Publication number: 20040097563
Abstract: 4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy, amino, carboxy, etc.; R6 is hydrogen, carbamoyl, cyano, carboxy, C1-6 alkoxycarbonyl, etc. and R7 is amino or C1-6 alkanoylamino. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and the like.
Type:
Application
Filed:
November 3, 2003
Publication date:
May 20, 2004
Inventors:
Toshiki Murata, Sachiko Sasaki, Takashi Yoshino, Yuka Ikegami, Tsutomu Masuda, Mitsuyuki Shimada, Takuya Shintani, Makoto Shimazaki, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Masaomi Umeda, Hiroshi Komura, Nagahiro Yoshida
Patent number: 6638940
Abstract: Compounds of formula
are described, wherein R1 and R2 are for example, independently of each other, halogen, C1-C6-alkyl, C3-C6-cycloalkyl, halogen-C1-C6-alkyl, halogen-C3-C6-cycloalkyl, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl and halogen-C2-C4-alkinyl;
R3 is hydrogen, OH, halogen, C1-C6-alkoxy, or —O—C(═O)—C1-C6-alkyl;
R4 is for example phenyl, benzyl, phenoxy or benzyloxy, which is substituted by substituents selected from the group consisting of halogen, cyano, NO2, C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cyclalkyl-C1-C6-alkyl, halogen-C1-C6-alkyl, C1-C6-alkoxy, C3-C8-cycloalkoxy, C3-C8-cycloalkoxy-C1-C6-alkyl, C3-C8-cycloalkoxy-C1-C6-alkoxy, halogen-C1-C6-alkoxy, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl, halogen-C2-C4-alkinyl, C2-C6-alkenyloxy, C2-C6-alkinyloxy, halogen-C2-C6-alkenyloxy, halogen-C2-C6-alkenyloxy, —NR6—C(═O)—O—C1-C6-alkyl, —NR6—C(═O)—O-halogen-C1-C6-alkyl, —C(R7)═N&
Type:
Grant
Filed:
February 25, 2002
Date of Patent:
October 28, 2003
Assignee:
Syngenta Crop Protection, Inc.
Inventor:
Stephan Trah
Patent number: 6638962
Abstract: Compound of formula (I):
wherein:
X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—,
Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted,
R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted,
or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle,
T represents —CH(R5)—, —N(R5)— or —N(R5)CO—,
V represents hydrogen or unsubstituted or substituted aryl or heteroaryl,
A2 represents [C(R6)(R′6)]p,
R7 and R8 are as defined in the description,
their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing t
Type:
Grant
Filed:
January 16, 2002
Date of Patent:
October 28, 2003
Assignee:
Les Laboratoires Servier
Inventors:
Patrick Casara, Thierry Le Diguarher, Gilbert Dorey, John Hickman, Alain Pierre, Gordon Tucker, Nicolas Guilbaud
Patent number: 6624179
Abstract: A geometrical isomer of an acrylonitrile compound represented by the formula (I) or of its salt, or a mixture thereof:
[wherein T is phenyl or pyridyl, which is substituted by R2, Q is phenyl, thienyl, pyridyl or benzyl, which may be substituted by R3, R1 is —C(═O)R4 or —C(═S)R4, R4 is alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, cycloalkyl, cycloalkyloxy, cycloalkylthio, —N(R5)R6, phenyl, phenoxy, phenylthio, benzyl, benzyloxy, benzylthio, —J, —O—J or —S—J], wherein the geometrical isomer has a longer retention time when analyzed by reversed phase liquid chromatography in which a packing comprising silica having chemically bonded thereto an alkyl group selected from trimethyl, octyl and octadecyl, is used as the stationary phase, and a polar solvent selected from water, methanol and acetonitrile, is used as the mobile phase, and the geometrical isomer mixture contains such ge
Type:
Grant
Filed:
January 24, 2002
Date of Patent:
September 23, 2003
Assignee:
Ishihara Sangyo Kaisha Ltd.
Inventors:
Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Tsuyoshi Ueda, Akihiro Hisamatsu, Mayumi Kanamori
Publication number: 20030153596
Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.
Type:
Application
Filed:
July 9, 2002
Publication date:
August 14, 2003
Inventors:
Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
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