Plural Nitrogens Patents (Class 562/561)
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Publication number: 20030083267Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: ApplicationFiled: August 22, 2001Publication date: May 1, 2003Applicant: Biogen, Inc., a Massachusetts corporationInventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
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Publication number: 20030083384Abstract: Provided are processes and synthetic intermediates useful for the preparation of &agr;-difluoromethylornithine (DFMO) having the formula 1Type: ApplicationFiled: August 19, 2002Publication date: May 1, 2003Applicant: Bristol-Myers Squibb Company to Women First HealthCare, Inc.Inventors: Jingyang Zhu, Scott T. Chadwick, Benjamin A. Price, Shannon X. Zhao, Carrie A. Costello, Purushotham Vemishetti
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Patent number: 6528684Abstract: R or S aminocarnitine and their derivatives with formula (I) where Y is as described in the description, starting with aspartic acid with the same configuration as the aminocarnitine desired. This process has advantage in the type of reactants used, reduced volumes of solvents and the possibility of avoiding purification of intermediate products.Type: GrantFiled: December 21, 2001Date of Patent: March 4, 2003Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Natalina Dell'uomo, Maria Ornella Tinti, Francesco De Angelis
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Patent number: 6525024Abstract: This invention is directed to novel sulfonimide (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds having the following structure: wherein A, B, X, R, R1, R2, n, q, and r are as defined herein. 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: GrantFiled: April 17, 2001Date of Patent: February 25, 2003Assignee: Idun Pharmaceuticals, Inc.Inventors: Robert J. Ternansky, Patricia L. Gladstone, Kevin J. Tomaselli
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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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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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Publication number: 20020156318Abstract: Processes for preparing N-methyl-L-alanine derivatives and novel intermediates of the process. The derivatives and intermediates are useful for preparing cell-binding agent/maytansinoid complexes.Type: ApplicationFiled: December 3, 2001Publication date: October 24, 2002Inventors: Ann M. Eldridge, Johann Hiebl
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Patent number: 6465686Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: April 13, 2001Date of Patent: October 15, 2002Assignee: Pharmacia CorporationInventors: Margaret L. Grapperhaus, James A. Sikorski, Alok K. Awasthi, Lijuan J. Wang, Barnett S. Pitzele, Donald W. Hansen, Jr., Pamela T. Manning
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Patent number: 6462229Abstract: (±)-&agr;-(Difluoromethyl)-ornithine is separate into its isomers using (−)-O,O′-di-p-toluoyl-L-tartaric acid. (−)-&agr;-(Difluoromethyl)-ornithine monohydrochloride monohydrate and in particular the (−)-isomer are inhibitors of ornithine decarboxylase and thereby have numerous pharmacological actions.Type: GrantFiled: July 20, 2001Date of Patent: October 8, 2002Assignee: Lonza Ltd.Inventor: Thomas Meul
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Publication number: 20020137124Abstract: The invention relates to a process for the production of dipeptide crystals (generic formula AcXYNH2) with high purity (>95 %), by enzymatic synthesis with a protease in organic media of reversed micelles, starting from derivatives of the two constituent amino acids (AcXOEt and YNH2). A membrane and hydro-cyclone reactor was designed which enables the continuous and simultaneous synthesis and crystallisation of the dipeptides. The dipeptide crystals thus prepared are continuously removed and further separated from the remaining liquid by filtration or centrifugation. After drying, the crystals are dissolved in hot methanol. By decreasing the temperature, the dipeptide re-crystallises, originating a high purity product. After re-crystallisation the product is filtered and dried.Type: ApplicationFiled: April 26, 2002Publication date: September 26, 2002Inventors: Duarte Miguel Franca Teixeira Dos Prazeres, Ana Isabel Jorge Dias, Ana Sofia Feliciano Santos, Joaquim Manuel Sampaio Cabral, Maria Luisa Mourato Serraiheiro
