Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Patent number: 7407976Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: November 15, 2004Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark T. Miller, Sarah S. Hadida Ruah, Peter D. J. Grootenhuis, Matthew Hamilton
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Publication number: 20080145335Abstract: Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.Type: ApplicationFiled: November 20, 2007Publication date: June 19, 2008Applicant: Neuren Pharmaceuticals LimitedInventors: Margaret Anne Brimble, Paul William Richard Harris, Frank Sieg
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Patent number: 7388017Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.Type: GrantFiled: June 27, 2003Date of Patent: June 17, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D Tung, Scott L Harbeson, David D Deininger, Mark A Murcko, Govinda R Bhisetti, Luc J Farmer
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Publication number: 20080139547Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: February 7, 2008Publication date: June 12, 2008Applicant: PHARMACYCLICS, INC.Inventor: Martin SENDZIK
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Patent number: 7378397Abstract: Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) are of formula Ia: wherein: R1 is an optionally substituted 4-, 5- or 6-membered heterocyclic ring having one or more heteroatoms, in which at least one carbon atom of the ring is substituted with O or S; X1 is —CO— or —CS— or —CH2CO— or CH(R4) wherein R4 is H or optionally substituted alkyl or —COOH or —COOR11 wherein R11 is optionally substituted alkyl; X2 and X3 (which may be the same or different) are —CO— or —CS—; Z is —CH2— or —S— or —O— or —NH—; Q is O or S; R2 is H or optionally substituted alkyl or an optionally substituted carbocyclic ring; R3 is H or optionally substituted alkyl or an optionally substituted mono- or polycyclic ring, optionally having one or more heteroatoms in the ring(s) and optionally being a fused ring; or R2 and R3 together form an optionally substituted mono- or polycyclic ring optionally having one or more heteroatoms in the ring(s) and optionally being aType: GrantFiled: February 1, 2006Date of Patent: May 27, 2008Assignee: The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth Near DublinInventor: Julie A. Kelly
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Publication number: 20080119476Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: July 1, 2005Publication date: May 22, 2008Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Patent number: 7371777Abstract: The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRx1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.Type: GrantFiled: August 16, 2002Date of Patent: May 13, 2008Assignee: Eisai Co., Ltd.Inventors: Richard Clark, Fumiyoshi Matsuura, Eita Emori, Masanobu Shinoda, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
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Publication number: 20080108820Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.Type: ApplicationFiled: September 22, 2004Publication date: May 8, 2008Inventors: Silvio A. Campagna, Francis G. Fang, James J. Kowalczyk, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
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Patent number: 7368576Abstract: The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of metastasis and tumor colonization.Type: GrantFiled: July 5, 2006Date of Patent: May 6, 2008Assignee: Probiodrug AGInventors: Stephan von Hoersten, Hans-Ulrich Demuth, Torsten Hoffmann
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Publication number: 20080085924Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: December 1, 2003Publication date: April 10, 2008Applicant: BAYER CROPSCINCE AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Losel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jorg Nico Greul
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Patent number: 7348346Abstract: The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: GrantFiled: March 8, 2005Date of Patent: March 25, 2008Assignee: Abbott LaboratoriesInventors: Irini Akritopoulou-Zanze, Daria Darczak, Jürgen Dinges, Stevan W. Djuric, Ethan D. Hoff, Hana A. Kopecka, Jyoti R. Patel, Zhonghua Pei, Qi Shuai, Kathy Sarris, Hing L. Sham, Paul E. Wiedeman
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Patent number: 7345043Abstract: Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC.Type: GrantFiled: April 1, 2005Date of Patent: March 18, 2008Assignee: Miikana TherapeuticsInventors: Sampath K. Anandan, Xiao-Yi Xiao, Dinesh V. Patel, John Ward
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Patent number: 7345180Abstract: A dipeptidyl peptidase IV inhibitor which is satisfactory in respect of activity, stability and safety and has an excellent action as a pharmaceutical agent. A compound represented by the following general formula or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each represents hydrogen, an optionally substituted C1-6 alkyl group, or —COOR5 whereupon R5 represents hydrogen or an optionally substituted C1-6 alkyl group, or R1, R2, and a carbon atom together represent a 3- to 6-membered cycloalkyl group, R3 represents hydrogen or an optionally substituted C6-10 aryl group, R4represents a hydrogen or a cyano group, D represents —CONR6-, —CO— or —NR6CO—, R6 represents hydrogen or an optionally substituted C1-6 alkyl group, E represents —(CH2)m— whereupon m is 1 to 3, —CH2OCH2—, or —SCH2—, n is 0 to 3, and A represents an optionally substituted bicyclic heterocyclic group or bicyclic hydrocarbon group.Type: GrantFiled: January 30, 2004Date of Patent: March 18, 2008Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Takuji Kakigami, Mitsuru Oka, Noriyasu Katoh, Masahiro Yoshida, Masahiro Shirai, Toru Murase, Masao Sakairi, Takayo Murase, Mitsuaki Takeuchi, Yuji Hayashi, Motohiro Takeda, Mitsuhiro Makino
