The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 548/201)
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Patent number: 7687490Abstract: An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including bata-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis.Type: GrantFiled: April 12, 2006Date of Patent: March 30, 2010Assignee: Meiji Seika Kaisha, Ltd.Inventors: Takahisa Maruyama, Yuko Kano, Takashi Ando, Takehiko Sawabe, Nobuyoshi Baba, Hiromi Takata, Hisashi Suzuki, Kazuhiro Aihara, Toshiki Fujita
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Patent number: 7674827Abstract: Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds for combating animal pests The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.Type: GrantFiled: November 15, 2006Date of Patent: March 9, 2010Assignee: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Publication number: 20100029722Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: December 19, 2007Publication date: February 4, 2010Inventors: Natalie Dales, Zaihui Zhang, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Shaoyi Sun
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Publication number: 20090286835Abstract: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: October 3, 2008Publication date: November 19, 2009Applicant: AstraZeneca ABInventors: Hakan BLADH, Frank Burkamp, Balint Gabos, Peter Hansen, Svetlana Ivanova, Karolina Lawitz
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Publication number: 20090281152Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein R1, R2 and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: July 9, 2007Publication date: November 12, 2009Inventors: Gerard Martin Paul Giblin, Mairi Gibson, Adrian Hall
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Patent number: 7612059Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 13, 2005Date of Patent: November 3, 2009Assignee: Vicuron Pharmaceuticals, Inc.Inventors: Jeffrey Jacobs, Rakesh K Patel, Jason G Lewis, Dinesh V Patel, Zhengyu Yuan
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Publication number: 20090270433Abstract: A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. [wherein R1 represents hydrogen, R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc.Type: ApplicationFiled: September 19, 2008Publication date: October 29, 2009Applicant: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimlyo Tabata
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Publication number: 20090270460Abstract: Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.Type: ApplicationFiled: May 22, 2007Publication date: October 29, 2009Inventors: Michael Gregory Bell, Robert Anthony Doti, Michael James Genin, Peter Ambrose Lander, Tianwei Ma, Peter Rudolph Manninen, Jason Matthew Ochoada, Fucheng Qu, Lindsay Scott Stelzer, Ryan Edward Stites, Alan M. Warshawsky
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Patent number: 7589213Abstract: Therapeutic compounds, compositions, medicaments, and methods are disclosed herein.Type: GrantFiled: March 17, 2008Date of Patent: September 15, 2009Inventor: David W. Old
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Publication number: 20090203919Abstract: A method for producing crystal A of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid by dissolving 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid in methanol or a mixed solvent of methanol and water (the volume ratio of methanol to water is 90/10 or more), then adding water until the ratio of methanol to water becomes 7/3, and further adding a specific amount of a seed crystal at a specific timing during the addition of water.Type: ApplicationFiled: June 22, 2007Publication date: August 13, 2009Inventor: Mitsutaka Kitamura
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Publication number: 20090197865Abstract: In one embodiment the invention provides a method of combating cyanide poisoning, which comprises administering to a subject a compound capable of releasing 3-mercapto-pyruvate in vivo. In other embodiments the invention also provides pharmaceutical compositions comprising a compound capable of releasing 3-mercaptopyruvate in vivo, as well as novel compounds that are capable of releasing 3-mercaptopyruvate in vivo.Type: ApplicationFiled: June 28, 2007Publication date: August 6, 2009Inventors: Herbert T. Nagasawa, David J.W. Goon, Daune L. Crankshaw, Robert Vince
