Amide In Acid Moiety Patents (Class 560/41)
-
Patent number: 7563930Abstract: Provided are crystalline forms of Cinacalet HCl and processes for their preparation.Type: GrantFiled: November 22, 2006Date of Patent: July 21, 2009Assignee: Teva Pharmaceutical Industries LtdInventors: Shlomit Wizel, Revital Lifshitz-Liron, Sharon Avhar-Maydan
-
Publication number: 20090111874Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.Type: ApplicationFiled: March 24, 2006Publication date: April 30, 2009Applicant: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU PHARMENTERPRISESInventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
-
Publication number: 20090047379Abstract: The present invention relates to novel benzamide compounds may be used to provide desirable property of sweetness and to a foodstuff, chewing gum, medicinal product, toothpaste, alcoholic beverage, aqueous beverage, snack, sauce, confection, baked good, dairy product or cereal.Type: ApplicationFiled: August 17, 2007Publication date: February 19, 2009Inventors: Mark L. Dewis, Debra Merrit, Kevin Miller, Zhen Chen, Laurens Reiber
-
Publication number: 20090030227Abstract: The object is to provide: a method for producing a polymer having a stable right-handed or left-handed helical structure from a single type of monomer in a per-selective manner and controlling the proportion between a polymer having the right-handed helical structure and a polymer having the left-handed helical structure; and a polymeric material which can be used for the formation of any of the right-handed and left-handed helical structures.Type: ApplicationFiled: December 1, 2006Publication date: January 29, 2009Applicant: Japan Science and Technology AgencyInventors: Kento Okoshi, Eiji Yashima, Hisanari Onouchi, Shin-ichiro Sakurai, Takashi Kajitani
-
Publication number: 20090017509Abstract: An improved method for preparing ramipril is disclosed, and also an intermediate for use in the method.Type: ApplicationFiled: June 19, 2008Publication date: January 15, 2009Applicant: sanofi-aventis Deutschland GmbHInventors: Holger BERK, Frank ZOCHER, Hans-Wolfram FLEMMING, Rainer GAULER, Rudolf LEHNERT, Wolfgang LAUX
-
Patent number: 7473796Abstract: New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the ?-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents.Type: GrantFiled: July 16, 2007Date of Patent: January 6, 2009Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Wayne C. Widdison
-
Publication number: 20080319055Abstract: A method of providing a cooling sensation to the skin or the mucous membranes of the body by applying thereto a compound of Formula I in which X is H or (CH2)n—R, n is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, phenyl, C1-C4 straight or branched alkyl, or, a C1-C4 straight or branched alkoxy, or X and Y form together a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— which forms together with the carbon atoms to which they are attached a 5-membered ring; and R is a group with non-bonding electrons, R1 is H or C1-C5 branched alkyl, R2 and R3 are C1-C4 branched alkyls, or R2 and R3 taken together form a monocyclic, bicyclic or tricyclic radical of up to 10 carbons provided that R1, R2 and R3 together comprise at least 6 carbons. The compounds may be incorporated into products such as dentifrices, foodstuffs, confectionery, beverages, and cosmetic and medicinal preparations.Type: ApplicationFiled: March 15, 2006Publication date: December 25, 2008Applicant: GIVAUDAN SAInventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Jay Patrick Slack
-
Publication number: 20080293962Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure for tissues.Type: ApplicationFiled: August 4, 2008Publication date: November 27, 2008Applicant: L'Oreal S.A.Inventors: Maria Dalko, Yann Mahe, Lionel Breton
-
Patent number: 7449603Abstract: Provided is a process for preparing Cinacalcet, (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethane amine and intermediates thereof.Type: GrantFiled: April 27, 2007Date of Patent: November 11, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Revital Lifshitz-Liron
-
