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1. 发明申请

WO2010119984A1 3-ARYL OR HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE 审中-公开
标题翻译： 3-ARYL或HETEROARYL取代的INDOLE DORIVATIVE
公开(公告)号：WO2010119984A1
公开(公告)日：2010-10-21
申请号：PCT/JP2010/056965
申请日：2010-04-14
申请人： BANYU PHARMACEUTICAL CO.,LTD. , FUJIMURA, Takashi , KISHINO, Hiroyuki , MIZUTANI, Takashi , SAKURABA, Shunji , SASAKI, Takahide , SATO, Nagaaki
发明人： FUJIMURA, Takashi , KISHINO, Hiroyuki , MIZUTANI, Takashi , SAKURABA, Shunji , SASAKI, Takahide , SATO, Nagaaki
IPC分类号： C07D209/42 , A61K31/404 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/497 , A61P3/04 , A61P43/00 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/04
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; Y1 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; Y1和Y2均表示氢原子或Y1和Y2一起形成-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。

2. 发明申请

WO2010117085A1 ARYL INDOLE DERIVATIVES 审中-公开
标题翻译： ARYL INDOLE DORIVATIVES
公开(公告)号：WO2010117085A1
公开(公告)日：2010-10-14
申请号：PCT/JP2010/056636
申请日：2010-04-07
申请人： BANYU PHARMACEUTICAL CO.,LTD. , KISHINO, Hiroyuki , MIZUTANI, Sayaka , SAKURABA, Shunji , SATO, Nagaaki
发明人： KISHINO, Hiroyuki , MIZUTANI, Sayaka , SAKURABA, Shunji , SATO, Nagaaki
IPC分类号： C07D209/14 , A61K31/496 , A61P3/04 , A61P43/00 , C07D401/04 , C07D417/04
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 R 1 is a hydrogen atom, halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkyloxy, or haloC 1-6 alkyloxy; R 2 represents C 1-6 alkyl or haloC 1-6 alkyl; R 3 represents a hydrogen atom, C 1-6 alkyl, or haloC 1-6 alkyl; and Ar represents an aryl or heteroaryl, wherein the aryl or the heteroaryl may be substituted with 1 to 3 substituents such as halogen, C 1-6 alkyl, haloC 1-6 alkyl, and C 1-6 alkyloxy.
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。

3. 发明申请

WO2010126164A1 INDOLE-2-CARBOXAMIDE DERIVATIVE 审中-公开
标题翻译：吲哚-2-羧酰胺衍生物
公开(公告)号：WO2010126164A1
公开(公告)日：2010-11-04
申请号：PCT/JP2010/057848
申请日：2010-04-27
申请人： BANYU PHARMACEUTICAL CO.,LTD. , HAGA, Yuji , MIZUTANI, Sayaka , SATO, Nagaaki
发明人： HAGA, Yuji , MIZUTANI, Sayaka , SATO, Nagaaki
IPC分类号： C07D403/06 , A61K31/4725 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P19/10 , A61P23/00 , A61P25/04 , A61P43/00 , C07D403/12 , C07D403/14
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, R 1 represents a hydrogen atom, a halogen, a C 1-6 alkyl, etc,; R 2 represents a C 1-6 alkyl, or a halo-C 1-6 alkyl; R 3 represents a hydrogen atom, a C 1-6 alkyl, etc.; R 4 represents a hydrogen atom, a C 1-6 alkyl, a halo-C 1-6 alkyl, etc.; or R 3 and R 4 , taken together with the nitrogen atom to which they bond, form a 3- to 6-membered aliphatic nitrogen-containing hetero ring; or R 3 and Y 3 , taken together, form -CH 2 -CH 2 -; Y 1 and Y 2 are both hydrogen atoms; or Y 1 and Y 2 , taken together, form -CH 2 -CH 2 -; and Y 3 represents a hydrogen atom; or Y 3 and R 3 , taken together, form -CH 2 -CH 2 -].
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 - ]。

4. 发明申请

WO2010126163A1 HETEROARYLTHIOMETHYL PYRIDINE DERIVATIVE 审中-公开
标题翻译：异丁基二甲基吡啶衍生物
公开(公告)号：WO2010126163A1
公开(公告)日：2010-11-04
申请号：PCT/JP2010/057847
申请日：2010-04-27
申请人： BANYU PHARMACEUTICAL CO.,LTD. , KAMEDA, Minoru , KOBAYASHI, Kensuke , NAKAMA, Chisato , ANDO, Makoto , SATO, Nagaaki
发明人： KAMEDA, Minoru , KOBAYASHI, Kensuke , NAKAMA, Chisato , ANDO, Makoto , SATO, Nagaaki
IPC分类号： C07D401/14 , A61K31/444 , A61K31/4545 , A61K31/541 , A61P3/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P25/02 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D413/14 , C07D417/14 , C07D451/04
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D451/04
摘要： The present invention relates to a compound represented by a formula (I): wherein X is a group represented by or the like; Y is a group represented by or the like; and Ar 1 is a group represented by or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由式（I）表示的化合物：其中X是由等表示的基团; Y是由等表示的基团; 和Ar 1是由其表示的基团或其药学上可接受的盐。

5. 发明申请

WO2004031175A2 N-SUBSTITUTE-2-OXODIHYDROPYRIDINE DERIVATES 审中-公开
标题翻译： N-取代-2-氧代二氢吡啶衍生物
公开(公告)号：WO2004031175A2
公开(公告)日：2004-04-15
申请号：PCT/JP2003/012290
申请日：2003-09-25
申请人： BANYU PHARMACEUTICAL CO., LTD. , SATO, Nagaaki , ANDO, Makoto , ISHIKAWA, Shiho , NAGASE, Tsuyoshi , NAGAI, Keita , KANATANI, Akio
发明人： SATO, Nagaaki , ANDO, Makoto , ISHIKAWA, Shiho , NAGASE, Tsuyoshi , NAGAI, Keita , KANATANI, Akio
IPC分类号： C07D401/14
CPC分类号： C07D213/80 , C07D401/04 , C07D401/14
摘要： A compound of the formula (I): (wherein Ar 1l and Ar 2 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; R 1 and R 2 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, f ormyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R 1 , R 4 and R 5 are independently hydrogen, cyano, halogen 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 11和Ar 2独立地为芳基或杂芳基，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，芳基，低级低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 1，R 4和R 5独立地是氢，氰基，卤素羟基或低级烷基，低级烷氧基或低级烷硫基，最后三个基团任选被选自以下的取代基取代：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）或其盐或酯可用作神经肽Y受体拮抗剂，也可用作为治疗贪食症，肥胖症或糖尿病的药物。

6. 发明公开

EP2264026A1 ALKYLAMINOPYRIDINE DERIVATIVE 审中-公开
标题翻译：烷基氨基吡啶衍生物
公开(公告)号：EP2264026A1
公开(公告)日：2010-12-22
申请号：EP09718266.1
申请日：2009-03-04
申请人： Banyu Pharmaceutical Co., Ltd.
发明人： ANDO, Makoto , ITO, Hirokatsu , KAMEDA, Minoru , KAWAMOTO, Hiroshi , KOBAYASHI, Kensuke , MIYAZOE, Hiroshi , NAKAMA, Chisato , SATO, Nagaaki , TSUJINO, ToshiakI
IPC分类号： C07D401/14 , A61K31/4545 , A61K31/46 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/55 , A61P3/04 , A61P3/10 , A61P43/00 , C07D413/14 , C07D417/14 , C07D451/02 , C07D498/08
CPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D498/08
摘要： The present invention relates to a compound that is useful for treatment of, for example, hypertension, arteriosclerosis, bulimia and obesity because of having an antagonistic action to a neuropeptide Y receptor and is represented by formula (I)

[wherein R 1 represents hydrogen, cyano, or the like;
R represents a group represented by formula (II);

X 1 represents C 1-4 lower alkylene or the like; X 2 represents lower alkylene or the like; and Het represents a 5-membered heteroaromatic ring that has at least one nitrogen atom and, in addition, one or two hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms]
or to a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由于具有对神经肽Y受体的拮抗作用而用于治疗例如高血压，动脉硬化，贪食症和肥胖症的化合物，并由式（I）表示[其中R 1表示氢，氰基或类似的; R表示由式（II）表示的基团; X1代表C1-4低级亚烷基等; X2代表低级亚烷基等; 并且Het表示具有至少一个氮原子并且另外具有一个或两个选自氮，硫和氧原子的杂原子的5-元杂芳环]或其药学上可接受的盐。

