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1. 发明专利

JP2012102124A Compound having s1p receptor binding potency, and use thereof 有权
标题翻译：具有S1P受体结合点的化合物及其用途
公开(公告)号：JP2012102124A
公开(公告)日：2012-05-31
申请号：JP2011286064
申请日：2011-12-27
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： HABASHITA HIROSHI , NAKADE SHINJI
IPC分类号： C07C217/58 , A61K31/137 , A61K31/155 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/197 , A61K31/27 , A61K31/275 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/404 , A61K31/407 , A61K31/417 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/438 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5375 , A61K31/54 , A61K31/55 , A61K31/551 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C235/48 , C07C311/51 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/333 , C07D209/40 , C07D211/10 , C07D211/46 , C07D211/60 , C07D211/70 , C07D213/36 , C07D213/71 , C07D213/74 , C07D213/85 , C07D215/12 , C07D215/18 , C07D217/04 , C07D233/64 , C07D239/42 , C07D241/04 , C07D241/24 , C07D261/10 , C07D265/30 , C07D271/06 , C07D277/04 , C07D277/28 , C07D295/08 , C07D295/10 , C07D295/18 , C07D307/00 , C07D307/38 , C07D317/58 , C07D333/20 , C07D333/34 , C07D333/58 , C07D413/12 , C07D487/08 , C07D491/113
CPC分类号： C07C217/60
摘要： PROBLEM TO BE SOLVED: To provide safety medicaments with less side effect, exerting high immunosuppressive effect.SOLUTION: There are provided a compound represented by general formula (I) (wherein rings A and D are each a cyclic group which may have a substituent; E and G are each a bond or a spacer having 1 to 8 atoms in its main chain; L is hydrogen or a substituent; X is an amino group which may have a substituent or a heterocyclic group which contains at least one nitrogen atom and which may have a substituent; and n is 0 to 3, wherein when n is 2 or more, multiple rings A are the same or different), the salt thereof, N-oxide body thereof, a solvate thereof or their prodrugs thereof and the medicaments containing them. The compound represented by formula (I) is capable of binding S1P (sphingosine-1-phosphoric acid) receptors (in particular, EDG-1 and/or EDG-6), and is useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases and the like.
摘要翻译：要解决的问题：提供具有较少副作用的安全性药物，发挥高免疫抑制作用。提供由通式（I）表示的化合物（其中环A和D各自为可以具有取代基的环状基团; E和G各自为键或具有1至8个原子的间隔基其主链; L是氢或取代基; X是可以具有取代基的氨基或含有至少一个氮原子并且可以具有取代基的杂环基;并且n是0至3，其中当n是 2个以上，多个环A相同或不同），其盐，N-氧化物体，其溶剂合物或其前药以及含有它们的药物。由式（I）表示的化合物能够结合S1P（鞘氨醇-1-磷酸）受体（特别是EDG-1和/或EDG-6），并且可用于预防和/或治疗移植排斥反应，自身免疫性疾病，过敏性疾病等。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2013151528A Compound capable of binding s1p receptor and pharmaceutical use thereof 有权
标题翻译：结合S1P受体的化合物及其药物应用
公开(公告)号：JP2013151528A
公开(公告)日：2013-08-08
申请号：JP2013048980
申请日：2013-03-12
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： NAKADE SHINJI , MIZUNO HIROKI , ONO TAKEJI , MINAMI SHINJI , SAGA HIROSHI , HAGIYA HIROSHI , KOMIYA TAKAKI , HABASHITA HIROSHI , KURATA HARUTO , OTSUKI KAZUHIRO , KUSUMI KENSUKE
IPC分类号： C07C47/27 , A61K20060101 , A61K31/11 , A61K31/135 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/222 , A61K31/27 , A61K31/277 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/472 , A61K45/00 , A61P1/04 , A61P9/10 , A61P11/06 , A61P17/04 , A61P19/02 , A61P21/04 , A61P29/00 , A61P31/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07B61/00 , C07C69/734 , C07C229/14 , C07C229/22 , C07C229/36 , C07C233/47 , C07C255/16 , C07C255/38 , C07C255/41 , C07C271/22 , C07C317/18 , C07D205/04 , C07D207/16 , C07D211/04 , C07D211/60 , C07D211/62 , C07D217/04 , C07D333/16 , C07D405/06
CPC分类号： C07C229/36 , A61K31/197 , A61K31/198 , A61K31/397 , A61K31/401 , A61K31/44 , A61K31/445 , A61K45/06 , C07C229/14 , C07C229/22 , C07C229/34 , C07C233/47 , C07C255/16 , C07C255/41 , C07C271/22 , C07C323/12 , C07D205/04 , C07D207/16 , C07D211/62 , C07D211/70 , C07D217/04
摘要： PROBLEM TO BE SOLVED: To provide compounds capable of binding S1P receptor (particularly, EDG-6, preferably, EDG-1 and EDG-6).SOLUTION: There are provided compounds such as methyl-3-[4-(3-phenylpropoxy)phenyl]propanoate, salts thereof, solvated materials thereof, or prodrugs thereof. The compounds are capable of binding S1P receptors (in particular, EDG-6, preferably, EDG-1 and EDG-6), and are useful for preventing and/or treating rejection in transplantation, graft versus host diseases, autoimmune diseases, allergic diseases and the like.
摘要翻译：要解决的问题：提供能够结合S1P受体（特别是EDG-6，优选EDG-1和EDG-6）的化合物。溶液：提供化合物，例如甲基-3- [4-（3-苯基丙氧基）苯基]丙酸酯，其盐，溶剂化物或其前药。这些化合物能够结合S1P受体（特别是EDG-6，优选EDG-1和EDG-6），并且可用于预防和/或治疗移植排斥反应，移植物抗宿主病，自身免疫性疾病，过敏性疾病等等。