Patent number: 7439383Abstract: The present invention is directed to novel phenytoin derivative compounds and the use of such compounds as sodium channel blockers. Such compositions have utility as anti-cancer agents and can be used to limit or prevent PCa growth and/or metastasis.Type: GrantFiled: April 18, 2003Date of Patent: October 21, 2008Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
-
Publication number: 20080221209Abstract: Disclosed are enantiomers of amino-phenyl-acetic acid octadec-9-(Z)-enyl ester, and salts thereof, including pharmaceutical compositions, uses and a process for the manufacture thereof.Type: ApplicationFiled: February 25, 2008Publication date: September 11, 2008Inventors: Yaacov Herzig, Jeffrey Sterling, Vladimir Ioffe, Yuriy Raizi, Istvan Miskolczi, Andras Zekany
-
Publication number: 20080221210Abstract: The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I), wherein R1, R2, n, Y, Y?, R3, R4, W and R5 are as defined in the specification.Type: ApplicationFiled: March 22, 2005Publication date: September 11, 2008Applicant: Karo Bio ABInventors: Ana Maria Garcia Collazo, Thomas Anders Wilson Norin, Neerai Garg, Anton Joakim Lofstedt, Tomas Fredrik Hansson, Lars Jesper Hallberg, Peter Brandt
-
Patent number: 7419970Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.Type: GrantFiled: April 11, 2005Date of Patent: September 2, 2008Assignee: L'OrealInventors: Maria Dalko, Yann Mahe, Lionel Breton
-
Patent number: 7405320Abstract: Disclosed are compounds that include two or more haptens conjugated by a spacer or a carrier. The haptens may include diethylenetriaminepentaacetate (DTPA), histimine-succinyl-glutamine (HSG), or combinations of DTPA and HSG. The compound also includes an effector molecule which may be conjugated to one or more of the haptens, the spacer/carrier, or both. The effector molecule may be conjugated by a number of linkages including an ester linkage, an imino linkage, an amino linkage, a sulfide linkage, a thiosemicarbazone linkage, a semicarbazone linkage, an oxime linkage, an ether linkage, or combinations of these linkages. Also disclosed are methods of synthesizing the compounds and/or precursors of the compounds.Type: GrantFiled: February 11, 2004Date of Patent: July 29, 2008Assignee: Immunomedics, Inc.Inventors: William J. McBride, David M. Goldenberg, Carl Noren, Hans J. Hansen
-
Patent number: 7405307Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: September 13, 2007Date of Patent: July 29, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
-
Publication number: 20080161325Abstract: The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: November 13, 2007Publication date: July 3, 2008Inventors: Yvette M. Fobian, John N. Freskos, Barbara Jagodzinska
-
Patent number: 7393967Abstract: Provided is a process for preparing cinacalcet, (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethane amine.Type: GrantFiled: April 27, 2007Date of Patent: July 1, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Revital Lifshitz-Liron
-
Publication number: 20080114062Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C?—C—(CH2)2CO2H, meta-C?—C—(CH2)2OH, meta-C?C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C?Type: ApplicationFiled: February 21, 2005Publication date: May 15, 2008Applicant: UNIVERSITY COLLEGE LONDON Wolfson Institute for Biomedical ResearchInventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
-
Patent number: 7304167Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: January 24, 2006Date of Patent: December 4, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobs Jozef Backx
-
Patent number: 7294735Abstract: Isolated cinacalcet carbamate, processes for the preparation thereof, and processes for the use of cinacalcet carbamate as a reference marker and standard are provided. Also provided are cinacalcet salts substantially free of cinacalcet carbamate, and processes for the preparation thereof.Type: GrantFiled: May 23, 2006Date of Patent: November 13, 2007Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Revital Lifshitz-Liron, Yuriy Raizi, Revital Ramaty, Esti Marom
-
Patent number: 7288670Abstract: N-[N-(3,3-dimethylbutyl)-L-?-aspartyl]-L-phenylalanine 1-methyl ester is produced by hydrogenation of L-?-aspartyl-L-phenylalanine 1-methyl ester and 3,3-dimethylbutyraldehyde produced in situ by the hydrolysis or cleavage of a 3,3-dimethylbutyraldehyde precursor. The production method is efficient and low cost, as compared with conventional N-[N-(3,3-dimethylbutyl)-L-?-aspartyl]-L-phenylalanine 1-methyl ester synthesis.Type: GrantFiled: April 30, 2004Date of Patent: October 30, 2007Assignee: The Nutrasweet CompanyInventors: Indra Prakash, Kenneth E. Furlong, Handley E. Jackson, III
