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    • 47. 发明授权
      US08981087B2 Benzo [E] [1,3] oxazin-4-one derivatives as phosphoinositide 3-kinase inhibitors 有权
    • Benzo [E] [1,3] oxazin-4-one derivatives as phosphoinositide 3-kinase inhibitors
    • 苯并[E] [1,3]恶嗪-4-酮衍生物作为磷酸肌醇3-激酶抑制剂
    • US08981087B2
    • 2015-03-17
    • US13384310
    • 2010-07-23
    • Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
    • Stephen Joseph Shuttleworth , Franck Alexandre Silva , Alexander Richard Liam Cecil , Thomas James Hill
    • C07D265/24 , C07D413/04 , A61K31/536 , A61K31/5365 , A61P19/02
    • C07D265/24
    • Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)-alkyl. —C(O)—NH2, —C(O)—NH-alkyl, —SO2-alkyl, —SO2—NH2 or —SO2—NH-alkyl; R2 is aryl substituted with at least one nitrogen-containing group or R2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C1-C6 mono alkylamino, C1C6 bis alkylamino, C1C6 acylamino, C1-C6 aminoalkyl, mono (C1C6 alkyl)amino C1-C6 alkyl, bis (C1C6 alkyl)amino C1C6 alkyl, C1-C6-acylamino or C1 C6 alkynyl-NR11, R11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, —C(O)—R7, —C(O)—NH2, —C(O)—NH—R7, —SO2—R7, —SO2—NH2, —SO2—NH—R7, NH-acyl, NH-sulfonyl, NR7-acyl, NR7-sulfonyl, N—C(O)—NH—R7, N—SO2—NH—R7, N—C(O)—NR7R7 or N—SO2—NR7R7; and R7 is alkyl, aryl or heteroaryl, are useful as PI3K inhibitors and are useful in therapy.
    • 式（I）的化合物：其中：W是O，N-H，N-烷基，N-烯基，N-炔基，N-芳基，N-杂芳基或S; 每个X独立地是CH或N; R1是式（b）或R3是H，烷基，NH2，OH，= 0或卤素; 每个A和B独立地是CH或N; D是NHR4; R4是H，烷基，-C（O） - 烷基。 -C（O）-NH 2，-C（O）-NH-烷基，-SO 2 - 烷基，-SO 2 -NH 2或-SO 2 -NH-烷基; R2是被至少一个含氮基取代的芳基，或R2是含氮杂芳基，被含氮基取代的环烷基，含氮环烷基，C1-C6单烷基氨基，C1C6双烷基氨基，C1C6酰基氨基，C1- C 1 -C 6烷基，单（C 1 -C 6烷基）氨基C 1 -C 6烷基，双（C 1 -C 6烷基）氨基C 1 -C 6烷基，C 1 -C 6酰基氨基或C 1 -C 6炔基-NR 11，R 11是H，烷基，烯基，炔基，芳基，杂芳基， ，O-烷基，NH-烷基，N-二烷基，-C（O）-R 7，-C（O）-NH 2，-C（O）-NH-R7，-SO 2 -R 7，-SO 2 -NH 2 - SO2-NH-R7，NH-酰基，NH-磺酰基，NR7-酰基，NR7-磺酰基，N-C（O）-NH-R7，N-SO2-NH-R7，N-C（O）-NR7R7或 N-SO2-NR7R7; 和R7是烷基，芳基或杂芳基，可用作PI3K抑制剂，并且可用于治疗。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 49. 发明授权
      US5180418A Herbicidally active thiadiazabicyclononanes and nonenes 失效
    • Herbicidally active thiadiazabicyclononanes and nonenes
    • US5180418A
    • 1993-01-19
    • US732988
    • 1991-07-19
    • Georg Pissiotas , Hans Moser , Hans-Georg Brunner , Eginhard Steiner
    • Georg Pissiotas , Hans Moser , Hans-Georg Brunner , Eginhard Steiner
    • A01N37/32 , A01N37/38 , A01N43/38 , A01N43/40 , A01N43/824 , A01N43/90 , A01N53/00 , C07C323/35 , C07C323/40 , C07C331/28 , C07D207/40 , C07D207/404 , C07D207/408 , C07D207/44 , C07D207/452 , C07D209/48 , C07D211/88 , C07D265/24 , C07D265/26 , C07D471/04 , C07D487/04 , C07D513/04 , C07F7/08
    • C07D207/408 , A01N37/38 , A01N43/90 , A01N53/00 , C07C323/35 , C07C323/40 , C07C331/28 , C07D207/452 , C07D209/48 , C07D211/88 , C07D265/26 , C07D471/04 , C07D487/04 , C07D513/04 , C07F7/0812
    • Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 alkenyl, halo-C.sub.3 -C.sub. 8 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.4 alkyl or halo-C.sub.3 -C.sub.7 cycloalkyl, or benzyl which is unsubstituted or substituted at the phenyl ring by up to three identical or different substituents selected from halogen, C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkoxy, or is an alkali metal ion, an alkaline earth metal ion or an ammonium ion, the group --[CHR.sub.6 --(CH.sub.2).sub.m ]--COOR.sub.7, or the group [CHR.sub.6 --(CH.sub.2).sub.t --Si(R.sub.8).sub.3 ]; R.sub.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.1 -C.sub.8 alkoxy-C.sub.2 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkylthio-C.sub.2 -C.sub.8 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sub.8 is C.sub.1 - C.sub.4 alkyl; R.sub.9 is C.sub.1 -C.sub.4 alkyl; R.sub.10 is C.sub.1 -C.sub.4 alkyl or phenyl; or R.sub.9 and R.sub.10, together with the carbon atom to which they are bonded, form a cyclohexane ring; R.sub.11 is C.sub.1 -C.sub.8 alkyl; R.sub.12 is hydrogen or C.sub.1 -C.sub.8 alkyl; R.sub.13 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 alkenyl or C.sub.3 -C.sub.7 alkynyl; X, Y, Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Z.sub.1 and Z.sub.2 are each independently oxygen or sulfur; n is 0, 1, 2, 3 or 4; m is 0, 1, 2, 3 or 4; q is 1 or 2; and t is 0, 1, 2, 3 or 4, have good pre- and post-emergence selective herbicidal and growth regulating properties.
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