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1. 发明申请

US20060128756A1 Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses 审中-公开
标题翻译：杂芳基取代的吡咯衍生物，其制备及其治疗用途
公开(公告)号：US20060128756A1
公开(公告)日：2006-06-15
申请号：US11339390
申请日：2006-01-25
申请人： Tomio Kimura , Kazumasa Aoki , Akira Nakao , Shigeru Ushiyama , Takaichi Shimozato , Nobuyuki Ohkawa
发明人： Tomio Kimura , Kazumasa Aoki , Akira Nakao , Shigeru Ushiyama , Takaichi Shimozato , Nobuyuki Ohkawa
IPC分类号： C07D401/02 , A61K31/444 , C07D401/14
CPC分类号： C07D451/02 , C07D401/04 , C07D401/14 , C07D453/02 , C07D455/02 , C07D471/04 , C07D487/04
摘要： Compounds having activity against production of an inflammatory cytokine of formula (I)′: A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is (IIa)′, (IIb)′ or (IIc)′: m′ is 1; E′ is nitrogen; D′ is >C(R5′), R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 5-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′ is hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′ is alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′is oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.
摘要翻译：具有抗式产生式（I）的炎性细胞因子的活性化合物的化合物：A'是吡咯; R 1是苯基或萘基; R 2是吡啶基或嘧啶基; （IIa）'，（IIb）'或（IIc）'：m'为1; E'是氮; D'是> C（R 5'），R 5'是氢，取代基α'或取代基β'; B'是含氮5元杂环; R 4'是1至3个取代基α'，取代基β'和取代基γ'的取代基; R 1'和R 3'连接到与R 2'连接的吡咯原子相邻的吡咯的两个原子上; 取代基α'是羟基，硝基，氰基，卤素，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或-NR a R b B。 R a，O和R b'是氢，烷基，烯基，炔基，芳烷基或烷基磺酰基，或者R a'和R“ b'与氮原子形成杂环基; 取代基β'是烷基，烯基，炔基，芳烷基或环烷基; 取代基γ'是氧代，羟基亚氨基，烷氧基亚氨基，亚烷基，亚烷基二氧基，烷基亚磺酰基，烷基磺酰基，芳基，芳氧基，亚烷基或芳亚烷基。

2. 发明申请

US20050283006A1 Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses 审中-公开
标题翻译：杂芳基取代的吡咯衍生物，其制备及其治疗用途
公开(公告)号：US20050283006A1
公开(公告)日：2005-12-22
申请号：US10411061
申请日：2003-04-10
申请人： Tomio Kimura , Kazumasa Aoki , Akira Nakao , Shigeru Ushiyama , Takaichi Shimozato , Nobuyuki Ohkawa , Takayoshi Nagasaki , Takanori Yamazaki
发明人： Tomio Kimura , Kazumasa Aoki , Akira Nakao , Shigeru Ushiyama , Takaichi Shimozato , Nobuyuki Ohkawa , Takayoshi Nagasaki , Takanori Yamazaki
IPC分类号： C07D401/04 , C07D401/14 , C07D451/02 , C07D453/02 , C07D455/02 , C07D471/04 , C07D487/04 , C07D491/20 , C07D41/14 , C07D43/02
CPC分类号： C07D451/02 , C07D401/04 , C07D401/14 , C07D453/02 , C07D455/02 , C07D471/04 , C07D487/04
摘要： Compounds having activity against production of inflammatory cytokines of formula (I)′: A′ is pyrrole; R1′ is aryl or heteroaryl; R2′ is heteroaryl having at least one nitrogen atom; R3′ is (IIa)′, (IIb)′ or (IIc)′: m′ is 1 or 2; one of D′ and E′ is nitrogen and the other is >C(R5′)—, R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 4- to 7-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′: hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′: alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′: oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.
摘要翻译：具有抗式产生式（I）的炎性细胞因子的化合物的化合物：A'是吡咯; R 1是芳基或杂芳基; R 2是具有至少一个氮原子的杂芳基; （IIa）'，（IIb）'或（IIc）'：m'为1或2; D'和E'之一是氮，另一个是> C（R 5'） - ，R 5'是氢，取代基α'或取代基β'; B'是含氮的4-至7-元杂环; R 4'是1至3个取代基α'，取代基β'和取代基γ'的取代基; R 1'和R 3'连接到与R 2'连接的吡咯原子相邻的吡咯的两个原子上; 取代基α'：羟基，硝基，氰基，卤素，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或-NR a R b b。 R a，O和R b'是氢，烷基，烯基，炔基，芳烷基或烷基磺酰基，或者R a'和R“ b'与氮原子形成杂环基; 取代基β'：烷基，烯基，炔基，芳烷基或环烷基; 取代基γ'：氧代，羟基亚氨基，烷氧基亚氨基，亚烷基，亚烷基二氧基，烷基亚磺酰基，烷基磺酰基，芳基，芳氧基，亚烷基或芳烷基。