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Publication number: 20080064679Abstract: Water-soluble cannabinoid compounds that are agonists of CB1 and CB2 cannabinoid receptors are provided. The compounds are made water-soluble by derivatization of the alkyl side chain and/or the phenolic hydroxyl group of tetrahydrocannabinol. The water-soluble cannabinoids are useful for the treatment of appetite loss, pain, multiple sclerosis, nausea and vomiting, and epilepsy.Type: ApplicationFiled: June 23, 2005Publication date: March 13, 2008Inventors: Billy R. Martin, Raj K. Razdan, Anu Mahadevan
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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: 20080058389Abstract: The invention relates to novel carboxamides of formula (I), in which M represents a phenyl ring, pyridine ring or pyrimidine, pyridazine or pyrazine ring, respectively monosubstituted by R8, or represents a thiazole ring substituted by R8-A; R8 represents hydrogen, fluorine, chlorine, methyl, isopropyl, methylthio or trifluoromethyl; R8 can also represent methoxy; R8-A represents hydrogen, methyl, methylthio or trifluoromethyl; L1 represents C1-C10 alkene (alkanediyl); Q represents O, S, SO, SO2 or NR9; L2 represents a direct bond, SiR10R11 or CO; R represents hydrogen, C1-C8 alkyl, C1-C8 alkoxy, C1-C4 alkoxy-C1-C4-alkyl, C1-C4 alkylthio-C1-C4-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C6 haloalkyl, C2-C6-haloalkenyl, C2-C6 haloalkynyl or C3-C6 cycloalkyl; A represents the group of formula (AI); the remaining substituents are defined in claim 1.Type: ApplicationFiled: January 22, 2005Publication date: March 6, 2008Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Benoit Hartmann, Jorg Nico Greul, Stefan Herrmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Patent number: 7335645Abstract: The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain; B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine.Type: GrantFiled: March 1, 2005Date of Patent: February 26, 2008Assignee: Probiodrug AGInventors: Hans-Ulrich Demuth, Torsten Hoffmann, Dagmar Schlenzig, Ulrich Heiser
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Patent number: 7332513Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: GrantFiled: November 4, 2005Date of Patent: February 19, 2008Assignee: Renopharm Ltd.Inventors: Peter Assaf, Elham Gazaleen-Mariee, Michael Naveh
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Patent number: 7332487Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, —Alk—CO—, —COCH2—, —Alk—O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, —Alk—CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 15, 2006Date of Patent: February 19, 2008Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 7307093Abstract: Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.Type: GrantFiled: November 18, 2004Date of Patent: December 11, 2007Assignees: The University of Tennessee Research Foundation, Ohio State University Research FoundationInventors: Duane D. Miller, Veeresa Gududuru, James T. Dalton, Eunju Hurh
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Patent number: 7294642Abstract: 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: GrantFiled: September 8, 2003Date of Patent: November 13, 2007Assignee: Elan Pharmaceuticals, Inc.Inventors: Yvette M. Fobian, John N. Freskos, Barbara Jagodzinska
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Publication number: 20070249608Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: April 18, 2007Publication date: October 25, 2007Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Patent number: 7285554Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substiType: GrantFiled: April 7, 2006Date of Patent: October 23, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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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: 7273866Abstract: Novel 2-arylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders that are responsive to the opening of the KCNQ potassium channels, including pain and migraineType: GrantFiled: December 9, 2003Date of Patent: September 25, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Yong-Jin Wu, Jason M. Guernon
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Patent number: 7273863Abstract: The present invention includes benzophenone compounds (I) which are useful in the treatment of HIV infections.Type: GrantFiled: August 31, 2000Date of Patent: September 25, 2007Assignee: SmithKline Beecham CorporationInventors: Clarence Webster Andrews, III, Joseph Howing Chan, George Andrew Freeman, Karen Rene Romines, Jeffrey H. Tidwell, Pascal Maurice Charles Pianetti
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7247635Abstract: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4?CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more sType: GrantFiled: June 17, 2005Date of Patent: July 24, 2007Assignee: Astellas Pharma Inc.Inventors: Hirokazu Kubota, Yasuhiro Yonetoku, Keizo Sugasawa, Masashi Funatsu, Souichirou Kawazoe, Akira Toyoshima, Yoshinori Okamoto, Jun Ishikawa, Makoto Takeuchi
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Publication number: 20070167622Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: January 8, 2007Publication date: July 19, 2007Inventors: Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Kang Le, Qiang Zhang
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Patent number: 7244849Abstract: A method of preparing a compound of formula (I), and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: May 29, 2002Date of Patent: July 17, 2007Assignee: Glaxo Group LimitedInventors: Thierry Boyer, Caroline Jane Day, Andrew Jonathan Whitehead, Richard Anthony Henson
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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: 7232838Abstract: This invention concerns the use of a compound of formula (I?), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(?O)2—; mono- or di(C1-6alkyl)aminoS(?O)2; —C(?N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally subsType: GrantFiled: August 9, 2002Date of Patent: June 19, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Christopher John Love, Guy Rosalia Eugeen Van Lommen, Julien Georges Pierre-Olivier Doyon, Jean-Pierre André Marc Bongartz, Marcel Jozef Maria Van der AA, Robert Jozef Maria Hendrickx, Peter Jacobus Johannes Antonius Buijnsters, Ludwig Paul Cooymans, Nele Vandermaesen, Erwin Coesemans, Gustaaf Maria Boeckx
