Additional Nitrogen In Acid Moiety Patents (Class 560/169)
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Patent number: 7135587Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5?, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.Type: GrantFiled: November 30, 2001Date of Patent: November 14, 2006Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Alfred Jonczyk, Oliver Schadt, Simon Goodman
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7015349Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.Type: GrantFiled: March 26, 2003Date of Patent: March 21, 2006Assignee: The Gillette CompanyInventors: Anwar Jardien, Roman Rariy, Gurpreet S. Ahluwalia, Douglas Shander
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Patent number: 6965049Abstract: Provided is a zwitterionic lipid compound represented by formula (I) given below: In formula (I), m and n are independently integers of 1 to 4, p is an integer of 7 to 21, one R is NH3+, and each other R is H.Type: GrantFiled: February 23, 2004Date of Patent: November 15, 2005Assignee: Oxygenix Co., Ltd.Inventors: Eishun Tsuchida, Shinji Takeoka, Keitaro Sou, Katsura Mori
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Patent number: 6962905Abstract: A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.Type: GrantFiled: April 19, 2000Date of Patent: November 8, 2005Assignee: AstraZeneca ABInventor: David Gustafsson
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Patent number: 6949516Abstract: The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: May 5, 2003Date of Patent: September 27, 2005Assignee: Cytovia, Inc.Inventors: John F. W. Keana, Sui Xiong Cai, John Guastella, Wu Yang, John A. Drewe, Eckard Weber
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Patent number: 6939986Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.Type: GrantFiled: February 22, 2002Date of Patent: September 6, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Patent number: 6916948Abstract: Derivatives of bis-(1,3-dihydroxy-prop-2-yl)amine are disclosed, together with the use of such derivatives and of bis(1,3-dihydroxy-prop-2-yl)amine itself in the preparation of polymers, in particular dendrimers. Some of the derivatives may be useful as non-ionic surfactants.Type: GrantFiled: September 12, 2001Date of Patent: July 12, 2005Assignee: Isis Innovation LimitedInventors: George W. J. Fleet, David Scott, Malcolm Finn, Thomas Krūlle
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Patent number: 6897334Abstract: Methods are provided for the improved production of a creatine ester by in situ production of an acid catalyst.Type: GrantFiled: August 25, 2003Date of Patent: May 24, 2005Assignee: Board of Regents of the University of NebraskaInventor: Jonathan Vennerstrom
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Patent number: 6875884Abstract: Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.Type: GrantFiled: July 28, 2000Date of Patent: April 5, 2005Assignee: Kirin Beer Kabushiki KaishaInventors: Janak Padia, Michael Hocker, Tsuyoshi Nishitoba, Hirohi Ohashi, Eiji Sawa
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Patent number: 6858748Abstract: The novel compound of the disclosure is 4-chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic acid methyl ester (3F-19), and it alone or in combination with 4-(4-Ethoxy-phenyl)-2-(N?-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13), appears useful in humans as therapeutic means for the eradication of tumors from the human's colon.Type: GrantFiled: January 13, 2004Date of Patent: February 22, 2005Assignee: Research Foundation of the University of Central FloridaInventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Krasnykh Olga Petrovna, Lisovskaja Natalja Anatoljevna, Elena A. Goun
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Patent number: 6855711Abstract: Use of a compound of formula (I), wherein R1 is H or hydrocarbyl; R2 is a hydrophobic radical; R3 is 3-(C2-C6)acyl-4-hydroxyphenyl, 3-hydroxyimino (C2-C6)-alkyl-4-hydroxyphenyl, or COOZ, wherein Z is H, (C1-C6) alkyl, aryl, aryl or ar(C1-C6) alkyl; and n is 1-20; and of a compound of formula (II), wherein R4 is (C1-C6) alkyl, cyano (C1-C6) alkyl, (C1-C6) alkoxy (C1-C6) alkyl or —CH2NR7R8, wherein R7 and R8, the same or different, is each H or (C1-C6) alkyl, or together with the N atom form a saturated or unsaturated 5-7 membered ring optionally containing a further heteroatom selected from N, O or S, the further N atom being optionally substituted, and either R5 is H and R6 is (C2-C6) acyl or hydroxyimino (C2-C6) alkyl, or R5 and R6 together with the phenyl ring form a quinoline, a 1,2,3,4-tetrahydroquinoline or a perhydroquinoline ring, for the preparation of pharmaceutical compositions for the treatment of Parkinson's disease or stroke.Type: GrantFiled: June 7, 2000Date of Patent: February 15, 2005Assignees: Yeda Research and Development Co. Ltd., Technion Research and Development Foundation Ltd.Inventors: Rivka Warshawsky, Moussa B. H. Youdim, Dorit Ben-Shachar, Abraham Warshawsky
