公开(公告)号：US08623903B2

公开(公告)日：2014-01-07

申请号：US13368687

申请日：2012-02-08

申请人： Akira Kugimiya ,  Yuki Tachibana

发明人： Akira Kugimiya ,  Yuki Tachibana

IPC分类号： A61K31/416 ,  C07D231/56

CPC分类号： C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D419/14 ,  C07D471/04

摘要： The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1═X2—X3═X4— is a formula of —C(R1)═C(R2)—C(R3)═C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of —Z—R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 本发明提供具有DP受体拮抗作用的吲哚羧酸衍生物和包含所述化合物作为活性成分的药物组合物，还有用于治疗过敏性疾病的治疗剂。 通式（I）的化合物：其中环A为芳族碳环等; 环B为含氮非芳族杂环等; -X1 = X2-X3 = X4-的式为-C（R1）= C（R2）-C（R3）= C（R4） - 等的式; X5为C（R5）或N; R1，R2，R3，R4和R5独立地为氢原子，卤素原子等; R6是-Z-R10等的化合物，其中Z是亚烷基等，R 10是羧基等; R7是任选取代的烷氧基等; R8独立地是卤素原子等; R9独立地是任选取代的烷基等; Y是单键等; n为0等 q为0等; 其药学上可接受的盐或其溶剂合物。

公开(公告)号：US08207196B2

公开(公告)日：2012-06-26

申请号：US12024530

申请日：2008-02-01

申请人： Motonari Uesugi ,  Salih J. Wakil ,  Lutfi Abu-Elheiga ,  Qian Mao ,  Shinji Kamisuki ,  Akira Kugimiya

发明人： Motonari Uesugi ,  Salih J. Wakil ,  Lutfi Abu-Elheiga ,  Qian Mao ,  Shinji Kamisuki ,  Akira Kugimiya

IPC分类号： A61K31/4709 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/4436 ,  A61P3/10

CPC分类号： A61K31/4439 ,  A61K31/426 ,  A61K31/4709 ,  C07D277/10 ,  C07D277/22 ,  C07D277/24 ,  C07D417/04 ,  C07D417/14

摘要： The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.

摘要翻译： 本发明涉及使用脂肪抑制素A和/或其衍生物和/或类似物治疗和/或预防一种或多种代谢紊乱。 在其它方面，用于治疗和/或预防一种或多种代谢紊乱的化合物利用A-B-C三方结构，其中A，B和C是相同或不相同的结构，并在本文中进行详细描述。 在具体方面，例如，代谢障碍包括肥胖或糖尿病。

公开(公告)号：US08143285B2

公开(公告)日：2012-03-27

申请号：US11991551

申请日：2006-09-04

申请人： Akira Kugimiya ,  Yuki Tachibana

发明人： Akira Kugimiya ,  Yuki Tachibana

IPC分类号： A61K31/404 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12

CPC分类号： C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D419/14 ,  C07D471/04

摘要： The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of -X1=X2-X3=X4- is a formula of —C(R1)═C(R2)—C(R3)═C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of -Z-R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.;a pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 本发明提供具有DP受体拮抗作用的吲哚羧酸衍生物和包含所述化合物作为活性成分的药物组合物，还有用于治疗过敏性疾病的治疗剂。 通式（I）的化合物：其中环A为芳族碳环等; 环B为含氮非芳族杂环等; -X1 = X2-X3 = X4-的公式为-C（R1）= C（R2）-C（R3）= C（R4） - 等的式; X5为C（R5）或N; R1，R2，R3，R4和R5独立地为氢原子，卤素原子等; R6是-Z-R10等的化合物，其中Z是亚烷基等，R 10是羧基等; R7是任选取代的烷氧基等; R8独立地是卤素原子等; R9独立地是任选取代的烷基等; Y是单键等; n为0等 q为0等; 其药学上可接受的盐或其溶剂合物。

