Benzene Ring In A Substituent Attached To The Ring Nitrogen Of The Five Membered Hetero Ring By Nonionic Bonding Patents (Class 548/578)
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Publication number: 20020032189Abstract: A compound of the formula: 1Type: ApplicationFiled: August 16, 2001Publication date: March 14, 2002Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Publication number: 20010053851Abstract: Para-alkynyl phenyl heteroaromatic amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: ApplicationFiled: April 25, 2001Publication date: December 20, 2001Inventor: Paige E. Mahaney
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Publication number: 20010039353Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided.Type: ApplicationFiled: February 21, 2001Publication date: November 8, 2001Inventors: Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
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Patent number: 6313132Abstract: The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary tract incontinence, and methods for preparing the compounds of Formula (I).Type: GrantFiled: September 27, 1999Date of Patent: November 6, 2001Assignee: Pharmacia ABInventors: Rolf Johansson, Martin Haraldsson, Erik Ringberg, Ian Vagberg, Katarina Beierlein, Rikard Emond, Birger Sjoberg
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Patent number: 6271395Abstract: A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula wherein the substituents are defined as in the application having a strong affinity for optical receptors, central analgesic, diuretic, anti-arrythmic, hypotensive and cerebral anti-ischemic activity.Type: GrantFiled: December 15, 1994Date of Patent: August 7, 2001Assignee: Hoechst Marion RoussolInventors: François Clemence, Odile Le Martret, Françoise Delevallee, Michel Fortin
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Publication number: 20010004669Abstract: Compounds of the formula 1Type: ApplicationFiled: January 10, 2001Publication date: June 21, 2001Inventors: Bertrand L. Chenard, John E. Macor, Barbara E. Segelstein
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Patent number: 6211364Abstract: The present invention provides intermediate for the preparation of indane-like compounds which are useful for the modulation of a muscarinic receptor.Type: GrantFiled: June 10, 1999Date of Patent: April 3, 2001Assignee: Eli Lilly and CompanyInventors: Bret E Huff, Michael A Staszak, John S Ward
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Patent number: 6136803Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.Type: GrantFiled: December 10, 1998Date of Patent: October 24, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Jules Freedman, Mark W. Dudley
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Patent number: 6118001Abstract: Disclosed are hydroxamic and carboxylic acid derivatives which are useful inhibitors of matrix metalloproteinase and/or TNF.alpha.-mediated diseases, including degenerative diseases and certain cancers.Type: GrantFiled: August 7, 1997Date of Patent: September 12, 2000Assignee: Darwin Discovery, Ltd.Inventors: David Alan Owen, John Gary Montana, John Fraser Keily, Robert John Watson, Andrew Douglas Baxter
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Patent number: 6100428Abstract: An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.Type: GrantFiled: October 6, 1999Date of Patent: August 8, 2000Assignee: The University of KansasInventors: Laxminarayan Bhat, Gunda I. Georg
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Patent number: 6008377Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxyl)benzoyl]benzoyl]benzo[b]-thiophenes.Type: GrantFiled: August 21, 1998Date of Patent: December 28, 1999Assignee: Eli Lilly and CompanyInventors: Charles D Jones, John M. McGill
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Patent number: 5968968Abstract: Diphenyl-cyclopropene derivatives, their nontoxic, pharmaceutically acceptable acid addition salts and compositions are kapa opiods useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome and stroke.Type: GrantFiled: December 8, 1998Date of Patent: October 19, 1999Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Verity Sabin
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Patent number: 5948809Abstract: (-)Cis-6(S)-phenyl-5(R)-?4-(2-pyrrolidin-1-yl ethoxy)phenyl!-5,6,7,8-tetrahydro-naphthalen-2-ol D-tartrate, pharmaceutical compositions comprising this compound, and an advantageous process for preparing the compound.Type: GrantFiled: April 28, 1998Date of Patent: September 7, 1999Assignee: Pfizer IncInventors: Charles K. Chiu, Morgan Meltz
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Patent number: 5945443Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compound of formulae IV having the structure: ##STR1## wherein X.sub.9 ;R.sub.1, R.sub.2, R.sub.3, R.sub.4 ;and n are as described in the specification.Type: GrantFiled: March 3, 1998Date of Patent: August 31, 1999Assignee: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
