent inhibitory activity against glucoside hydrolase, thus are useful for hyperglycemic symptoms and various disorders caused by hyperglycemia.Type: GrantFiled: September 29, 1981Date of Patent: December 4, 1984Assignee: Takeda Chemical Industries, Ltd.Inventors: Satoshi Horii, Yukihiko Kameda, Hiroshi Fukase
-
Patent number: 4381305Abstract: New derivatives of 1,2-ethylenediamine and salts thereof endowed with vascular antispasmodic and antiallergic activity; processes for preparing them, some new intermediates useful in their preparation and pharmaceutical compositions containing them.Type: GrantFiled: June 5, 1981Date of Patent: April 26, 1983Assignee: Simes S.p.A.Inventors: Cesare Casagrande, Giorgio Ferrari
-
Patent number: 4329367Abstract: 1-(Aralkoxyphenyl)-2 or 3-(bis-arylalkylamino)-alkanes, e.g. those of the formula: ##STR1## or therapeutically acceptable salts thereof are hypotensive and cardioactive agents.Type: GrantFiled: December 24, 1980Date of Patent: May 11, 1982Assignee: Ciba-Geigy CorporationInventor: John E. Francis
-
Patent number: 4259257Abstract: The invention relates to novel 1-phenyl-2-amino-1,3-propanediol-N-alkyl derivatives having the general formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl having from 1 to 8 carbon atoms or phenoxymethyl, andR.sub.2 is hydrogen, alkyl having from 1 to 8 carbon atoms or 2,2-diphenylethyl,with the proviso that if R.sub.1 is phenoxymethyl then R.sub.2 may stand only for methyl, and if R.sub.2 is 2,2-diphenylethyl then R.sub.1 may stand only for hydrogen, and its isomers and pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The novel 1-phenyl-2-amino-1,3-propanediol-N-alkyl derivatives having the general formula I possess significant anti-anginose activity and show several other biological activities.Type: GrantFiled: September 7, 1979Date of Patent: March 31, 1981Assignee: Egyt Gyogyszervegyeszeti GyarInventors: Laszlo Levai, Gabor Fazekas, Lujza Petocz, Katalin Grasser