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1. 发明授权

US4256640A Tetrahydrothiopyrano[2,3-b]indole derivatives 失效
标题翻译：四氢噻喃并[2,3-b]吲哚衍生物
公开(公告)号：US4256640A
公开(公告)日：1981-03-17
申请号：US39382
申请日：1979-05-15
申请人： Yasuo Makisumi , Susumu Takada , Takashi Sasatani , Natsuki Ishizuka
发明人： Yasuo Makisumi , Susumu Takada , Takashi Sasatani , Natsuki Ishizuka
IPC分类号： A61K31/40 , A61K31/445 , A61P25/04 , A61P29/00 , C07D209/30 , C07D495/04
CPC分类号： C07D495/04 , C07D209/30
摘要： Tetrahydrothiopyrano[2,3-b]indole derivative represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl, --COR.sup.5 (wherein R.sup.5 is alkyl, alkenyl, aryl or alkoxy) or ##STR2## (wherein Y is alkylene, oxoalkylene, hydroxyalkylene and R.sup.6 and R.sup.7 are each hydrogen or alkyl): R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl or dialkylaminoalkyl or ##STR3## is pyrrolidino, piperidino, piperazino, 4-alkylpiperazino, 4-arylpiperazino or morpholino; R.sup.4 is hydrogen or alkyl; A is methylene, alkylmethylene, ethylene, alkylethylene; X is hydrogen or one or two groups selected from the group consisting of halogen, alkyl, alkoxy, hydroxy and halogenoalkyl; and n is an integer of 0 to 2 and its pharmaceutically acceptacle salts; synthesized from 2-propargylthioindole or 2-(4-hydroxy-2-butynylthio)-indole; useful as analgesic and anti-inflammatory agent.
摘要翻译：由式I表示的四氢噻喃[2,3-b]吲哚衍生物：其中R 1是氢，烷基，羟烷基，烯基，芳烷基，芳基，-COR 5（其中R 5是烷基，烯基，芳基或烷氧基）或（其中Y是亚烷基，氧代亚烷基，羟基亚烷基，R 6和R 7各自是氢或烷基）：R 2是氢或烷基; R 3是氢，烷基，羟基烷基，烯基，芳烷基，芳基或二烷基氨基烷基，或者是吡咯烷子基，哌啶子基，哌嗪子基，4-烷基哌嗪基，4-芳基哌嗪基或吗啉代; R4是氢或烷基; A是亚甲基，烷基亚甲基，亚乙基，烷基亚乙基; X是氢或选自卤素，烷基，烷氧基，羟基和卤代烷基的一个或两个基团; n为0〜2的整数及其药学上可接受的盐; 由2-炔丙基硫吲哚或2-（4-羟基-2-丁炔硫基） - 吲哚合成; 用作镇痛和抗炎剂。

2. 发明申请

US20080103139A1 3-Carbamoyl-2-Pyridone Derivative 有权
标题翻译： 3-氨基甲酰基-2-吡啶酮衍生物
公开(公告)号：US20080103139A1
公开(公告)日：2008-05-01
申请号：US11628804
申请日：2005-10-28
申请人： Natsuki Ishizuka , Takashi Sasatani , Yoshiharu Hiramatsu , Masanao Inagaki , Masahide Odan , Hiroshi Hashizume , Susumu Mitsumori , Yasuhiko Fujii , Yoshikazu Fukui , Hideaki Watanabe , Jun Sato
发明人： Natsuki Ishizuka , Takashi Sasatani , Yoshiharu Hiramatsu , Masanao Inagaki , Masahide Odan , Hiroshi Hashizume , Susumu Mitsumori , Yasuhiko Fujii , Yoshikazu Fukui , Hideaki Watanabe , Jun Sato
IPC分类号： A61K31/5377 , C07D221/04 , A61K31/435 , C07D211/84 , A61K31/4412 , A61P17/00 , C07D401/12 , A61K31/496 , A61K31/506 , C07D413/12
CPC分类号： C07D213/82
摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1 is optionally substituted C1-C8 alkyl and the like; R2 is C1-C6 alkyl; R3 is C1-C6 alkyl and the like; or R2 and R3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein R5 is hydrogen and the like; X1 is a single bond and the like; X2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R6)—, wherein R6 is hydrogen and the like, and the like; X3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译：本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1是任选取代的C 1 -C 8烷基等; R 2是C 1 -C 6烷基; R 3是C 1 -C 6烷基等; 或R 2和R 3与相邻碳原子一起可以形成任选取代的5至10元非芳族碳环; R 4是氢等; G为选自下式的基团：其中R 5为氢等; X 1是单键等; X 2是任选取代的C 1 -C 8亚烷基，其可以被一个或两个-O-或-N（R 6） - 基团取代，其中R 0 > 6是氢等; X 3是单键等; 其药学上可接受的盐或溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