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Publication number: 20020072542Abstract: The present invention contains novel compounds useful as nitric oxide synthase inhibitors.Type: ApplicationFiled: April 13, 2001Publication date: June 13, 2002Inventors: Barnett S. Pitzele, James A. Sikorski, Ronald Keith Webber
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Publication number: 20020068701Abstract: This invention relates to positively charged non-natural amino acids, methods of making thereof, and utilization thereof in peptides. In one embodiment, the invention relates to non-natural amino acids that closely replicate the natural amino acids lysine and arginine.Type: ApplicationFiled: January 10, 2002Publication date: June 6, 2002Applicant: Medical University of South CarolinaInventor: Thomas A. Dix
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Patent number: 6399819Abstract: A process for purifying creatine is described in which the creatine to be purified in the form free of water of crystallization is introduced into a saturated aqueous solution of creatine monohydrate, in which the creatine free of water of crystallization is dissolved with hydration, crystals of creatine monohydrate precipitate from the aqueous solution and these are separated off from the aqueous solution.Type: GrantFiled: December 12, 2000Date of Patent: June 4, 2002Assignee: BASF AktiengesellschaftInventors: Knut Kessel, Günter Scherr, Thomas Bogenstätter, Stefan Orsten, Dirk Franke
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Patent number: 6364914Abstract: Herein is disclosed a method of crystallization with the particle size distribution being controlled, characterized in that while crystals are being precipitated by vacuum concentration crystallization, the temperature of the slurry is periodically varied up and down during the concentration of the crystallization mother liquor (i.e., the slurry), which method is an excellent one free from the defects of the conventional methods.Type: GrantFiled: March 19, 1999Date of Patent: April 2, 2002Assignee: Ajinomoto Co., Inc.Inventors: Hiroshi Ueda, Hiroshi Fukushi, Muneyuki Ozawa
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Patent number: 6355618Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y 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: April 7, 2000Date of Patent: March 12, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
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Publication number: 20020019566Abstract: This invention provides improvements in certain processes for alkylating amino acids whereby yields based on amino acid are improved. More specifically, the invention provides a process for the preparation of amino acid derivatives in free acid or salt form, in which the nitrogen atoms of two or more amino acid molecules are linked by a hydrocarbyl or substituted hydrocarbyl group, which comprises reacting, in an aqueous medium at a pH in the range 7-14, a compound of the formula X-A-Y where X and Y are halo atoms which may be the same or different and A is a hydrocarbyl or substituted hydrocarbyl group, in which X and Y are attached to aliphatic or cycloaliphatic carbon atoms, with an amino acid (or salt thereof), wherein the reaction is carried out in the presence of dissolved cations of an alkaline earth metal or of a transition metal and/or wherein the unreacted amino acid is recovered and recycled.Type: ApplicationFiled: June 25, 2001Publication date: February 14, 2002Applicant: The Associated Octel Company LimitedInventors: Rajeshkumar Natrwarlal Patel, Jonathan Richard Wiley, Peter Michael Radley, Robert Graham Tyson
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Publication number: 20020016366Abstract: The present invention is directed towards compounds of the general formula (I) 1Type: ApplicationFiled: April 25, 2001Publication date: February 7, 2002Inventor: Gunter Knaup
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Patent number: 6344483Abstract: The current invention discloses halogenated amidino amino acid derivatives useful as nitric oxide synthase inhibitors, and pharmaceutically acceptable salts thereof.Type: GrantFiled: January 31, 2000Date of Patent: February 5, 2002Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Barnett S. Pitzele, Dale P. Spangler, Mihaly V. Toth, R. Keith Webber, Arija A. Bergmanis, Timothy J. Hagen, Sofya Tsymbalov