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Patent number: 7560462Abstract: Substituted urea compounds useful in the treatment of diseases and C1-3alkyleneOR3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X1 is null, —O—, —S—, —CH2—, or —N(R1)—; X2 is —O—, . -£>. -, or —N(R1)—,—. . Y xs 0 or S; or =y represents two hydrogen atoms attached to a common carbon atom, —W is selected from the group consisting of heteroaryl, aryl, heterocycloalkyl, cycloalkyl, and C1-6alkyl substituted with a heteroaryl. or aryl group; R6 is —C?C—R7 or heteroaryl; R8, R9, and R10, independently, are selected from the group consisting of halo, optionally substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OCP3, CF3, NO2, CN, NC, N(R3)2, OR3, CO2R3, C(O)N (R3)2, C(O)R3, N(R1)COR3, N(R1)C(O)OR3, N(R8)C(O)OR3, N(R1)C(O)C1-3alkyleneC(O)R3, N(R1)C(O)C1 -3alkyleneC(O)OR3, N(R1)C(O)C1-3alkyleneOR3, N(R1)C(O)C1-3alkyleneNHC(O)OR3, N(R1)C(O)C1-3alkyleneSO2.Type: GrantFiled: July 1, 2005Date of Patent: July 14, 2009Assignee: ICOS CorporationInventors: John Joseph Gaudino, Adam Wade Cook
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Patent number: 7553975Abstract: A family of compounds capable of inhibiting the activity of farnesyl transferase.Type: GrantFiled: May 30, 2006Date of Patent: June 30, 2009Assignee: Ipsen Pharma S.A.S.Inventors: Thomas D. Gordon, Barry A. Morgan
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Publication number: 20090163560Abstract: A compound having a structure and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.Type: ApplicationFiled: February 17, 2009Publication date: June 25, 2009Inventors: David W. Old, Danny T. Dinh
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Patent number: 7541475Abstract: This invention is directed to processes for making substituted thiazoles. The substituted thiazole, ethyl 2-(4-hydroxyphenyl)-4-methyl-1,3-thiazole-5-carboxylate, also known as TEI-6720, is useful for treatment of gout and hyperuricemia. This compound belongs to a class of substituted thiazoles that inhibit xanthine oxidase and thus block uric acid production.Type: GrantFiled: July 30, 2004Date of Patent: June 2, 2009Assignee: Abbott LaboratoriesInventors: Timothy A. Robbins, Helen Zhu, Jun Shao
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Patent number: 7531563Abstract: The present invention relates to novel thiazoline acids and derivatives thereof useful as chelators of trivalent metals in therapeutic applications. For example, the thiazoline acid derivatives are useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.Type: GrantFiled: September 15, 2006Date of Patent: May 12, 2009Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090030210Abstract: There is provided a process for producing an optically active 2-alkylcysteine or a salt thereof, characterized by allowing cells of microorganism or treated products thereof having an activity of stereoselective hydrolysis of the amide bond of a 2-alkyl-L-cysteinamide or a salt thereof to act on a 2-alkylcysteinamide consisting of a mixture of D- and L-isomers or a salt thereof; and allowing the obtained 2-alkyl-L-cysteine and 2-alkyl-D-cysteinamide to react with an aldehyde or a ketone, or an acetal or ketal thereof, so as to derive therefrom a 4-alkylthiazolidine-4-carboxylic acid or a salt thereof and a 4-alkylthiazolidine-4-carboxamide or a salt thereof, thereby efficiently separating and obtaining a 2-alkyl-L-cysteine or a salt thereof, or a 2-alkyl-D-cysteine or a salt thereof. There is also provided a process for producing a 4-alkylthiazolidine-4-carboxylic acid or a salt thereof from the 2-alkylcysteine or a salt thereof.Type: ApplicationFiled: September 19, 2008Publication date: January 29, 2009Applicant: Mitsubishi Gas Chemical Company, Inc.Inventors: Yasushi Higuchi, Akinori Tanaka, Ryuji Hasemi, Masaki Sugita
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Publication number: 20090018104Abstract: Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.Type: ApplicationFiled: October 6, 2006Publication date: January 15, 2009Applicant: Astellas Pharma Inc.Inventors: Junji Sato, Kazuyuki Hattori, Hirokazu Kubota, Ryosuke Munakata, Toru Asano, Junko Maeda, Masakatsu Kawakami, Akio Kamikawa
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Patent number: 7468360Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.Type: GrantFiled: August 8, 2007Date of Patent: December 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20080306125Abstract: Compounds of formula. wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.Type: ApplicationFiled: February 2, 2007Publication date: December 11, 2008Inventors: Michael Gregory Bell, Michael James Genin, Peter Ambrose Lander, Lindsay Scott Stelzer, Robert Anthony Doti, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Jason Matthew Ochoada, Quanrong Shen, Alan M. Warshawsky, Tianwei Ma, Ryan Edward Stites
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Publication number: 20080181866Abstract: Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R3, X, V, W, T, Z, R, Y1, and p are as defined herein.Type: ApplicationFiled: November 20, 2007Publication date: July 31, 2008Inventors: Martin Robert Leivers, Franz Ulrich Schmitz, Ronald Conrad Griffith, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Stephanie Anna Chan, Roopa Rai, Irina Slobodov, Tony Loc Ton