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Patent number: 5912343Abstract: A compound comprising at least one cyclic amine, having an organolithium side-chain, defined according to formula (I) ##STR1## wherein Z is a lithium atom (Li); R.sub.1 is selected from the group consisting of organic groups containing from 1 to about 12 carbon atoms and a bridging bond; each R.sub.2 is independently selected from the group consisting of hydrogen, organic groups containing from 1 to about 12 carbon atoms, and a bridging bond; each R.sub.3 is independently selected from the group consisting of hydrogen and organic groups containing from 1 to about 12 carbon atoms; a is an integer from 4 to about 16; and b is an integer from 0 to about 12; and optionally including a bridge, formed by the selection of two of said bridging bonds, the bridge having 0 to about 6 carbon atoms between the bridging ring members.Type: GrantFiled: December 31, 1996Date of Patent: June 15, 1999Assignee: Bridgestone CorporationInventors: David F. Lawson, William L. Hergenrother, Michael L. Kerns
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Patent number: 5847159Abstract: 1-?.omega.-(3,4-Dihydro-2-naphthalenyl)alkyl!cyclic amine derivative of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are H, halogen, OH, alkyl, alkoxy, hydroxymethyl, etc., or R.sup.1 and R.sup.2 combine to form methylenedioxy, trimethylene, etc., R.sup.3 is H, etc., R.sup.4 is H, OH, alkyl, etc., R.sup.5 is H, alkyl, etc., p is integer of from 2 to 6, and q is integer of from 3 to 7, provided that when p is 2, and q is 5, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are not simultaneously H, or salts thereof, or N-oxide derivatives thereof, or a process for preparing the same, or pharmaceutical composition containing the same. The compounds of the present invention show potent inhibitory effect on the micturition reflex, and are useful as agents for treatment of frequent urination and urinary incontinence.Type: GrantFiled: October 14, 1997Date of Patent: December 8, 1998Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Naoki Kai, Aki Kanehira, Toshiya Morie, Katsuhiko Hino, Katsuyoshi Kawashima, Isao Shimizu, Kazuhisa Akiyama
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Patent number: 5843983Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 represents a saturated heterocyclic group attached to the bond or group represented by A through a ring carbon atom; R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a, R.sup.3b, R.sup.3c and R.sup.3d are hydrogen or various other groups or atoms; and A represents a single bond or an alkylene group having from 1 to 6 carbon atoms are serotonin 2 receptor antagonists and have the ability to inhibit the activity of squalene synthase. They can not only prevent and inhibit the development and progression of arteriosclerosis but can also inhibit thrombosis in arteriosclerotic lesions and can improve hemodynamics.Type: GrantFiled: February 10, 1997Date of Patent: December 1, 1998Assignee: Sankyo Company, LimitedInventors: Koichi Fujimoto, Naoki Tanaka, Fumitoshi Asai, Taketoshi Ogawa, Teiichiro Koga, Tatsuo Tanimoto, Yoshio Tsujita, Hiroyuki Koike
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Patent number: 5804595Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.Type: GrantFiled: December 5, 1995Date of Patent: September 8, 1998Assignee: Regents of the University of MinnesotaInventors: Philip S. Portoghese, An-Chih Chang
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Patent number: 5792786Abstract: The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non.about.steroidal anti.about.inflammatory agents which include a carboxylic acid group. The compounds involve the use of tromethamine or ethanolamine derivative to link the acyl groups derived from fatty acids to the therapeutic compounds.Type: GrantFiled: April 12, 1996Date of Patent: August 11, 1998Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Robert George Whittaker, Veronika Judith Bender, Wayne Gerrard Reilly
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Patent number: 5756762Abstract: The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and a process for preparing an intermediate thereof.Type: GrantFiled: January 9, 1997Date of Patent: May 26, 1998Assignee: Merrell Pharmaceuticals Inc.Inventor: H. Michael Kolb
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Patent number: 5756760Abstract: A 1-substituted-2-diphenylphosphinonaphthalene represented by formula (I): ##STR1## wherein at least one of R.sup.1, R.sup.2, R.sup.3, and R.sup.4, which may be the same or different, represents a lower alkyl group having 1 to 4 carbon atoms which may be substituted with an alkoxy group, a phenyl group or --OR.sup.6 (wherein R.sup.6 represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms or an alcohol-protective group), and the rest of them represent a hydrogen atom; A represents a single bond or a methylene group; and R.sup.5 represents a substituted or unsubstituted phenyl group; and a transition metal complex comprising the 1-substituted-2-diphenylphosphinonaphthalene as a ligand. The transition metal complex is useful as a catalyst in asymmetric synthesis.Type: GrantFiled: March 7, 1997Date of Patent: May 26, 1998Assignee: Takasago International CorporationInventors: Sotaro Miyano, Tetsutaro Hattori, Yasuko Komuro, Hidenori Kumobayashi
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Patent number: 5744458Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.The compound of formula II has the structure: ##STR1## wherein X.sub.4, X.sub.5 ;R.sub.1, R.sub.2 ; andAr and n are as described in the specification.Type: GrantFiled: July 23, 1997Date of Patent: April 28, 1998Assignee: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