3. 发明专利

JP2004196822A Triazaspiro[5.5]undecane derivatives and drugs containing the same as the active ingredient 审中-公开
公开(公告)号：JP2004196822A
公开(公告)日：2004-07-15
申请号：JP2004066592
申请日：2004-03-10
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： HABASHITA HIROSHI , HAMANO SHINICHI , SHIBAYAMA SHIRO , TAKAOKA YOSHIKAZU
IPC分类号： C07D471/10 , A61K31/499 , A61K31/5377 , A61P1/04 , A61P1/16 , A61P3/10 , A61P11/06 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/06 , A61P37/08
摘要： PROBLEM TO BE SOLVED: To provide triazaspiro[5.5]undecane derivatives, and a drug containing the same as the active ingredient. SOLUTION: Triazaspiro[5.5]undecane derivatives of formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R 1 is formula (II) or formula (III); R 2 is an alkyl or alkynyl etc.; R 3 , R 4 are each H, a (substituted) alkyl etc., or R 3 and R 4 together to form formula (IV); R 5 is H or an alkyl). Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc. COPYRIGHT: (C)2004,JPO&NCIPI

4. 发明专利

JP2007015927A Heterocyclic bicyclo ring compound and heterocyclic tricyclo ring compound and medicine comprising the same 审中-公开
标题翻译：杂环双环环化合物和杂环三环环化合物和包含它们的药物
公开(公告)号：JP2007015927A
公开(公告)日：2007-01-25
申请号：JP2003349033
申请日：2003-10-08
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： SHIBAYAMA SHIRO , HABASHITA HIROSHI
IPC分类号： C07D487/08 , A61K31/55 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/02 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/14 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08
摘要： PROBLEM TO BE SOLVED: To obtain a compound having a CXCR3 antagonism and a medicine composition containing the same. SOLUTION: The compound is represented by general formula 1 (ring A is a heterocyclic bicyclo ring or tricyclo ring; Ring B is a cyclic group such as a phenyl ring or the like; Y is a spacer having 1-4 atoms of main chain), its salt, its solvate or its prodrug. The medicine composition comprises the compound, its salt, its solvate or its prodrug. The medicine composition comprises one kind or a combination of two or more kinds of a nonsteroid-based antiinflammatory agent, antirheumatic medicine, immunosuppressive agent, TNFα inhibitor, prostaglandin synthase inhibitor, IL-6 inhibitor, interferon γ agonist, etc., such as 1,3,3-trimethyl-6-(4-nitrobenzoyl)-6-azabicyclo[3.2.1]octane, etc. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：待解决的问题：获得具有CXCR3拮抗作用的化合物和含有该化合物的药物组合物。解决方案：化合物由通式1表示（环A是杂环双环或三环）;环B是环基，例如苯环等; Y是具有1-4个原子的间隔基主链），其盐，其溶剂化物或其前药。药物组合物包含化合物，其盐，其溶剂合物或其前药。药物组合物包含一种或两种或更多种非甾体类抗炎剂，抗风湿药，免疫抑制剂，TNFα抑制剂，前列腺素合酶抑制剂，IL-6抑制剂，干扰素γ激动剂等的一种或组合，例如1 ，3,3-三甲基-6-（4-硝基苯甲酰基）-6-氮杂双环[3.2.1]辛烷等。版权所有（C）2007，JPO＆INPIT

