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1. 发明申请

US20110124674A1 5/5-OR 5/6-MEMBERED CONDENSED RING CYCLOALKYLAMINE DERIVATIVE 审中-公开
标题翻译： 5/5或5/6会议凝结环状环丙基胺衍生物
公开(公告)号：US20110124674A1
公开(公告)日：2011-05-26
申请号：US13054804
申请日：2009-07-14
申请人： Hiroyuki Kishino , Nagaaki Sato , Takao Suzuki
发明人： Hiroyuki Kishino , Nagaaki Sato , Takao Suzuki
IPC分类号： A61K31/454 , C07D401/06 , C07D417/14 , C07D471/04 , A61K31/4545 , C07D405/06 , A61K31/4525 , C07D495/04 , A61P3/10
CPC分类号： C07D401/06 , A61K31/4525 , A61K31/454 , A61K31/4545 , C07D401/14 , C07D405/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D495/04
摘要： Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中Q是CH或N; R1a，R1b，R1c和R1d独立地为C1-6烷基，卤代-C1-6烷基等; R2是氢原子等; R 3独立地为氢原子，C 1-6烷基等，或两个R 3一起形成桥，例如亚甲基等; R4a和R4b独立地为氢原子，C1-6烷基等; Z是双环芳香杂环等; Ar是苯环等; m1和m2分别为0,1或2; n为1〜4的整数。化合物及其盐作为黑色素浓缩激素受体拮抗剂，可用作中枢系统疾病，心血管疾病，代谢紊乱等的预防或治疗。

2. 发明申请

US20120028990A1 3 ARYL OR HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE 审中-公开
标题翻译： 3 ARYL或HETEROARYL取代的INDOLE DERIVATIVE
公开(公告)号：US20120028990A1
公开(公告)日：2012-02-02
申请号：US13260746
申请日：2010-04-14
申请人： Takashi Fujimura , Hiroyuki Kishino , Takashi Mizutani , Shunji Sakuraba , Takahide Sasaki , Nagaaki Sato
发明人： Takashi Fujimura , Hiroyuki Kishino , Takashi Mizutani , Shunji Sakuraba , Takahide Sasaki , Nagaaki Sato
IPC分类号： A61K31/404 , A61K31/4439 , A61K31/4725 , A61P3/04 , C07D403/12 , A61K31/496 , C07D417/14 , C07D409/14 , C07D405/14 , A61K31/454
CPC分类号： C07D405/04 , C07D209/18 , C07D405/14 , C07D409/04 , C07D417/04
摘要： A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.
摘要翻译：提供作为各种疾病的预防或治疗有效的3-芳基或杂芳基取代的吲哚衍生物。 [解决方法]提供由式（I）表示的化合物或其药学上可接受的盐。在该式中，R 1表示氢原子，C 1-6烷基等; R2表示氢原子，C1-6烷基等; Z表示芳基或杂芳基（条件是不包括咪唑基）; W表示由式（w-1）或（w-2）表示的基团。在该式中，R 3表示C 1-6烷基等; Y 1和Y 2均表示氢原子或Y 1和Y 2一起形成-CH 2 -CH 2 - ; Q表示CH或N; Ar表示苯基，呋喃基等; R4和R5各自独立地表示氢原子或C1-6烷基或R4和R5以及氮原子形成吡咯烷等。

3. 发明申请

US20120022078A1 ARYL INDOLE DERIVATIVES 审中-公开
标题翻译： ARYL INDOLE DORIVATIVES
公开(公告)号：US20120022078A1
公开(公告)日：2012-01-26
申请号：US13258006
申请日：2010-04-07
申请人： Hiroyuki Kishino , Sayaka Mizutani , Shunji Sakuraba , Nagaaki Sato
发明人： Hiroyuki Kishino , Sayaka Mizutani , Shunji Sakuraba , Nagaaki Sato
IPC分类号： A61K31/496 , A61P3/04 , C07D403/10 , C07D417/14 , C07D401/14
CPC分类号： C07D401/04 , A61K31/496 , C07D209/14 , C07D417/04
摘要： A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is a hydrogen atom, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, or haloC1-6alkyloxy; R2 represents C1-6alkyl or haloC1-6alkyl; R3 represents a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents an aryl or heteroaryl, wherein the aryl or the heteroaryl may be substituted with 1 to 3 substituents such as halogen, C1-6alkyl, haloC1-6alkyl, and C1-6alkyloxy.
摘要翻译：提供了一种新的芳基吲哚衍生物，其作为各种疾病的预防或补救是有效的。由式（I）表示的化合物或其药学上可接受的盐：（I）其中R 1是氢原子，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R 2表示C 1-6烷基或卤代C 1-6烷基; R 3表示氢原子，C 1-6烷基或卤代C 1-6烷基; 并且Ar表示芳基或杂芳基，其中芳基或杂芳基可以被1至3个取代基例如卤素，C 1-6烷基，卤代C 1-6烷基和C 1-6烷氧基取代。

