Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/75)
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Patent number: 7459558Abstract: A method of treating in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein the substituents are defined in accordance with the disclosure.Type: GrantFiled: April 13, 2005Date of Patent: December 2, 2008Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auquet, Jeremiah Harnett
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Publication number: 20080293952Abstract: A method of preparation of (S)—N-methyl-3-(1-naphthyloxy)-3-(2-mienyl)propylamine of Formula (I) and its pharmaceutically acceptable salts, comprising a) reaction of (RS)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with optically active D-tartaric acid or an acid salt derived from D-tartaric acid forming a mixture of diastereoisomeric salts of N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine and D-tartaric acid (2:1), b) isolation of the salt (S)—N,N-dimethyl-3-(naphthyloxy)-3-(2-thienyl)propylamine/D-tartrate (2:1) from the mixture of diastereoisomeric salts in an organic solvent, water or a mixture thereof and release of (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine by action of an inorganic or organic base, c) demethylation of (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine by action of an alkylchloroformate of formula ClCOOR (R=C1-C5 alkyl, or C6-C12 aryl or alkylraryl), especially phenyl, ethyl or methyl chloroformate, and d) hydrolytic release of the duloxetiType: ApplicationFiled: December 22, 2006Publication date: November 27, 2008Inventors: Ludek Ridvan, Kamal Jarrah, Josef Cinibulk, Monika Zatopkova, Lukas Placek
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Publication number: 20080287693Abstract: The invention relates to a process for the preparation of duloxetine (1a), comprising the reaction between 1-fluoronaphthalene and 3-N,N-dimethylamino-1-(2-thienyl)-propan-1-ol in the presence of 1,3-dimethyl-2-oxo-hexahydropyrimidine (DMPU) as the solvent; a method for the identification of duloxetine enantiomers and for the determination of its optical purity is also disclosed.Type: ApplicationFiled: October 13, 2006Publication date: November 20, 2008Inventors: Samuele Frigoli, Claudio Fuganti, Roberta Pizzocaro
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Patent number: 7435563Abstract: The present invention relates to a process for the preparation of enantiomerically pure (S)-3-methyl-amino-1-(thien-2-yl)propan-1-ol of the formula II-S by obtainment of (S)-3-hydroxy-3-thien-2-ylpropionitrile from its enantiomer mixture with the R isomer and the subsequent reaction of (S)-3-hydroxy-3-thien-2-ylpropionitrile with hydrogen and methylamine in the presence of a catalyst to give II-S.Type: GrantFiled: July 31, 2003Date of Patent: October 14, 2008Assignee: BASF AktiengesellschaftInventor: Rainer Stürmer
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Publication number: 20080207923Abstract: (S)—N,N-Dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine maleate (DNT-maleate) and polymorphs of DNT-maleate, compositions of DNT-maleate and its polymorphs, processes for the preparation of DNT-maleate and its polymorphs, and processes for the preparation of duloxetine hydrochloride from DNT-maleate are provided. Processes for preparing chemically pure duloxetine and chemically pure duloxetine intermediates are also provided. In addition, chemically pure DNT and salts thereof are provided.Type: ApplicationFiled: October 30, 2007Publication date: August 28, 2008Inventors: Santiago Ini, Mili Abramov
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Publication number: 20080171887Abstract: A compound of formula 10 is useful in making duloxetine.Type: ApplicationFiled: December 20, 2007Publication date: July 17, 2008Inventors: Karel Pospisilik, Bohumil Dymacek
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Patent number: 7399871Abstract: DNT-Oxal crystalline forms and processes for making DNT-Oxal crystalline forms are provided.Type: GrantFiled: March 8, 2006Date of Patent: July 15, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Santiago Ini, Anita Liberman, Tamas Koltai
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Publication number: 20080167351Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.Type: ApplicationFiled: February 13, 2006Publication date: July 10, 2008Inventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
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Publication number: 20080167472Abstract: Disclosed herein is a class of tunable phenylacetylene compounds as well as compositions and methods for their use as host compounds for ligand binding. In certain examples the hosts report binding events by exhibiting altered spectroscopic properties, such as different fluorescent emission spectra.Type: ApplicationFiled: December 14, 2007Publication date: July 10, 2008Inventors: Michael M. Haley, Darren W. Johnson, Orion B. Berryman, Charles A. Johnson, Calden N. Stimpson
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Publication number: 20080167331Abstract: The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.Type: ApplicationFiled: March 14, 2008Publication date: July 10, 2008Inventor: Robert M. Burk
