Additional -c(=x) Bonded Directly To The Five-membered Hetero Ring (e.g., N N-butyryl-l-proline, Etc.) Patents (Class 548/533)
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Publication number: 20080234344Abstract: The invention provides novel compounds of general formula I wherein R1, R2 and R3 are independently hydrogen, OR4, C1-C6 alkyl or C2-C6 alkenyl, R4 is hydrogen, C1-C6 alkyl or C2-C6 alkenyl, —N-(AA) represents the residue of an amino acid or of a peptide which is bonded over the N-terminus of the amino acid or the peptide and the peptide is composed of 2 to 6, that means 2, 3, 4, 5 or 6, amino acids, wherein the C-terminus of the amino acid or the peptide is optionally esterified with a C1-C16 hydrocarbon moiety and n is an integer of 1 to 5. The compounds are in particular useful for cosmetic applications.Type: ApplicationFiled: March 23, 2005Publication date: September 25, 2008Inventors: Jochen Klock, Philippe Emmanuel Maillan, Juergen H. Vollhardt, Raphael Beumer
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Patent number: 7410995Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked sulfonamides of heterocyclic thioesters.Type: GrantFiled: August 14, 1998Date of Patent: August 12, 2008Assignee: GPI Nil Holdings Inc.Inventors: Douglas T. Ross, Hansjörg Sauer, Gregory S. Hamilton, Joseph P. Steiner
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Publication number: 20080188545Abstract: Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.Type: ApplicationFiled: December 20, 2007Publication date: August 7, 2008Inventors: Asaf R. Alimardanov, Lalitha Krishnan, Maotang Zhou, Ting-Zhong Wang, Jianxin Ren, John Leo Considine, Charles C. Wu, Jason Brazzillo, Panolil Raveendranath, Girija Raveendranath, Vijay Raveendranath, Sanjay Raveeendranath, Karen Sutherland, Mahmoud Mirmehrabi, Subodh S. Deshmukh
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Patent number: 7390910Abstract: The invention provides compounds of formula (I): wherein E, A, B?, R6, R7, R8, and R9 are defined in the specification which compounds exhibit anticancer activity and are useful for treating cancer.Type: GrantFiled: August 4, 2004Date of Patent: June 24, 2008Assignee: WyethInventors: Arie Zask, Joshua Kaplan, Ayako Yamashita, Chuan S. Niu, Gary Harold Birnberg, Emily Norton, Kinwang Cheung, Ronald Suayan, Vincent Sandanayaka, Philip Ross Hamann, Semiramis Ayral-Kaloustian
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Publication number: 20080145335Abstract: Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.Type: ApplicationFiled: November 20, 2007Publication date: June 19, 2008Applicant: Neuren Pharmaceuticals LimitedInventors: Margaret Anne Brimble, Paul William Richard Harris, Frank Sieg
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Patent number: 7378440Abstract: The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.Type: GrantFiled: July 27, 2004Date of Patent: May 27, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Dieter Kadereit, Elisabeth Defossa, Karl Schoenafinger, Thomas Kalbunde, Andreas Herling
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Patent number: 7338976Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic esters and amides.Type: GrantFiled: August 14, 1998Date of Patent: March 4, 2008Assignee: GPI NIL Holdings, Inc.Inventors: Douglas T. Ross, Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 7323489Abstract: A proline ester represented by the following formula (I): wherein R1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.Type: GrantFiled: September 8, 2003Date of Patent: January 29, 2008Assignee: Toaeiyo Ltd.Inventors: Takayuki Furuishi, Kunihiro Minami, Takayuki Minowa, Miho Komine, Kunihiko Kimura
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Patent number: 7279584Abstract: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an ?-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.Type: GrantFiled: August 18, 2004Date of Patent: October 9, 2007Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Kazuyuki Tomisawa, Dai Tatsuta, Tomomichi Yoshida, Chihiro Yokoo