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Patent number: 6844299Abstract: This invention generally relates to new polyol ester derivatives of polyamines for use as dispersant additives compatible in synthetic ester-based turbo oils. The dispersant additives of the present invention consist of a hydrocarbon acid, a polyol, an amine carrier such as diacid or cyclic anhydride and a polyamine. The hydrocarbon acid makes up the non-polar hydrocarbon portion of the dispersant and the polyamine functions as the polar headgroup. The diacid or cyclic anhydride provides a means for attaching the polar polyamine to the dispersant structure through an amide linkage. Different dispersant structures are obtained by varying the hydrocarbon acid, the polyol and the nature of the polyamine.Type: GrantFiled: February 20, 2003Date of Patent: January 18, 2005Assignee: BP Corporation North America Inc.Inventors: Paul W. Bessonette, Patrick E. Godici, Kim E. Fyfe, Jeenok T. Kim
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Publication number: 20040249187Abstract: The invention relates to a method for producing chiral amino acid derivatives, characterised in that free carboxylic acid groups in an amino acid derivative are first converted into nitro ketones, and said nitro ketones are then converted into the corresponding nitro alcohols and amino alcohols by means of reduction. The invention also relates to the nitro ketones and nitro alcohols obtained as intermediate products.Type: ApplicationFiled: July 30, 2004Publication date: December 9, 2004Inventors: Joachim Rudolph, Frithjof Hannig
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Publication number: 20040171608Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteasome inhibitors.Type: ApplicationFiled: December 18, 2003Publication date: September 2, 2004Applicant: Millennium Pharmaceuticals, Inc.Inventors: Francois Soucy, Louis Flamondon, Mark Behnke, William Roush
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Patent number: 6774243Abstract: Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: October 30, 2001Date of Patent: August 10, 2004Assignee: Agouron Pharmaceuticals, Inc.Inventors: Qingping Tian, Naresh K. Nayyar, Srinivasan Babu, Junhua Tao, Terence Jarold Moran, Raymond Dagnino, Jr., Lennert J. Mitchell, Jr., Travis Paul Remarchuk, Michael Joseph Melnick, Steven Lee Bender
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Patent number: 6750253Abstract: The present invention relates to compounds of the formula wherein R1 independently represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro, provided that when R1 represents one substituent, it is in the ortho position, and when R1 represents more than one substituent, at least one R1 substituent is in the ortho position; R2 is one substituent in the ortho position, said substituent being selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1Type: GrantFiled: February 22, 2002Date of Patent: June 15, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Erik Rytter Ottosen
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Publication number: 20040072907Abstract: A magnetic circuit component having a plurality of claws arranged in a plurality of rows, with the base of each claw connected to a common yoke. A plurality of non-interlaced coils constituting a multi-phase winding are included, with the coils being wound around the bases of corresponding claws, and being distributed uniformly in the direction of motion.Type: ApplicationFiled: July 30, 2003Publication date: April 15, 2004Inventors: Dragovich S. Peter, Prins J. Thomas, Zhou Ru
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Patent number: 6720400Abstract: The present invention relates to an improved process for the continuous preparation of polyisocyanates with a biuret structure comprising the steps of continuously reacting excess amounts of organic diisocyanates having exclusively aliphatically and/or cycloaliphatically bound isocyanate groups with organic diamines having exclusively aliphatically and/or cycloaliphatically bound primary amino groups at temperatures above 170° C. and adding acid before or during the reaction.Type: GrantFiled: May 15, 2001Date of Patent: April 13, 2004Assignee: Bayer AktiengesellschaftInventors: Reinhard Halpaap, Dieter Mager, Siegfried Oeckl, Harald Mertes
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Publication number: 20040054216Abstract: The present invention provides a method for industrially producing an optically active lysine derivative useful as a pharmaceutical intermediate. More particularly, the present invention provides a production method including protecting an amino group or an amino group and carboxyl group of optically active 2-amino-6-methyl-6-nitroheptanoic acid with a protecting group, reducing a nitro group to synthesize a 6,6-dimethyl lysine derivative and reacting the 6,6-dimethyl lysine derivative with an acetic acid derivative.Type: ApplicationFiled: August 13, 2003Publication date: March 18, 2004Applicant: AJINOMOTO CO., INC.Inventors: Masakazu Nakazawa, Daisuke Takahashi, Norimasa Onishi, Masaki Naito, Kunisuke Izawa, Kenzo Yokozeki