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Patent number: 7402600Abstract: Compounds or their salts having general formulas (I) and (II) wherein: s=is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.Type: GrantFiled: September 26, 2005Date of Patent: July 22, 2008Assignee: NicOx S.A.Inventor: Piero Del Soldato
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Patent number: 7361676Abstract: There are provided a solid preparation containing a single crystal of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid, an excipient and a disintegrating agent, and a method for producing the same.Type: GrantFiled: March 28, 2003Date of Patent: April 22, 2008Assignee: Teijin LimitedInventors: Michio Iwai, Kazuhiro Nakamura, Masahiko Dohi, Hiroko Mochizuki, Seiji Mochizuki
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Patent number: 7342032Abstract: Computer game systems respond to the spatial state of a pointing device. Changes in the spatial state of a hand held or mobile unit, or plurality of units drive a game scheme maintained in a computer. Position and attitude of the mobile device cause program branching functions which are bases upon a game rule set. In example, a game scheme executed on a computing apparatus may be incorporated into a mobile telephone having a GPS and electronic compass. Physical states relating to position and pointing attitude of the telephone as described in part by position or attitude parameters, drives computer programming code to takes actions which depend on measured position and attitude values thus making computer games for mobile users are made highly interactive. User gestures including simple pointing actions allow a user to express desires to a computer in an express and direct fashion.Type: GrantFiled: March 17, 2003Date of Patent: March 11, 2008Assignee: Solvay Pharmaceuticals, Inc.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Arnoldus H. J. Herremans, Herman H. van Stuivenberg, Jessica A. R. Dijksman, Andrew C. McCreary
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Publication number: 20080015219Abstract: Disclosed and described herein are compounds of the formula or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed and described.Type: ApplicationFiled: May 14, 2007Publication date: January 17, 2008Inventors: DAVID W. OLD, VINH X. NGO
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Patent number: 7319150Abstract: The invention concerns a method for synthesizing styryl isoxazole, styryl pyrazole and styryl isothazole derivatives in a synthesis step followed by a recrystallization in a basic alcohol medium.Type: GrantFiled: July 24, 2003Date of Patent: January 15, 2008Assignees: Laboratoires Mayoly Spindler, Centre National De La Recherche Scientifique, Universite De Montpellier 2Inventors: Damien Gloux, Marc Criton, Jean-Louis Montero
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Patent number: 7309714Abstract: The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 26, 2003Date of Patent: December 18, 2007Assignee: Merck & Co., Inc.Inventors: Joseph L. Duffy, Robert J. Mathvink, Ann E. Weber, Jinyou Xu
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Publication number: 20070281981Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 11, 2007Publication date: December 6, 2007Inventors: DAVID W. OLD, Danny T. Dinh
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Patent number: 7294718Abstract: Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. 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, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.Type: GrantFiled: December 9, 2004Date of Patent: November 13, 2007Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Joseph Cherian
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Patent number: 7285670Abstract: A useful and efficient method of preparing an alkylated thiazoline carboxylic acid, or a derivative thereof, comprises coupling a substituted aryl nitrile such as, for example, 2,4-dimethoxybenzonitrile or 4-methoxybenzonitrile, with a cysteine ester to form a substituted thiazoline carboxylic acid ester; optionally hydrolyzing the substituted thiazoline carboxylic acid ester to form a substituted thiazoline carboxylic acid; optionally, protecting the carboxyl group; alkylating the thiazoline ring at the 4-carbon position, as indicated in Structural Formula (I), with a compound of the formula R1-L, wherein R1 is as defined above and L is a leaving group, in the presence of a phase transfer catalyst; and, optionally, deprotecting the carboxyl group. In one embodiment of the present invention, a cinchona-alkaloid derived phase transfer catalyst is used to alkylate a protected substituted thiazoline carboxylic acid.Type: GrantFiled: October 3, 2005Date of Patent: October 23, 2007Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Rayomand H. Gimi, Peter D. McDonnell, Paul Wolstenholme-Hogg