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Patent number: 7265150Abstract: This invention relates to novel compositions and uses of N-heterocyclic carboxylic acids and carboxylic acid isosteres for treating a vision disorder, improving vision, treating memory impairment or enhancing memory performance in an animal.Type: GrantFiled: August 14, 1998Date of Patent: September 4, 2007Assignee: GPI NIL Holdings Inc.Inventors: Douglas T. Ross, Hansjörg Sauer, Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 7250520Abstract: The present invention relates to an improved synthesis of pyrrole capping group precursors.Type: GrantFiled: October 28, 2004Date of Patent: July 31, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventor: Michael Wallace
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Patent number: 7250409Abstract: Anlogs of ningalin B lacking inherent cytotoxic activity may be employed to reverse multi-drug resistant (MDR) phenotype and to resensitize transformed cells, including a human colon cancer cell line (HCT116/VM46), with respect to a variety of cytotoxic agents, e.g., vinblastine and doxorubicin. In many instances, resensitization is achieved at lower doses than the prototypical agent verapamil. Total synthesis of ningalin B and its analogs was achieved using a concise, efficient approach based on a heterocyclic azadiene Diels-Alder strategy (1,2,4,5-tetrazine?1,2-diazine?pyrrole) ideally suited for construction of the densely functionalized pyrrole core found in the natural product is detailed.Type: GrantFiled: March 1, 2001Date of Patent: July 31, 2007Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 7189754Abstract: The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonize the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, saturated or unsaturated 3–8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl.Type: GrantFiled: March 19, 2002Date of Patent: March 13, 2007Assignee: Applied Research Systems ARS Holding NVInventors: Matthias Schwarz, Anna Quattropani, Alexander Scheer, Jerome Dorbais, Vincent Pomel
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Patent number: 7022677Abstract: Disclosed are the novel compounds as growth hormone secretagogues represented by structural Formula (I), wherein R1 is, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, or substituted or unsubstituted amino, X is —CO— or —SO2—, Y is Formula (II), wherein n is an integer from 0–4, R4 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, R5 and R6 are independently selected from hydrogen, substituted or unsubstituted alkyl, or R5 and R6 or R4 and R5 are taken together to form substituted or unsubstituted alkylene, R2 is hydrogen, or substituted or unsubstituted alkyl, R3 is substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, D is substituted or unsubstituted amino, substituted or unsubstituted alkoxy, or substituted or unsubstituted alkylthio, * represents an asymmetric center, and phType: GrantFiled: February 17, 2000Date of Patent: April 4, 2006Assignees: Kaken Pharmaceutical Co., Ltd., Molecular Research InstituteInventors: Nobuo Ishiyama, Hirohide Ishige, Mitsuo Mimura, Tadashi Okuno, Kiyoharu Ukai, Takeshi Kiyofuji, Shinji Tauchi, Kiyoshi Inoguchi, Ping Huang, Linda J. Maki, legal representative, Gilda H. Loew, deceased
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Patent number: 6972331Abstract: 4-Oxo-4,5-dihydro-3H-pyrrolo[3,2-d] pyrimidine-7-carboxylic acid methyl ester and process for preparing are provided. The process for producing the 4-oxo-4,5-dihydro-3H-pyrrole[3,2-d]pyrimidine-7-carboxylic acid methyl ester comprises condensing 3-amino-1H-pyrrole-2,4-dicarboxylic acid dimethyl ester with formamidine acetate. The 4-oxo-4,5-dihydro-3H-pyrrole[3,2-d]pyrimidine- 7-carboxylic acid methyl ester is useful as a precusor for providing 9-deaza-hypoxanthine, a key intermediate for producing certain PNP inhibitors.Type: GrantFiled: April 23, 2003Date of Patent: December 6, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Christopher D. Winslow, Philip E. Morris, Jr.