-
Patent number: 7253299Abstract: A process for purifying N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine which comprises subjecting N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine contaminated with impurities to crystallization from a solvent comprising a water-soluble non-protic organic solvent, thereby removing the impurities into the mother liquor and giving crystals of N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine, according to which N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine having a high quality can be obtained in a high yield and a high productivity and which is suitable for practice on an industrial scale.Type: GrantFiled: July 10, 2002Date of Patent: August 7, 2007Assignee: Kaneka CorporationInventors: Yasuhiro Iida, Hajime Manabe, Yasuyoshi Ueda
-
Patent number: 7238830Abstract: The present invention provides N-alkylaspartyl dipeptideester compounds and salts thereof, such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-?-aspartyl]-L-phenylalanine 1-methyl ester, which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester compounds and method of producing the novel aspartyl dipeptide ester compounds.Type: GrantFiled: March 16, 2001Date of Patent: July 3, 2007Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Kazuko Yuzawa, Tadashi Takemoto, Ryoichiro Nakamura
-
Patent number: 7193103Abstract: Synthesis of N-[N-(3,3-dimethylbutyl)-L-?-aspartyl]-L-phenylalanine 1-methyl ester by treating N-(3,3-dimethylbutyl)-L-aspartic acid with ketones to give oxazolidinone derivatives, which are condensed with L-phenylalanine methyl ester.Type: GrantFiled: July 30, 2004Date of Patent: March 20, 2007Assignee: The Nutrasweet CompanyInventor: Indra Prakash
-
Patent number: 7183317Abstract: It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.Type: GrantFiled: July 8, 2004Date of Patent: February 27, 2007Assignee: Atherogenics, Inc.Inventors: James A. Sikorski, Jayraz Luchoomun, Charles Q. Meng, Uday Saxena
-
Patent number: 7179934Abstract: Certain ?-amino acids that bind to the alpha-2-delta (?2?) subunit of a calcium channel are disclosed. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders. Also disclosed are methods of making the ?-amino acids.Type: GrantFiled: September 24, 2004Date of Patent: February 20, 2007Assignee: Warner-Lambert Company LLCInventors: Peter Garth Blazecka, Joseph Richard Bozelak, Norman Lloyd Colbry, Timothy Thomas Curran, Annise Paige Goodman, Kevin E. Henegar, Garrett Hoge, Paul D. Johnson, Augustine Tobi Osuma, Mark Stephen Plummer, Jacob Bradley Schwarz, Derek Clinton Vrieze, Ji Zhang
-
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
-
Patent number: 7115296Abstract: The present invention relates to a novel N-alkylaspartyl amide derivative, a salt form thereof, a sweetening agent containing the same and a sweetened food or drink containing the N-alkylaspartyl amide derivative as an effective ingredient.Type: GrantFiled: August 8, 2003Date of Patent: October 3, 2006Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Kazuko Yuzawa
-
Patent number: 7037939Abstract: The present invention relates to a compound represented as formula (I): wherein A is R2-N(R3R4), wherein Ar is a substituted or unsubstituted phenyl group, m is an integer between 0 to 4, Het is a substituted or unsubstituted 4 to 8 member heterocyclic group, n is an integer between 0 to 4; R3 and R4 are independently H, or R2 is or wherein X is (CH2)y—Ar?, R6, or (CH2)z-Het?, wherein Ar? is a substituted or unsubstituted phenyl group, y is an integer between 0 to 2, R6 is a substituted or unsubstituted linear or a branched C1-10 alkyl group, z is an integer between 0 to 2, and Het? is a 6 to 12 member heterocyclic group; B is OR1 or wherein R1 is H or C2-5 alkyl group.Type: GrantFiled: December 31, 2003Date of Patent: May 2, 2006Assignee: Industrial Technology Research InstitueInventors: Jenn-Tsang Hwang, Yu-Long Chang, Chung-Niang Yao, Chrong-Shiong Hwang
-