5. 发明专利

JP2004359641A Ccr5 activator 审中-公开
公开(公告)号：JP2004359641A
公开(公告)日：2004-12-24
申请号：JP2003162764
申请日：2003-06-06
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： SHIBAYAMA SHIRO , SUGIYAMA TETSUYA , HABASHITA HIROSHI
IPC分类号： C07D471/10 , A61K31/438 , A61K31/499 , A61P1/04 , A61P1/16 , A61P3/10 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08
摘要： PROBLEM TO BE SOLVED: To provide a CCR5 activator having various actions such as CCR5 activating action, action to induce the migration activity to a CCR5 expression cell, action to induce desensitization of CCR5 and action to induce the internalization of CCR5 and, accordingly, useful as various medicines. SOLUTION: This CCR5 activator contains a compound expressed by formula (I), its salt or their prodrugs. In formula (I), the ring A is a nitrogen-containing mono-, di- or tricyclic heterocyclic group which may have substituents; the ring B is a 5 or 6-membered nitrogen-containing heterocyclic group which may have substituents; W is H, a (substituted)hydrocarbon group or a (substituted)heterocyclic group; and Y is a bond or a main-chain spacer containing 1-10 atoms. COPYRIGHT: (C)2005,JPO&NCIPI

6. 发明专利

JP2014240432A Ｓ１Ｐ受容体結合能を有する化合物およびその医薬用途有权
标题翻译： S1P受体结合能力的化合物及其医疗用途
公开(公告)号：JP2014240432A
公开(公告)日：2014-12-25
申请号：JP2014190026
申请日：2014-09-18
申请人：小野薬品工業株式会社 , Ono Pharmaceut Co Ltd
发明人： NAKADE SHINJI , MIZUNO HIROKI , ONO TAKEJI , MINAMI SHINJI , SAGA HIROSHI , HAGIYA HIROSHI , KOMIYA TAKAKI , HABASHITA HIROSHI , KURATA HARUTO , OTSUKI KAZUHIRO , KUSUMI KENSUKE
IPC分类号： C07D205/04 , A61K20060101 , A61K31/11 , A61K31/135 , A61K31/197 , A61K31/198 , A61K31/222 , A61K31/27 , A61K31/277 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/405 , A61K31/47 , A61K31/472 , A61K45/00 , A61P1/04 , A61P3/10 , A61P11/00 , A61P11/06 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C229/14 , C07C229/22 , C07C229/36 , C07C233/47 , C07C255/16 , C07C255/41 , C07C271/22 , C07D207/16 , C07D209/08 , C07D211/04 , C07D211/22 , C07D211/60 , C07D211/62 , C07D217/04 , C07D405/06
CPC分类号： C07C229/36 , A61K31/197 , A61K31/198 , A61K31/397 , A61K31/401 , A61K31/44 , A61K31/445 , A61K45/06 , C07C229/14 , C07C229/22 , C07C229/34 , C07C233/47 , C07C255/16 , C07C255/41 , C07C271/22 , C07C323/12 , C07D205/04 , C07D207/16 , C07D211/62 , C07D211/70 , C07D217/04
摘要：【課題】S1P受容体(特にEDG−6、好ましくはEDG−1およびEDG−6)結合能を有する化合物の提供。【効果】一般式(I)で示される本発明化合物、その塩、その溶媒和物、またはそれらのプロドラッグはS1P受容体(特にEDG−6、好ましくはEDG−1およびEDG−6)結合能を有し、移植に対する拒絶反応、移植片対宿主病、自己免疫性疾患、アレルギー性疾患等の予防および/または治療に有用である。(式中、環Aは環状基;環Bは置換基を有していてもよい環状基;Xは主鎖の原子数1〜8のスペーサー等;Yは主鎖の原子数1〜10のスペーサー等;nは0、1;nが0の場合、mは1、かつR1は水素原子、置換基;nが1の場合、mは0、1〜7の整数、かつR1は置換基、かつmが2以上のときR1は同じでも異なっていてもよい)。【選択図】なし
摘要翻译：要解决的问题：提供具有化合物的S1P受体（特别是EDG-6，优选EDG-1和EDG-6）结合能力。溶液：通式（I）的化合物，其盐，其溶剂合物或前药具有S1P受体（特别是EDG-6，优选EDG-1和EDG-6）结合能力，并且可用于预防和/或治疗针对移植，移植物抗宿主病，自身免疫疾病，过敏性疾病等的排斥反应。（其中环A为环状基团;环B为可以具有取代基的环状基团; X为原子序数为1〜8的主链间隔基等，Y为主链间隔基或其原子序数为1〜10; n为0,1; n为0时，m为1，R为氢原子，取代基为n，n为1，m为0〜7的整数， R是取代基，当m为2以上时，可以相同或不同）。