公开(公告)号：US20110172217A1

公开(公告)日：2011-07-14

申请号：US13062328

申请日：2009-09-02

申请人： Masahiko Fujioka ,  Susumu Mitsumori ,  Akira Kugimiya ,  Daisuke Taniyama

发明人： Masahiko Fujioka ,  Susumu Mitsumori ,  Akira Kugimiya ,  Daisuke Taniyama

IPC分类号： A61K31/541 ,  A61K31/5383 ,  A61P29/00 ,  C07D498/04

CPC分类号： C07D498/04 ,  A61K31/5383 ,  A61K31/541

摘要： The present invention provides compounds or a pharmaceutically acceptable salt thereof which inhibit the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and are therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused morpholine compound shown in the present specification, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供了抑制PI3K活性以调节包括细胞的生长，分化，存活，增殖，迁移，代谢等许多生物学过程的化合物或其药学上可接受的盐，因此可用于预防/治疗 的疾病，包括炎性疾病，动脉硬化，血管/循环系统疾病，癌症/肿瘤，免疫系统疾病，细胞增殖性疾病，感染性疾病等。 通过提供本说明书中所示的环稠合的吗啉化合物或其药学上可接受的盐来解决上述问题。

公开(公告)号：US07842692B2

公开(公告)日：2010-11-30

申请号：US11989132

申请日：2006-07-20

申请人： Akira Kugimiya ,  Itsuo Makino ,  Naohiro Onodera

发明人： Akira Kugimiya ,  Itsuo Makino ,  Naohiro Onodera

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/437

CPC分类号： C07D471/04

摘要： The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases.A compound of the general formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1═X2—X3═X4— is a formula of —C(R1)═C(R2)—C(R3)═N— etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is optionally substituted C1-C6 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is optionally substituted C1-C6 alkyl etc.; R9 is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.

摘要翻译： 本发明产生具有DP受体拮抗活性的氮杂吲哚衍生物和包含所述化合物作为活性成分的药物组合物，并进一步提供治疗过敏性疾病的治疗剂。 通式（I）的化合物，其中环A是芳族碳环等; 环B为3〜8元含氮非芳族杂环等; -X 1 = X 2 -X 3 = X 4 - 的式为-C（R 1）= C（R 2）-C（R 3）= N-等的式 R1，R2，R3，R4和R5独立地是氢原子或卤素原子等; R6是任选取代的C 1 -C 6烷氧基等; R7独立地为卤素原子等; R8是任选取代的C 1 -C 6烷基等; R9是羧基等。 M是磺酰基等。 Y是单键等; L1，L2和L3是任选含有一个或两个杂原子等的单键或亚烷基; n为0等 q为0等; 其药学上可接受的盐或水合物。

公开(公告)号：US20070299114A1

公开(公告)日：2007-12-27

申请号：US11664299

申请日：2005-10-04

申请人： Akira Kugimiya ,  Nobuhiro Haga ,  Eiichi Kojima

发明人： Akira Kugimiya ,  Nobuhiro Haga ,  Eiichi Kojima

IPC分类号： A61K31/44 ,  A61K31/164 ,  A61K31/18 ,  A61K31/19 ,  A61K31/34 ,  A61K31/357 ,  C07C233/00 ,  C07C61/00 ,  C07D209/02 ,  C07D333/00 ,  C07D319/06 ,  C07D307/02 ,  C07D263/02 ,  C07D235/00 ,  C07D233/00 ,  C07D211/00 ,  C07D207/00 ,  C07C311/01 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/4164 ,  A61K31/421

CPC分类号： C07C237/20 ,  C07C57/42 ,  C07C57/60 ,  C07C59/64 ,  C07C229/34 ,  C07C233/11 ,  C07C235/34 ,  C07C235/36 ,  C07C255/43 ,  C07C257/20 ,  C07C275/42 ,  C07C309/66 ,  C07C311/08 ,  C07C311/35 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07D207/337 ,  C07D209/08 ,  C07D213/64 ,  C07D213/70 ,  C07D213/74 ,  C07D235/06 ,  C07D235/08 ,  C07D235/26 ,  C07D257/06 ,  C07D263/14 ,  C07D263/16 ,  C07D307/42 ,  C07D307/52 ,  C07D307/66 ,  C07D309/14 ,  C07D319/06 ,  C07D333/20 ,  C07D333/24 ,  C07D333/36 ,  C07D403/10

摘要： The present invention provides a compound represented by the formula (I): wherein X1 is N or CR2, X2 is N or CR4, R1 to R6 are each independently hydrogen, halogen, lower alkyl, lower alkoxy etc., a broken line is a single bond or a double bond etc., Y is COORA, CONHB(CRCRD)pCOORA, CONRERF, CONRB(CRCRD)pCONRERF etc., RA to RF, RH and RJ are each independently hydrogen, lower alkyl etc., RG is lower alkyl, aryl heterocycle etc., p is 1 or 2, ring A is optionally substituted phenyl, optionally substituted indolyl etc., X3 is O, S or NR13, X4 is CR7 or N, X5 is CR8 or N, X6 is CR9 or N, X7 is CR10 or N, R7 to R12 are each independently hydrogen, halogen, lower alkyl etc., R13 and R14 are each independently hydrogen, lower alkyl etc., W is hydrogen, lower alkyl, NR15R16 etc., and R15 to R21 are each independently hydrogen, lower alkyl etc.), or a pharmaceutically acceptable salt or a solvate thereof, and a pharmaceutical composition containing them.