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Patent number: 6706922Abstract: A method of forming polymers in the presence of nucleic acid using template polymerization. Also, a method of having the polymerization occur in heterophase systems. These methods can be used for the delivery of nucleic acids, for condensing the nucleic acid, for forming nucleic acid binding polymers, for forming supramolecular complexes containing nucleic acid and polymer, and for forming an interpolyelectrolyte complex.Type: GrantFiled: November 16, 2001Date of Patent: March 16, 2004Assignee: Mirus CorporationInventors: Jon A. Wolff, James E. Hagstrom, Vladimir G. Budker, Vladimir S. Trubetskoy, Paul M. Slattum, Lisa J. Hanson
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Patent number: 6693187Abstract: Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R1, R2, R3, R4, X, Y, Z and n are as defined herein. The compounds are useful as phosphitylating agents, e.g., in the phosphitylation of 3′ and 5′ hydroxyl groups of nucleosides and oligonucleotides. Also provided are phosphonocarboxylate and H-phosphonite carboxylate analogs of the compounds of formula (I). The compounds enable synthesis of phosphinocarboxylate and phosphonocarboxylate oligonucleotides having reduced internucleotide charge and enhanced nuclease resistance.Type: GrantFiled: October 17, 2000Date of Patent: February 17, 2004Assignee: Lievre Cornu LLCInventor: Douglas J. Dellinger
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Publication number: 20040024224Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: ApplicationFiled: May 15, 2003Publication date: February 5, 2004Applicant: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
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Patent number: 6664412Abstract: The present invention provides a method for industrially producing an optically active lysine derivative useful as a pharmaceutical intermediate. More particularly, the present invention provides a production method including protecting an amino group or an amino group and carboxyl group of optically active 2-amino-6-methyl-6-nitroheptanoic acid with a protecting group, reducing a nitro group to synthesize a 6,6-dimethyl lysine derivative and reacting the 6,6-dimethyl lysine derivative with an acetic acid derivative.Type: GrantFiled: October 29, 2002Date of Patent: December 16, 2003Assignee: Ajinomoto Co., Inc.Inventors: Masakazu Nakazawa, Daisuke Takahashi, Norimasa Onishi, Masaki Naito, Kunisuke Izawa, Kenzo Yokozeki
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Publication number: 20030228986Abstract: This invention generally relates to new polyol ester derivatives of polyamines for use as dispersant additives compatible in synthetic ester-based turbo oils. The dispersant additives of the present invention consist of a hydrocarbon acid, a polyol, an amine carrier such as diacid or cyclic anhydride and a polyamine. The hydrocarbon acid makes up the non-polar hydrocarbon portion of the dispersant and the polyamine functions as the polar headgroup. The diacid or cyclic anhydride provides a means for attaching the polar polyamine to the dispersant structure through an amide linkage. Different dispersant structures are obtained by varying the hydrocarbon acid, the polyol and the nature of the polyamine.Type: ApplicationFiled: February 20, 2003Publication date: December 11, 2003Inventors: Paul W. Bessonette, Patrick E. Godici, Kim E. Fyfe, Jeenok T. Kim
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Patent number: 6649587Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.Type: GrantFiled: April 27, 2000Date of Patent: November 18, 2003Assignee: SLIL Biomedical CorporationInventors: Benjamin Frydman, Laurence J. Marton
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Publication number: 20030207859Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.Type: ApplicationFiled: January 9, 2003Publication date: November 6, 2003Inventors: James M. Balkovec, Mark L. Greenlee, Steven H. Olson, Gregory P. Rouen
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Patent number: 6639097Abstract: This invention relates to a new fungicidally active compound of formula (I), a method of combating fungi at a locus infested or liable to be infested therewith, and an agricultural composition where X is H or O−A+ and A is a radical (II).Type: GrantFiled: July 29, 2002Date of Patent: October 28, 2003Assignee: Bayer Cropscience GmbHInventors: Norman John De'Ath, John Klostermyer
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Publication number: 20030181391Abstract: The present invention is directed to novel dipeptides thereof, represented by the general Formula I: 1Type: ApplicationFiled: May 5, 2003Publication date: September 25, 2003Applicant: Cytovia, Inc.Inventors: John F.W. Keana, Sui Xiong Cai, John Guastella, Wu Yang, John A. Drewe, Eckard Weber
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Publication number: 20030176398Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.Type: ApplicationFiled: June 11, 2002Publication date: September 18, 2003Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
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Patent number: 6599940Abstract: One aspect of the present invention relates to 2-hydroxymethylglutamic acid and congeners thereof. A second aspect of the invention relates to a method of synthesizing 2-hydroxymethylglutamic acid and congeners thereof.Type: GrantFiled: September 13, 2001Date of Patent: July 29, 2003Assignee: Georgetown UniversityInventor: Alan P. Kozikowski