7. 发明公开

EP2210880A1 BENZOXAZINONE DERIVATIVE 有权转让
标题翻译：苯并恶嗪酮衍生物
公开(公告)号：EP2210880A1
公开(公告)日：2010-07-28
申请号：EP08836571.3
申请日：2008-10-02
申请人： Banyu Pharmaceutical Co., Ltd.
发明人： ISHIKAWA, Shiho , MIZUTANI, Takashi , NAGASE, Tsuyoshi , SATO, Nagaaki , TAKAHASHI, Hidekazu
IPC分类号： C07D239/80 , A61K31/517 , A61K31/536 , A61P1/00 , A61P1/04 , A61P1/10 , A61P1/16 , A61P1/18 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P3/12 , A61P5/00 , A61P5/24 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00
CPC分类号： C07D239/80 , C07D265/18 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04
摘要： [PROBLEMS]
To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases.
[MEANS FOR SOLVING PROBLEMS]
The compound, which is for use as an active ingredient, is represented by the formula (I):

[wherein R 1 represents optionally halogenated C 1-6 alkyl, etc.; R 2 represents, e.g., a group represented by the formula (II-1) or (II-4)

(wherein W represents C 1-6 alkylene, etc. and R represents C 1-6 alkyl, etc.); R 3 represents hydrogen, C 1-6 alkyl, etc.; X represents -O-, -NH-, etc.; and Y 1 , Y 2 , Y 3 , and Y 4 each independently represents -CH-, -N-, etc.].
摘要翻译： [问题]提供可用作治疗循环系统疾病，神经系统疾病，代谢疾病，生殖系统疾病和消化道疾病的药物的化合物。 [用于解决课题的手段]用作有效成分的化合物由式（I）表示：[其中，R 1表示可以被卤素化的C 1-6烷基等。 R2表示例如由式（II-1）或（II-4）表示的基团（其中W表示C1-6亚烷基等，R表示C1-6烷基等）。 R3代表氢，C1-6烷基等; X表示-O - ， - NH-等; Y 1，Y 2，Y 3和Y 4各自独立地表示-CH - ， - N-等]。

8. 发明公开

EP1944301A1 NOVEL BENZOXATHIIN DERIVATIVE 审中-公开
标题翻译：新的苯并吖庚因衍生物
公开(公告)号：EP1944301A1
公开(公告)日：2008-07-16
申请号：EP06822742.0
申请日：2006-10-25
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： SASAKI, Takahide , SATO, Nagaaki , TAKAHASHI, Toshiyuki , MIZUTANI, Takashi
IPC分类号： C07D327/06 , A61K31/4025 , A61K31/4365 , A61K31/4535 , A61K31/454 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/20 , A61P25/22
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; X 1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X 2 represents a group represented by the following formula (II): (wherein R 4 and R 5 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 X 3 -X 6 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代表氮原子，硫原子等; R1代表芳基等; 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）等等; X和Y中的一个代表氧原子，另一个代表硫烷基等; 和X 3 -X 6分别代表-CH-，氮原子等。

9. 发明公开

EP1852423A1 CRYSTAL OF 4(3H)-QUINAZOLINONE DERIVATIVE 审中-公开
标题翻译： 4（3H） - 喹唑啉酮衍生物的晶体
公开(公告)号：EP1852423A1
公开(公告)日：2007-11-07
申请号：EP06714041.8
申请日：2006-02-13
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAGASE, Tsuyoshi , SATO, Nagaaki , KANATANI, Akio , TOKITA, Shigeru
IPC分类号： C07D239/91 , A61K31/517 , A61K45/00 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P3/12 , A61P5/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22
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-methy 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H3与组胺H3受体偶联能力的物质或抑制组胺H3受体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°）

10. 发明公开

EP2145884A1 INDOLEDIONE DERIVATIVE 有权转让
标题翻译： INDOLEDIONE派生词
公开(公告)号：EP2145884A1
公开(公告)日：2010-01-20
申请号：EP08738975.5
申请日：2008-03-27
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： TAKAHASHI, Toshiyuki , NAGASE, Tsuyoshi , SATO, Nagaaki
IPC分类号： C07D401/14 , A61K31/4155 , A61K31/4439 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P3/12 , A61P5/00 , A61P5/50 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/16 , A61P13/12 , A61P15/00 , A61P15/08
CPC分类号： C07D403/04
摘要： A compound represented by the general formula (I-a):

[wherein R 1a and R 2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R 3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R 4a and R 5a each means lower alkyl, lower cycloalkyl, etc. or R 4a and R 5a are bonded to each other to form lower cycloalkylidene; and R 6a 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R1a和R2a各自表示氢，低级环烷基，低级烷基等; R3a是指氢，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彼此键合形成低级亚环烷基; 和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，作为各种循环系统疾病，神经系统疾病，代谢疾病，生殖系疾病，消化道疾病，肿瘤，感染症等的治疗剂有用。

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