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Patent number: 6933269Abstract: Polyaspartate derivatives, especially hydrophobically modified and/or hydrophilically modified polyaspartate derivatives, most especially polyaspartate derivatives that are both hydrophilically and hydrophobically modified, for use in detergent compositions, specifically laundry detergent compositions for providing cleaning, dispersancy, especially soil dispersion, builder properties and/or improved whitening of fabrics contacted by such detergent compositions; and methods for making such polyaspartate derivatives, and methods and articles employing such detergent compositions, are provided.Type: GrantFiled: July 31, 2002Date of Patent: August 23, 2005Assignee: The Procter & Gamble CompanyInventors: Glenn Thomas Jordan, IV, Eugene Paul Gosselink
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Patent number: 6869974Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.Type: GrantFiled: April 11, 2000Date of Patent: March 22, 2005Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Patent number: 6740760Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.Type: GrantFiled: July 1, 2002Date of Patent: May 25, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6713503Abstract: Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which include: 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-4-methyl-benzoyl)-5-oxo-2,5-dihydro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07), 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10), 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl ester (3F-11), 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid (3F-15), and 4,4-Dihydroxy-5-4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) as well as some novel derivatives of these compounds claimed (see Table 2).Type: GrantFiled: December 4, 2002Date of Patent: March 30, 2004Assignee: University of Central FloridaInventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Krasnykh Olga Petrovna, Pimenova Elena Valentinovna, Elena A. Goun
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Patent number: 6713628Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.Type: GrantFiled: November 18, 2002Date of Patent: March 30, 2004Assignee: Kaneka CorporationInventors: Yasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse
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Patent number: 6713502Abstract: Novel anti-infective and methods of using them are provided.Type: GrantFiled: November 5, 2002Date of Patent: March 30, 2004Assignee: SmithKline Beecham CorporationInventors: Dashyant Dhanak, Thomas Carr
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Publication number: 20040058971Abstract: This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for usein the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.Type: ApplicationFiled: March 14, 2003Publication date: March 25, 2004Inventors: Jeffrey Alan Dodge, Britta Evers, Louis Nickolaus Jungheim, Brian Stephen Muehl, Gerd Ruehter, Kenneth Jeff Thrasher
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Publication number: 20040048802Abstract: The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.Type: ApplicationFiled: May 20, 2003Publication date: March 11, 2004Inventors: Amy Ripka, Jeffrey Allen Campbell, Andrew Charles Good, Paul Michael Scola, Ny Sin, Brian Venables
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Publication number: 20040006233Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains.Type: ApplicationFiled: June 13, 2003Publication date: January 8, 2004Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Publication number: 20030232788Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: ApplicationFiled: February 7, 2003Publication date: December 18, 2003Applicant: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Vincent J. Kalish, Edward D. Robinson, Brett R. Ullman
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Patent number: 6660741Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: where R1 is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said R1 further comprising a cyclic or bicyclic structure; R2 is methyl, CH2CH3, (CH2)2CH3, C(CH3)3, phenyl, 3,4-dichiorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH2-(N-Boc-4-piperidine), 4-tetrahydropyran, CH2-4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; R3 is R2 or C3-8alkyl, R4 is C1-3alkyl; and R5 is NH2, OH, NHOH, NHOCH3, N(CH3)OH, N(CH3)OCH3, NHCH2CH3, NH(CH2CH3), NHCH2(2,4-(OCH3)2Ph, NHCH2(4-NO2)Ph, NHN(CH3)2, proline, or 2-hydroxymethyl pyrrolidine.Type: GrantFiled: March 19, 2002Date of Patent: December 9, 2003Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: William G. Bornmann, Francis Sirotnak, Howard Scher, Ephraim Vidal, Christopher Borella, David Scheinberg
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Publication number: 20030220320Abstract: Anlogs of ningalin B lacking inherent cytotoxic activity may be employed to reverse multi-drug resistant (MDR) phenotype and to resensitize transformed cells, including a human colon cancer cell line (HCT116/VM46), with respect to a variety of cytotoxic agents, e.g., vinblastine and doxorubicin. In many instances, resensitization is achieved at lower doses than the prototypical agent verapamil. Total synthesis of ningalin B and its analogs was achieved using a concise, efficient approach based on a heterocyclic azadiene Diels-Alder strategy (1,2,4,5-tetrazine → 1,2-diazine → pyrrole) ideally suited for construction of the densely functionalized pyrrole core found in the natural product is detailed.Type: ApplicationFiled: November 7, 2002Publication date: November 27, 2003Inventor: Dale L Boger
