公开(公告)号：EP2128134A1

公开(公告)日：2009-12-02

申请号：EP07830926.7

申请日：2007-10-31

申请人： Shionogi&Co., Ltd.

发明人： ENDOH, Takeshi ,  FUJII, Yasuhiko ,  KOJIMA, Eiichi ,  TADANO, Genta ,  YAMAGUCHI, Naoko ,  ADACHI, Yo ,  TAGASHIRA, Sachie ,  TACHIBANA, Yuki ,  ONODERA, Naohiro

IPC分类号： C07D209/08 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/02 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D209/86 ,  C07D211/96 ,  C07D213/81 ,  C07D215/20

CPC分类号： C07D209/86 ,  C07D211/96 ,  C07D213/81 ,  C07D215/20 ,  C07D241/04 ,  C07D243/08 ,  C07D263/32 ,  C07D277/28 ,  C07D295/22 ,  C07D295/26 ,  C07D307/81 ,  C07D307/91

摘要： A compound represented by the general formula (I):

wherein R 1 is

wherein R 26 and R 28 are each independently lower alkyloxy and the like; n 1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula:

wherein R 6 and R 7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R 2 is a hydrogen atom and the like; R 3 is optionally substituted lower alkyl and the like; R 4 is a hydrogen atom; or R 3 and R 4 may be taken together with an adjacent carbon atom to from a ring; R 5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 由通式（I）表示的化合物：其中R 1是其中R 26和R 28各自独立地为低级烷氧基等; n 1为0〜3的整数， Z是可以被选自取代基组a等的取代基中断的任选取代的C 1 -C 5亚炔基; A是由下式表示的基团：其中R 6和R 7各自独立地为低级烷基等; m和n各自独立地为0,1或2; R 2是氢原子等; R 3是任选取代的低级烷基等; R 4是氢原子; 或R 3和R 4可以与相邻的碳原子一起与环一起取代; R 5是羟基等，或光学活性异构体，其药学上可接受的盐或溶剂化物。

公开(公告)号：EP3129370A1

公开(公告)日：2017-02-15

申请号：EP15727077.8

申请日：2015-04-10

申请人： Shionogi & Co., Ltd.

发明人： KUSAKABE, Ken-ichi ,  TADANO, Genta ,  KOMANO, Kazuo ,  FUCHINO, Kouki ,  NAKAHARA, Kenji

IPC分类号： C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  A61K31/535 ,  A61K31/54 ,  A61P25/28

CPC分类号： C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D498/04

摘要： The present invention provides a compound which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or phylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins. A compound of the formula (I) wherein X is -S- or -O-, R
3a is alkyl, haloalkyl or the like, R
2a is H, halogen, alkyloxy, haloalkyloxy or the like, R
2b is H or the like, R
3b is H or alkyl, ring A and ring B is each independently a substituted or unsubstituted aromatic carbocycle, a substituted or unsubstituted aromatic heterocycle or the like, and R
1 is substituted or unsubstituted alkyl or the like, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供具有抑制β淀粉样蛋白产生的效果，特别是抑制BACE1的效果的化合物，作为淀粉状蛋白β蛋白的产生，分泌和/或沉积诱发的疾病的治疗剂或药剂是有用的。 其中X是-S-或-O-，R 3a是烷基，卤代烷基等，R 2a是H，卤素，烷氧基，卤代烷氧基等，R 2b是H等等，R 3b是 H或烷基，环A和环B各自独立地为取代或未取代的芳族碳环，取代或未取代的芳族杂环等，并且R 1为取代或未取代的烷基或类似物，或其药学上可接受的盐。

公开(公告)号：EP2634188A1

公开(公告)日：2013-09-04

申请号：EP11836380.3

申请日：2011-10-27

申请人： Shionogi & Co., Ltd.

发明人： MASUI, Moriyasu ,  TADANO, Genta

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D487/04 ,  A61K31/519

摘要： The present invention provides, for example, the following compound:

wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle,
X 1 -X 2 =X 3 is CR 6 -CR 6 =CR 7 , N-CR 6 =CR 7 , CR 5 -N=CR 7 or CR 5 -CR 6 =N, R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R 2a and R 2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R 4a , R 4b , R 5 , R 6 and R 7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like,
its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid β production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid β proteins.

摘要翻译： 本发明提供例如以下化合物：其中环A为取代或未取代的碳环或取代或未取代的杂环，X 1 -X 2 = X 3为CR 6 -CR 6 = CR 7，N-CR 6 = CR 7，CR 5 -N = CR7或CR5-CR6 = N，R1是取代或未取代的烷基，取代或未取代的烯基等，R2a和R2b各自独立地为氢，取代或未取代的烷基等，R4a，R4b，R5，R6和R7各自为 卤素，羟基，取代或未取代的烷基等，其药学上可接受的盐或其溶剂合物具有抑制β淀粉样蛋白产生，特别是BACE1抑制活性的作用，并且可用作治疗由生产， 淀粉样蛋白β蛋白的分泌或沉积。

公开(公告)号：EP3150573A1

公开(公告)日：2017-04-05

申请号：EP15799305.6

申请日：2015-05-28

申请人： Shionogi & Co., Ltd.

发明人： TADANO, Genta ,  IKARASHI, Fumiya ,  OKAMOTO, Kazuya ,  MAKI, Toshikatsu ,  HAGIHARA,Motoyuki

IPC分类号： C07C45/49 ,  C07C49/794 ,  C07D239/94 ,  C07D403/12 ,  C07D413/12 ,  C07B61/00

CPC分类号： C07D403/12 ,  C07B61/00 ,  C07B2200/13 ,  C07C45/49 ,  C07C49/794 ,  C07C321/04 ,  C07D239/94 ,  C07D295/03 ,  C07D413/12

摘要： The present invention relates to a Sonogashira-Carbonylation reaction using two types of gas, as well as novel crystals which can control a heat of the said reaction and the process of producing the same. In addition, the present invention relates to a ligand (additive) to prevent the deactivation of a palladium catalyst.

摘要翻译： 本发明涉及使用两种类型的气体的Sonogashira-羰基化反应，以及可控制所述反应的热的新型晶体及其生产方法。 此外，本发明涉及防止钯催化剂失活的配体（添加剂）。

公开(公告)号：EP2912035A1

公开(公告)日：2015-09-02

申请号：EP13848316.9

申请日：2013-10-23

申请人： Shionogi & Co., Ltd.

发明人： KUSAKABE, Ken-ichi ,  YOSHIDA, Syuhei ,  NAKAHARA, Kenji ,  HASEGAWA, Tsuyoshi ,  TADANO, Genta ,  FUCHINO, Kouki

IPC分类号： C07D413/12 ,  A61K31/5355 ,  A61K31/536 ,  A61K31/5365 ,  A61K31/553 ,  A61P25/28 ,  A61P43/00 ,  C07D498/04

CPC分类号： C07D413/12 ,  C07D413/04 ,  C07D413/14 ,  C07D498/04 ,  C07D498/10

摘要： The present invention provides a compound which has an effect of inhibiting amyloid &bgr; production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid &bgr; proteins. A compound of the formula (I): wherein X is —C(R3a)(R3b)—, —C(R3a)(R3b)—C(R3c)(R3d)— or —C(R3a)═C(R3c)—, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R3a, R3b, R3c and R3d are each independently hydrogen, halogen or the like, R4 is hydrogen or halogen, Ring B is substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供了具有抑制淀粉样蛋白和bgr的作用的化合物。 特别是抑制BACE1的作用，并且其可用作由淀粉样蛋白的生产，分泌和/或沉积诱导的疾病的治疗或预防剂。 蛋白质。 式（I）化合物：其中X为-C（R 3a）（R3b） - ， - （R3a）（R3b）-C（R3c）（R3d） - 或-C（R3a）= C（R3c） - ，R1是取代或未取代的烷基等，R2a，R2b，R3a，R3b，R3c和R3d各自独立地为氢，卤素等，R4为氢或卤素，环B为取代或未取代的碳环或取代或未取代的 未取代的杂环或其药学上可接受的盐。

公开(公告)号：EP2703401A1

公开(公告)日：2014-03-05

申请号：EP12777702.7

申请日：2012-04-25

申请人： Shionogi & Co., Ltd.

发明人： TADA, Yukio ,  KUSAKABE, Ken-ichi ,  TADANO, Genta

IPC分类号： C07D417/04 ,  A61K31/541 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07D417/14 ,  C07D491/048 ,  C07D491/056

CPC分类号： C07D417/04 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/4858 ,  C07D417/14 ,  C07D491/048 ,  C07D491/056

摘要： The present invention provides a compound of formula (I):

wherein ring B is substituted or unsubstituted carbocycle or heterocycle,
R 1 is substituted or unsubstituted alkyl or the like,
R 2a and R 2b are each independently hydrogen, substituted or unsubstituted alkyl or the like,
R 3 , R 4a and R 4b are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like, a dashed line represents a presence or absence of a bond,
R 5 is hydrogen, substituted or unsubstituted alkyl or the like,
R 6 is halogen, hydroxy, substituted or unsubstituted alkyl or the like,
p is an integer of 0 to 3,
or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.

摘要翻译： 本发明提供了式（I）化合物：其中环B为取代或未取代的碳环或杂环，R 1为取代或未取代的烷基等，R 2a和R 2b各自独立地为氢，取代或未取代的烷基等，R 3 ，R4a和R4b各自独立地为氢，卤素，取代或未取代的烷基等，虚线表示存在或不存在键，R5为氢，取代或未取代的烷基等，R6为卤素，羟基，取代的 或未取代的烷基等，p为0〜3的整数，或其药学上可接受的盐，其具有抑制β淀粉样蛋白产生的效果，特别是抑制BACE1的效果，并且可用作治疗或预防 由淀粉样蛋白β蛋白的产生，分泌和/或沉积诱发的疾病。