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Publication number: 20080146624Abstract: The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 18, 2007Publication date: June 19, 2008Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Eddy Wai Tsun Yue
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Patent number: 7381842Abstract: Compounds of the formulae I, II, III, IV and V wherein R1 i.a. is C4-C9cycloalkanoyl, C1-C12alkanoyl, C4-C6alkenoyl, or benzoyl; R2 is for example phenyl, C1-C20alkyl, C3-C8cycloalkyl, C2-C20alkanoyl, or benzoyl; Ar1 is R4S-phenyl or NR5R6-phenyl, each of which optionally is substituted; or Ar1 i.a. is optionally substituted; or Ar1 is naphthyl or anthracyl each of which is unsubstituted or substituted; or Ar1 is benzoyl, naphthalenecarbonyl, phenanthrenecarbonyl, anthracenecarbonyl or pyrenecarbonyl, each of which is unsubstituted or substituted, or Ar1 is 3,4,5-trimethoxyphenyl, phenoxyphenyl or biphenyl; Ar2 i.a.Type: GrantFiled: April 11, 2005Date of Patent: June 3, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Kazuhiko Kunimoto, Hidetaka Oka, Masaki Ohwa, Junichi Tanabe, Hisatoshi Kura, Jean-Luc Birbaum
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Publication number: 20080119538Abstract: Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: July 6, 2007Publication date: May 22, 2008Inventors: DAVID W. OLD, Vinh X. Ngo
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Publication number: 20080119539Abstract: Compounds of the formula are disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: September 6, 2007Publication date: May 22, 2008Inventors: David W. Old, Robert M. Burk, Todd S. Gac
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Publication number: 20080108835Abstract: The present invention relates to a method for purifying (1S)-3-METHYLAMINO-1-(2-THIENYL)-1-PROPANOL by distilling a reaction mixture which comprises between 25 and 99% by weight of (IS)-3-METHYLAMINO-1-(2-THIENYL)-1-PROPANOL.Type: ApplicationFiled: December 31, 2005Publication date: May 8, 2008Inventors: Rainer Sturmer, Jurgen Dauwel, Maria Kesseler, Brigitte Achatz, Michael Breuer
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Patent number: 7368472Abstract: The present invention concerns 1,2,4-triaminobenzene derivatives of the general formula I or pharmaceutically acceptable salts thereof and the use thereof.Type: GrantFiled: December 18, 2003Date of Patent: May 6, 2008Assignee: H. Lundbeck A/SInventors: Mario Rottlander, Andreas Ritzen, Morten Bang Norgaard, Nikolay Khanzhin, Christian Wenzel Tornoe
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Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
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Patent number: 7273952Abstract: Substituted C-cyclohexylmethylamine derivatives, methods for the production thereof, pharmaceuticals containing said compounds, the use of substituted C-cyclohexylmethylamine derivatives for producing pharmaceuticals, and method of pain treatment using the pharmaceuticals.Type: GrantFiled: March 31, 2003Date of Patent: September 25, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Corinna Maul, Helmut Buschmann, Michael Finkam, Babette-Yvonne Koegel
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Patent number: 7259172Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 2, 2004Date of Patent: August 21, 2007Assignee: MethylGene Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Patent number: 7205320Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: January 12, 2004Date of Patent: April 17, 2007Assignee: Memory Pharmaceuticals Corp.Inventors: Richard A. Schumacher, William F. Brubaker, Michael De Vivo, Hans-Jürgen Ernst Hess, Allen Hopper, Ashok Tehim, Ruiping Liu, Axel Unterbeck
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Patent number: 7179926Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts and solvates, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.Type: GrantFiled: July 25, 2005Date of Patent: February 20, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Yazhong Huang, Shuanghua Hu, Andrew P. Degnan
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Patent number: 7173052Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: GrantFiled: December 2, 2004Date of Patent: February 6, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, Martin J. Procter, Colin P. Sambrook Smith
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Patent number: 7169938Abstract: The invention relates to a process for preparing enantiomerically enriched aryl-aminopropanols and to their use and also to intermediates.Type: GrantFiled: March 18, 2003Date of Patent: January 30, 2007Inventors: Markus Eckert, Claus Dreisbach, Boris Bosch, Andreas Stolle
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7135487Abstract: The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: May 29, 2003Date of Patent: November 14, 2006Assignee: Eli Lilly and CompanyInventors: Macklin B Arnold, Stephen R Baker, Thomas J Bleisch, Buddy E Cantrell, Ana M Escribano, Ken Matsumoto, Tracey E McKennon, Paul L Ornstein, Richard L Simon, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M Zimmerman