3. 发明申请

US20090030014A1 Indole Derivative Having Pgd2 Receptor Antagonist Activity 有权
标题翻译：具有Pgd2受体拮抗剂活性的吲哚衍生物
公开(公告)号：US20090030014A1
公开(公告)日：2009-01-29
申请号：US11989138
申请日：2006-07-20
申请人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
发明人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
IPC分类号： A61K31/496 , C07D487/00 , C07D401/02 , A61K31/4439 , A61P25/28 , A61K31/404 , A61K31/454 , C07D403/02
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention creates an indole 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 generic 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.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl 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，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是芳族碳环等; 环B为3〜8元含氮非芳族杂环等; R1，R2，R3，R4和R5独立地是氢原子或卤素原子等; R6是C2-C4烷氧基等; R7独立地为卤素原子等; R8独立地为C1-C4烷基等。 R9是羧基等。 Y是单键等; M是磺酰基等。 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。

4. 发明授权

US08106051B2 Utilities of amide compounds 有权
标题翻译：酰胺化合物的实用性
公开(公告)号：US08106051B2
公开(公告)日：2012-01-31
申请号：US12081662
申请日：2008-04-18
申请人： Teruo Yamamori , Kiyoshi Nagata , Natsuki Ishizuka , Katsunori Sakai
发明人： Teruo Yamamori , Kiyoshi Nagata , Natsuki Ishizuka , Katsunori Sakai
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495
CPC分类号： C07D213/75 , A61K31/165 , A61K31/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments.Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or bicyclic aromatic carbocyclic group or aromatic heterocyclic group, each of which may be optionally substituted, or the like; R is a hydrogen or the like; Z is oxygen or the like; Y1 and Y2 are a hydrogen, a lower alkyl, or the like; n is an integer of 0 to 2; the broken line is the presence or absence of a bond; and the wavy line represents a cis- or trans-geometrical isomerism with respect to the double bond; are disclosed.
摘要翻译：提供具有增强载脂蛋白A表达活性的化合物，其用作药物。式（I）的化合物：其中环A和Ar 1独立地是单环或双环芳族碳环基或芳族杂环基，其各自可以被任选取代;等等; R为氢等; Z是氧等; Y1和Y2是氢，低级烷基等; n为0〜2的整数，虚线是存在或不存在债券; 并且波浪线表示相对于双键的顺式或反式几何异构体; 被披露。

5. 发明申请

US20070054902A1 Isoxazole derivatives as peroxisome proliferator-activated receptors agonists 审中-公开
标题翻译：异恶唑衍生物作为过氧化物酶体增殖物激活受体激动剂
公开(公告)号：US20070054902A1
公开(公告)日：2007-03-08
申请号：US10581322
申请日：2004-11-29
申请人： Yoshikazu Fukui , Takasi Sasatani , Ken-ichi Sasatani , Natsuki Ishizuka , Toshisada Yano , Yasuhiko Kanda , Nobuo Chomei
发明人： Yoshikazu Fukui , Takasi Sasatani , Ken-ichi Sasatani , Natsuki Ishizuka , Toshisada Yano , Yasuhiko Kanda , Nobuo Chomei
IPC分类号： A61K31/5383 , A61K31/4245 , A61K31/42 , C07D413/14
CPC分类号： C07D417/12 , C07D261/08 , C07D261/18 , C07D413/04 , C07D413/06 , C07D413/12
摘要： A compound of formula (I): (wherein R1-R10 are each independently hydrogen, halogen, optionally substituted lower alkyl or the like, X1 is —O—, —S—, —NR11— (wherein R11 is hydrogen, lower alkyl or the like), —CR12R13CO—, —(CR12R13)mO—, —O(CR12R13)m- (wherein R12 and R13 are each independently hydrogen or lower alkyl and m is a integer between 1 and 3) or the like, X2 is a bond, —O—, —S—, —NR14— (wherein R14 is hydrogen, lower alkyl or the like, R14 and R6 can be taken together with the neighboring atom to form a ring) or —CR15R16— (wherein R15 and R16 are each independently hydrogen or lower alkyl, R15 and R6 or R10 can be taken together with the neighboring carbon atom to form a ring, R16 and R9 can be joined together to form a bond), X3 is COOR17, C(═NR17)NR18OR19 or the like), a pharmaceutically acceptable salt or a solvate thereof.
摘要翻译：式（I）的化合物：其中R 1〜R 10各自独立地为氢，卤素，任选取代的低级烷基等，X 1， / SUP>是-O - ， - S - ， - NR 11 - （其中R 11是氢，低级烷基等），-CR 12 - （CR 12）13 - ， - （CR 12）， - （CR 12）（其中R 12和R 12各自独立地为氢或低级烷基，m为1和...之间的整数） 3）等，X 2是一个键，-O - ， - S-，-NR 14 - （其中R 14是氢，低级烷基等，R 14和R 6可以与相邻原子一起形成环）或-CR 15 R 16 - （其中R 15和R 16各自独立地是氢或低级烷基，R 15和 R 6或R 10可以与相邻的碳原子一起形成环，R 16和R 9， S 可以连接在一起形成键），X 3是COOR 17，C（-NR 17）NR 18 其药学上可接受的盐或其溶剂化物。

6. 发明授权

US08178681B2 3-carbamoyl-2-pyridone derivatives 有权
标题翻译： 3-氨基甲酰基-2-吡啶酮衍生物
公开(公告)号：US08178681B2
公开(公告)日：2012-05-15
申请号：US11628804
申请日：2005-10-28
申请人： Natsuki Ishizuka , Yoshiharu Hiramatsu , Yasuhiko Fujii , Yoshikazu Fukui
发明人： Natsuki Ishizuka , Yoshiharu Hiramatsu , Yasuhiko Fujii , Yoshikazu Fukui
IPC分类号： C07D221/04 , C07D213/62 , A61K31/54 , A61K31/435
CPC分类号： C07D213/82
摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1 is optionally substituted C1-C8 alkyl and the like; R2 is C1-C6 alkyl; R3 is C1-C6 alkyl and the like; or R2 and R3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein R5 is hydrogen and the like; X1 is a single bond and the like; X2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R6)—, wherein R6 is hydrogen and the like, and the like; X3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译：本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1为任选取代的C 1 -C 8烷基等; R2是C1-C6烷基; R3是C1-C6烷基等; 或者R 2和R 3与相邻碳原子一起可以形成任选取代的5至10元非芳族碳环; R4是氢等; G是选自下式的基团：其中R5是氢等; X1是单键等; X2是任选取代的C1-C8亚烷基，其可以被一个或两个-O-或-N（R 6） - 基团取代，其中R 6是氢等; X3是单键等; 药学上可接受的盐或其溶剂合物，以及药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