3. 发明申请

US20070049620A1 Cyclic tertiary amine compound 审中-公开
标题翻译：环状叔胺化合物
公开(公告)号：US20070049620A1
公开(公告)日：2007-03-01
申请号：US11301296
申请日：2005-12-12
申请人： Tomio Kimura , Nobuyuki Ohkawa , Akira Nakao , Takayoshi Nagasaki , Takaichi Shimozato
发明人： Tomio Kimura , Nobuyuki Ohkawa , Akira Nakao , Takayoshi Nagasaki , Takaichi Shimozato
IPC分类号： A61K31/444 , A61K31/4439 , C07D401/14 , C07D403/14
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444
摘要： A cyclic tertiary amine compound which is capable of inhibiting the production of inflammatory cytoines. The compound having a structure represented by the following formula (I): wherein A represents an optionally substituted trivalent group which is benzene, pyrimidine, pyrrole, pyridine, pyridazine, furan, thiopene, pyrazole, imidazole, isoxazole or isothiazole; R1 represents an aryl or a heteroaryl group, which is unsubstituted or substituted; R2 represents a heteroaryl group which is unsubtituted or substituted; and R3 represents a cyclic tertiary amino group, or a pharmacologically acceptable salt of the compound.
摘要翻译：能够抑制炎性细胞因子产生的环状叔胺化合物。具有由下式（I）表示的结构的化合物：其中A表示任选取代的三价基团，其为苯，嘧啶，吡咯，吡啶，哒嗪，呋喃，噻吩，吡唑，咪唑，异恶唑或异噻唑; R 1表示未取代或取代的芳基或杂芳基; R 2表示未取代或取代的杂芳基; R 3表示化合物的环状叔氨基或药理学上可接受的盐。

4. 发明申请

US20050159444A1 Bicyclic unsaturated tertiary amine compounds 审中-公开
标题翻译：双环不饱和叔胺化合物
公开(公告)号：US20050159444A1
公开(公告)日：2005-07-21
申请号：US11039423
申请日：2005-01-19
申请人： Tomio Kimura , Nobuyuki Ohkawa , Kazumasa Aoki , Akira Nakao , Takayoshi Nagasaki
发明人： Tomio Kimura , Nobuyuki Ohkawa , Kazumasa Aoki , Akira Nakao , Takayoshi Nagasaki
IPC分类号： A61K31/4745 , C07D455/02
CPC分类号： A61K31/4745 , C07D455/02
摘要： A bicyclic unsaturated tertiary amine compound capable of inhibiting the production of inflammatory cytokines. The compound has the following formula (I): wherein A represents pyrrole or pyrazole, R1 represents an aryl group or a heteroaryl group which may be substituted, R2 represents a heteroaryl group which may be substituted, and R3 represents an indolizine group, or a pharmacologically acceptable salt thereof, a pharmacologically acceptable ester thereof or a pharmacologically acceptable derivative thereof.
摘要翻译：能够抑制炎性细胞因子产生的双环不饱和叔胺化合物。化合物具有下式（I）：其中A表示吡咯或吡唑，R 1表示可被取代的芳基或杂芳基，R 2表示可以被取代的杂芳基，R 3表示中氮茚基，或其药理学上可接受的盐，其药理学上可接受的酯或其药理学上可接受的衍生物。

5. 发明授权

US07122666B2 Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses 失效
标题翻译：杂芳基取代的吡咯衍生物，其制备及其治疗用途
公开(公告)号：US07122666B2
公开(公告)日：2006-10-17
申请号：US10354648
申请日：2003-01-30
申请人： Tomio Kimura , Akira Nakao , Nobuyuki Ohkawa , Takayoshi Nagasaki , Takanori Yamazaki
发明人： Tomio Kimura , Akira Nakao , Nobuyuki Ohkawa , Takayoshi Nagasaki , Takanori Yamazaki
IPC分类号： C07D207/00 , C07D209/00
CPC分类号： C07D451/02 , C07D401/04 , C07D401/14 , C07D453/02 , C07D455/02 , C07D471/04 , C07D487/04
摘要： Compounds having activity against production of an inflammatory cytokine of formula (I)′: A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is (IIa)′, (IIb)′ or (IIc)′: m′ is 1; E′ is nitrogen; D′ is >C(R5′)—, R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 5-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′ is hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′ is alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′ is oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.
摘要翻译：具有抗式产生式（I）的炎性细胞因子的活性化合物的化合物：A'是吡咯; R 1是苯基或萘基; R 2是吡啶基或嘧啶基; （IIa）'，（IIb）'或（IIc）'：m'为1; E'是氮; D'是> C（R 5'） - ，R 5'是氢，取代基α'或取代基β'; B'是含氮5元杂环; R 4'是1至3个取代基α'，取代基β'和取代基γ'的取代基; R 1'和R 3'连接到与R 2'连接的吡咯原子相邻的吡咯的两个原子上; 取代基α'是羟基，硝基，氰基，卤素，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基或-NR a R b B。 R a，O和R b'是氢，烷基，烯基，炔基，芳烷基或烷基磺酰基，或者R a'和R“ b'与氮原子形成杂环基; 取代基β'是烷基，烯基，炔基，芳烷基或环烷基; 取代基γ'是氧代，羟基亚氨基，烷氧基亚氨基，亚烷基，亚烷基二氧基，烷基亚磺酰基，烷基磺酰基，芳基，芳氧基，亚烷基或芳亚烷基。

6. 再颁专利

USRE43858E1 Substituted cycloalkene derivative 有权
标题翻译：取代的环烯烃衍生物
公开(公告)号：USRE43858E1
公开(公告)日：2012-12-11
申请号：US13224745
申请日：2006-09-13
申请人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
发明人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
IPC分类号： A61K31/335 , C07D317/72
摘要： A compound of formula (I) Wherein X, Y, ring A, ring B, l, m, R1, R2, R4 and R5 are as defined herein, to supress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-α, pharmacologically acceptable salts therefor, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.
摘要翻译：式（I）化合物其中X，Y，环A，环B，l，m，R 1，R 2，R 4和R 5如本文所定义，以抑制由内毒素诱导的细胞内信号转导或细胞活化并抑制细胞反应由于细胞内信号转导和细胞活化，例如过量产生炎症介质如TNF-α，其药理学上可接受的盐，其制备方法，以及含有上述取代的环烯烃衍生物作为活性成分的药物，其优于与细胞内信号转导或由内毒素诱导的细胞活化以及对细胞内信号转导和细胞的细胞反应相关的诸如败血症（败血症休克，弥散性血管内凝血，多器官功能衰竭等）的疾病的预防和/或治疗激活。

7. 发明申请

US20090233952A1 SUBSTITUTED CYCLOALKENE DERIVATIVE 有权
公开(公告)号：US20090233952A1
公开(公告)日：2009-09-17
申请号：US12066813
申请日：2006-09-13
申请人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
发明人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
IPC分类号： A61K31/443 , C07D317/72 , A61K31/357 , C07D405/08 , A61K31/4025 , C07D319/04 , C07D405/10
CPC分类号： C07C311/14 , C07C2601/16 , C07C2602/50 , C07D303/38 , C07D307/94 , C07D317/72 , C07D319/08 , C07D321/10 , C07D327/04 , C07D339/06 , C07D339/08 , C07D493/04 , C07D493/10
摘要： [Object] To provide a substituted cycloalkene derivative having an action to suppress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-α, pharmacologically acceptable salts therefor, a medicament containing them as an active ingredient, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.[Solution] A compound represented by the general formula (I): {whereinX and Y represent a group in which X and Y together with a carbon atom to which they are bound form ring A (the ring is 3- to 7-membered heterocyclyl ring or 3- to 7-membered cycloalkyl ring), each represents a hydrogen atom, or X and Y together represent a substituent of ring B. l and m, independently from each other, represent an integer of 0 to 3, and l+m is 1 to 3. R1 is an aliphatic hydrocarbon group and the like which may be substituted with a group selected from Substituent group β and Substituent group γ. n represents an integer of 0 to 3. R2 is a C1-C6 alkyl group and the like which may be substituted with a group selected from a hydrogen atom and Substituent group β. R3 is a phenyl group, 5- to 6-membered heteroaryl group and the like which may be substituted with a group selected from Substituent group ε. R5 is a C1-C6 alkyl group and the like which may be substituted with a group selected from a hydrogen atom and Substituent group β. Provided that in the case where R3 is a phenyl group which may be substituted with a group selected from Substituent group ε, X and Y represent a group in which X and Y together with a carbon atom to which they are bound form ring A, or X and Y together represent a substituent of ring B.

8. 发明授权

US07935835B2 Substituted cycloalkene derivative 有权
标题翻译：取代的环烯烃衍生物
公开(公告)号：US07935835B2
公开(公告)日：2011-05-03
申请号：US12066813
申请日：2006-09-13
申请人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
发明人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
IPC分类号： C07D319/00 , C07D315/00 , C07D327/00
CPC分类号： C07C311/14 , C07C2601/16 , C07C2602/50 , C07D303/38 , C07D307/94 , C07D317/72 , C07D319/08 , C07D321/10 , C07D327/04 , C07D339/06 , C07D339/08 , C07D493/04 , C07D493/10
摘要： A compound of formula (I) Wherein X, Y, ring A, ring B, l, m, R1, R2, R4 and R5 are as defined herein, to supress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-α, pharmacologically acceptable salts therefor, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.
摘要翻译：式（I）化合物其中X，Y，环A，环B，l，m，R 1，R 2，R 4和R 5如本文所定义，以抑制由内毒素诱导的细胞内信号转导或细胞活化并抑制细胞反应由于细胞内信号转导和细胞活化，例如过量产生炎症介质如TNF-α，其药理学上可接受的盐，其制备方法，以及含有上述取代的环烯烃衍生物作为活性成分的药物，其优于与细胞内信号转导或由内毒素诱导的细胞活化以及对细胞内信号转导和细胞的细胞反应相关的诸如败血症（败血症休克，弥散性血管内凝血，多器官功能衰竭等）的疾病的预防和/或治疗激活。