7. 发明专利

JP2012031201A Pharmaceutical composition for treatment of disease due to vascular constriction or vasodilation 有权
标题翻译：用于治疗由血管扩张或血管扩张引起的疾病的药物组合物
公开(公告)号：JP2012031201A
公开(公告)日：2012-02-16
申请号：JP2011239881
申请日：2011-11-01
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： NAKADE SHINJI , SUZUKI HIDEHIRO , HABASHITA HIROSHI
IPC分类号： C07D211/48 , A61K31/437 , A61K31/445 , A61K31/451 , A61K31/4545 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P9/14 , A61P13/12 , A61P25/06 , A61P43/00 , C07D211/52 , C07D401/12 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/445 , C07D211/48
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic and/or preventing agent for a disease due to vascular constriction or vasodilation comprising an EDG-5 modulator EDG (Endothelia differentiation gene)-5 modulator; and also to provide a new EDG-5 antagonist.SOLUTION: A therapeutic and/or preventing agent for a disease due to vascular constriction or vasodilation comprises a EDG-5 modulator. Since EDG-5 modulator specifically binds EDG-5 and shows antagonistic or agonistic action, EDG-5 antagonist is useful for treating and/or preventing for a disease due to vascular constriction, for example, cerebrovascular spasmodic disorder after subarachnoid hemorrhage or stroke, cardiovasucular spasmodic disorder, hypertension, renal disease, cardiac infarction, cardiac angina, arrhythmia, facilitation of the portal blood pressure involved in liver cirrhosis, varicosity involved in liver cirrhosis and the like; or EDG-5 agonist is useful for treating and/or preventing for a disease due to vasodilation of blood vessels, for example, chronic headache (such as migraine, tension-type headache, mixed-type headache thereof, or migrainous neuralgia), haemorrhoid, congestive disorder and the like.
摘要翻译：要解决的问题：提供由于包含EDG-5调节剂EDG（内皮分化基因）-5调节剂的血管收缩或血管舒张引起的疾病的治疗和/或预防剂; 并提供新的EDG-5拮抗剂。解决方案：由于血管收缩或血管舒张引起的疾病的治疗和/或预防剂包括EDG-5调节剂。由于EDG-5调节剂特异性结合EDG-5并且具有拮抗作用或激动作用，因此EDG-5拮抗剂可用于治疗和/或预防由于血管收缩引起的疾病，例如蛛网膜下腔出血或中风后的脑血管性痉挛障碍痉挛性疾病，高血压，肾脏疾病，心肌梗死，心脏心绞痛，心律失常，促进肝硬化引起的门静脉血压，涉及肝硬化的静脉曲张等; 或EDG-5激动剂可用于治疗和/或预防由于血管血管扩张引起的疾病，例如慢性头痛（如偏头痛，紧张型头痛，混合型头痛或偏头痛神经痛），痔疮，充血障碍等。版权所有（C）2012，JPO＆INPIT

8. 发明专利

JP2009137969A Aminocarboxylic acid derivative and medicinal use thereof 有权
标题翻译：氨基甲酰胆酸衍生物和药物用途
公开(公告)号：JP2009137969A
公开(公告)日：2009-06-25
申请号：JP2008315456
申请日：2008-12-11
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： HABASHITA HIROSHI , KURATA HARUTO , NAKADE SHINJI
IPC分类号： C07C229/14 , A61K31/216 , A61K31/397 , A61K31/4035 , A61K31/4245 , A61K31/437 , A61K31/44 , A61K31/4725 , A61K31/69 , A61K31/695 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D205/04 , C07D205/12 , C07D209/44 , C07D211/70 , C07D271/06 , C07D409/06 , C07D413/04 , C07D471/04 , C07F5/04 , C07F7/18
CPC分类号： C07F5/027 , A61K31/12 , A61K31/166 , A61K31/197 , A61K31/215 , A61K31/397 , A61K31/4035 , A61K31/41 , A61K31/437 , A61K31/4409 , A61K31/4412 , A61K31/4439 , A61K31/4725 , A61K31/55 , A61K31/69 , A61K45/06 , C07C229/14 , C07C2602/10 , C07D205/04 , C07D211/70 , C07D271/06 , C07D401/12 , C07D409/06 , C07D471/04 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a compound represented by formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same, wherein all symbols are described in the specification. SOLUTION: The compound represented by formula (I) has ability to bind to an S1P receptor (particularly, EDG-1, EDG-6 and/or EDG-8), and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供由式（I）表示的化合物，其盐，其N-氧化物形式，其溶剂化物或其前药，以及含有该化合物的药物，其中所有符号为在说明书中描述。解决方案：由式（I）表示的化合物具有与S1P受体（特别是EDG-1，EDG-6和/或EDG-8）结合的能力，并且可用于预防和/或治疗排斥反应移植物抗宿主病，自身免疫性疾病，过敏性疾病，神经变性疾病等。版权所有（C）2009，JPO＆INPIT

9. 发明专利

JP2007015930A Heterocyclic bicyclo ring and heterocyclic tricyclo ring compounds and drugs comprising the same 审中-公开
标题翻译：杂环双环环和杂环三环环化合物和包含它们的药物
公开(公告)号：JP2007015930A
公开(公告)日：2007-01-25
申请号：JP2004266040
申请日：2004-09-13
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： HABASHITA HIROSHI , SUZUKI AKIRA , SHIBAYAMA SHIRO , TANIHIRO TATSUYA , KANEKO YOUSUKE , EGASHIRA HIROSHI , NISHIYAMA HIDEJI , YAMATSUTA KATSURA , FUJITA SETSUKO
IPC分类号： C07D209/52 , A61K31/403 , A61K45/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To provide a compound having antagonism to CXCR3 or having 11β-HSD1 inhibitory effect. SOLUTION: The compound having antagonism to CXCR3 is useful in preventing and/or treating CXCR3-mediated diseases such as inflammation or allergic diseases, metabolic or endocrine diseases, cancer, infectious diseases or diseases accompanying infection. The compound having 11β-HSD1 inhibitory effect is useful in preventing and/or treating diseases caused by the excess production of cortisol such as type II diabetes, impaired glucose tolerance, hyperglycemia, insulin resistance, lipid metabolic error, lipemia, hyperlipemia, hypertriglyceridemia, obesity, atherosclerosis, syndrome X, Cushing's syndrome, hypertension, cognitive impairment, memory impairment, depression, anxiety, dementia, Alzheimer's disease, osteoporosis, glaucoma, or immune diseases. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供对CXCR3具有拮抗作用或具有11β-HSD1抑制作用的化合物。解决方案：对CXCR3具有拮抗作用的化合物可用于预防和/或治疗CXCR3介导的疾病如炎症或过敏性疾病，代谢或内分泌疾病，癌症，感染性疾病或伴随感染的疾病。具有11β-HSD1抑制作用的化合物可用于预防和/或治疗由过量产生皮质醇引起的疾病，例如II型糖尿病，葡萄糖耐量降低，高血糖症，胰岛素抵抗，脂代谢异常，脂血症，高脂血症，高甘油三酯血症，肥胖症，动脉粥样硬化，X综合症，库兴综合征，高血压，认知障碍，记忆障碍，抑郁，焦虑，痴呆，阿尔茨海默病，骨质疏松症，青光眼或免疫疾病。版权所有（C）2007，JPO＆INPIT

10. 发明专利

JP2011057688A Compound capable of binding s1p receptor and pharmaceutical use thereof 有权
标题翻译：结合S1P受体的化合物及其药物应用
公开(公告)号：JP2011057688A
公开(公告)日：2011-03-24
申请号：JP2010242153
申请日：2010-10-28
申请人： Ono Pharmaceut Co Ltd , 小野薬品工業株式会社
发明人： NAKADE SHINJI , MIZUNO HIROKI , ONO TAKEJI , MINAMI SHINJI , SAGA HIROSHI , HAGIYA HIROSHI , KOMIYA TAKAKI , HABASHITA HIROSHI , KURATA HARUTO , OTSUKI KAZUHIRO , KUSUMI KENSUKE
IPC分类号： C07C229/12 , A61K20060101 , A61K31/11 , A61K31/135 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/222 , A61K31/27 , A61K31/277 , A61K31/325 , A61K31/337 , A61K31/38 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/445 , A61K31/472 , A61K45/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07C229/14 , C07C229/22 , C07C229/36 , C07C233/47 , C07C255/16 , C07C255/41 , C07C271/22 , C07C317/36 , C07D205/04 , C07D207/16 , C07D207/34 , C07D211/04 , C07D211/60 , C07D211/62 , C07D217/04 , C07D333/32 , C07D405/06
CPC分类号： C07C229/36 , A61K31/197 , A61K31/198 , A61K31/397 , A61K31/401 , A61K31/44 , A61K31/445 , A61K45/06 , C07C229/14 , C07C229/22 , C07C229/34 , C07C233/47 , C07C255/16 , C07C255/41 , C07C271/22 , C07C323/12 , C07D205/04 , C07D207/16 , C07D211/62 , C07D211/70 , C07D217/04
摘要： PROBLEM TO BE SOLVED: To provide a compound having an ability to bind to a sphingosine-1-phosphate (hereinafter referred to as S1P in some cases) receptor which is useful as a medicament and to provide a medicament containing the same as an active ingredient.
SOLUTION: The compounds represented by formula (IA-1-1), salts thereof, solvates thereof or compounds in which carboxyl groups thereof are esterified. A compound having an ability to bind to an S1P receptor, (in particular EDG-6, preferably EDG-1 and EDG-6), for example the compounds represented by general formula (IA-1-1), salts thereof, solvates thereof or their prodrug have an ability to bind to the S1P receptor, (in particular EDG-6, preferably EDG-1 and EDG-6), and they are useful as preventives and/or remedies in rejection in transplantation, rejection of a transplanted organ, transplantation versus host disease, autoimmune diseases, allergic diseases and the like.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供具有与用作药物的鞘氨醇-1-磷酸酯（以下称为S1P）的受体结合能力的化合物，并提供含有其的药物活性成分。解决方案：由式（IA-1-1）表示的化合物，其盐，溶剂合物或其羧基被酯化的化合物。具有与S1P受体（特别是EDG-6，优选EDG-1和EDG-6）结合的能力的化合物，例如由通式（IA-1-1）表示的化合物，其盐，溶剂合物或其前药具有与S1P受体（特别是EDG-6，优选EDG-1和EDG-6）结合的能力，并且它们可用作移植排斥反应中的预防剂和/或补救剂，移植器官的排斥，移植与宿主疾病，自身免疫性疾病，过敏性疾病等。版权所有（C）2011，JPO＆INPIT

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