4. 发明申请

US20100168156A1 Novel Benzoxathiine Derivative 失效
标题翻译：新型苯并噻嗪衍生物
公开(公告)号：US20100168156A1
公开(公告)日：2010-07-01
申请号：US12084017
申请日：2006-10-25
申请人： Takashi Mizutani , Nagaaki Sato , Takahide Sasaki , Toshiyuki Takahashi
发明人： Takashi Mizutani , Nagaaki Sato , Takahide Sasaki , Toshiyuki Takahashi
IPC分类号： A61K31/4365 , A61K31/4523 , A61K31/4436 , A61K31/39 , C07D497/04 , C07D401/12 , C07D411/04 , C07D411/12 , A61P25/30 , A61P3/06 , A61P19/06 , A61P1/16 , A61P9/10 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/32 , A61P25/08
CPC分类号： C07D327/06 , C07D497/04
摘要： Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X2 represents a group represented by the following formula (II): (wherein R4 and R5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X3-X6 respectively represent —CH—, a nitrogen atom or the like.
摘要翻译：公开了由下式（I）表示的化合物及其药学上可接受的盐。该化合物可用于治疗肥胖症，糖尿病等。 [式（I）中，Ar表示苯环等， X1表示氮原子，硫原子等; R1表示芳基等; X2表示由下式（II）表示的基团：（其中R4和R5分别表示低级烷基等，m表示2-4的数）等; X和Y中的一个表示氧原子，另一个表示硫烷基等; X3-X6分别表示-CH-，氮原子等。

5. 发明申请

US20090137576A1 Novel Piperidine Derivative 有权
标题翻译：新型哌啶衍生物
公开(公告)号：US20090137576A1
公开(公告)日：2009-05-28
申请号：US11921435
申请日：2006-05-29
申请人： Shiho Ishikawa , Tsuyoshi Nagase , Nagaaki Sato , Hidekazu Takahashi , Shigeru Tokita , Toshihiro Wada
发明人： Shiho Ishikawa , Tsuyoshi Nagase , Nagaaki Sato , Hidekazu Takahashi , Shigeru Tokita , Toshihiro Wada
IPC分类号： A61K31/5386 , C07D498/10 , C07D417/14 , A61K31/438 , C07D401/02 , A61K31/4545 , C07D401/14 , C07D405/14 , A61K31/506 , A61K31/497 , A61P3/04 , A61P3/10 , A61P3/00 , A61P9/00 , A61P7/00 , A61P9/12 , A61P25/28 , A61P25/30 , A61P25/16 , A61P25/18
CPC分类号： C07D519/00 , C07D401/12 , C07D471/10 , C07D491/107 , C07D491/20 , C07D498/10
摘要： Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.
摘要翻译：公开了对组胺H3受体的结合具有拮抗作用的物质或对组胺H3受体不断显示的活性的抑制作用。由式（I）表示的化合物或其药学上可接受的盐; （I）其中R 1表示可被取代的苯基等，R 2表示可被取代的氰基等，或者R 1和R 2一起形成可被取代的脂肪族杂环; R3表示由下式（II-1）表示的基团; 并且X1至X4全部表示碳原子等：（II-1）其中R4和R5代表低级烷基等; m1表示2〜4的整数。

