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1. 发明授权

US07157487B2 Vla-4 inhibitors 失效
标题翻译： Vla-4抑制剂
公开(公告)号：US07157487B2
公开(公告)日：2007-01-02
申请号：US10451159
申请日：2001-12-28
申请人： Atsushi Nakayama , Nobuo Machinaga , Yoshiyuki Yoneda , Yuichi Sugimoto , Jun Chiba , Toshiyuki Watanabe , Shin Iimura
发明人： Atsushi Nakayama , Nobuo Machinaga , Yoshiyuki Yoneda , Yuichi Sugimoto , Jun Chiba , Toshiyuki Watanabe , Shin Iimura
IPC分类号： A61K31/405 , C07D209/04
CPC分类号： C07D263/58 , C07C275/42 , C07D209/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D471/04 , C07D491/04
摘要： The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1-WB- (in which, WA is substituted or unsubstituted aryl, etc., A1 is —NR1—, single bond, —C(O)—, etc., and WB is substituted or unsubstituted arylene, etc.), R is single bond, —NH—, —OCH2—, alkenylene, etc., X is —C(O)—, —CH2—, etc., and M is, for example, the following formula: (in which, R11, R12 and R13 each independently represents hydrogen, hydroxyl, amino, halogen, etc., R14 is hydrogen or lower alkyl, Y represents —CH2—O—, etc., Z is substituted or unsubstituted arylene, etc., A2 is single bond, etc, and R10 is hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same. This compound or salt thereof selectively inhibits binding of cell adhesion molecules to VLA-4 and exhibits high bioavailability so that it is useful as a preventive and/or remedy for inflammatory diseases, autoimmune diseases, metastasis, bronchial asthma, rhinostenosis, diabetes, and the like.
摘要翻译：本发明涉及由下式（I）表示的化合物：（其中，W表示W A，A，B， - （其中，W A是取代或未取代的芳基等，A 1是-NR 1 - 单键，-C （O） - 等，W B是取代或未取代的亚芳基等），R是单键，-NH-，-OCH 2 - ，亚烯基等等，X是-C（O） - ， - CH 2 - 等，M是例如下式：（其中R 11， R 12，R 12和R 13各自独立地表示氢，羟基，氨基，卤素等，R 14是氢或低级烷基，Y表示-CH 2 -O-O-等，Z是取代或未取代的亚芳基等，A 2是单键等，R“ 10是羟基或低级烷氧基））或其盐; 和含有该药物的药物。该化合物或其盐选择性地抑制细胞粘附分子与VLA-4的结合并且表现出高的生物利用度，使得其可用作炎性疾病，自身免疫性疾病，转移，支气管哮喘，鼻窦炎，糖尿病的预防和/或补救。喜欢。

2. 发明授权

US08129366B2 VLA-4 inhibitory drug 失效
标题翻译： VLA-4抑制药
公开(公告)号：US08129366B2
公开(公告)日：2012-03-06
申请号：US12097269
申请日：2006-12-13
申请人： Nobuo Machinaga , Shin Iimura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
发明人： Nobuo Machinaga , Shin Iimura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
IPC分类号： A61K31/553 , C07D243/08
CPC分类号： C07D409/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/08 , C07D491/048 , C07D491/056 , C07D491/08 , C07D495/04
摘要： There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.A compound represented by the following formula (I): wherein R1 represents a hydrogen atom or a C1-8 alkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group, or a benzyloxy group which may be substituted; Q represents a monocyclic or bicyclic nitrogen-containing heterocyclic group which may be substituted, and has a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents a bicyclic aromatic hydrocarbon ring group which may be substituted, or a bicyclic aromatic heterocyclic group which may be substituted; R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; and A1 represents a nitrogen atom or C—R3d (wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group), or a salt thereof, or a VLA-4 inhibitory drug comprising the compound or the salt as an active ingredient.
摘要翻译：提供口服吸收性良好的VLA-4抑制药物，口服给药时具有足够的抗炎作用。由下式（I）表示的化合物：其中R1表示氢原子或C1-8烷基; R2表示氢原子，卤素原子，C1-8烷氧基或可被取代的苄氧基; Q表示可以被取代的单环或双环含氮杂环基，并且具有氮原子作为键合位点; Y表示氧原子或CH2; W表示可被取代的双环芳香族烃环基或可被取代的双环芳香族杂环基; R3a，R3b和R3c各自独立地表示氢原子，卤素原子，C1-8烷氧基或C1-8烷基; A1表示氮原子或C-R3d（其中R3d表示氢原子，卤原子，C1-8烷氧基或C1-8烷基）或其盐或VLA-4抑制药，其包含化合物或盐作为活性成分。