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Patent number: 5739158Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.Type: GrantFiled: July 1, 1992Date of Patent: April 14, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Brian R. de Costa, Kenner C. Rice, Nancy M. Gray, Patricia C. Contreras, Arthur E. Jacobson, Andrew Thurkauf, Lilian A. Radesca, Wayne D. Bowen, J. Michael Walker
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Patent number: 5739157Abstract: The present invention relates to pyrrolidine derivatives, and more particularly to the compound (S)-1-?(S)-2-(4-methoxybenzamido)-3-methylbutyryl!-N-?(S)-2-methyl-1-(trif luoroacetyl)propyl!pyrrolidine-2-carboxamide, shown by formula I, and solvates thereof. The present invention also provides pharmaceutical compositions, intermediates and methods of preparation of the compound. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).Type: GrantFiled: July 25, 1996Date of Patent: April 14, 1998Assignee: Zeneca LimitedInventors: Stephen John Pegg, George Joseph Sependa, Elwyn Peter Davies, Chris Allan Veale
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Patent number: 5708018Abstract: Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from hydrogen, C.sub.1 -C.sub.8 alkyl, OCH.sub.3, OH, OSO.sub.2 CF.sub.3, OSO.sub.2 CH.sub.3, SOR.sub.5, CO.sub.2 R.sub.5, CONH.sub.2, CONR.sub.5 R.sub.6, COR.sub.5, CN, SO.sub.2 NH.sub.2, SO.sub.2 NR.sub.5 R.sub.6, SO.sub.2 R.sub.5, --OCO--(C.sub.1 -C.sub.6 alkyl), --NCO--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 O--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 OH, --CO-Aryl, --NHSO.sub.2 -Aryl, --NHSO.sub.2 --(C.sub.1 -C.sub.6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R.sub.1 and R.sub.2 together form --O(CH.sub.2).sub.1-2 O-- or --(CH.sub.2).sub.3-6 -- (except that only one of R.sub.1 and R.sub.2 can be hydrogen or OH in any such compound); R.sub.3 and R.sub.4 are independently chosen from C.sub.2 -C.sub.4 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.Type: GrantFiled: February 2, 1996Date of Patent: January 13, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Susanne R. Haadsma-Svensson, Bengt R. Andersson, Clas A. Sonesson, Chiu-Hong Lin, R. Nicholas Waters, Kjell A. I. Svensson, Per A. E. Carlsson, Lars O. Hansson, N. Peter Stjernlof
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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
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Patent number: 5650425Abstract: The present disclosure relates to compounds of the general formulae: ##STR1## wherein DRUG is a steroid agonist or antagonist, a mixed agonist-antagonist, or a partial agonist, and to the use of such compounds as anti-inflammatory and anti-tumor agents.Type: GrantFiled: April 4, 1994Date of Patent: July 22, 1997Assignee: Pharmos CorporationInventors: Anat Biegnon, Marcus Brewster
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Patent number: 5637583Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: September 27, 1994Date of Patent: June 10, 1997Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 5591856Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.Type: GrantFiled: January 10, 1995Date of Patent: January 7, 1997Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: David G. Wettlaufer, Peter A. Nemoto
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Patent number: 5556864Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 is aryl; R.sup.2 is hydrogen, alkyl, alkoxy, halogen or cyano; R.sup.3 is a group of formula --B--NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently hydrogen, alkyl or substituted alkyl or R.sup.4 and R.sup.5, together with the nitrogen to which they are attached, form a heterocycle, and B is alkylene or a group of formula --CH.sub.2 CH(OR.sup.6)CH.sub.2 --, where R.sup.6 is hydrogen, alkanoyl, substituted alkanoyl or arylcarbonyl, or a group of formula --D--R.sup.7, where D is a single bond or alkylene and R.sup.7 is a heterocycle; and A is alkylene; and pharmaceutically acceptable salts and esters thereof] are useful for the treatment and prevention of circulatory diseases and psychosis.Type: GrantFiled: January 5, 1995Date of Patent: September 17, 1996Assignee: Sankyo Company, LimitedInventors: Koichi Fujimoto, Naoki Tanaka, Fumitoshi Asai, Tomiyoshi Ito, Hiroyuki Koike
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Patent number: 5521309Abstract: An anionic polymerization initiator includes the C-lithio reaction product of an organolithium compound and a tertiary-amino allyllithium or a tertiary-amino xylyllithium. When used in an anionic polymerization, a functional group from the initiator is incorporated onto the head of the growing polymer and a lithium atom is incorporated at the "living" end of the polymer chain prior to quenching. The initiator may be used to polymerize a monomer(s) including diolefin monomers, monovinyl aromatic monomers and trienes, and the living ends of the polymers are effectively maintained even at temperatures of up to 300.degree. F. and higher. Such polymers exhibit an increased efficiency in coupling termination reactions, and products prepared from such polymers exhibit improved hysteresis characteristics. Products such as tires and the like can be prepared from such polymers and from vulcanizable elastomer compositions employing the polymers.Type: GrantFiled: December 23, 1994Date of Patent: May 28, 1996Assignee: Bridgestone CorporationInventors: Thomas A. Antkowiak, James E. Hall, David F. Lawson, John R. Schreffler, Mark L. Stayer, Jr.