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Patent number: 7119211Abstract: Disclosed is a process for commercial preparation of 3-(methylamino)-1-(2-thienyl)propan-1-ol (hereinafter abbreviated as “MMAA”) of the formula below: The process is carried out by the diastereomeric salt formation method using optically active mandelic acid or its derivatives, or an optically active tartaric acid derivative as the resolving agent. The product compound, diastereomeric satls, is useful as the intermediate for producing pharmaceuticals, such as duloxetine.Type: GrantFiled: September 23, 2004Date of Patent: October 10, 2006Assignee: Yamakawa Chemical Industry Co., Ltd.Inventors: Kenichi Sakai, Rumiko Sakurai, Atsushi Yuzawa, Kaoru Hatahira
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Patent number: 7101900Abstract: Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1–C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1–C6-alkyl, C1–C6-alkoxy, C1–C4-haloalkyl, C1–C4-haloalkoxy, C1–C4-alkylthio, C1–C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1–C6-alkyl, thienyl-C1–C4-alkyl, or pyrazolyl-C1–C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1–C6-alkyl, C1–C6-alkoxy, C1–C4-haloalkyl, C1–C4-haloalkoxy, C1–C4-alkylthio, C1–C4-alkoxyalkoxy, C1–C6-alkylcarbonyl; n is 0–5; p is, depending on the number of free valencies, 0–4.Type: GrantFiled: February 22, 2005Date of Patent: September 5, 2006Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Karl Eicken, Ingo Rose, Thomas Grote, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz
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Patent number: 7087639Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.Type: GrantFiled: January 20, 2004Date of Patent: August 8, 2006Assignee: LKT Laboratories, Inc.Inventors: Luke K. T. Lam, Nayaz Ahmed
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Patent number: 7049337Abstract: Aminotetralin derivatives and pharmacological analogs thereof which contain an N-propynyl group exhibit differential dopaminergenic receptor activity. The subject compounds are useful in affecting dopamine receptor activity, particularly in exhibiting differing activity among the various dopamine receptor subtypes. The compounds are useful in treating CNS disorders in mammals in general, and humans in particular.Type: GrantFiled: May 17, 2001Date of Patent: May 23, 2006Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Patent number: 7038084Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: February 24, 2004Date of Patent: May 2, 2006Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 7026094Abstract: New oxime sulfonate compounds of the formula (I) and (II), wherein R1 is C1-C12alkyl, C1C4haloalkyl, hydrogon, OR9, NR10R11, SR12 or is phenyl which is unsubstituted or substituted by OH, C1-C18alkyl, halogen and/or C1-C12alkoxy; R2, R3, R4 and R5 are for example hydrogen or C1-C12alkyl; R6 is for example is C1-C18alkylsulfonyl, phenyl-C1-C3alkylsulfonyl or phenylsulfonyl; R?6 is for example phenylenedisulfonyl or diphenylenedisulfonyl; R7, R8 and R9 for example are hydrogen or C1-C6alkyl; R10 and R11, are for example hydrogen or C1-C18alkyl; R12 is for example hydrogen, phenyl or C1-C18alkyl; A is S, O, NR13, or a group of formula A1, A2 or A3, R21 and R22 independently of one other have one of the meanings given for R7; R23, R24, R25 and R26 independently of one another are for example hydrogen, C1-C4alkyl, halogen or phenyl; Z is CR22 or N; and Z1 is CR22 or N; and Z1 is CR22 or N; and Z1 is CH2, S, O or NR13 are particularly suitable as photo-latent acids in resist applications.Type: GrantFiled: May 23, 2002Date of Patent: April 11, 2006Assignee: Ciba Specialty Chemicals Corp.Inventors: Akira Matsumoto, Hitoshi Yamato, Toshikage Asakura, Masaki Ohwa, Peter Murer
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Patent number: 7019024Abstract: 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: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6998423Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: August 29, 2003Date of Patent: February 14, 2006Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Patent number: 6984738Abstract: The present invention is to provide a process for producing an optically active amino alcohol which is useful for the synthesis of natural substances and as an intermediate for drugs and agricultural chemicals in a high yield, a high selectivity and an economical manner with a good working efficiency and the present invention relates to a process for producing an optically active amino alcohol represented by the following formula (2) (in the formula, R1 is a hydrocarbon group, a substituted hydrocarbon group, an aromatic heterocyclic group, a substituted aromatic heterocyclic group, an aliphatic heterocyclic group or a substituted aliphatic heterocyclic group; R2 and R3 each independently is hydrogen atom, a hydrocarbon group, a substituted hydrocarbon group, an acyl group, an acyloxy group, an alkyloxycarbonyl group, an aralkyloxycarbonyl group, an aryloxycarbonyl group, an aromatic heterocyclic group, a substituted aromatic heterocyclic group, an aliphatic heterocyclic group or a substituted aliphatic hType: GrantFiled: October 17, 2003Date of Patent: January 10, 2006Inventors: Tohru Yokozawa, Kenji Yagi, Takao Saito