6. 发明申请

US20080139589A1 Crystal of 4(3H)-Quinazolinone Derivative 失效
标题翻译： 4（3H） - 喹唑啉酮衍生物的晶体
公开(公告)号：US20080139589A1
公开(公告)日：2008-06-12
申请号：US11884138
申请日：2006-02-13
申请人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
发明人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
IPC分类号： A61K31/517 , C07D239/72 , A61P3/04 , A61P3/10 , A61P25/00
CPC分类号： C07D239/91 , A61K31/517 , A61K45/06
摘要： A substance that has a potency antagonistic to coupling of histamine with histamine H3 receptor or a potency of inhibiting the constant activity of histamine H3 receptor. There is provided a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that in the powder X- ray diffractometry, has peaks at 6.4°, 9.7°, 10.2°, 12.9°, 14.2°, 14.7°, 16.0°, 16.3°, 16.8°, 17.6°, 19.5°, 20.3°, 20.6°, 21.2°, 21.8°, 22.1°, 22.4°, 22.6°, 24.0°, 24.3°, 24.9°, 25.7°, 25.9°, 26.5°, 26.7°, 27.4°, 29.1°, 29.4°, 32.3° and 39.0° diffraction angles(2θ±0.2°).
摘要翻译：具有拮抗组胺与组胺H3受体的拮抗作用或抑制组胺H3受体的恒定活性的效力的物质。提供2-甲基3- {4- [3-（1-吡咯烷基）丙氧基]苯基} -5-三氟甲基-4（3H） - 喹唑啉酮的晶型I，其在粉末X射线衍射中具有峰在6.4°，9.7°，10.2°，12.9°，14.2°，14.7°，16.0°，16.3°，16.8°，17.6°，19.5°，20.3°，20.6°，21.2°，21.8°，22.1°，22.4° °，22.6°，24.0°，24.3°，24.9°，25.7°，25.9°，26.5°，26.7°，27.4°，29.1°，29.4°，32.3°和39.0°衍射角（2θ±0.2°）。

7. 发明申请

US20050154025A1 Novel pyridone derivatives 失效
标题翻译：新型吡啶酮衍生物
公开(公告)号：US20050154025A1
公开(公告)日：2005-07-14
申请号：US10505476
申请日：2003-03-14
申请人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
发明人： Nagaaki Sato , Tsuyoshi Nagase , Keita Nagai , Makoto Ando , Akio Kanatani
IPC分类号： A61K31/444 , A61P1/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P43/00 , C07D401/14 , C07D41/14
CPC分类号： C07D401/14 , A61K31/444
摘要： A compound of the formula (I): wherein R1 is hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, hydroxy, lower alkoxy or aralkyloxy; R2 and R3 are each independently hydrogen, halogen or halo-lower alkyl; and R4 and R are each independently hydrogen or halogen, is useful as a pharmaceutical composition for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, etc., nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
摘要翻译：式（I）的化合物：其中R 1是氢，卤素，氰基，低级烷基，卤代低级烷基，羟基，低级烷氧基或芳烷氧基; R 2和R 3各自独立地为氢，卤素或卤代低级烷基; R 4和R 4各自独立地为氢或卤素，可用作治疗与NPY相关的各种疾病的药物组合物，例如心血管疾病如心绞痛，急性或充血性心力衰竭，心肌梗死，高血压，肾病，电解质异常，血管痉挛等，神经系统疾病如贪食症，抑郁症，焦虑症，癫痫，癫痫，痴呆，疼痛，酒精中毒，药物戒断，昼夜节律紊乱，精神分裂症，记忆障碍，睡眠障碍，认知障碍等，代谢疾病如肥胖，糖尿病，激素异常，痛风，脂肪肝等，生殖器官或生殖障碍如不育症，早产，性功能障碍等，胃肠道疾病，呼吸系统疾病，炎症性疾病或青光眼等。

8. 发明授权

US06869966B2 N-substituted-2-oxodihydropyridine derivatives 失效
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：US06869966B2
公开(公告)日：2005-03-22
申请号：US10641017
申请日：2003-08-15
申请人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
发明人： Nagaaki Sato , Makoto Ando , Shiho Ishikawa , Tsuyoshi Nagase , Keita Nagai , Akio Kanatani
IPC分类号： A61P3/04 , C07D213/80 , C07D401/04 , C07D401/14 , C07D401/02 , A61K31/44 , C07D213/02
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl;R3, R4 and R5 are independently hydrogen, cyano, halogen or hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
摘要翻译：式（I）的化合物（其中Ar 1和Ar 2独立地是芳基或杂芳基，其中任何一个任选被选自氰基，卤素，硝基，低级烷基，卤代低级烷基，羟基 - 低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基，低级烯基，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，低级烷基磺酰基氨基，芳基磺酰基氨基，羟基，低级烷氧基，低级烷氧基，芳氧基，杂芳氧基，低级烷硫基，羧基，甲酰基，低级烷酰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，二低级烷基氨基甲酰基，低级烷基磺酰基，芳基磺酰基，芳基和杂芳基; R 1和R 2独立地为低级烷基，环 - 低级烷基，环（低级烷基） - 低级烷基或低级烷氧基，其中任何一个任选被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰氨基，羟基，低级烷氧基，甲酰基，低级烷基氧羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 3，R 4和R 5独立地是氢，氰基，卤素或羟基，或低级烷基，低级烷氧基或低级烷硫基，最后三个基团是任选的被选自卤素，低级烷基氨基，二低级烷基氨基，低级烷酰基氨基，羟基，低级烷氧基，甲酰基，低级烷氧基羰基，低级烷基氨基甲酰基和二低级烷基氨基甲酰基的取代基取代）或其盐或酯是有用的作为神经肽Y受体拮抗剂，也可用作治疗贪食症，肥胖症或糖尿病的药剂。