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Publication number: 20030130204Abstract: Peptido and peptidomimetic compounds of the formula: 1Type: ApplicationFiled: November 6, 2002Publication date: July 10, 2003Inventors: Peter Scott Dragovich, Stephen Evan Webber, Thomas Jay Prins, Ru Zhou, Joseph Timothy Marakovits, Theodore O. Johnson
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Publication number: 20030105351Abstract: The present invention provides a method for industrially producing an optically active lysine derivative useful as a pharmaceutical intermediate. More particularly, the present invention provides a production method including protecting an amino group or an amino group and carboxyl group of optically active 2-amino-6-methyl-6-nitroheptanoic acid with a protecting group, reducing a nitro group to synthesize a 6,6-dimethyl lysine derivative and reacting the 6,6-dimethyl lysine derivative with an acetic acid derivative.Type: ApplicationFiled: October 29, 2002Publication date: June 5, 2003Applicant: AJINOMOTO CO. INCInventors: Masakazu Nakazawa, Daisuke Takahashi, Norimasa Onishi, Masaki Naito, Kunisuke Izawa, Kenzo Yokozeki
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Patent number: 6569636Abstract: An assay is disclosed for determining whether a test compound modulates the activity of an enzyme having a metallated active site. The assay method employs a comparison of the binding ability of the metallated and unmetallated forms of the enzyme to the test compound.Type: GrantFiled: May 27, 1999Date of Patent: May 27, 2003Assignee: Hawaii Biotechnology Group, Inc.Inventors: Paul G. Grothaus, Dana E. Davis, Sean O'Malley
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Publication number: 20030096864Abstract: The present invention is substituted amines of formula (X) 1Type: ApplicationFiled: June 29, 2001Publication date: May 22, 2003Inventors: Lawrence Y. Fang, Roy Hom, Varghese John, Michel Maillaird
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Patent number: 6562963Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.Type: GrantFiled: July 31, 2001Date of Patent: May 13, 2003Inventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
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Patent number: 6559334Abstract: The invention relates to novel optically active polymerizable dipeptides, to the process for the preparation thereof, to the polymerization thereof and to the use of the polymers as adsorbents for the chromatographic separation of enantiomers.Type: GrantFiled: August 12, 1994Date of Patent: May 6, 2003Assignee: Bayer AktiengesellschaftInventors: Walter Lange, Michael Grosse-Bley, Bruno Bömer, Rolf Grosser, Franz-Peter Hoever
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Publication number: 20030083513Abstract: This invention discloses a substance which is a betaine ester of a functional alcohol that has an amido bond in its molecule and releases the functional alcohol.Type: ApplicationFiled: July 2, 2002Publication date: May 1, 2003Applicant: KAO CORPORATIONInventors: Koichi Murayama, Shigeyoshi Tanaka, Atsushi Katayama, Ryoichi Hirayama, Takami Gema
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Publication number: 20030044368Abstract: Provided is a deodorant having excellent masking and deodorizing effects of scalp odor, body odor and foot odor.Type: ApplicationFiled: February 21, 2002Publication date: March 6, 2003Inventor: Keiji Tsuchikura
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Patent number: 6504047Abstract: The present invention is directed towards compounds of the general formula (I) (I) are important intermediates for the preparation of pharmaceuticals. Further intermediates, process for the preparation of (I) and use thereof.Type: GrantFiled: April 25, 2001Date of Patent: January 7, 2003Assignee: Degussa AGInventor: Günter Knaup
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Publication number: 20030004367Abstract: New secondary amines are described which are prepared from inexpensive, commercially available raw materials, are stable at room temperature, and are reactive toward electrophiles. The secondary amines are prepared by the addition of one or more primary amines with one or more male (amide/ester) and fumar (amide/ester) Michael receptors. The above amines can be used as coreactants with aliphatic polyisocyanates for polyurea coatings. The novel secondary amines are also described as particularly useful as part of a two-part liquid pavement marking composition for pavement markings.Type: ApplicationFiled: July 22, 2002Publication date: January 2, 2003Applicant: 3M Innovative Properties CompanyInventors: Richard G. Hansen, Dean M. Moren, Mark D. Purgett
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Patent number: 6495522Abstract: The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I: where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: August 28, 2000Date of Patent: December 17, 2002Assignee: Cytovia, Inc.Inventors: Yan Wang, Sui Xiong Cai, Eckard Weber, Gordon B. Mills, Douglas R. Green, Lufeng Guan
