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    • 26. 发明申请
    • PYRAZOLO [1, 5-A] PYRIMIDINE COMPOUNDS AS CB1 RECEPTOR ANTAGONIST
    • PYRAZOLO [1,5-A]吡嗪类化合物作为CB1受体拮抗剂
    • WO2008004698A3
    • 2008-03-20
    • PCT/JP2007063762
    • 2007-07-04
    • MITSUBISHI TANABE PHARMA CORPTANIMOTO KOICHIOI MARIKOTSUBOI YASUNORIMORITANI YASUNORI
    • TANIMOTO KOICHIOI MARIKOTSUBOI YASUNORIMORITANI YASUNORI
    • C07D487/04A61K31/519A61P25/00
    • C07D487/04
    • The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R 1 and R 2 are the same or different and each an optionally substituted aryl group etc, R 0 is hydrogen atom, an alkyl group etc, E is a group of the formula: -C(=O)- or -SO 2 -, R is a group of the following formula [i], [ii] or [iii] etc: Ring A is (a) a C 3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R 3 is an alkyl group optionally substituted by an alkylthio group, R 4 is hydrogen atom, an alkyl group etc, one of R A and R B is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.
    • 本发明提供具有下式[I]的具有CB1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物:其中R 1和R 2, SUP>相同或不同,各自为任选取代的芳基等,R 0为氢原子,烷基等,E为下式基团-C(= O) - 或 -SO 2 - ,R是下式[i],[ii]或[iii]等的基团:环A是(a)C 3-8 任选地与苯环稠合的环烷基或(b)苯环,Q是单键或亚甲基,环B是4-至7-元脂族杂环基,所述环状基团通过其环碳结合 原子与相邻的氮原子,X是硫原子等,R 3是任选被烷硫基取代的烷基,R 4是氢原子,烷基等 R A和R B之一是烷基等,另一个是氢原子,烷基等或药物 其可接受的盐。
    • 27. 发明专利
    • COMPUESTOS DE IMIDAZOLIN-2-ONA.
    • ES2362877T3
    • 2011-07-14
    • ES04728708
    • 2004-04-21
    • MITSUBISHI TANABE PHARMA CORPMITSUBISHI TANABE PHARMA CORP
    • KUBO AKIRAIMASHIRO RITSUOOGASAWARA AKIHITONAKAJIMA TATSUONAKANE TETSUMIYOSHI HIDETAKA
    • C07D401/04A61K31/4439A61K31/506A61P3/10A61P7/02A61P9/10A61P19/00A61P25/16A61P25/28A61P29/00A61P37/06C07D401/14C07D403/04C07D403/14C07D405/14C07D409/14
    • Un compuesto seleccionado entre los compuestos base libre de estructuras 399 a 478, o una de sus sales farmacéuticamente aceptables. 399 Etilo 1,1-Dioxotetrahidrotiofen-3-ilamino 400 Etilo trans-4-(Metilcarbamoil)ciclohexilamino 401 Etilo 1,5-Dimetil-5-hidroxihexilamino 402 Isopropilo 1,5-Dimetil-5-hidroxihexilamino 403 Etilo cis-4-Hidroxi-4-metilciclohexilamino 404 Isopropilo trans-4-Hidroxi-4-metilciclohexilamino 405 Isopropilo trans-4-(1-Hidroxi-1-metiletil)ciclohexilamino 406 Etilo trans-4-Hidroxi-4-metilciclohexilamino 407 Isopropilo cis-4-Hidroxi-4-metilciclohexilamino 408 Etilo trans-4-(1-Hidroxi-1-metiletil)ciclohexilamino 409 Etilo (S)-1,2-Dimetil-2-hidroxipropilamino 410 Isopropilo (S)-1,2-Dimetil-2-hidroxipropilamino 411 Etilo 1,3-Dimetil-3-hidroxibutilamino 412 Isopropilo 1,3-Dimetil-3-hidroxibutilamino 413 Isopropilo 2-Mercapto-2-metilpropilamino 414 Isopropilo 1,1-Bishidroximetilpropilamino 415 Isopropilo 2-Hidroxi-2-metilpropilamino 416 Etilo 4-Piperidilamino 417 1,2-Dimetil-2-hidroxipropilo Isopropilamino 418 1,2-Dimetil-2-hidroxipropilo cis-4-Hidroxi-4-metilciclohexilamino 419 1,2-Dimetil-2-hidroxipropilo (S)-1,2-Dimetil-2-hidroxipropilamino 420 1,2-Dimetil-2-hidroxipropilo Trans-4-Hidroxi-4-metilciclohexilamino 421 2-Hidroxi-1,1,2-trimetilpropilo Isopropilamino 422 