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Patent number: 6339173Abstract: The present invention provides novel amide-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof wherein; (a) Y is a direct link or an alkylene of 1 to about 20 carbon atoms; (b) R1 is H or a lipophilic moiety; (c) R2, R3, and R4 are positively charged moieties, or at least one but not all of R2,R3, or R4 is a positive moiety and the remaining are independently selected from H, an alkyl moiety of 1 to about 6 carbon atoms, or a heterocyclic moiety of about 5 to about 10 carbon atoms; (d) n and p are independently selected integers from 0 to 8, such that the sum of n and o is from 1 to 16; (e) X− is an anion or polyanion and (f) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid; provided that if Y is a direct link and the sum of n and p is 1 then one of either R3 or R4 must have an alkyl moiety of at least 10 carbon atoms.Type: GrantFiled: June 7, 1999Date of Patent: January 15, 2002Assignee: Promega Biosciences, Inc.Inventors: David Aaron Schwartz, William J. Daily, Brian Patrick Dwyer, Kumar Srinivasan, Bob Dale Brown
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Patent number: 6329548Abstract: Herein is disclosed an aqueous stable lysine solution containing an acid radical in such amount that the solubility of lysine therein has been increased than in the corresponding aqueous lysine base solution, whereby during storage of lysine in the form of a free-lysine solution (liquid composition), the precipitation of lysine base crystals due to the drop in temperature is prevented thereby improving the handling thereof during transportation (transfer) etc.Type: GrantFiled: March 3, 2000Date of Patent: December 11, 2001Assignee: Ajinomoto Co., Inc.Inventors: Kazuhiro Hasegawa, Toshiya Tanabe, Keita Minami
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Patent number: 6316595Abstract: The invention provides compounds and processes for synthesis of peptide nucleic acids (PNA). The compounds include temporary amino protecting groups that are base-labile, and protection groups for the exocyclic amino function of the nucleotide base that is compatible with the base-labile amino protecting group. Cleavage of an oligomer comprising these compounds from a solid support can be achieved using weak or medium strength acids.Type: GrantFiled: February 1, 2000Date of Patent: November 13, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Breipohl, Eugen Uhlmann, Jochen Knolle
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Publication number: 20010027214Abstract: Stable and non hygroscopic salts consisting of lower alkanoyl-L-carnitine magnesium citrates are disclosed which are suitable for preparing solid compositions useful as dietary/nutritional supplements for human use and as fodder supplement for veterinary purposes.Type: ApplicationFiled: September 24, 1999Publication date: October 4, 2001Inventors: NAZARENO SCAFETTA, MARIA ORNELLA TINTI
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Publication number: 20010023304Abstract: An aminopolycarboxylate is described, which is represented by the following formula (1): 1Type: ApplicationFiled: January 17, 2001Publication date: September 20, 2001Inventors: Masahiro Aoki, Yasushi Hara
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Patent number: 6255277Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.Type: GrantFiled: May 10, 1995Date of Patent: July 3, 2001Assignees: Brigham and Women's Hospital, NitroMed, Inc.Inventors: Jonathan Stamler, Joseph Loscalzo, John D. Folts
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Patent number: 6255503Abstract: Water-soluble dodecandioates wherein the cationic moiety is selected from the group comprising the cations of basic aminoacids (e.g. lysine) and choline and orally or parenterally administrable compositions containing same, are disclosed.Type: GrantFiled: November 30, 1999Date of Patent: July 3, 2001Assignee: Sigma-Tau Healthscience S.p.A.Inventors: Mosé Santaniello, Nazareno Scafetta, Maria Ornella Tinti
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Patent number: 6248866Abstract: A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as an improved method for synthesizing the same, the derivative having the formula: wherein: Q1 and Q2 may be the same or different and are amino protective groups; Q3 is an amino protective group which is orthogonal to Q1 and Q2; and Z is a hydroxy protective group.Type: GrantFiled: August 19, 1998Date of Patent: June 19, 2001Assignee: University of Florida Research Foundation, IncorporatedInventor: Raymond J. Bergeron, Jr.