7. 发明授权

US07956082B2 Indole derivative having PGD2 receptor antagonist activity 有权
标题翻译：具有PGD2受体拮抗剂活性的吲哚衍生物
公开(公告)号：US07956082B2
公开(公告)日：2011-06-07
申请号：US11989138
申请日：2006-07-20
申请人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
发明人： Akira Kugimiya , Michitaka Shichijo , Yoshiharu Hiramatsu , Natsuki Ishizuka
IPC分类号： A61K31/496 , A61K31/4439 , A61K31/404 , A61K31/454 , A61P25/28 , C07D487/00 , C07D401/02 , C07D403/02
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention creates an indole 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 generic 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.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl 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，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是芳族碳环等; 环B为3〜8元含氮非芳族杂环等; R1，R2，R3，R4和R5独立地是氢原子或卤素原子等; R6是C2-C4烷氧基等; R7独立地为卤素原子等; R8独立地为C1-C4烷基等。 R9是羧基等。 Y是单键等; M是磺酰基等。 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。

8. 发明授权

US08124625B2 Method of enhancing the expression of apolipoprotein AI using olefin derivatives 有权
标题翻译：使用烯烃衍生物增强载脂蛋白AI表达的方法
公开(公告)号：US08124625B2
公开(公告)日：2012-02-28
申请号：US10489365
申请日：2001-09-14
申请人： Teruo Yamamori , Kiyoshi Nagata , Natsuki Ishizuka , Kunio Hayashi
发明人： Teruo Yamamori , Kiyoshi Nagata , Natsuki Ishizuka , Kunio Hayashi
IPC分类号： A61K31/445 , A61K31/44
CPC分类号： C07D213/06 , A61K31/215 , A61K31/40 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/57 , C07D215/04 , C07D215/14 , C07D235/18 , C07D241/42 , C07D263/57 , C07D277/66 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D417/06 , C07D471/04
摘要： Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I): in which Ar1 and Ar2 are independently a phenyl, naphthyl, or monocyclic or bicyclic aromatic heterocyclic group, which may be optionally substituted; —X— is —N═CZ2—, —CY2═CZ2—, —CY2Y3—CHZ2—, —S—, —O—, or the like; Y1, Y2, Y3, Z1 and Z2 are independently a hydrogen, a halogen, a lower alkyl, a phenyl, or the like; Z1 and Z2 may be independently a linker group that may combine with Ar2 and Ar1 to form a condensed ring; m is 0 or 1, and n is 0 to 2; a prodrug thereof, a pharmaceutically acceptable salt or solvate thereof; are disclosed.
摘要翻译：提供了具有增强载脂蛋白A表达的活性的化合物。式（I）化合物：其中Ar 1和Ar 2独立地为可任意取代的苯基，萘基或单环或双环芳族杂环基; -X-是-N = CZ2-，-CY2 = CZ2-，-CY2Y3-CHZ2-，-S-，-O-等; Y 1，Y 2，Y 3，Z 1和Z 2独立地为氢，卤素，低级烷基，苯基等; Z1和Z2可以独立地是可以与Ar2和Ar1结合形成稠环的连接基团; m为0或1，n为0至2; 其前药，其药学上可接受的盐或溶剂合物; 被披露。