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Patent number: 7262183Abstract: This invention relates to substituted 5-membered N-Herterocyclic neurotrophic compounds of formula (I) or pharmaceutically acceptable salts or hydrates thereof, wherein R1, R2, R3, R4, V, W, X, Y, and Z are as defined in the description; their preparation methods, compositions comprising the same, and their use as inhibitors of FK560 binding proteases (FKBPs) activity for treating and preventing neurodegenerative diseases and other nerve disorders associated with nerve injuries or other related diseases.Type: GrantFiled: December 5, 2002Date of Patent: August 28, 2007Assignees: Instititute of Pharmacology and Toxicology, Academy of Military Medical Sciences P.L.A.Inventors: Song Li, Liqin Zhao, Lili Wang, Beifen Shen, Liuhong Yun
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Patent number: 7256211Abstract: The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EP4 agonistic action and thus are considered useful for the prevention and/or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc.Type: GrantFiled: January 20, 2004Date of Patent: August 14, 2007Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Tohru Kambe, Toru Maruyama, Kaoru Kobayashi, Kousuke Tani, Yoshihiko Nakai, Toshihiko Nagase, Takayuki Maruyama, Kiyoto Sakata, Hideyuki Yoshida, Shinsei Fujimura, Akio Nishiura, Nobutaka Abe
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Patent number: 7244754Abstract: The invention relates to the compounds (2R,4R), (2S,4R)-2-methylthiazolidine-2,4-dicarboxylic acid and (2RS,4R)-2-methylthiazolidine-2,4-dicarboxylic acid and salts of said compounds, the use thereof for the prophylaxis and/or treatment of neurodegenerative diseases, methods for the prophylaxis and/or treatment of neurodegenerative diseases, and pharmaceutical compositions containing said compounds together with physiologically compatible carriers, auxiliary agents, and/or solvents.Type: GrantFiled: April 21, 2006Date of Patent: July 17, 2007Inventor: Rudy Susilo
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Patent number: 7241900Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.Type: GrantFiled: November 23, 2005Date of Patent: July 10, 2007Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Pawel K. Grzywacz, Rafal R. Sicinski
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Patent number: 7230021Abstract: The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A—B, K, Q, X, Y, Z, R and R1 are as defined in Claim 1.Type: GrantFiled: March 13, 2003Date of Patent: June 12, 2007Assignee: The Texas A&M University SystemInventors: Daniel Romo, Jun Liu, Nam Song Choi, Zonggao Shi
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Patent number: 7163952Abstract: The present invention relates to an azole compound represented by the formula [I] wherein W is S or O; R is —COOR7, —X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is —(CH2)m—X— (X is —N(R8)—, —C(R9)(R10)—, —CO— or —CO—N(R8)—); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is —(Y)s1-(A2)s-Z (Y is —O—, —S(O)t—, —N(R13)—, —N(R14)—CO—, —N(R14)—SO2—, —SO2—N(R14)— and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.Type: GrantFiled: December 3, 2002Date of Patent: January 16, 2007Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Tomoyuki Ikemoto, Shohei Sakata, Hiroshi Maegawa, Atsunori Kashiwagi
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Patent number: 7126004Abstract: The present invention relates to novel thiazoline acids and derivatives thereof useful as chelators of trivalent metals in therapeutic applications. For example, the thiazoline acid derivatives are useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.Type: GrantFiled: September 17, 2004Date of Patent: October 24, 2006Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 7119208Abstract: Compounds for the treatment of sickle-cell disease, and methods for their use are provided. The compounds have a dual mode of action. First, binding of the compounds to hemoglobin increases the oxygen affinity of both normal and sickle hemoglobin. Secondly, binding of these compounds to the N-terminal amino acid of sickle hemoglobin results in destabilization of potential contacts between sickle hemoglobin molecules, preventing polymerization and the formation of fibrous precipitates of the sickle hemoglobin. The compounds are also useful for inducing hypoxia, e.g. to augment cancer treatments.Type: GrantFiled: March 14, 2005Date of Patent: October 10, 2006Assignee: Virginia Commonwealth UniversityInventors: Martin K. Safo, Richmond Danso-Danquah, Gajanan S. Joshi, Donald J. Abraham