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Patent number: 5491233Abstract: A catalytic asymmetric reduction process, which, by hydrogenating trisubstituted olefins, yields a corresponding organic compound having a high level of enantiomeric purity is disclosed. The process is also effective for the catalytic asymmetric reduction of certain enamines and related compounds to yield a corresponding amine or related compound, respectively, having a high level of enantiomeric purity. The reduction process utilizes a chiral metal catalyst that includes a metal or metal complex that is selected from groups 3, 4, 5, or 6, lanthanides and actinides. Moreover, the process uses hydrogen as the stoichiometric reducing agent and may be carried out at pressures ranging from about 0.5 to 200 atmospheres. The reaction can also be carried out using an acidic compound as a rate enhancing additive.Type: GrantFiled: July 12, 1994Date of Patent: February 13, 1996Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Richard D. Broene, Nancy E. Lee
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Patent number: 5312930Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.Type: GrantFiled: December 31, 1992Date of Patent: May 17, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: Lap T. Cheng, Andrew E. Feiring, Wilson Tam
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Patent number: 5286878Abstract: A process is provided whereby organic carbonyl substrates, including esters, ketones and amides, are reduced in a reaction with a silane reducing reagent and a catalyst. Effective catalysts broadly include those which consist of a group 4, 5 or 6 metal which either: a) is in less than its maximum oxidation state or is capable of being converted to a complex in less than its maximum oxidation state; and/or is a group 4, 5 or 6 metal hydride. Exemplary catalysts include titanium-containing catalysts such as (bis trimethylphosphine) titanocene, trimethyl phosphine adduct of a (hydrido) silyl complex of titanocene, titanocene dichloride and titanocene monochloride.Type: GrantFiled: November 21, 1990Date of Patent: February 15, 1994Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Kristina A. Kreutzer, Esther Spaltenstein
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Patent number: 5278185Abstract: The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.Type: GrantFiled: November 4, 1992Date of Patent: January 11, 1994Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5250539Abstract: The invention relates to 1,2,3,4,5,6-hexahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds, and their use as steroid 5.alpha.-reductase inhibitors.Type: GrantFiled: October 21, 1991Date of Patent: October 5, 1993Assignee: Eli Lilly and CompanyInventors: Kenneth S. Hirsch, Charles D. Jones
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Patent number: 5239084Abstract: Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: September 10, 1992Date of Patent: August 24, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Guerry, Synese Jolidon
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Patent number: 5234944Abstract: A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula ##STR1## wherein R.sub.6 is selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually hydrogen or alkyl of 1 to 5 carbon atoms or taken together with the carbon atoms to which they are attached form a cycloalkyl of 3 to 6 carbon atoms optionally containing a heteroatom selected from the group consisting of --S--, --O-- and --N--, one of A and B has the formula ##STR2## and the other has the formula ##STR3## R is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Z is selected from the group consisting of --(CH.sub.2).sub.n --, branched alkylene of 2 to 8 carbon atoms and --CH.sub.2 O--, n is an integer of 0 to 5, X, X' and X" are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 4 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.Type: GrantFiled: November 3, 1992Date of Patent: August 10, 1993Assignee: Roussel UCLAFInventors: Francois Clemence, Odile Le Martret, Francoise Delevallee, Michel Fortin
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Patent number: 5223498Abstract: Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.Type: GrantFiled: December 28, 1989Date of Patent: June 29, 1993Assignee: The Boots Company plcInventor: Balasubramanian Gopalan
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Patent number: 5177067Abstract: Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: June 19, 1991Date of Patent: January 5, 1993Assignee: Hoffmann-LaRoche Inc.Inventors: Philippe Guerry, Synese Jolidon
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Patent number: 5155268Abstract: The present invention provides novel sulfonanilide and benzene-alkylaminium compounds which are the products of processes utilizing novel intermediates. Both the novel compounds and the novel intermediates are useful for the therapeutic or prophylactic treatment of arrhythmic activity.Type: GrantFiled: October 12, 1989Date of Patent: October 13, 1992Assignee: The Upjohn CompanyInventor: Jackson B. Hester, Jr.