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Patent number: 7208528Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: September 15, 1999Date of Patent: April 24, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7196108Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.Type: GrantFiled: March 6, 2003Date of Patent: March 27, 2007Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
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Patent number: 7196201Abstract: The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utilityType: GrantFiled: June 26, 2002Date of Patent: March 27, 2007Assignee: SmithKline Beecham CorporationInventors: Curt Dale Haffner, Darryl Lynn McDougald, Amarjit Sab Randhawa, Steven Michael Reister, David N Deaton
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Patent number: 7186735Abstract: The present invention relates to acylated arylcycloalkylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: August 7, 2003Date of Patent: March 6, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart, Peter Below
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Patent number: 7179819Abstract: Compounds that selectively inhibit the binding of ligands to ?4?1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.Type: GrantFiled: February 26, 2004Date of Patent: February 20, 2007Assignees: Daiichi Pharmaceutical Co., Ltd., Pharmacopeia Drug Discovery, Inc.Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Iimura Shin, Yoshiyuki Yoneda
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Patent number: 7169932Abstract: Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: December 4, 2003Date of Patent: January 30, 2007Assignee: Pfizer Inc.Inventors: David John Kucera, Robert William Scott
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Patent number: 7166590Abstract: A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.; R3 is (substituted) alkyl, carbocyclic ring, hetero ring; J is O, NR16 (R16 is H, substituted alkyl); R4 is (substituted) alkyl, carbocyclic ring, hetero ring.] or non-toxic salt thereof, and an N-type calcium channel blocker comprising it as an active ingredient. The compounds of the formula (I) possess an inhibitory action on N-type calcium channel, so they are useful as agent for the prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis or epilepsy etc. or agent for the treatment of pain.Type: GrantFiled: May 28, 2002Date of Patent: January 23, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7160923Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: November 14, 2000Date of Patent: January 9, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7157490Abstract: 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 3, 2003Date of Patent: January 2, 2007Assignee: Merck & Co., Inc.Inventors: Vincent J. Colandrea, Scott D. Edmondson, Robert J. Mathvink, Anthony Mastracchio, Ann E. Weber, Jinyou Xu
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Patent number: 7157479Abstract: A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof Wherein X1 represents O or S; R1 and R2 are independently H or C1-3 alkyl or R1 and R2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3–5 membered cycloalkyl ring; R3 and R4 independently represent H, halogen, —CH3 and —OCH3; R5 represents H or C1-6 alkyl X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, CF3, C1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R6 is pyridyl, the N is unsubstituted.Type: GrantFiled: May 29, 2002Date of Patent: January 2, 2007Assignee: Glaxo Group LimitedInventor: Francoise Jeanne Gellibert
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Patent number: 7148219Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: April 29, 2005Date of Patent: December 12, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 7148242Abstract: N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl]-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes or imidazacyclo4-7alkanes have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections.Type: GrantFiled: June 14, 2002Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Jeffrey Jacobs, Rakesh K. Jain, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 7144885Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disordersType: GrantFiled: February 21, 2003Date of Patent: December 5, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips, Scott M. Wilhelm, Qian Zhao
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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: 7125442Abstract: A lightfast additive and an ink composition including the same include a benzophenone moiety for lightfastness and a moiety for wettability and the ability to stabilize a colorant, wherein the two moieties are covalently bonded. The lightfast additive may exhibit effective ultraviolet (UV) light absorption capacity, effective wettability, and an ability to stabilize a colorant. The ink composition utilizing the light fast additive thus has an improved lightfastness and long-term storage stability.Type: GrantFiled: May 24, 2004Date of Patent: October 24, 2006Assignee: Samsung Electronics Co., Ltd.Inventors: Kyung-hoon Lee, Seung-min Ryu, Yeon-kyoung Jung
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Patent number: 7109347Abstract: The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more preferred embodiment, the compounds of the present invention are useful for the treatment of metastasis and tumor colonization.Type: GrantFiled: March 30, 2005Date of Patent: September 19, 2006Assignee: Probiodrug AGInventors: Stephan von Hoersten, Hans-Ulrich Demuth, Torsten Hoffmann
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura