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1. 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。

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

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。

4. 发明授权

US08067396B2 Amino alcohol compounds or phosphonic acid derivatives thereof 有权
标题翻译：氨基醇化合物或其膦酸衍生物
公开(公告)号：US08067396B2
公开(公告)日：2011-11-29
申请号：US12460884
申请日：2009-07-24
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/675 , C07F9/28
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： A compound having a formula II(a): wherein R1 and R2 are hydrogen lower alkyl, lower aliphatic acyl, or lower alkoxycarbonyl; R4 is C1-C4 alkyl; n is 2 or 3; X is a formula ═N-D, wherein D is hydrogen, C1-C6 alkyl or phenyl; Y is ethylene, ethynylene, —CO—CH2—, —CH(OH)—CH2— or phenylene; Z is C1-C6 alkylene; R5 is C3-C10 cycloalkyl or C6-C10 aryl; R6 and R7 are hydrogen, lower alkyl, halogeno lower alkyl, lower alkoxy or lower alkylthio; and R10 and R11 are hydrogen or lower alkyl.
摘要翻译：具有式II（a）的化合物：其中R 1和R 2是氢低级烷基，低级脂族酰基或低级烷氧基羰基; R4是C1-C4烷基; n为2或3; X是式= N-D，其中D是氢，C 1 -C 6烷基或苯基; Y是亚乙基，亚乙炔基，-CO-CH 2 - ， - CH（OH）-CH 2 - 或亚苯基; Z是C1-C6亚烷基; R5是C3-C10环烷基或C6-C10芳基; R6和R7是氢，低级烷基，卤代低级烷基，低级烷氧基或低级烷硫基; R 10和R 11为氢或低级烷基。

5. 发明申请

US20070149597A1 Medicinal composition as immunosuppressant 审中-公开
标题翻译：药用组合物作为免疫抑制剂
公开(公告)号：US20070149597A1
公开(公告)日：2007-06-28
申请号：US11698698
申请日：2007-01-26
申请人： Takahide Nishi , Takaichi Shimozato , Takashi Kagari , Hiromi Doi
发明人： Takahide Nishi , Takaichi Shimozato , Takashi Kagari , Hiromi Doi
IPC分类号： A61K31/401 , A61K31/40 , A61K31/366 , A61K31/22
CPC分类号： C07D207/335 , A61K9/2018 , A61K9/2059 , A61K31/00 , A61K31/133 , A61K31/137 , A61K31/22 , A61K31/366 , A61K31/40 , A61K31/404 , A61K31/47 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： A pharmaceutical composition useful as a preventive or therapeutic agent for immune-related diseases. The pharmaceutical composition includes at least HMG-COA reductase inhibitor and at least one amino alcohol compound having the following formula (I), a pharmacologically acceptable salt thereof, or a pharmacologically acceptable ester thereof wherein R1 and R2 each represents hydrogen; R3 represents lower alkyl or hydroxymethyl; R4 represents hydrogen, alkyl, alkoxy or halogen; R5 represents hydrogen, halogeno, cyclohexyl or phenyl; X represents vinylene (CH═CH), oxygen, sulfur or methylated nitrogen; Y represents a single bond, oxygen, sulfur or carbonyl; Z represents a single bond or C1-C8 alkylene; n is 2 or 3.
摘要翻译：用作免疫相关疾病的预防或治疗剂的药物组合物。药物组合物至少包含HMG-COA还原酶抑制剂和至少一种具有下式（I）的氨基醇化合物，其药学上可接受的盐或其药理学上可接受的酯，其中R 1和R 2 各自表示氢; R 3表示低级烷基或羟甲基; R 4表示氢，烷基，烷氧基或卤素; R 5表示氢，卤代，环己基或苯基; X表示亚乙烯基（CH-CH），氧，硫或甲基化氮; Y表示单键，氧，硫或羰基; Z表示单键或C 1 -C 8亚烷基; n为2或3。

6. 发明授权

US07199150B2 Amino alcohol compounds 有权
标题翻译：氨基醇化合物
公开(公告)号：US07199150B2
公开(公告)日：2007-04-03
申请号：US10889657
申请日：2004-07-12
申请人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
发明人： Takahide Nishi , Takaichi Shimozato , Futoshi Nara , Shojiro Miyazaki
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/335 , C07D307/52 , C07D333/20 , C07F9/572 , C07F9/65515 , C07F9/655345 , Y02P20/55
摘要： Amino alcohol compounds and phosphonic acid compounds having excellent immunosuppressive activity, pharmacologically acceptable salts thereof and pharmacologically acceptable esters thereof, and pharmaceutical compositions comprising such compounds, the compounds having the following formula: wherein R1 and R2 each represent hydrogen, or a protecting group of the amino group; R3 represents hydrogen, or a protecting group of the hydroxyl group; R4 represents a lower alkyl group; n is 1 to 6; X represents oxygen or nitrogen, which is unsubstituted or substituted with a lower alkyl group; Y represents ethylene; Z represents a C1–C10 alkylene; R5 represents an aryl group; and R6 and R7 each represents hydrogen; provided that when R5 represents hydrogen, then Z represents a group other than a single bond or a straight chain C1–C10 alkylene group.
摘要翻译：具有优异的免疫抑制活性的氨基醇化合物和膦酸化合物，其药学上可接受的盐和药理学上可接受的酯，以及包含这些化合物的药物组合物，具有下式的化合物：

7. 发明授权

US07910617B2 Method for suppressing the number of peripheral blood lymphocytes using an amino alcohol compound 有权
标题翻译：使用氨基醇化合物抑制外周血淋巴细胞数的方法
公开(公告)号：US07910617B2
公开(公告)日：2011-03-22
申请号：US10588818
申请日：2005-02-23
申请人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
发明人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
IPC分类号： A61K31/40
CPC分类号： A61K31/40
摘要： A method for suppressing the number of peripheral blood lymphocytes involving administering to a human in need thereof a pharmaceutically effective amount of a compound which is (2R) -2-amino-2-methyl-4-{1-methyl-5-[4-(4-methylphenyl)butanoyl]pyrrol-2-yl}butan-1-ol or a pharmacologically acceptable salt thereof, such as the hydrochloride salt.
摘要翻译：一种抑制外周血淋巴细胞数量的方法，包括向有需要的人施用药学有效量的化合物，其是（2R）-2-氨基-2-甲基-4- {1-甲基-5- [4 - （4-甲基苯基）丁酰基]吡咯-2-基}丁-1-醇或其药理学上可接受的盐，例如盐酸盐。

8. 发明申请

US20100081702A1 PHARMACEUTICAL COMPOSITION FOR PROPHYLAXIS OR TREATMENT OF HEPATITIS 审中-公开
标题翻译：用于预防或治疗乙型肝炎的药物组合物
公开(公告)号：US20100081702A1
公开(公告)日：2010-04-01
申请号：US12624214
申请日：2009-11-23
申请人： Takaichi Shimozato , Takashi Kagari , Hiromi Doi
发明人： Takaichi Shimozato , Takashi Kagari , Hiromi Doi
IPC分类号： A61K31/40 , A61K31/381 , C07D207/333 , C07D333/22 , A61P1/16
CPC分类号： C07D207/335 , A61K31/381 , A61K31/404 , C07D333/22 , Y02A50/463
摘要： Object The present invention provides a pharmaceutical composition for prophylaxis or treatment of hepatitis.Solution A pharmaceutical composition for prophylaxis or treatment of hepatitis, comprising a compound represented by the general formula (I): wherein R1 represents a C1-C4 alkyl group, R2 and R3 which are the same or different represent a hydrogen atom, a C1-C4 alkyl group, or a C1-C4 alkoxy group, X represents a sulfur atom or a nitrogen atom substituted by a methyl group, and n represents an integer of 3 or 4, or a pharmacologically acceptable salt thereof as an active ingredient.
摘要翻译：发明内容本发明提供一种预防或治疗肝炎的药物组合物。溶液用于预防或治疗肝炎的药物组合物，其包含由通式（I）表示的化合物：其中R1表示C1-C4烷基，R2和R3可相同或不同，表示氢原子，C1- C4烷基或C1-C4烷氧基，X表示硫原子或被甲基取代的氮原子，n表示3或4的整数或其药理学上可接受的盐作为有效成分。

9. 发明申请

US20080113961A1 Heterocyclic compound 失效
标题翻译：杂环化合物
公开(公告)号：US20080113961A1
公开(公告)日：2008-05-15
申请号：US11975664
申请日：2007-10-19
申请人： Takahide Nishi , Tsuyoshi Nakamura , Yukiko Sekiguchi , Yumiko Mizuno , Takaichi Shimozato , Futoshi Nara
发明人： Takahide Nishi , Tsuyoshi Nakamura , Yukiko Sekiguchi , Yumiko Mizuno , Takaichi Shimozato , Futoshi Nara
IPC分类号： A61K31/4245 , C07D413/14
CPC分类号： C07D413/10 , C07D413/14
摘要： A compound having immunosuppressive activity with low toxicity or a pharmacological salt thereof. The compound has a general formula (I) shown below or a pharmacologically acceptable salt thereof, or a pharmacologically acceptable prodrug thereof
摘要翻译：具有低毒性的免疫抑制活性的化合物或其药理学盐。该化合物具有下述通式（I）或其药理学上可接受的盐或其药理学上可接受的前药

10. 发明申请

US20070191468A1 Amino alcohol compound 有权
标题翻译：氨基醇化合物
公开(公告)号：US20070191468A1
公开(公告)日：2007-08-16
申请号：US10588818
申请日：2005-02-23
申请人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
发明人： Takahide Nishi , Toshiyasu Takemoto , Shojiro Miyazaki , Takaichi Shimozato , Futoshi Nara , Takashi Izumi
IPC分类号： A61K31/401 , A61P1/04
CPC分类号： A61K31/40
摘要： A pharmaceutical composition is provided that has a low toxicity, demonstrates superior physicochemical properties and pharmacokinetics, and has superior peripheral blood lymphocyte count lowering activity. The pharmaceutical composition contains a compound having general formula (I): [Chemical Formula 1] (wherein R1 represents a methyl group or an ethyl group, R2 represents a methyl group or an ethyl group, and R3 represents a phenyl group substituted with 1 to 3 substituents selected from the group consisting of a halogen atom, a lower alkyl group, a cycloalkyl group, a lower alkoxy group, a halogeno lower alkyl group, a lower aliphatic acyl group and a cyano group), a pharmacologically acceptable salt thereof or a pharmacologically acceptable ester thereof.
摘要翻译：提供毒性低的药物组合物，具有优异的物理化学性质和药代动力学，并且具有优异的外周血淋巴细胞计数降低活性。药物组合物含有具有通式（I）的化合物：[化学式1]（其中R 1表示甲基或乙基，R 2表示甲基基团或乙基，R 3表示被1〜3个选自卤素原子，低级烷基，环烷基，低级烷氧基，低级烷氧基，卤代低级烷基，低级脂肪酰基和氰基），其药学上可接受的盐或其药理学上可接受的酯。

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