2-Hidroxi-1,1,2-trimetilpropilo Trans-4-Hidroxi-4-metilciclohexilamino 423 3-Hidroxi-3-metilbutilo Isopropilamino 424 3-Hidroxi-3-metilbutilo 1,1-Dimetil-2-hidroxietilamino 425 3-Hidroxi-3-metilbutilo 2,2-Dimetil-3-hidroxipropilamino 426 3-Hidroxi-3-metilbutilo 1-Hidroximetilciclopentilamino 427 3-Hidroxi-3-metilbutilo trans-4-Hidroxi-4-metilciclohexilamino 428 3-Hidroxi-3-metilbutilo 4-Tetrahidropiranilamino 429 3-Hidroxi-3-metilbutilo (R)-1,2-Dimetil-2-hidroxipropilamino 430 3-Hidroxi-3-metilbutilo (S)-1,2-Dimetil-2-hidroxipropilamino 431 3-Hidroxi-3-metilbutilo trans-4-Hidroxiciclohexilamino 432 3-Hidroxi-3-metilbutilo 1-Metanosulfonilpiperidin-4-ilamino 433 3-Hidroxi-3-metilbutilo 1-Etanosulfonilpiperidin-4-ilamino 434 4-Tetrahidropiranilo Isobutilamino 435 4-Tetrahidropiranilo Isopropilamino 436 4-Tetrahidropiranilo trans-4-Hidroxi-4-metilciclohexilamino 437 4-Tetrahidropiranilo Ciclopropilamino 438 4-Tetrahidropiranilo 2,2-Dimetilpropilamino 439 1-Acetilpiperidin-4-ilo trans-4-Hidroxi-4-metilciclohexilamino 440 1-Acetilpiperidin-4-ilo 2,2-Dimetilpropilamino 441 1-Acetilpiperidin-4-ilo Isopropilamino 442 1-Acetilpiperidin-4-ilo Isobutilamino 443 1-Acetilpiperidin-4-ilo Ciclopropilamino 444 4-Tetrahidropiranil (R)-1,2-Dimetil-2-hidroxipropilamino 445 4-Tetrahidropiranil (S)-1,2-Dimetil-2-hidroxipropilamino 446 4-Tetrahidropiranilo (S)-2-Hidroxi-1-metiletilamino 447 4-Tetrahidropiranilo (S)-1-Hidroximetilpropilamino 448 4-Tetrahidropiranilo 1,1-Dimetil-2-hidroxietilamino 449 4-Tetrahidropiranilo 4-Tetrahidropiranilamino 450 1-Acetilpiperidin-4-ilo 1,1-Dimetil-2-hidroxietilamino 451 1-Acetilpiperidin-4-ilo 4-Tetrahidropiranilamino 452 1-Acetilpiperidin-4-ilo (S)-1-Hidroximetilpropilamino 453 1-Acetilpiperidin-4-ilo (S)-1,2-Dimetil-2-hidroxipropilamino 454 4-Tetrahidropiranilo trans-4-Hidroxiciclohexilamino 455 1-Acetilpiperidin-4-ilo trans-4-Hidroxiciclohexilamino 456 1-Metanosulfonilpiperidin-4-ilo trans-4-Hidroxiciclohexilamino 457 1-Metanosulfonilpiperidin-4-ilo trans-4-Hidroxi-4-metilciclohexilamino 458 1-Metanosulfonilpiperidin-4-ilo Isopropilamino 459 4-Tetrahidropiranilo 1-Metanosulfonilpiperidin-4-ilamino 460 1-Acetilpiperidin-4-ilo 1-Metanosulfonilpiperidin -4-ilamino 461 Isopropilo 1-Acetilpiperidin-4-ilamino 462 Isopropilo 1-Metanosulfonilpiperidin-4-ilamino 463 Isopropilo 1-(Isopropilosulfonil)piperidin-4-ilamino 464 Isopropilo 1-(Propilsulfonil)piperidin-4-ilamino 465 Isopropilo 1-(Butilsulfonil)piperidin-4-ilamino 466 Isopropilo 1-(Isobutiloxicarbonil)piperidin-4-ilamino 467 Isopropilo 1-butirilpiperidin-4-ilamino 468 Etilo 1-Acetilpiperidin-4-ilamino 469 Etilo 1-Metanosulfonilpiperidin-4-ilamino 470 Etilo 1-Etanosulfonilpiperidin-4-ilamino 471 Isopropilo 1-Etilcarbamoilpiperidin-4-ilamino 472 Isopropilo 1-Propilcarbamoilpiperidin-4-ilamino 473 Isopropilo 1-Isopropilcarbamoilpiperidin-4-ilamino 474 Isopropilo 1-Etanosulfonilpiperidin-4-ilamino 475 Isopropilo 1-Metoxicarbonilpiperidin-4-ilamino 476 Isopropilo 1-Etoxicarbonilpiperidin-4-ilamino 477 1-Metanosulfonilpiperidin-4-ilo Isopropilamino 478 1-Etanosulfonilpiperidin-4-ilo Isopropilamino