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Patent number: 6949678Abstract: Compounds of the formulae I, II, III, IV and V wherein R1 i.a. is C4-C9cycloalkanoyl, C1-C12alkanoyl, C4-C6alkenoyl, or benzoyl; R2 is for example phenyl, C1-C20alkyl, C3-C8cycloalkyl, C2-C20alkanoyl, or benzoyl; Ar1 is R4S-phenyl or NR5R6-phenyl, each of which optionally is substituted; or Ar1 i.a. is optionally substituted; or Ar1 is naphthyl or anthracyl each of which is unsubstituted or substituted; or Ar1 is benzoyl, naphthalenecarbonyl, phenanthrenecarbonyl, anthracenecarbonyl or pyrenecarbonyl, each of which is unsubstituted or substituted, or Ar1 is 3,4,5-trimethoxyphenyl, phenoxyphenyl or biphenyl; Ar2 i.a.Type: GrantFiled: December 12, 2000Date of Patent: September 27, 2005Assignee: Ciba Specialty Chemicals Corp.Inventors: Kazuhiko Kunimoto, Hidetaka Oka, Masaki Ohwa, Junichi Tanabe, Hisatoshi Kura, Jean-Luc Birbaum
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Patent number: 6916347Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): where R1 and R2 are each individually selected from a hydrogen atom, a C1 to C3 alkyl group, a C1 to C5 mono or dihydroxyalkyl group, phenyl or benzyl optionally substituted with an alkoxy group, or R1 and R2 together with the nitrogen atom to which they are attached form a piperazine, piperidine, imidazole, or morpholine ring.Type: GrantFiled: May 4, 2004Date of Patent: July 12, 2005Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
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Patent number: 6900353Abstract: The present invention provides compounds of formula (I): useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: September 28, 2001Date of Patent: May 31, 2005Assignee: Eli Lilly and CompanyInventors: Buddy Eugene Cantrell, Winton Dennis Jones, Jr., Timothy Alan Shepherd, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6887871Abstract: There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.Type: GrantFiled: February 20, 2001Date of Patent: May 3, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Peter Hamley, Antonio Mete, Austen Pimm
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6841569Abstract: Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.Type: GrantFiled: June 21, 2002Date of Patent: January 11, 2005Assignee: SK CorporationInventors: Yong-Moon Choi, Ki-Ho Lee
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Patent number: 6840965Abstract: The object of the invention are p-aminophenol derivatives of general formula (I) or physiologically tolerated, water-soluble salts thereof and oxidative coloring preparations based on a developer-coupler combination containing at least one p-aminophenol derivative of formula (I).Type: GrantFiled: March 9, 2001Date of Patent: January 11, 2005Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6835745Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, R3, X, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 10, 2003Date of Patent: December 28, 2004Assignee: WyethInventors: Richard D. Coghlan, William F. Fobare, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
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Publication number: 20040249170Abstract: This invention provides a process for the synthesis of(S)-3-Methylamino-1-2-thienyl)-1-propanol, a key intermediate in the synthesis of duloxetine.Type: ApplicationFiled: July 7, 2004Publication date: December 9, 2004Inventor: Alfio Borghese
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Publication number: 20040198780Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: March 23, 2004Publication date: October 7, 2004Applicant: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Publication number: 20040158079Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.Type: ApplicationFiled: January 20, 2004Publication date: August 12, 2004Applicant: LKT Laboratories, Inc.Inventors: Luke K.T. Lam, Nayaz Ahmed
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Patent number: 6774244Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is selected from C1 to C5 alkyl or hydroxyalkyl, a C3 to C6 cyclic ring containing hetero atoms selected from O, S and N atoms, and —CH2—Ar where Ar is an aromatic ring wherein the aromatic ring may be substituted with one or two hydroxy C1 to C3 alkoxy, or amino groups.Type: GrantFiled: January 18, 2002Date of Patent: August 10, 2004Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
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Publication number: 20040127721Abstract: Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.Type: ApplicationFiled: November 25, 2003Publication date: July 1, 2004Applicants: University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Mariappan Anbazhagan, Richard R. Tidwell
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Patent number: 6750355Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): where R1 and R2 are each individually selected from a hydrogen atom, a C1 to C3 alkyl group, a C1 to C5 mono or dihydroxyalkyl group, phenyl or benzyl optionally substituted with an alkoxy group, or R1 and R2 together with the nitrogen atom to which they are attached form a piperazine, piperidine, imidazole, or morpholine ring.Type: GrantFiled: January 18, 2002Date of Patent: June 15, 2004Assignee: The Procter & Gamble CompanyInventors: Mu-Ill Lim, Yuh-Guo Pan
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Patent number: 6723745Abstract: Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 aklene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 akylene group.Type: GrantFiled: January 7, 2003Date of Patent: April 20, 2004Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Toshiyasu Takemoto, Takaichi Shimozato, Futoshi Nara