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Patent number: 6235929Abstract: A novel class of tripeptide &agr;-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M1—AA—AA—AA—CO—NR3R4.Type: GrantFiled: December 27, 1996Date of Patent: May 22, 2001Assignee: Georgia Tech Research CorporationInventor: James C Powers
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Patent number: 6197750Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to 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: GrantFiled: October 22, 1998Date of Patent: March 6, 2001Assignee: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Robert J. Ternansky
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Patent number: 6156735Abstract: The present invention is directed to an arginine-silicate complex and its use in the prevention and treatment of atherosclerosis, as a dietary supplement and for promotion of structural integrity of bones and cartilage.Type: GrantFiled: December 13, 1999Date of Patent: December 5, 2000Assignee: Nutrition 21Inventors: Mark F. McCarty, Jan Zielinski
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Patent number: 6156222Abstract: Perfluoroalkyl-allyloxy- and perfluoroalkyl-iodopropyloxy-substituted polyaminoacids or poly-R.sub.F -fluoroallyl-substituted polyaminoacids which contain, in random distribution, q units of A-1, r units of A-2, s units of A-3 and t units of A-4 in which A-1 and A-2 are perfluoroalkyl-substituted amino groups of the formulae ##STR1## A-3 is a hydrophilically substituted amino or amido group of the formula ##STR2## and A-4 is a substituted amino or amido group of the formula ##STR3## where the variables are as defined herein, are useful to provide oil repellency to paper and as foam stabilizers in alcohol resistant--aqueous fire-fighting foam fire-fighting foam compositions.Type: GrantFiled: January 20, 1999Date of Patent: December 5, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: John Jennings, Ted Deisenroth, Marlon Haniff
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Patent number: 6150542Abstract: The invention relates to agents preventing (the formation of) human malodor. In particular, the invention relates to the use of several classes of compounds which can act as such agents in cosmetic products, such as deodorants and antiperspirants. These compounds are normally odorless or nearly so, but upon contacting the skin as for example, in skin care compositions or in personal care compositions, they prevent malodor.The compounds under consideration are compounds of the formula:X--(Z).sub.n --CO--NH--CH--(COO--Y)--CH.sub.2 CH.sub.2 CONH.sub.2I.Type: GrantFiled: April 13, 1999Date of Patent: November 21, 2000Assignee: Givaudan Roure (International) SAInventors: Gonzalo Acuna, Georg Frater, Peter Gygax
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Patent number: 6130315Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.Type: GrantFiled: August 24, 1998Date of Patent: October 10, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
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Patent number: 6127573Abstract: The present invention relates to a TEMPO-catalyzed oxidation of primary alcohols, RCH.sub.2 OH to corresponding carboxylic acids, RCOOH in the presence of catalytic in the presence of catalytic amount of NaClO and stoichiometric amount of NaClO.sub.2 as an oxidant.Type: GrantFiled: April 1, 1999Date of Patent: October 3, 2000Assignee: Merck & Co., Inc.Inventors: Jing Li, Zhiguo Song, David M. Tschaen, Mangzu Zhao
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Patent number: 6077877Abstract: The present invention provides amine/amide catalysts for use in catalyzing the formation of polyurethane. The amine/amide catalysts, which have low fugitivity due to their reactivity with isocyanates, and good catalytic activity, have the structure ##STR1## wherein Q is C.sub.z H.sub.2z+1, or (CH.sub.2).sub.n N(R.sup.3).sub.k T, T is a monovalent C.sub.1 -C.sub.4 alkyl, amino-C.sub.1 -C.sub.4 -alkyl, mono-C.sub.1 -C.sub.4 -alkylamino-C.sub.1 -C.sub.4 -alkyl, or di-C.sub.1 -C.sub.4 -alkylamino-C.sub.1 -C.sub.4 -alkyl group, or T is a divalent alkyl, amine substituted alkyl, alkylaminoalkyl, or alkoxyalkyl group which forms with the nitrogen atom shown in structure (I) to which T is attached a cyclic structure which incorporates up to 6 carbon atoms in the ring as well as the nitrogen atom shown in structure (I), which cyclic structure may be substituted with C.sub.1 to C.sub.4 alkyl;k=0 or 1, being 1 if T is a monovalent group and 0 if T is a divalent group; R.sup.2 .dbd.H or C.sub.z H.sub.2z+1 ; R.sup.3 .dbd.Type: GrantFiled: April 3, 1997Date of Patent: June 20, 2000Assignee: CK Witco CorporationInventors: Richard M. Gerkin, K. Kaye Robinson