9. 发明申请

US20090036457A1 Utilities of olefin derivatives 有权
标题翻译：烯烃衍生物的实用性
公开(公告)号：US20090036457A1
公开(公告)日：2009-02-05
申请号：US12230993
申请日：2008-09-09
申请人： Teruo Yamamori , Kiyoshi Nagata , Natsuki Ishizuka , Kunio Hayashi
发明人： Teruo Yamamori , Kiyoshi Nagata , Natsuki Ishizuka , Kunio Hayashi
IPC分类号： A61K31/498 , A61K31/47 , A61K31/44 , A61K31/4436 , A61K31/4184 , A61K31/428 , A61K31/423 , A61P9/10
CPC分类号： C07D213/06 , A61K31/215 , A61K31/40 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/57 , C07D215/04 , C07D215/14 , C07D235/18 , C07D241/42 , C07D263/57 , C07D277/66 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D413/06 , C07D417/06 , C07D471/04
摘要： Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I): in which Ar1 and Ar2 are independently a phenyl, naphthyl, or monocyclic or bicyclic aromatic heterocyclic group, which may be optionally substituted; —X— is —N═CZ2-, —CY2═CZ2-, —CY2Y3—CHZ2-, —S—, —O—, or the like; Y1, Y2, Y3, Z1 and Z2 are independently a hydrogen, a halogen, a lower alkyl, a phenyl, or the like; Z1 and Z2 may be independently a linker group that may combine with Ar2 and Ar1 to form a condensed ring; m is 0 or 1, and n is 0 to 2; a prodrug thereof, a pharmaceutically acceptable salt or solvate thereof; are disclosed.
摘要翻译：提供了具有增强载脂蛋白A表达的活性的化合物。式（I）化合物：其中Ar 1和Ar 2独立地为可任意取代的苯基，萘基或单环或双环芳族杂环基; -X-是-N-CZ2-，-CY2-CZ2-，-CY2Y3-CHZ2-，-S-，-O-等; Y 1，Y 2，Y 3，Z 1和Z 2独立地为氢，卤素，低级烷基，苯基等; Z1和Z2可以独立地是可以与Ar2和Ar1结合形成稠环的连接基团; m为0或1，n为0至2; 其前药，其药学上可接受的盐或溶剂合物; 被披露。

10. 发明申请

US20080318958A1 New utilities of tricyclic compounds 审中-公开
标题翻译：三环化合物的新用途
公开(公告)号：US20080318958A1
公开(公告)日：2008-12-25
申请号：US12222773
申请日：2008-08-15
申请人： Natsuki Ishizuka , Katsunori Sakai , Kunio Hayashi
发明人： Natsuki Ishizuka , Katsunori Sakai , Kunio Hayashi
IPC分类号： A61K31/4418 , A61K31/505 , A61K31/4965 , A61K31/50 , A61K31/502 , A61K31/498 , A61K31/53 , A61K31/426 , A61K31/495 , A61P9/00
CPC分类号： C07D213/06 , A61K31/15 , A61K31/155 , A61K31/357 , A61K31/40 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/47 , A61K31/495 , A61K31/4965 , A61K31/498 , A61K31/50 , A61K31/502 , A61K31/505 , A61K31/53 , C07D213/16 , C07D213/30 , C07D213/40 , C07D213/64 , C07D215/04 , C07D237/08 , C07D237/12 , C07D237/14 , C07D239/26 , C07D239/52 , C07D241/12 , C07D241/42 , C07D251/30 , C07D257/04 , C07D277/22 , C07D277/24 , C07D319/20 , C07D401/10 , C07D405/10 , C07D409/04 , C07D409/10
摘要： Pharmaceutical compositions for enhancing the expression of apoAI are provided, which are used as medicaments for treatment of cardiovascular diseases on the basis of improving the functions of HDL.Pharmaceutical compositions for enhancing the expression of apoAI which comprises a compound of formula (I): in which X1 and X1 are independently an aryl or heteroaryl that may be optionally substituted, a hydrogen, a halogen, or the like; ring A is a benzene ring or 6-membered aromatic heterocyclic ring containing 1 to 3 N atoms that may be optionally condensed with another aromatic ring; R1 to R4 are independently a hydrogen, a halogen, a lower alkyl, a lower alkoxy or the like; a prodrug thereof, a pharmaceutically acceptable salt or solvate of them are disclosed.
摘要翻译：提供了用于增强载脂蛋白A表达的药物组合物，其用于治疗心血管疾病的药物，其基础是改善HDL的功能。用于增强载脂蛋白A表达的药物组合物，其包含式（I）化合物：其中X1和X1独立地为可任意取代的芳基或杂芳基，氢，卤素等; 环A是含有1〜3个N原子的苯环或6元芳族杂环，其可以任选地与另一个芳环稠合; R 1至R 4独立地为氢，卤素，低级烷基，低级烷氧基等; 公开了其前药，药学上可接受的盐或溶剂合物。

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