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Publication number: 20030216584Abstract: The present invention provides processes for removing organic solvent from crystals of atorvastatin hemi-calcium containing organic solvent. In one process, the organic solvent is displaced by vapor diffusion of water in a vessel maintained at elevated humidity. In a second process, the organic solvent is removed by fluidized bed drying. The present invention further provides atorvastatin hemi-calcium containing 1% or less organic solvent, which can be obtained from atorvastatin hemi-calcium that has been crystallized from an organic solvent-containing solution by practice of the processes of the invention.Type: ApplicationFiled: February 19, 2003Publication date: November 20, 2003Inventors: Judith Aronhime, Dalia Maidan-Hanoch
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Publication number: 20030216427Abstract: The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.Type: ApplicationFiled: December 26, 2002Publication date: November 20, 2003Inventors: Serge Halazy, Matthias Schwarz, Bruno Antonsson, Agnes Bombrun, Jean-Claude Martinou, Dennis Church
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Patent number: 6627760Abstract: The present invention relates to a novel form of (S)-1-[N2-(1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline known under the generic name lisinopril. Further, the present invention also relates to the use of the novel amorphous form of lisinopril for the treatment of hypertension and other cardiovascular diseases, pharmaceutical compositions containing it as well as processes for the preparation of the novel amorphous form of lisinopril.Type: GrantFiled: June 25, 2001Date of Patent: September 30, 2003Assignee: AstraZeneca ABInventor: Ronald John Roberts
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Publication number: 20030171301Abstract: The present invention relates to a novel form of (S)-1-[N2-(1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline known under the generic name lisinopril. Further, the present invention also relates to the use of the novel amorphous form of lisinopril for the treatment of hypertension and other cardiovascular diseases, pharmaceutical compositions containing it as well as processes for the preparation of the novel amorphous form of lisinopril.Type: ApplicationFiled: June 25, 2001Publication date: September 11, 2003Inventor: Ronald John Roberts
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Publication number: 20030134802Abstract: Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.Type: ApplicationFiled: February 10, 2003Publication date: July 17, 2003Inventors: Hans-Ulrich Demuth, Konrad Glund, Dagmar Schlenzig, Susanne Kruber
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Publication number: 20030100599Abstract: Provided are compounds of formula (I) 1Type: ApplicationFiled: December 6, 2002Publication date: May 29, 2003Applicant: Genentech, Inc.Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
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Publication number: 20030100770Abstract: New compounds have the formula: 1Type: ApplicationFiled: July 1, 2002Publication date: May 29, 2003Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger D. Norcross
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Patent number: 6541635Abstract: The present invention discloses a method for producing angiotensin converting enzyme inhibitor of the following formula (I) and pharmaceutically acceptable salts thereof, in which a compound of the following formula (II), wherein R and R1 are defined as in the specification, is subjected to a de-protective reaction of silyl group in non-aqueous medium. This reaction is easily carried out only in the non-aqueous medium, so that by-product is minimized and the yield is high.Type: GrantFiled: June 25, 2002Date of Patent: April 1, 2003Assignee: Everlight USA, Inc.Inventors: Mong-Jong Tien, Yu-Liang Liu
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Patent number: 6534657Abstract: Ferrocene anchored chiral ligands and metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The metal complexes according to the present invention are useful as catalysts in asymmetric reactions, such as, hydrogenation, hydride transfer, allylic alkylation, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, olefin metathesis, hydrocarboxylation, isomerization, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition; epoxidation, kinetic resolution and [m+n] cycloaddition. The new ligands are effective for asymmetric Pd-catalyzed allylic alkylation reactions and Ag-catalyzed [3+2] cyclization of azomethine ylides.Type: GrantFiled: February 9, 2001Date of Patent: March 18, 2003Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Patent number: 6518436Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S) -ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxy-anhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.Type: GrantFiled: November 21, 2001Date of Patent: February 11, 2003Assignee: Kaneka CorporationInventors: Yasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse
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Patent number: 6515179Abstract: A 2- or 4-nitrobenzenesulfonamide is allowed to react with an alkali metal alkoxide to remove a nitrobenzenesulfonyl group to thereby obtain an amine corresponding to the amide. Furthermore, a method for producing an amine derivative by allowing the resulting amine without isolation to react with an activated, substituted oxycarbonyl compound or an activated acyl compound is provided. According to this method, a corresponding free amine and its substituted derivative can be produced easily and industrially advantageously from the 2- or 4-nitrobenzenesulfonamide without using a thiol compound.Type: GrantFiled: June 11, 2002Date of Patent: February 4, 2003Assignee: Kaneka CorporationInventor: Nobuo Nagashima
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Patent number: 6500959Abstract: This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.Type: GrantFiled: June 28, 2000Date of Patent: December 31, 2002Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Joseph P. Steiner
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Publication number: 20020161240Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains.Type: ApplicationFiled: February 28, 2002Publication date: October 31, 2002Applicant: ARIAD Gene Therapeutics, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Patent number: 6462072Abstract: This invention relates to low molecular weight, small molecule cyclic esters and amides having an affinity for FKBP-type immunophilins, pharmaceutical compositions comprising the same, and methods of using the same to effect a neuronal activity.Type: GrantFiled: September 21, 1998Date of Patent: October 8, 2002Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, David C. Limburg
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Publication number: 20020137686Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds having the following structure: 1Type: ApplicationFiled: July 18, 2001Publication date: September 26, 2002Inventors: Robert J. Ternansky, Patricia L. Gladstone, Kevin J. Tomaselli, Bin Chao, Steven D. Linton
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Publication number: 20020137946Abstract: This invention is directed to compounds and intermediates of Formulae (6 and 3), useful in preparing herbicidal sulfonamides of Formula (1), including all geometric and stereoisomers thereof, and agricultural salts thereof, wherein X is H, F or Cl; Y is F or Cl; R1 is C1-C3 haloalkyl, C2-C4 alkoxyalkyl; C2-C6 haloalkoxyalkyl or C2-C6 cyanoalkyl; R2 is H, C1-C4 alkyl, C1-C4 haloalkyl; C3-C4 alkenyl, C3-C4 alkynyl, C2-C4 alkoxyalkyl, C2-C4 alkylcarbonyl or C2-C4 alkoxycarbonyl; R3 is H or OH; R4 is H, F or Cl; and R5 is F or Cl; provided that when R3 is H then R4 is F or Cl and when R3 is OH then R4 is H.Type: ApplicationFiled: January 4, 2002Publication date: September 26, 2002Applicant: DEGUSSA AGInventors: Eric Deguyon Taylor, Viacheslav Alexandrovich Petrov, Matthias Schaeffer, Karlheinz Drauz, Anne Vogt, Christoph Weckbecker, Steven H. Swearingen, Balreddy Kamireddy
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Patent number: 6455571Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.Type: GrantFiled: October 19, 1999Date of Patent: September 24, 2002Assignee: Abbott LaboratoriesInventors: Clarence J. Maring, Yu Gui Gu, Hui-Ju Chen, Yuanwei Chen, David A. Degoey, William J. Flosi, Vincent L. Giranda, David J. Grampovnik, Warren M. Kati, Dale J. Kempf, April Kennedy, Larry L. Klein, Allan C. Krueger, Zhen Lin, Darold L. Madigan, Keith F. McDaniel, Steven W. Muchmore, Hing L. Sham, Kent D. Stewart, Vincent S. Stoll, Minghua Sun, Noah P. Tu, Frank L. Wagenaar, Gary T. Wang, Sheldon Wang, Paul E. Wiedeman, Yibo Xu, Ming C. Yeung, Chen Zhao, Stephen Hanessian, Malken Bayrakdarian, Xuehong Luo
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Patent number: 6455705Abstract: A method of isolating 1-[N2-((S)-ethoxycarbonyl)-3-phenylpropyl)-N6-trifluoroacetyl]-L-lysyl-L-proline (lisinopril (TFA) ethyl ester, LPE). The solvent or solvent mixture used for the extraction is also a main constituent of the solvent or solvent mixture from which the crystallization takes place. High yield as well as good purity of the end product are obtained, without distillation. 1-[N2-((S)-ethoxycarbonyl)-3-phenylpropyl)-N6-trifluoroacetyl]-L-lysyl-L-proline (lisinopril (TFA) ethyl ester, LPE) is described as a precursor for producing an ACE inhibitor.Type: GrantFiled: December 24, 1998Date of Patent: September 24, 2002Assignee: Degussa AktiengesellschaftInventors: Matthias Kottenhahn, Roland Möller, Michael Kraft, Karlheinz Drauz, Klaus Stingl
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Publication number: 20020091089Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: ApplicationFiled: April 16, 2001Publication date: July 11, 2002Inventors: Donald S. Karanewsky, Vincent J. Kalish, Edward D. Robinson, Brett R. Ullman
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Publication number: 20020077455Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: April 20, 2001Publication date: June 20, 2002Applicant: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
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Publication number: 20020068730Abstract: There is provided compounds of formula I, 1Type: ApplicationFiled: July 10, 2001Publication date: June 6, 2002Inventors: Tord Inghardt, Arne N. Svensson