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Patent number: 6020526Abstract: The present invention provides novel amide-based cationic lipids of the general structure: ##STR1## or a salt, or solvate, or enantiomers thereof wherein; (a) Y is a direct link or an alkylene of 1 to about 20 carbon atoms; (b) R.sub.1 is H or a lipophilic moiety; (c) R.sub.2, R.sub.3, and R.sub.4 are positively charged moieties, or at least one but not all of R.sub.2, R.sub.3, or R.sub.4 is a positive moiety and the remaining are independently selected from H, an alkyl moiety of 1 to about 6 carbon atoms, or a heterocyclic moiety of about 5 to about 10 carbon atoms; (d) n and p are independently selected integers from 0 to 8, such that the sum of n and o is from 1 to 16; (e) X.sup.- is an anion or polyanion and (f) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid; provided that if Y is a direct link and the sum of n and p is 1 then one of either R.sub.3 or R.sub.4 must have an alkyl moiety of at least 10 carbon atoms.Type: GrantFiled: July 22, 1996Date of Patent: February 1, 2000Assignee: Genta, IncorporatedInventors: David Aaron Schwartz, William J. Daily, Brian Patrick Dwyer, Kumar Srinivasan, Bob Dale Brown
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Patent number: 6015792Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.Type: GrantFiled: March 13, 1998Date of Patent: January 18, 2000Assignee: Bioresearch, Inc.Inventors: Robert J. Kurtz, William D. Fuller
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Patent number: 6008250Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.Type: GrantFiled: March 13, 1998Date of Patent: December 28, 1999Assignee: Bioresearch, Inc.Inventors: Robert J. Kurtz, William D. Fuller
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Patent number: 5986074Abstract: The present invention relates to novel metal chelates, exemplified as technetium-99m or rhenium chelates, and to the process of preparing such metal chelates from corresponding ligands. These ligands and their corresponding metal chelates are synthesized to have a cysteinylethylene (EC) structure, a monothiourea (MTU) structure, or a dithiourea (DTU) structure. The present invention further relates to a pharmaceutical composition comprising a metal chelate, for example, a .sup.99m Tc-chelate, to the use of the composition for renal imaging and examination of renal function, and to a kit for preparing such a composition prior to use.Type: GrantFiled: December 18, 1997Date of Patent: November 16, 1999Assignee: Emory UniversityInventors: Luigi G. Marzilli, Malgorzata Lipowska, Lory Hansen, Andrew Taylor, Jr.
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Patent number: 5973003Abstract: Novel substituted .beta. amino acid derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.Type: GrantFiled: September 26, 1997Date of Patent: October 26, 1999Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
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Patent number: 5973113Abstract: A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as a method for synthesizing the same, the derivative having the formula: ##STR1## wherein: Q.sub.1 and Q.sub.2 may be the same or different and are amino protective groups;Q.sub.3 is an amino protective group which is orthogonal to Q.sub.1 and Q.sub.2 ; andZ is a hydroxy protective group.Type: GrantFiled: October 31, 1997Date of Patent: October 26, 1999Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5955053Abstract: The present invention relates to novel metal chelates, exemplified as technetium-99m or rhenium chelates, and to the process of preparing such metal chelates from corresponding ligands. These ligands and their corresponding metal chelates are synthesized to have a cysteinylethylene (EC) structure, a thioacetamidethiourea (TATU) structure, or a dithiourea (DTU) structure. The present invention further relates to a pharmaceutical composition comprising a metal chelate, for example, a .sup.99m Tc-chelate, to the use of the composition for renal imaging and examination of renal function, and to a kit for preparing such a composition prior to use.Type: GrantFiled: May 6, 1996Date of Patent: September 21, 1999Assignee: Emory UniversityInventors: Luigi Gaetano Marzilli, Malgorzata Lipowska, Lory Hansen, Andrew Taylor, Jr.