3. 发明申请

US20130065882A1 VLA-4 inhibitory drug 审中-公开
标题翻译： VLA-4抑制药
公开(公告)号：US20130065882A1
公开(公告)日：2013-03-14
申请号：US13573673
申请日：2012-10-03
申请人： Nobuo Machinaga , Shin Iimura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
发明人： Nobuo Machinaga , Shin Iimura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
IPC分类号： A61K31/404 , C07D409/14 , A61K31/4025 , C07D405/14 , C07D401/14 , A61K31/4725 , C07D413/14 , A61K31/454 , A61K31/403 , A61K31/496 , A61K31/553 , A61P35/00 , A61P25/00 , A61P37/06 , A61P35/02 , A61P17/06 , A61P29/00 , A61P3/10 , A61P19/02 , A61P11/02 , A61P35/04 , C07D403/14
CPC分类号： C07D409/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/08 , C07D491/048 , C07D491/056 , C07D491/08 , C07D495/04
摘要： This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy
摘要翻译：本发明涉及具有良好口服吸收性且口服给药时具有足够抗炎作用的VLA-4抑制药物，其中活性成分由式（I）表示，或其盐：Q表示任选取代的单环或具有氮原子的双环含氮杂环基作为键合位置; Y表示氧原子或CH2; W表示任选取代的双环芳烃环基或任选取代的双环芳族杂环基; A1表示氮原子或C-R3d，其中R3d表示氢原子，卤素原子，C1-8烷氧基或C1-8烷基; R1表示H或C1-8烷基; R 2表示H，卤素，C 1-8烷氧基

4. 发明授权

US06756378B2 VLA-4 inhibitor compounds 失效
标题翻译： VLA-4抑制剂化合物
公开(公告)号：US06756378B2
公开(公告)日：2004-06-29
申请号：US10034585
申请日：2001-12-28
申请人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
发明人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
IPC分类号： C07D20712
CPC分类号： C07D207/08 , C07C275/42 , C07C2601/02 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/22 , C07D207/24 , C07D209/12 , C07D211/26 , C07D211/34 , C07D211/38 , C07D213/55 , C07D217/02 , C07D277/04 , C07D277/28 , C07D277/48 , C07D295/13 , C07D295/185 , C07D307/33 , C07D311/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/02 , C07D413/06 , C07D491/04
摘要： Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are pharmaceutical compositions, methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion, which involve compounds of Formula I.
摘要翻译：公开了选择性抑制配体与α4β1整联蛋白（VLA-4）的结合的化合物及其制备方法。在一个实施方案中，本发明的化合物由式I表示：作为VLA-4介导的细胞粘附的选择性抑制剂，本发明的化合物可用于治疗与这种粘附相关的病症，包括但不限于此作为炎症和自身免疫反应的病症，糖尿病，哮喘，牛皮癣，炎性肠病，移植排斥反应和肿瘤转移。还公开了药物组合物，抑制VLA-4介导的细胞粘附的方法和治疗与LA-4介导的细胞粘附相关的病症的方法，涉及式I化合物。

5. 发明申请

US20090233901A1 VLA-4 INHIBITORY DRUG 失效
标题翻译： VLA-4抑制药物
公开(公告)号：US20090233901A1
公开(公告)日：2009-09-17
申请号：US12097269
申请日：2006-12-13
申请人： Nobuo Machinaga , Shin Iimura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
发明人： Nobuo Machinaga , Shin Iimura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
IPC分类号： A61K31/403 , A61K31/553 , A61K31/54 , A61K31/5377 , A61K31/415 , C07D409/14 , C07D417/14 , C07D413/14 , C07D403/00 , C07D403/02 , C07D231/56 , C07D403/14 , C07D405/14
CPC分类号： C07D409/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/08 , C07D491/048 , C07D491/056 , C07D491/08 , C07D495/04
摘要： There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.A compound represented by the following formula (I): wherein R1 represents a hydrogen atom or a C1-8 alkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group, or a benzyloxy group which may be substituted; Q represents a monocyclic or bicyclic nitrogen-containing heterocyclic group which may be substituted, and has a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents a bicyclic aromatic hydrocarbon ring group which may be substituted, or a bicyclic aromatic heterocyclic group which may be substituted; R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; and A1 represents a nitrogen atom or C—R3d (wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group), or a salt thereof, or a VLA-4 inhibitory drug comprising the compound or the salt as an active ingredient.
摘要翻译：提供口服吸收性良好的VLA-4抑制药物，口服给药时具有足够的抗炎作用。由下式（I）表示的化合物：其中R1表示氢原子或C1-8烷基; R2表示氢原子，卤素原子，C1-8烷氧基或可被取代的苄氧基; Q表示可以被取代的单环或双环含氮杂环基，并且具有氮原子作为键合位点; Y表示氧原子或CH2; W表示可被取代的双环芳香族烃环基或可被取代的双环芳香族杂环基; R3a，R3b和R3c各自独立地表示氢原子，卤素原子，C1-8烷氧基或C1-8烷基; A1表示氮原子或C-R3d（其中R3d表示氢原子，卤原子，C1-8烷氧基或C1-8烷基）或其盐或VLA-4抑制药，其包含化合物或盐作为活性成分。

6. 发明申请

US20070054909A1 VLA-4 inhibitor compounds 审中-公开
公开(公告)号：US20070054909A1
公开(公告)日：2007-03-08
申请号：US11594432
申请日：2006-11-08
申请人： John Baldwin , Edward McDonald , Kevin Moriarty , Christopher Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
发明人： John Baldwin , Edward McDonald , Kevin Moriarty , Christopher Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
IPC分类号： A61K31/5375 , A61K31/496 , A61K31/4439 , A61K31/426 , A61K31/401 , A61K31/405 , C07D403/02
CPC分类号： C07D207/08 , C07C275/42 , C07C2601/02 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/22 , C07D207/24 , C07D209/12 , C07D211/26 , C07D211/34 , C07D211/38 , C07D213/55 , C07D217/02 , C07D277/04 , C07D277/28 , C07D277/48 , C07D295/13 , C07D295/185 , C07D307/33 , C07D311/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/02 , C07D413/06 , C07D491/04
摘要： Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.

7. 发明申请

US20070232601A1 Vla-4 Inhibitor 审中-公开
标题翻译： Vla-4抑制剂
公开(公告)号：US20070232601A1
公开(公告)日：2007-10-04
申请号：US11629354
申请日：2005-06-14
申请人： Yoshiyuki Yoneda , Atsushi Nakayama , Nobuo Machinaga , Jun Chiba , Fumihito Muro
发明人： Yoshiyuki Yoneda , Atsushi Nakayama , Nobuo Machinaga , Jun Chiba , Fumihito Muro
IPC分类号： A61K31/535 , A61K31/40 , A61K31/425 , C07D207/00 , C07D263/00 , C07D277/62 , C07D265/28 , C07D241/00 , A61K31/445 , A61K31/497
CPC分类号： C07D417/14 , C07D413/14
摘要： An object of the present invention is to provide a compound which selectively inhibits binding of a ligand and α4β1 integrin (VLA-4), a process for producing the compound, and a medicament containing the compound. A compound represented by the formula (I) etc. or a salt thereof, a process for producing the compound or a salt thereof, a medicament containing the compound or a salt thereof, as well as a preventive and/or a therapeutic agent for a disease caused by cell adhesion, for example, inflammatory reaction, autoimmune disease, cancer metastasis, bronchial asthma, nasal obstruction, diabetes, arthritis, psoriasis, multiple sclerosis, inflammatory bowel disease and rejection reaction at transplantation, containing the compound or a salt thereof as a primary component. [wherein Y1 represents a divalent aryl group etc., V1 represents an aryl group etc., and R11 to R14 represent H, OH or a halogen atom etc.]
摘要翻译：本发明的目的是提供选择性抑制配体和α4β1整联蛋白（VLA-4）结合的化合物，该化合物的制备方法和含有该化合物的药物。由式（I）等表示的化合物或其盐，化合物或其盐的制备方法，含有该化合物或其盐的药物以及用于治疗和/ 包含其化合物或其盐的细胞粘附引起的疾病，例如炎性反应，自身免疫性疾病，癌症转移，支气管哮喘，鼻塞，糖尿病，关节炎，银屑病，多发性硬化，炎症性肠病和移植排斥反应主要组成部分。 [其中Y 1表示二价芳基等，V 1表示芳基等，R 11至R 11， 14表示H，OH或卤素原子等]

8. 发明授权

US07179819B2 VLA-4 inhibitor compounds 失效
标题翻译： VLA-4抑制剂化合物
公开(公告)号：US07179819B2
公开(公告)日：2007-02-20
申请号：US10787905
申请日：2004-02-26
申请人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Iimura Shin , Yoshiyuki Yoneda
发明人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Iimura Shin , Yoshiyuki Yoneda
IPC分类号： C07D277/04 , A61K31/425 , C07D207/12
CPC分类号： C07D207/08 , C07C275/42 , C07C2601/02 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/22 , C07D207/24 , C07D209/12 , C07D211/26 , C07D211/34 , C07D211/38 , C07D213/55 , C07D217/02 , C07D277/04 , C07D277/28 , C07D277/48 , C07D295/13 , C07D295/185 , C07D307/33 , C07D311/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/02 , C07D413/06 , C07D491/04
摘要： Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.
摘要翻译：公开了选择性抑制配体与α4β1整联蛋白（VLA-4）的结合的化合物及其制备方法。在一个实施方案中，本发明的化合物由式I表示：作为VLA-4介导的细胞粘附的选择性抑制剂，本发明的化合物可用于治疗与这种粘附相关的病症，包括但不限于此作为炎症和自身免疫反应的病症，糖尿病，哮喘，牛皮癣，炎性肠病，移植排斥反应和肿瘤转移。还公开了抑制VLA-4介导的细胞粘附的方法以及治疗与LA-4介导的细胞粘附相关的病症的方法。

9. 发明申请

US20120157437A1 VLA-4 INHIBITORY DRUG 审中-公开
标题翻译： VLA-4抑制药物
公开(公告)号：US20120157437A1
公开(公告)日：2012-06-21
申请号：US13363990
申请日：2012-02-01
申请人： Nobuo MACHINAGA , Shin Ilmura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
发明人： Nobuo MACHINAGA , Shin Ilmura , Yoshiyuki Yoneda , Jun Chiba , Fumihito Muro , Hideko Hoh , Atsushi Nakayama
IPC分类号： A61K31/404 , C07D401/14 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , A61K31/553 , A61P29/00 , A61P37/00 , A61P35/04 , A61P11/06 , A61P11/02 , A61P3/10 , A61P19/02 , A61P17/06 , A61P25/00 , A61P1/00 , A61P37/06 , A61P35/02 , A61P37/08 , A61P9/10 , A61P27/02 , A61P1/16 , A61P35/00 , C07D403/14
CPC分类号： C07D409/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/08 , C07D491/048 , C07D491/056 , C07D491/08 , C07D495/04
摘要： This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy group, or an optionally-substituted benzyloxy group; and R3a, R3b and R3c independently represent H, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group.
摘要翻译：本发明涉及具有良好口服吸收性且口服给药时具有足够抗炎作用的VLA-4抑制药物，其中活性成分由式（I）表示，或其盐：Q表示任选取代的单环或具有氮原子的双环含氮杂环基作为键合位置; Y表示氧原子或CH2; W表示任选取代的双环芳烃环基或任选取代的双环芳族杂环基; A1表示氮原子或C-R3d，其中R3d表示氢原子，卤素原子，C1-8烷氧基或C1-8烷基; R1表示H或C1-8烷基; R 2表示H，卤素，C 1-8烷氧基或任选取代的苄氧基; R3a，R3b和R3c独立地表示H，卤素原子，C1-8烷氧基或C1-8烷基。

10. 发明申请

US20070105935A1 Process for producing pyrrolidine derivative 失效
标题翻译：制备吡咯烷衍生物的方法
公开(公告)号：US20070105935A1
公开(公告)日：2007-05-10
申请号：US10556043
申请日：2004-05-07
申请人： Atsushi Nakayama , Nobuo Machinaga , Yoshiyuki Yoneda , Masaki Setoguchi
发明人： Atsushi Nakayama , Nobuo Machinaga , Yoshiyuki Yoneda , Masaki Setoguchi
IPC分类号： A61K31/405 , C07D403/02
CPC分类号： C07D207/12
摘要： This invention provides an industrially useful process for producing 1,4-transcyclohexanecarboxylic acid derivative (1) which has excellent VLA-4 inhibitory action and safety, and an intermediate which is useful in such method. More particularly, this invention relates to a process for converting a compound of formula (I) into a compound of formula (VI) by the reaction scheme:
摘要翻译：本发明提供了具有优异的VLA-4抑制作用和安全性的1,4-反式环己烷羧酸衍生物（1）的工业上有用的方法和可用于该方法的中间体。更具体地，本发明涉及通过反应方案将式（I）化合物转化为式（VI）的化合物的方法：

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