摘要翻译： 本发明提供由式（I）表示的化合物：其中X 1是N或CR 2，X 2是N或CR R 4和R 6各自独立地为氢，卤素，低级烷基，低级烷氧基等，虚线为单键 或双键等，Y是COOR A，CONHB（CR），R D，D，D，CO， CONR E E E>，，，，>>>）））））））<<<<<<<<<<<<<<<<<<<<<<<<<<<<<<<<<<< 其中R 1，R 2，R 2，R 2，...，...， H H和R H各自独立地为氢，低级烷基等，R G为低级烷基，芳基杂环等，p为1或2， 环A是任选取代的苯基，任选取代的吲哚基等，X 3是O，S或NR 13，X 4是CR 0 或者N，X 5是CR 8或N，X 6是CR 9， 或N，X 7是CR 10或N，R 7至R 12 UP>各自独立地为氢，卤素，低级烷基等，R 13和R 14各自独立地为氢，低级烷基等，W为氢，低级烷基， R 15，R 16等，R 15至R 21各自独立地为氢，低级烷基等。 ）或其药学上可接受的盐或溶剂化物，以及含有它们的药物组合物。

公开(公告)号：US20130012538A1

公开(公告)日：2013-01-10

申请号：US13484702

申请日：2012-05-31

申请人： Motonari Uesugi ,  Salih J. Wakil ,  Lutfi Abu-Elheiga ,  Qian Mao ,  Shinji Kamisuki ,  Akira Kugimiya

发明人： Motonari Uesugi ,  Salih J. Wakil ,  Lutfi Abu-Elheiga ,  Qian Mao ,  Shinji Kamisuki ,  Akira Kugimiya

IPC分类号： A61K31/4439 ,  A61K31/4709 ,  A61P3/06 ,  A61P3/00 ,  A61P9/12 ,  A61P35/00 ,  A61P9/00 ,  A61K31/425 ,  A61P3/10

CPC分类号： A61K31/4439 ,  A61K31/426 ,  A61K31/4709 ,  C07D277/10 ,  C07D277/22 ,  C07D277/24 ,  C07D417/04 ,  C07D417/14

摘要： The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.

公开(公告)号：US20120142687A1

公开(公告)日：2012-06-07

申请号：US13368687

申请日：2012-02-08

申请人： Akira KUGIMIYA ,  Yuki Tachibana

发明人： Akira KUGIMIYA ,  Yuki Tachibana

IPC分类号： A61K31/454 ,  C07D403/04 ,  A61K31/405 ,  C07D401/14 ,  A61K31/4545 ,  A61P11/06 ,  A61K31/4375 ,  C07D403/06 ,  A61K31/496 ,  C07D413/14 ,  A61K31/5377 ,  A61P37/00 ,  C07D401/04 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D419/14 ,  C07D471/04

摘要： The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1═X2—X3═X4— is a formula of —C(R1)═C(R2)—C(R3)═C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of —Z—R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.

摘要翻译： 本发明提供具有DP受体拮抗作用的吲哚羧酸衍生物和包含所述化合物作为活性成分的药物组合物，还有用于治疗过敏性疾病的治疗剂。 通式（I）的化合物：其中环A为芳族碳环等; 环B为含氮非芳族杂环等; -X 1 = X 2 -X 3 = X 4 - 的化学式为-C（R 1）= C（R 2）-C（R 3）= C（R 4） X5为C（R5）或N; R1，R2，R3，R4和R5独立地为氢原子，卤素原子等; R6是-Z-R10等的化合物，其中Z是亚烷基等，R 10是羧基等; R7是任选取代的烷氧基等; R8独立地是卤素原子等; R9独立地是任选取代的烷基等; Y是单键等; n为0等 q为0等; 其药学上可接受的盐或其溶剂合物。