Patent number: 6992207Abstract: The invention refers to new alkylating di- and tripeptides based on a melphalan unit, and one or two additional amino acids or amino acid derivatives, which can be used in the treatment of carcinogenic diseases. Further, the invention refers to a pharmaceutical composition comprising the alkylating peptides of the invention.Type: GrantFiled: June 11, 2001Date of Patent: January 31, 2006Assignee: Oncopeptides ABInventors: Rolf Lewensohn, Joakim Gullbo, Rolf Larsson, Hans Ehrsson, Kristina Luthman
-
Patent number: 6989384Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: July 23, 2003Date of Patent: January 24, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Ye Hua, Hiep The Luu, Fora P. Chan, Theodore O. Johnson, Jr., Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Shao Song Chu, Brian Walter Eastman
-
Patent number: 6989461Abstract: Catalyst for the asymmetric (transfer) hydrogenation represented by the formula MLaXbSc, where M is a transition metal, to be chosen from rhodium and ruthenium, and X is a counter ion and S is a ligand, a ranges from 0.5 to 3 and b and c, each independently, range from 0 to 2, and L is a chiral ligand having the formula (1), where Cn together with the two 2 O-atoms and the P-atom forms a substituted or non-substituted ring with 2-4 C-atoms, R1 and R2 each independently represent H, an optionally substituted alkyl, aryl, alkaryl or aralkyl group or may form a (heterocyclic) ring together with the N-atom to which they are bound. And a process for the asymmetric (transfer) hydrogenation of an olefinically unsaturated compound, ketone, imine or oxime derivate in the presence of a hydrogen donor and of a catalyst, use being made of a catalyst represented by formula MLaXbSc, where M is a transition metal, to be chosen from rhodium, iridium and ruthenium, X is a counter ion, S is a ligand, a ranges from 0.Type: GrantFiled: July 6, 2001Date of Patent: January 24, 2006Assignee: DSM IP Assets B.V.Inventors: Michel Berg Van Den, Ben Feringa, Adriaan Jacobus Minnaard, Johannes Gerardus Vries De
-
Patent number: 6972340Abstract: Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.Type: GrantFiled: August 29, 2001Date of Patent: December 6, 2005Assignee: Abbott LaboratoriesInventors: Gang Liu, Bruce G. Szczepankiewicz, Zhonghua Pei, Zhili Xin, David A. Janowick
-
Patent number: 6960588Abstract: Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors.Type: GrantFiled: September 12, 2000Date of Patent: November 1, 2005Assignee: Altana Pharma AGInventor: Thomas Martin
-
Patent number: 6949557Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.Type: GrantFiled: April 29, 2003Date of Patent: September 27, 2005Assignee: Dabur Research FoundationInventors: Asish Kumar Banerjee, Venkatachalam Sesha Giri, Rama Mukherjee, Kamal K. Kapoor, Gautam Desiraju, Manu Jaggi, Anu T. Singh, Sankar Kumar Dutta, Kalapatapu V. V. M. Sairam
-
Patent number: 6888022Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: February 20, 2001Date of Patent: May 3, 2005Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Thomas C. Britton, James J. Droste, Beverly K. Folmer, George W. Huffman, Varghese John, Lee H. Latimer, Thomas E. Mabry, Jeffrey S. Nissen, Warren J. Porter, Jon K. Reel, Eugene D. Thorsett, Jay S. Tung, Jing Wu, Clark Norman Eid, William Leonard Scott
-
Patent number: 6849648Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.Type: GrantFiled: October 4, 2002Date of Patent: February 1, 2005Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, William Glen Harter, James Lester Hicks, Patrick Michael O'Brien, Ly Pham, Joseph Armand Picard, William Howard Roark
-
Patent number: 6849757Abstract: Compounds having Formula I or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting angiogenesis in a mammal.Type: GrantFiled: July 10, 2003Date of Patent: February 1, 2005Assignee: Abbott LaboratoriesInventors: Megumi Kawai, Jack Henkin, George S. Sheppard, Richard A. Craig
-
Patent number: 6849649Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: October 28, 2003Date of Patent: February 1, 2005Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
-
Patent number: 6844448Abstract: The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive ?-bond of a substrate. The chiral, non-racemic catalysts of the present invention constitute the first examples of catalysts for nucleophilic additions that comprise a main-group metal and a tri- or tetra-dentate ligand.Type: GrantFiled: December 20, 2002Date of Patent: January 18, 2005Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Matthew S. Sigman
-
Patent number: 6841183Abstract: N-[N-[3-(2-hydroxy-substituted phenyl)propyl]-L-?-aspartyl]-L-phenylalanine 1-methyl ester derivatives, which are useful as sweeteners, may be conveniently produced by subjecting a 2-hydroxychroman derivative having various substituents on the benzene ring and aspartame to a reductive alkylation reaction. These compounds may be purified by subjecting such a derivative containing one or more impurities to a crystallization step to crystallize the same. Further, there are provided a process for producing dialkoxychroman derivatives useful as intermediates for the production of such aspartame derivatives in the above process, and novel dialkoxychroman derivatives thus produced, which are excellent as the production intermediate.Type: GrantFiled: March 29, 2002Date of Patent: January 11, 2005Assignee: Ajinomoto Co., Inc.Inventors: Kazutaka Nagashima, Shinji Fujita, Yuuichi Aoki, Shigeru Kawahara, Tadashi Takemoto, Eriko Ono
-
Patent number: 6838574Abstract: A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I): wherein R1 represents a dicarba-closo-dodecaboran-yl which may be substituted with a lower alkyl group, a lower alkenyl group, carboxyl group or the like; R2 represents carboxyl group, a lower alkoxycarbonyl group, or hydroxyl group; and X represents a single bond or a linking group such as —CO—Y1— wherein Y1 represents oxygen or —N(R3)— wherein R3 represents hydrogen or a lower alkyl.Type: GrantFiled: January 21, 2000Date of Patent: January 4, 2005Assignee: Institute of Medicinal Molecular Design, Inc.Inventor: Yasuyuki Endo
-
Publication number: 20040254344Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.Type: ApplicationFiled: July 13, 2004Publication date: December 16, 2004Inventors: Mark Gallop, Kenneth C Cundy, Randall A Scheuerman, Ronald W Barrett, Noa Zerangue
-
Patent number: 6831193Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.Type: GrantFiled: May 10, 2002Date of Patent: December 14, 2004Assignee: Abbott LaboratoriesInventors: Chih-Hung Lee, Richard J. Perner, Daniel P. Larson, John R. Koenig, Arthur R. Gomtsyan, Guo Zhu Zheng, Stanley DiDomenico, Andrew O. Stewart, Erol K. Bayburt
-
Publication number: 20040209873Abstract: Arylcycloalkyl derivatives having branched side chains, processes for their preparation and their use as pharmaceuticalsType: ApplicationFiled: February 27, 2004Publication date: October 21, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Christian Stapper, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Dirk Gretzke, Stefanie Keil, Hans-Ludwig Schaefer, Wolfgang Wendler
-
Patent number: 6806381Abstract: Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.Type: GrantFiled: October 17, 2002Date of Patent: October 19, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Ramakrishnan Chidambaram, Joydeep Kant, Raymond E. Weaver, Jurong Yu, Arun Ghosh
-
Publication number: 20040204368Abstract: An oxadiazole derivative of formula (I) and a non-toxic salt thereof, 1Type: ApplicationFiled: December 1, 2003Publication date: October 14, 2004Inventors: Kazuyuki Ohmoto, Kazuhito Kawabata
-
Patent number: 6803383Abstract: Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.Type: GrantFiled: September 27, 2002Date of Patent: October 12, 2004Assignee: The Scripps Research InstituteInventors: Dale L. Boger, David A. Cheresh
-
Patent number: 6794531Abstract: The present invention relates to a method of manufacturing aspartyl dipeptide ester compounds, which can be used as sweeteners, and aldehydes that can be used in the manufacturing processes.Type: GrantFiled: April 8, 2002Date of Patent: September 21, 2004Assignee: Ajinomoto Co., Inc.Inventors: Kazutaka Nagashima, Yuuichi Aoki, Tadashi Takemoto, Yusuke Amino, Nao Funakoshi, Eriko Ono
-
Patent number: 6784309Abstract: This invention relates to the purification of N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester by slurrying a mixture containing N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester with organic or aqueous organic solvents.Type: GrantFiled: April 14, 2000Date of Patent: August 31, 2004Assignee: The Nutrasweet CompanyInventors: Indra Prakash, Kurt Wachholder