9. 发明申请

US20120035155A1 INDOLE-2-CARBOXAMIDE DEIVATIVE 审中-公开
标题翻译：吲哚-2-羧酰胺衍生物
公开(公告)号：US20120035155A1
公开(公告)日：2012-02-09
申请号：US13263801
申请日：2010-04-17
申请人： Yuji Haga , Sayaka Mizutani , Nagaaki Sato
发明人： Yuji Haga , Sayaka Mizutani , Nagaaki Sato
IPC分类号： A61K31/4725 , C07D401/14 , A61P9/12 , A61P9/10 , A61P13/12 , A61P9/00 , A61P3/04 , A61P3/10 , A61P5/00 , A61P3/06 , A61P19/06 , A61P1/16 , A61P29/00 , A61P1/04 , C07D401/12
CPC分类号： C07D403/06 , C07D403/12 , C07D403/14
摘要： To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R1 represents a hydrogen atom, a halogen, a C1-6 alkyl, etc,; R2 represents a C1-6 alkyl, or a halo-C1-6 alkyl; R3 represents a hydrogen atom, a C1-6 alkyl, etc.; R4 represents a hydrogen atom, a C1-6 alkyl, a halo-C1-6 alkyl, etc.; or R3 and R4, taken together with the nitrogen atom to which they bond, form a 3- to 6-membered aliphatic nitrogen-containing hetero ring; or R3 and Y3, taken together, form —CH2—CH2—; Y1 and Y2 are both hydrogen atoms; or Y1 and Y2, taken together, form —CH2—CH2—; and Y3 represents a hydrogen atom; or Y3 and R3, taken together, form —CH2—CH2—].
摘要翻译：提供具有人QRFP受体拮抗活性的吲哚化合物，并且可用作各种疾病的预防或补救。提供式（I）化合物或其药学上可接受的盐：[其中，R 1表示氢原子，卤素，C 1-6烷基等; R 2表示C 1-6烷基或卤代C 1-6烷基; R3代表氢原子，C1-6烷基等; R 4表示氢原子，C 1-6烷基，卤代C 1-6烷基等; 或R 3和R 4与它们键合的氮原子一起形成3至6元脂族含氮杂环; 或R 3和Y 3一起形成-CH 2 -CH 2 - ; Y1和Y2都是氢原子; 或Y1和Y2一起形成-CH 2 -CH 2 - ; Y 3表示氢原子; 或Y 3和R 3一起形成-CH 2 -CH 2 - ]。

10. 发明申请

US20100056597A1 INDOLEDIONE DERIVATIVE 有权
标题翻译：绝对衍生
公开(公告)号：US20100056597A1
公开(公告)日：2010-03-04
申请号：US12532182
申请日：2008-03-27
申请人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
发明人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
IPC分类号： A61K31/4155 , C07D403/02 , A61P3/10
CPC分类号： C07D403/04
摘要： A compound represented by the general formula (I-a): [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
摘要翻译：由通式（I-a）表示的化合物：[其中R 1a和R 2a各自表示氢，低级环烷基，低级烷基等; R3a表示氢，低级环烷基，低级烷基等; R4a和R5a各自表示低级烷基，低级环烷基等，或者R4a和R5a彼此键合形成较低环烷叉基; R6a表示低级烷基，低级卤代烷基等〕。该化合物作为LCE抑制剂起作用，可用作各种循环系统疾病，神经疾病，代谢疾病，生殖疾病，消化道疾病，肿瘤，感染性疾病等的治疗剂。

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