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Patent number: 7105551Abstract: The present invention provides compounds of formula (I).Type: GrantFiled: December 19, 2001Date of Patent: September 12, 2006Assignee: SmithKline Beecham CorporationInventors: Rodolfo Cadilla, Romain Luc Marie Gosmini, Millard Hurst Lambert, III, Michael Lawrence Sierra
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Patent number: 7101901Abstract: The invention relates to the compounds (2R,4R), (2S,4R)-2-methylthiazolidine-2,4-dicarboxylic acid and (2RS,4R)-2-methylthiazolidine-2,4-dicarboxylic acid and salts of said compounds, the use thereof for the prophylaxis and/or treatment of neurodegenerative diseases, methods for the prophylaxis and/or treatment of neurodegenerative diseases, and pharmaceutical compositions containing said compounds together with physiologically compatible carriers, auxiliary agents, and/or solvents.Type: GrantFiled: February 24, 2003Date of Patent: September 5, 2006Inventor: Rudy Susilo
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Patent number: 7081537Abstract: A process for preparing ?-functionalized thiazolidines or oxazolidines, each of which are oxycarbonyl-functionalized in the 4-position, by adding a base to a reaction mixture comprising an oxycarbonyl-functionalized thiazolidine or oxazolidine and an electrophile at a temperature of greater than ?40° C.Type: GrantFiled: February 24, 2004Date of Patent: July 25, 2006Assignee: Consortium für elektrochemische Industrie GmbHInventors: Dieter Heldmann, Jürgen Stohrer
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Patent number: 6987104Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: January 17, 2006Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 6987120Abstract: Compounds of their salts having general formulas (I) and (II) wherein: s=is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.Type: GrantFiled: April 11, 2000Date of Patent: January 17, 2006Assignee: Nicox, S.A.Inventor: Piero Del Soldato
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Patent number: 6982335Abstract: A useful and efficient method of preparing an alkylated thiazoline carboxylic acid, or a derivative thereof, comprises coupling a substituted aryl nitrile such as, for example, 2,4-dimethoxybenzonitrile or 4-methoxybenzonitrile, with a cysteine ester to form a substituted thiazoline carboxylic acid ester; optionally hydrolyzing the substituted thiazoline carboxylic acid ester to form a substituted thiazoline carboxylic acid; optionally, protecting the carboxyl group; alkylating the thiazoline ring at the 4-carbon position, as indicated in Structural Formula (I), with a compound of the formula R1-L, wherein R1 is as defined above and L is a leaving group, in the presence of a phase transfer catalyst; and, optionally, deprotecting the carboxyl group. In one embodiment of the present invention, a cinchona-alkaloid derived phase transfer catalyst is used to alkylate a protected substituted thiazoline carboxylic acid.Type: GrantFiled: May 15, 2003Date of Patent: January 3, 2006Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Rayomand H. Gimi, Peter D. McDonnell, Paul Wolstenholme-Hogg
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Patent number: 6949543Abstract: The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.Type: GrantFiled: November 8, 2001Date of Patent: September 27, 2005Assignees: Yamanouchi Pharmaceutical Co., Ltd., Rational Drug Design LaboratoriesInventors: Toru Kontani, Junji Miyata, Wataru Hamaguchi, Yoji Miyazaki, Hiroshi Suzuki, Eiichi Nakai, Shunji Kageyama
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Patent number: 6916834Abstract: Preparation, use, and structure of endogenous Ah receptor ligand is disclosed.Type: GrantFiled: February 12, 2002Date of Patent: July 12, 2005Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Jiasheng Song, Margaret Clagett-Dame, Richard E. Peterson, William M. Westler, Rafal R. Sicinski
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Patent number: 6903220Abstract: 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 reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). 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: GrantFiled: May 15, 2003Date of Patent: June 7, 2005Assignee: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda
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Patent number: 6903119Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: July 13, 1999Date of Patent: June 7, 2005Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: RE39132Abstract: Phenyl- and pyridyl-substituted thiazoline acid derivatives useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.Type: GrantFiled: October 17, 2001Date of Patent: June 13, 2006Assignee: University of Florida, Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.