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Patent number: 6495597Abstract: Compounds of formula (I) wherein R4 is an ester or thioester group and R, R1, R2 and R3 are as defined in the specification, inhibit proliferation of tumor cells.Type: GrantFiled: October 5, 2000Date of Patent: December 17, 2002Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Andrew Paul Ayscough, Lisa Marie Pratt, Alan Hastings Drummond
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Patent number: 6469199Abstract: New secondary amines are described which are prepared from inexpensive, commercially available raw materials, are stable at room temperature, and are reactive toward electrophiles. The secondary amines are prepared by the addition of one or more primary amines with one or more male (amide/ester) and fumar (amide/ester) Michael receptors. The above amines can be used as coreactants with aliphatic polyisocyanates for polyurea coatings. The novel secondary amines are also described as particularly useful as part of a two-part liquid pavement marking composition for pavement markings.Type: GrantFiled: August 24, 1999Date of Patent: October 22, 2002Assignee: 3M Innovative Properties CompanyInventors: Richard G. Hansen, Dean M. Moren, Mark D. Purgett
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Patent number: 6451854Abstract: The present invention relates to &agr;-amino acid phenyl ester derivatives having general formula (I) wherein R1 is (C1-3)alkyloxy; R2 is (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R3 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R4 is (C1-6)alkyl; R5 and R6 are independently (C1-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl or aralkyl, each of which may be optionally substituted with (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, cyano or NR7R8; R7 and R8 are independently (C1-6)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these &agr;-amino acid phenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.Type: GrantFiled: January 18, 2001Date of Patent: September 17, 2002Assignee: Akzo Nobel N.V.Inventor: Niall Morton Hamilton
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Patent number: 6437171Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds of formula wherein R1, R1′, R2, R2′, R3 and R4 have the meaning given in the specification and pharmaceutically acceptable addition salts thereof, from 1,2-epoxides of formula wherein R1, R′, R2 and R2′ have the meaning given in the specification.Type: GrantFiled: June 8, 2000Date of Patent: August 20, 2002Assignee: Hoffman-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Patent number: 6420592Abstract: Phosphonamide compounds and methods of forming those compounds are provided. The inventive methods comprise forming a template opened-ring phosphonamide compound and optionally subjecting the template to a ring-closing metathesis reaction in the presence of a ring-closing catalyst (e.g., a Grubbs catalyst) to yield a heterocyclic phosphonamide. Advantageously, the template structures can be provided with a wide array of functional groups (e.g., amino acid side chains, peptides) chosen to provide particular properties to the compound.Type: GrantFiled: August 15, 2000Date of Patent: July 16, 2002Assignee: University of KansasInventors: Kevin T. Sprott, Paul R. Hanson
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Publication number: 20020065316Abstract: The present invention relates to novel active compounds named Citrullimycines, which are obtainable by cultivation of Streptomyces sp. ST 101396 (DSM 13309), and to their pharmaceutically acceptable salts and derivatives. The present invention further relates to a process for the production of the Citrullimycines, to the microorganism Streptomycetes sp. ST 101396 (DSM 13309), to the use of the Citrullimycines and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, for example as inhibitors of the neurotensin receptor, and to pharmaceutical compositions comprising Citrullimycines or a pharmaceutically acceptable salt or derivative thereof.Type: ApplicationFiled: October 1, 2001Publication date: May 30, 2002Inventors: Cordula Hopmann, Michael Kurz, Mark Bronstrup, Joachim Wink
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Patent number: 6376699Abstract: Hydroazinecarboxylic acid ester of the formula In which R1 is an optionally substituted alkyl group, an aryl group, an arylalkyl group or a cycloalkyl group, and R3 is an optionally substituted alkyl group.Type: GrantFiled: January 26, 2001Date of Patent: April 23, 2002Assignee: Lonza AGInventor: Ulrich Veith
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Publication number: 20020042537Abstract: The present invention provides a method for industrially producing an optically active lysine derivative useful as a pharmaceutical intermediate. More particularly, the present invention provides a production method including protecting an amino group or an amino group and carboxyl group of optically active 2-amino-6-methyl-6-nitroheptanoic acid with a protecting group, reducing a nitro group to synthesize a 6,6-dimethyl lysine derivative and reacting the 6,6-dimethyl lysine derivative with an acetic acid derivative.Type: ApplicationFiled: July 13, 2001Publication date: April 11, 2002Applicant: AJINOMOTO CO., INC.Inventors: Masakazu Nakazawa, Daisuke Takahashi, Norimasa Onishi, Masaki Naito, Kunisuke Izawa, Kenzo Yokozeki