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Patent number: 5948415Abstract: The present invention relates to new compounds, which are N.sup..delta. -substituted ornithine derivatives, having the formula (I)HOOC--CH(NH.sub.2)--(CH.sub.2).sub.3 --NH--(X).sub.h --(CH.sub.2).sub.j --(CHOH).sub.k --(CH.sub.2).sub.m --(O).sub.n --(CH.sub.2).sub.p --Rin which R represents a hydrocarbon alkyl radical or a perfluorinated alkyl radical, X is a divalent radical chosen from --CO--O--, --CO--NH-- and --SO.sub.2 --, h, j, k, m and n are, independently, zero or 1 and p is zero to 4, a salt of a compound of formula (I), an optical isomer of D or L configuration thereof or a mixture thereof. The invention also relates to a process for the preparation of these compounds, to their use, especially in cosmetics, and to compositions, especially cosmetic compositions, comprising them.Type: GrantFiled: April 17, 1996Date of Patent: September 7, 1999Assignee: L'OrealInventors: Michel Philippe, Thierry Bordier
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Patent number: 5936055Abstract: Disclosed is an acid-funtionalized polyurethane adduct and a process for the preparation of such adduct. The adduct having a linear or preferably branched structure comprises a plurality of internal urethane linkages and one or more terminal carboxylic acid groups per molecule. Such acid-funtionalized polyurethane adducts find value in the manufacture of crosslinked aqueous rubber latexes such as might be used in paint compositions.Type: GrantFiled: February 19, 1997Date of Patent: August 10, 1999Assignee: The Dow Chemical CompanyInventors: Michael J. Elwell, Hanno R. van der Wal, Camiel F. Bartelink, Henri J. Grunbauer
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Patent number: 5925339Abstract: The invention relates to agents preventing (the formation of) human malodor. In particular, the invention relates to the use of several classes of compounds which can act as such agents in cosmetic products, such as deodorants and antiperspirants. These compounds are normally odorless or nearly so, but upon contacting the skin as for example, in skin care compositions or in personal care compositions, they prevent malodor. The compounds under consideration are compounds of the formulaX--(Z).sub.n --CO--NH--CH--(COO--Y)--CH.sub.2 CH.sub.2 CONH.sub.2IThe definition of the substituents is given in the specification.Type: GrantFiled: June 19, 1997Date of Patent: July 20, 1999Assignee: Givaudan Roure SAInventors: Gonzalo Acuna, Georg Frater, Peter Gygax
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Patent number: 5914310Abstract: According to the invention, an improved class of amphoteric surfactant having improved surfactant properties characterized as mild and environmentally safe has been provided comprising compounds of the formula: ##STR1## The amphoteric surfactant of the subject invention have at least two hydrophobic moieties and at least two hydrophilic groups per molecule and are useful as emulsifiers, detergents, dispersants and solubilizing agents.Type: GrantFiled: July 30, 1997Date of Patent: June 22, 1999Assignee: Rhodia Inc.Inventors: Ji Li, Manilal Dahanayake, Robert Lee Reierson, David James Tracy
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Patent number: 5906985Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and m is 1 or 2, R.sup.1 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, phenyl, naphthyl, C.sub.1-10 alkyl-phenyl, C.sub.2-10 alkenyl-phenyl or C.sub.2-10 alkynyl-phenyl, said phenyl and naphthyl groups being optionally substituted, R.sup.2 is hydrogen or a protecting group, and Q is an acidic group; or a salt or ester thereof.Type: GrantFiled: August 21, 1997Date of Patent: May 25, 1999Assignees: Eli Lilly and Company Limited, Lilly, S.A.Inventors: Stephen Richard Baker, Almudena Rubio Esteban, John Goldsworthy, Concepcion Pedregal Tercero
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Patent number: 5892112Abstract: Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.Type: GrantFiled: January 21, 1994Date of Patent: April 6, 1999Assignees: Glycomed Incorporated, The University of FloridaInventors: Daniel E. Levy, Damian Grobelny, Cho Tang, Kevin R. Holme, Richard E. Galardy, Gregory S. Schultz, Asaad Nematalia, John H. Musser
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Patent number: 5889058Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.Type: GrantFiled: November 3, 1994Date of Patent: March 30, 1999Assignee: Celltech LimitedInventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
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Patent number: 5859295Abstract: This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.Type: GrantFiled: June 18, 1996Date of Patent: January 12, 1999Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Gerald A. Rosenthal
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Patent number: 5840972Abstract: A process is disclosed for the preparation of N.sup.G -monoalkyl-L-arginine and related compounds and salts thereof, for example N.sup.G -monomethyl-L-arginine by reacting N-alkylaminoiminomethane sulphonic acid of formula (II) with an amino acid of formula (III).Type: GrantFiled: February 22, 1995Date of Patent: November 24, 1998Assignee: Glaxo Wellcome Inc.Inventors: Rajnikant Patel, Amrik Singh Mahal, Donald Lloyd Winston Burford