Title:
膵臓リパーゼ阻害化合物、その合成および使用
Document Type and Number:
Japanese Patent JP4668536
Kind Code:
B2
Abstract:
The subject invention features compounds having the structure: wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1-C15 alkyl, C1-C8 alkylaryl, -C(O)OR4, -C(O)NR4R5, -CR6R6'OR4, -CR6R6'OC(O)R4, -CR6R6'OC(O)NHR7, -C(O)NR10R11, -C(O)NR8R9NR8R9, -N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1-C30 alkyl or branched C3-C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, -CH2-aryl, aryl -C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6' are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
Inventors:
Witter, David
Castel Hano, Erlind El
Castel Hano, Erlind El
Application Number:
JP2003554660A
Publication Date:
April 13, 2011
Filing Date:
December 20, 2002
Export Citation:
Assignee:
OSI Pharmaceuticals Incorporated
International Classes:
C07D498/04; A61K31/519; A61K31/5365; A61K31/542; A61P3/04; A61P3/06; A61P3/10; A61P43/00; C07B61/00; C07D333/38; C07D333/40; C07D409/12; C07D495/04; C07D498/02; C07D513/02; C07D513/04
Domestic Patent References:
| JP62114989A | ||||
| JP62132884A | ||||
| JP59219288A | ||||
| JP57072979A | ||||
| JP2005527469A |
Foreign References:
| WO1997048707A1 | ||||
| WO1998045298A1 | ||||
| US4159377 | ||||
| WO2001018181A1 | ||||
| WO2000040247A1 | ||||
| WO2000040569A1 | ||||
| WO2001053278A1 |
Other References:
Journal of Medicinal Chemistry,1998年,vol.41, No.10,1729-1740
Tetrahedron,1998年,54,10789-10800
Journal of Medicinal Chemistry,1999年,42(26),5437-5447
Tetrahedron,1998年,54,10789-10800
Journal of Medicinal Chemistry,1999年,42(26),5437-5447
Attorney, Agent or Firm:
Satoshi Kono
Makoto Nakamura
Kurata Masatoshi
Takashi Mine
Yoshihiro Fukuhara
Sadao Muramatsu
Ryo Hashimoto
Makoto Nakamura
Kurata Masatoshi
Takashi Mine
Yoshihiro Fukuhara
Sadao Muramatsu
Ryo Hashimoto