公开(公告)号：US20100069638A1

公开(公告)日：2010-03-18

申请号：US12622860

申请日：2009-11-20

申请人： Akira Kugimiya ,  Masahiko Fujioka ,  Yuki Tachibana ,  Takami Murashi

发明人： Akira Kugimiya ,  Masahiko Fujioka ,  Yuki Tachibana ,  Takami Murashi

IPC分类号： C07D401/04 ,  C07D211/44 ,  C07D241/04 ,  C07D211/34 ,  C07D405/12 ,  C07D413/12

CPC分类号： C07D295/26 ,  C07D207/14 ,  C07D207/48 ,  C07D211/58 ,  C07D211/70 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D231/12 ,  C07D231/40 ,  C07D235/08 ,  C07D235/30 ,  C07D235/32 ,  C07D243/08 ,  C07D261/08 ,  C07D261/18 ,  C07D263/32 ,  C07D263/58 ,  C07D265/36 ,  C07D271/10 ,  C07D277/24 ,  C07D277/28 ,  C07D285/12 ,  C07D285/135 ,  C07D295/096 ,  C07D295/155 ,  C07D307/42 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D333/36 ,  C07D401/12 ,  C07D413/12

摘要： The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.; a pharmaceutically acceptable salt or a hydrate thereof.

摘要翻译： 本发明提供具有DP受体拮抗活性的磺酰胺衍生物和含有上述化合物作为活性成分的药物组合物，还含有治疗过敏性疾病的治疗剂。 通式（II）的化合物：其中环A为芳族碳环等; 环B为含氮非芳族杂环等; 环C为芳香族碳环等; R1是羧基等; R2独立地为卤素原子等; R3是任选取代的烷氧基等; R4独立地为卤素原子等; R5独立地是任意取代的烷基等; M是磺酰基等。 Y是单键等。 L1是单键等; L2是单键等; k为0，1，2，3或4; n为0,1或2; q为0,1,2或3; 条件是当环B是含有一个或两个氮原子并且环C是苯环的6元含氮杂环时，a）k不为0; 其药学上可接受的盐或其水合物。

公开(公告)号：US08957219B2

公开(公告)日：2015-02-17

申请号：US13124788

申请日：2009-10-15

申请人： Koji Masuda ,  Shiro Kida ,  Kyohei Hayashi ,  Manabu Katou ,  Naoki Yoshikawa ,  Akira Kugimiya ,  Mado Nakajima ,  Nobuyuki Tanaka

发明人： Koji Masuda ,  Shiro Kida ,  Kyohei Hayashi ,  Manabu Katou ,  Naoki Yoshikawa ,  Akira Kugimiya ,  Mado Nakajima ,  Nobuyuki Tanaka

IPC分类号： A61K31/426 ,  A61K31/428 ,  C07D513/02 ,  C07D513/04 ,  C07D235/16 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/429 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D263/56 ,  C07D417/04 ,  C07D417/12

CPC分类号： C07D235/16 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/429 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D263/56 ,  C07D263/57 ,  C07D277/30 ,  C07D277/64 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D513/04

摘要： Disclosed is a compound which is useful as an endothelial lipase inhibitor.A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by the formula: —C(R1R2)—C(═O)—NR3R4 and a group represented by the formula: —R5, a broken line represents the presence or the absence of a bond, Z is —NR6—, ═N—, —O—, or —S—, R6 is halogen, substituted or unsubstituted alkyl or the like, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like.

摘要翻译： 公开了可用作内皮脂肪酶抑制剂的化合物。 一种具有对内皮脂肪酶具有抑制活性的药物组合物，其包含由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中环A是含氮杂环，环A可以被除代表的基团以外的取代基取代 通式为-C（R 1 R 2）-C（= O）-NR 3 R 4和由式-R 5表示的基团，虚线表示键的存在或不存在，Z为-NR 6 - ，= ，-O-或-S-，R 6为卤素，取代或未取代的烷基等，R 1和R 2各自独立地为氢，卤素，羟基，氰基，硝基，羧基或取代或未取代的烷基，R 3为氢或取代 或未取代的烷基，R 4为氢，取代或未取代的烷基等，R 3和R 4与它们所连接的相邻氮原子一起形成取代或未取代的环，R 5为氢，卤素，羟基，氰基，硝基 ，ca 取代或未取代的烷基，取代或未取代的链烯基，取代或未取代的炔基等。