9. 发明申请

US20130178521A1 Crystals of Substituted Cycloalkene Derivatives 有权
标题翻译：取代的环烯烃衍生物的晶体
公开(公告)号：US20130178521A1
公开(公告)日：2013-07-11
申请号：US13825875
申请日：2011-09-22
申请人： Nobuyuki Ohkawa , Kouki Iida , Takayoshi Nagasaki
发明人： Nobuyuki Ohkawa , Kouki Iida , Takayoshi Nagasaki
IPC分类号： C07D317/72
CPC分类号： C07D317/72 , A61K31/357
摘要： To provide potassium salts of substituted pyrrolidine derivatives, which suppress the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, and crystals thereof. The present invention provides potassium(2-chloro-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide and potassium(2-bromo-4-fluorophenyl){[(2R,3R,8R)-7-(ethoxycarbonyl)-2,3-bis(hydroxymethyl)-1,4-dioxaspiro[4.5]deca-6-en-8-yl]sulfonyl}azanide, each of which suppresses the production of an inflammatory mediator caused by intracellular signal transduction or cell activation induced by endotoxin, crystals thereof, and a pharmaceutical containing any of the same, and a prophylactic and/or therapeutic agent for sepsis containing any of the same.
摘要翻译：提供抑制由内毒素诱导的细胞内信号转导或细胞活化引起的炎性介质的产生的取代的吡咯烷衍生物的钾盐及其结晶。本发明提供了（2-氯-4-氟苯基）{[（2R，3R，8R）-7-（乙氧基羰基）-2,3-双（羟甲基）-1,4-二氧杂螺[4.5]十碳六（2-溴-4-氟苯基）{[（2R，3R，8R）-7-（乙氧基羰基）-2,3-双（羟甲基）二氧杂螺[4.5]十碳-6-烯-8-基]磺酰基}吖庚因，其各自抑制由内毒素诱导的细胞内信号转导或细胞活化引起的炎性介质的产生，其晶体和含有以及含有任何相同的败血症的预防和/或治疗剂。

10. 发明授权

US5559109A Method of treating a PAF-mediated pathology or for treating or preventing psoriasis, nephritis, asthma or shock by administering a PAF antagonist 失效
标题翻译：通过施用PAF拮抗剂治疗PAF介导的病理学或治疗或预防牛皮癣，肾炎，哮喘或休克的方法
公开(公告)号：US5559109A
公开(公告)日：1996-09-24
申请号：US320444
申请日：1994-10-07
申请人： Norio Nakamura , Nobuyuki Ohkawa , Takeshi Oshima , Masaaki Miyamoto , Yasuteru Iijima
发明人： Norio Nakamura , Nobuyuki Ohkawa , Takeshi Oshima , Masaaki Miyamoto , Yasuteru Iijima
IPC分类号： C07D213/56 , C07D243/08 , C07D295/185 , C07D295/192 , C07D295/194 , C07D295/26 , C07D317/60 , C07D333/24 , A61K31/55 , A61K31/40 , A61K31/495
CPC分类号： C07D295/185 , C07D213/56 , C07D243/08 , C07D295/192 , C07D295/194 , C07D295/26 , C07D317/60 , C07D333/24 , Y10S514/826 , Y10S514/863 , Y10S514/886 , Y10S514/921 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要： A method of treating a PAF-mediated pathology or for treating or preventing psoriasis, nephritis, asthma, inflammation or shock by administering an effective amount of a PAF antagonist of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each --R.sup.5, --CH.dbd.CH--R.sup.5 or --C.tbd.C--R.sup.5 ; R.sup.5 is an unsubstituted or substituted C.sub.6 -C.sub.14 carbocyclic aryl of an aromatic heterocyclic having from 5 to 14 ring atoms, of which from 1 to 5 are hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur, the heterocyclic group being unsubstituted or substituted; R.sup.3 is hydrogen, a C.sub.1 -C.sub.6 alkyl, cyano, or --R.sup.5 ; X is oxygen or sulfur; A is a 1,4-piperazin-1,4-diyl or a 1,4-homopiperazin-1,4-diyl; B is a C.sub.1 -C.sub.6 alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl; and R.sup.4 is an unsubstituted or substituted phenyl group.
摘要翻译：一种通过施用有效量的式-R5或-C 3BOND C-R5的PAF拮抗剂来治疗PAF介导的病理学或治疗或预防牛皮癣，肾炎，哮喘，炎症或休克的方法; R5是具有5至14个环原子的芳族杂环的未取代或取代的C6-C14碳环芳基，其中1至5个是选自氮，氧和硫的杂原子，杂环基团是未取代的或取代; R3是氢，C1-C6烷基，氰基或-R5; X是氧或硫; A是1,4-哌嗪-1,4-二基或1,4-高哌嗪-1,4-二基; B是C1-C6亚烷基，羰基，硫代羰基，亚磺酰基或磺酰基; R4是未取代或取代的苯基。

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