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Patent number: 5130330Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders and convulsions. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms, and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.Type: GrantFiled: January 31, 1990Date of Patent: July 14, 1992Assignee: G. D. Searle & Co.Inventors: Brian R. de Costa, Kenner C. Rice, Nancy M. Gray, Patricia C. Contreras, Arthur E. Jacobson, Andrew Thurkauf, Lilian A. Radesca, Wayne D. Bowen
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Patent number: 5128362Abstract: The present invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R.sub.2 is lower alkoxy; or R.sub.1 and R.sub.2 together form a methylenedioxy or ethylenedioxy ring; R.sub.3 and R.sub.4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R.sub.7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and ##STR2## where R.sub.13 and R.sub.14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy.The compounds of the present invention selectively inhibit .alpha..sub.2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.Type: GrantFiled: January 25, 1990Date of Patent: July 7, 1992Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Robert E. Zelle, Fatima Z. Basha
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Patent number: 5112866Abstract: The synthesis of novel ethanesulfonamide compounds is described. The novel ethanesulfonamide compounds have antisecretory activity and are used in the treatment of peptic ulcer disease. The intermediates used to prepare the ethanesulfonamides are useful in the treatment of osteoporosis and other bone wasting diseases.Type: GrantFiled: August 14, 1989Date of Patent: May 12, 1992Assignee: Ortho Pharmaceutical CorporationInventor: Ronald K. Russell
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Patent number: 5093355Abstract: Dopamine agonist compounds disclosed are useful in treating hypertension and congestive heart failure in mammals. The compounds have the following general formula (I) ##STR1## wherein: X is nitrogen or CH;R is hydrogen or lower alkyl;R.sub.1, R'.sub.1, R.sub.2, R'.sub.2, R.sub.3, R'.sub.3, R.sub.4, R'.sub.4, R.sub.5 and R'.sub.5 are each independently hydrogen, ##STR2## respectively represent --(CH.sub.2).sub.n -- and (CH.sub.2).sub.m wherein n and m are each independently an integer of from 1 to 10 and pharmaceutically acceptable salts, S stereoisomers and racemic and non-racemic mixtures thereof.Type: GrantFiled: June 24, 1991Date of Patent: March 3, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Lawrence E. Fisher, Joan M. Caroon, Joseph M. Muchowski, Roberto P. Rosenkranz, Deborah L. McClelland
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Patent number: 5047570Abstract: 3-Amino-2-cyanoacrylonitrile derivatives of the formula ##STR1## where R is substituted C.sub.1 -C.sub.10 -alkyl, substituted or unsubstituted styryl, substituted or unsubstituted phenyl or aromatic heterocyclyl, are prepared by treating a nitrile in an inert organic diluent at from 0.degree. to +30.degree. C. with a substituted or unsubstituted C.sub.1 -C.sub.6 -alkanol in the presence of a hydrogen halide and reacting the resulting iminoester hydrohalide directly or after isolation with malodinitrile in an inert organic diluent at from 20.degree. to 100.degree. C. in the presence of a base.Type: GrantFiled: February 10, 1989Date of Patent: September 10, 1991Assignee: BASF AktiengesellschaftInventor: Ernst Schefczik
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5037837Abstract: Novel phenoxypropylamine derivative having the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom, a hydroxy group, a lower alkyl group or a lower alkoxy group, and R.sub.3 and R.sub.4 represent a lower alkyl group, or R.sub.3 and R.sub.4 taken together represent a group having the formula (CH.sub.2).sub.m wherein m represents 4 or 5, and n represents an integer of from 2 to 6 or a pharmaceutically acceptable salt thereof.The compounds are useful as a 5-lipoxygenase inhibitor and an antiulcer agent.Type: GrantFiled: November 1, 1990Date of Patent: August 6, 1991Assignee: Terumo Kabushiki KaishaInventors: Yoshiyuki Shikata, Ryoichi Nanba, Isamu Endo, Masashi Isozaki, Tadashi Okumura, Masazumi Miyakoshi, Shingo Koyama
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Patent number: 5021429Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.Type: GrantFiled: December 22, 1986Date of Patent: June 4, 1991Assignee: Allen & Hansburys LimitedInventor: Michael Martin-Smith
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Patent number: 5013757Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.Type: GrantFiled: April 13, 1990Date of Patent: May 7, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi