公开(公告)号：EP1201665B1

公开(公告)日：2004-09-29

申请号：EP00948257.1

申请日：2000-07-27

申请人： Eisai Co., Ltd.

发明人： KAYANO, Akio ,  CHIBA, Hiroyuki ,  NAKAMURA, Taiju ,  SAKURAI, Shin ,  ISHIZUKA, Hiroyuki ,  SAITO, Hiroyuki ,  KOMATSU, Yuuki ,  SASHO, Manabu ,  SATO, Nobuaki ,  NEGI, Shigeto

IPC分类号： C07D477/02 ,  C07D477/20 ,  C07D463/00 ,  C07D499/00 ,  C07D501/00

CPC分类号： C07D477/20 ,  C07D477/02 ,  C07D477/08 ,  Y02P20/55

摘要： An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an inorganic acid salt (III) of an alkaline earth metal, wherein A is a basic antibiotic; R10 is a protected functional group to be used in organic synthesis; Ak-E is an alkaline earth metal; and B is an inorganic acid; carbapenem derivative-oxalic acid addition salts represented by general formula (II-I) and being useful as intermediates for the preparation of hydrochlorides of antimicrobial agents; and a process for preparing the same, (II-I) wherein A is a three- to seven-membered ring having at least one nitrogen atom; R1 is hydrogen or the like; R?2 and R5¿ are each hydrogen or a protecting group; R3 is a protecting group; R4 is hydrogen or the like; and R6 is hydrogen or the like.

公开(公告)号：EP1394152A1

公开(公告)日：2004-03-03

申请号：EP02720536.8

申请日：2002-04-19

申请人： Eisai Co., Ltd.

发明人： SUZUKI, Shuichi ,  KOTAKE, Makoto ,  MIYAMOTO, Mitsuaki ,  KAWAHARA, Tetsuya ,  KAJIWARA, Akiharu ,  HISHINUMA, Ieharu ,  OKANO, Kazuo ,  MIYAZAWA, Syuhei ,  CLARK, Richard ,  OZAKI, Fumihiro ,  SATO, Nobuaki ,  SHINODA, Masanobu ,  KAMADA, Atsushi ,  TSUKADA, Itaru ,  MATSUURA, Fumiyoshi ,  NAOE, Yoshimitsu ,  TERAUCHI, Taro ,  OOHASHI, Yoshiaki ,  ITO, Osamu ,  TANAKA, Hiroshi ,  MUSYA, Takashi ,  KOGUSHI, Motoji ,  KAWADA, Tsutomu ,  MATSUOKA, Toshiyuki ,  KOBAYASHI, Hiroko ,  CHIBA, Ken-ichi ,  KIMURA, Akifumi ,  ONO, Naoto

IPC分类号： C07D235/30 ,  A61K31/4184 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06

CPC分类号： C07D209/44

摘要： A 2-iminoimidazole derivative represented by the formula:
{wherein ring C represents a benzene ring, a pyridine ring, etc.; R 1 represents optionally substituted C 1-6 alkyl, etc.; R 201 represents hydrogen, halogen, acyl, etc. ; R 6 represents hydrogen, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, etc.; Y 1 represents a single bond,-CH 2 -, etc.; Y 2 represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula:
[wherein R 10 -R 14 represent hydrogen, C 1-6 alkyl, hydroxyl, C 1-6 alkoxy, etc., and R 11 and R 12 or R 12 and R 13 may bond together to form a 5- to 8-membered heterocycle], etc.} or a salt thereof.

摘要翻译： 由下式表示的2-亚氨基咪唑衍生物：其中环C表示苯环，吡啶环等; R1代表任选取代的C1-6烷基等; R201代表氢，卤素，酰基等; R6代表氢，C1-6烷基，C1-6烷氧基羰基等; Y1表示单键，-CH2-等; Y2表示单键，-CO-等; 并且Ar代表氢，由下式表示的基团：[其中R10-R14表示氢，C1-6烷基，羟基，C1-6烷氧基等，并且R11和R12或R12和R13可以键合在一起形成5 - 至8-元杂环]等等或其盐。

公开(公告)号：EP1479670A1

公开(公告)日：2004-11-24

申请号：EP03703358.6

申请日：2003-02-21

申请人： Eisai Co., Ltd.

发明人： OHI, Norihito ,  SATO, Nobuaki ,  KOHMURA, Naohiro

IPC分类号： C07D231/56 ,  C07D231/54 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/55 ,  A61P1/08 ,  A61P9/10 ,  A61P13/02 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/16 ,  A61P29/00

CPC分类号： A61K31/55 ,  A61K31/416 ,  A61K31/4439 ,  C07D231/54 ,  C07D401/12 ,  C07D405/12 ,  C07D487/06

摘要： The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
Wherein Z 11 and Z 12 each independently represent a carbonyl group, a methylene group, etc.;
-----------
represents a double bond or a single bond; R 1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R 2a , R 2b and R 2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3) a nitro group, etc.

摘要翻译： 本发明提供了具有优异JNK抑制作用的新的稠合吲唑化合物。 更具体地，它提供由下式表示的化合物，其盐或它们的水合物。 其中Z 11和Z 12各自独立地表示羰基，亚甲基等; -----------表示双键或单键; R 1a表示氢原子等; 环A表示苯环，萘环或5至10元芳族杂环等; 和R 2a，R 2b和R 2c各自独立地表示（1）氢原子，（2）卤素原子，（3）硝基等。

公开(公告)号：EP0773222B1

公开(公告)日：2001-10-04

申请号：EP95923546.6

申请日：1995-06-29

申请人： Eisai Co., Ltd.

发明人： SATO, Nobuaki ,  SASHO, Manabu ,  KAMATA, Atsushi ,  SUZUKI, Takaaki ,  SUGIYAMA, Isao ,  KATSU, Kanemasa ,  SUZUKI, Takeshi

IPC分类号： C07D477/20 ,  A61K31/40 ,  A61K31/445

CPC分类号： C07D477/20 ,  Y02P20/55

摘要： A carbapenem compound represented by general formula (I) or a salt thereof, wherein ring A represents a three- to seven-membered ring having at least one nitrogen atom and may have a substituent(s) in addition to R6; R1 represents hydrogen or methyl, R?2 and R5¿ represent each independently hydrogen or a hydroxyl-protecting group; R3 represents a carboxyl-protecting group; R4 represents hydrogen, lower alkyl or an amino-protecting group; R6 represents (1) hydrogen, (2) lower alkyl which may be substituted by optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or -NR7R8 (wherein R?7 and R8¿ represent each independently hydrogen, lower alkyl or an amino-protecting group), or (3) an amino- or imino-protecting group; and m represents 0 or 1. The compound has a potent antibacterial activity against both Gram-positive and Gram-negative bacteria, an excellent resistance to β-lactamase and DHP-I, and an excellent safety for the human body, thus being useful as a medicine.

摘要翻译： 由通式（I）表示的碳青霉烯化合物或其盐，其中环A表示除R6之外还具有至少一个氮原子并且可以具有取代基的三至七元环; R1代表氢或甲基，R2和R5各自独立地代表氢或羟基保护基; R3代表羧基保护基团; R4代表氢，低级烷基或氨基保护基; R6代表（1）氢，（2）可以被任意保护的羟基，氨基甲酰基，亚胺甲基，亚氨代乙酰基或-NR7R8取代的低级烷基（其中R7和R8各自独立地代表氢，低级烷基或氨基保护基 ），或（3）氨基或亚氨基保护基团; m表示0或1.该化合物对革兰氏阳性菌和革兰氏阴性菌均具有有效的抗菌活性，对β-内酰胺酶和DHP-I具有优异的抗性，并且对人体具有优异的安全性，因此可用作 一种药。

公开(公告)号：EP1391456A1

公开(公告)日：2004-02-25

申请号：EP02718622.0

申请日：2002-04-19

申请人： Eisai Co., Ltd.

发明人： SUZUKI, Shuichi ,  KOTAKE, Makoto ,  MIYAMOTO, Mitsuaki ,  KAWAHARA, Tetsuya ,  KAJIWARA, Akiharu ,  HISHINUMA, Ieharu ,  OKANO, Kazuo ,  MIYAZAWA, Syuhei ,  CLARK, Richard ,  OZAKI, Fumihiro ,  SATO, Nobuaki ,  SHINODA, Masanobu ,  KAMADA, Atsushi ,  TSUKADA, Itaru ,  MATSUURA, Fumiyoshi ,  NAOE, Yoshimitsu ,  TERAUCHI, Taro ,  OOHASHI, Yoshiaki ,  ITO, Osamu ,  TANAKA, Hiroshi ,  MUSYA, Takashi ,  KOGUSHI, Motoji ,  KAWADA, Tsutomu ,  MATSUOKA, Toshiyuki ,  KOBAYASHI, Hiroko ,  CHIBA, Ken-ichi ,  KIMURA, Akifumi ,  ONO, Naoto

IPC分类号： C07D233/88 ,  C07D401/06 ,  A61K31/4168 ,  A61K31/4439 ,  A61K31/4196 ,  A61K31/454

CPC分类号： C07D209/44

摘要： A 2-iminoimidazole derivative represented by the formula:
{wherein R 1 , R 2 and R 3 represent hydrogen, optionally substituted C 1-6 alkyl, etc.; R 6 represents hydrogen, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, etc.; Y 1 represents a single bond, -CH 2 -, etc.; Y 2 represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula:
[wherein R 10 -R 14 represent hydrogen, C 1-6 alkyl, hydroxyl, C 1-6 alkoxy, etc., and R 11 and R 12 or R 12 and R 13 may bond together to form a 5- to 8-membered heterocycle], etc.} or a salt thereof.

摘要翻译： 由下式表示的2-亚氨基咪唑衍生物：其中R1，R2和R3代表氢，任选取代的C1-6烷基等; R6代表氢，C1-6烷基，C1-6烷氧基羰基等; Y1表示单键，-CH2-等; Y2表示单键，-CO-等; 并且Ar代表氢，由下式表示的基团：[其中R10-R14表示氢，C1-6烷基，羟基，C1-6烷氧基等，并且R11和R12或R12和R13可以键合在一起形成5 - 至8-元杂环]等等或其盐。

公开(公告)号：EP1386912A1

公开(公告)日：2004-02-04

申请号：EP02720534.3

申请日：2002-04-19

申请人： Eisai Co., Ltd.

发明人： SUZUKI, Shuichi ,  KOTAKE, Makoto ,  MIYAMOTO, Mitsuaki ,  KAWAHARA, Tetsuya ,  KAJIWARA, Akiharu ,  HISHINUMA, Ieharu ,  OKANO, Kazuo ,  MIYAZAWA, Syuhei ,  CLARK, Richard ,  OZAKI, Fumihiro ,  SATO, Nobuaki ,  SHINODA, Masanobu ,  KAMADA, Atsushi ,  TSUKADA, Itaru ,  MATSUURA, Fumiyoshi ,  NAOE, Yoshimitsu ,  TERAUCHI, Taro ,  OOHASHI, Yoshiaki ,  ITO, Osamu ,  TANAKA, Hiroshi ,  MUSYA, Takashi ,  KOGUSHI, Motoji ,  KAWADA, Tsutomu ,  MATSUOKA, Toshiyuki ,  KOBAYASHI, Hiroko ,  CHIBA, Ken-ichi ,  KIMURA, Akifumi ,  ONO, Naoto

IPC分类号： C07D207/273 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/407 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  A61P9/00 ,  A61P11/06

CPC分类号： C07D209/44

摘要： A cyclic amidine derivative represented by the formula:
[wherein R 1 , R 2 and R 3 represent hydrogen, C 1-6 alkyl, aryl-C 1-6 alkyl, etc.; R 4 , R 5 and R 7 represent hydrogen, C 1-6 alkyl, etc.; Z represents 0 or 1; R 6 represents hydrogen, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y 1 represents a single bond, -CH 2 -, etc.; Y 2 represents a single bond, -CO-, etc.; Ar represents hydrogen, a group represented by the formula:
[wherein R 10 -R 14 represent hydrogen, C 1-6 alkyl, hydroxyl, C 1-6 alkoxy, etc., and R 11 and R 12 or R 12 and R 13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.

摘要翻译： 由下式表示的环状脒衍生物：其中R 1，R 2和R 3表示氢，C 1-6烷基，芳基-C 1-6烷基等; R 4，R 5和R 7代表氢，C 1-6烷基等; Z表示0或1; R 6表示氢，C 1-6烷基，C 1-6烷氧基羰基等; n表示1或2; Y 1表示单键，-CH 2 - 等; Y 2表示单键，-CO-等; Ar表示氢，由下式表示的基团：其中R 10 -R 14表示氢，C 1-6烷基，羟基，C 1-6烷氧基等，R 11和R 11， 12>或R 12和R 13可以键合在一起形成5-至8-元杂环或其盐。

公开(公告)号：EP1380576A1

公开(公告)日：2004-01-14

申请号：EP02724612.3

申请日：2002-04-15

申请人： Eisai Co., Ltd.

发明人： OINUMA, Hitoshi ,  OHI, Norihito ,  SATO, Nobuaki ,  SOEJIMA, Motohiro ,  SESHIMO, Hidenori ,  TERAUCHI, Taro ,  DOKO, Takashi ,  KOHMURA, Naohiro

IPC分类号： C07D231/56 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454

CPC分类号： C07D231/56

摘要： The present invention provides a novel 1 H -indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
Wherein R 1 is a C 6 -C 14 aromatic cyclic hydrocarbon group etc.; R 2 , R 4 and R 5 each independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C 1 -C 6 alkylene group etc.; X is a single bond, or a group represented by -CO-NH- or -NH-CO-, etc.; and Y is a C 3 -C 8 cycloalkyl group, a C 6 -C 14 aromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

摘要翻译： 本发明提供具有优异的JNK抑制作用的新型1H-吲唑化合物。 更具体地，它提供了由下式表示的化合物，其盐或其水合物。 其中R1为C6-C14芳族环状烃基等; R2，R4和R5各自独立地表示氢原子，卤素原子，氰基等。 L为单键或C1-C6亚烷基等; X是单键或由-CO-NH-或-NH-CO-等表示的基团; Y为碳数3〜8的环烷基，碳数6〜14的芳香族环状烃基或5〜14元的芳香族杂环基等。

公开(公告)号：EP1201665A1

公开(公告)日：2002-05-02

申请号：EP00948257.1

申请日：2000-07-27

申请人： Eisai Co., Ltd.

发明人： KAYANO, Akio ,  CHIBA, Hiroyuki ,  NAKAMURA, Taiju ,  SAKURAI, Shin ,  ISHIZUKA, Hiroyuki ,  SAITO, Hiroyuki ,  KOMATSU, Yuuki ,  SASHO, Manabu ,  SATO, Nobuaki ,  NEGI, Shigeto

IPC分类号： C07D477/02 ,  C07D477/20 ,  C07D463/00 ,  C07D499/00 ,  C07D501/00

CPC分类号： C07D477/20 ,  C07D477/02 ,  C07D477/08 ,  Y02P20/55

摘要： The present invention provides:

an industrially-excellent and novel process for producing a basic antibiotic·inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic·oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid:
(wherein the ring A means the basic antibiotic; R 10 means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively);
a novel oxalate useful as a production intermediate for producing an antibiotic·hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula:
(wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R 6 ; R 1 represents hydrogen or methyl group; R 2 and R 5 are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R 3 represents a carboxyl-protecting group; R 4 represents hydrogen, a lower alkyl group or an amino-protecting group; R 6 represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula:
(wherein R 7 and R 8 are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and
a process for producing its.

摘要翻译： 本发明提供：在工业上优和新方法用于生产基本antibiotic.inorganic酸的盐，例如，优良的生产过程用于制备盐酸盐在工业上，所做的是，一个生产过程，它包括使一个基本antibiotic.oxalate （II）盐交换与碱土金属盐（III）的无机酸的：（worin环的装置的基本抗生素; R <10>表示在有机合成中使用的保护的官能基团; AK- E表示碱土金属;且B是指无机酸，分别地）; 一种新颖的草酸作为生产用于在antibiotic.hydrochloride生产工业上，做了中间有用是草酸盐（II-I）由下式表示的碳代青霉烯化合物：（ worin环A darstellt 3-至7- 具有元环的至少一个氮原子，且环A可与其它除R <6> R上substituiertem <1> darstellt氢或甲基; R <2>和R <5>是相同的或不同 形成，且分别darstellt氢或羟基保护基; R <3>表示羧基保护基; R <4> darstellt氢，低级烷基或氨基保护基的; R <6> darstellt（1 ）氢，（2）任选被保护的羟基，氨基甲酰基，亚胺甲基，acetoimidoyl或可被由下式表示的取代基所substituiertem的低级烷基：（worin - [R <7>和R <8>是 相同或彼此和各darstellt氢，低级烷基或氨基保护基），或者（3个不同的 ）氨基保护基或亚氨基保护的基团; 且m是0或1）; 和用于生产其的过程。

公开(公告)号：EP1020440A1

公开(公告)日：2000-07-19

申请号：EP98921743.5

申请日：1998-05-21

申请人： Eisai Co., Ltd.

发明人： SUZUKI, Takaaki ,  SUGIYAMA, Isao ,  SASHO, Manabu ,  SATO, Nobuaki ,  KAMADA, Atsushi ,  ASHIZAWA, Kazuhide

IPC分类号： C07D207/26 ,  C07D207/27 ,  C07D413/06 ,  C07D417/06

CPC分类号： C07D477/20 ,  C07D207/12 ,  C07D263/22 ,  C07D413/06 ,  Y02P20/55

摘要： An efficient process for the stereoselective production of (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amin-3-yl]methyl]pyrrolidine-4-thiol or its salts, which are intermediates useful in producing carbapenem, by reacting a compound represented by general formula (I) (wherein R 1 represents lower alkylsulfonyl, optionally substituted arylsulfonyl or alkylsilyl; and R 2 represents an amino-protective group) with a compound represented by general formula (II), wherein R 3 represents optionally substituted lower alkyl or aryl; X represents oxygen or sulfur; Y represents azido or nitro; and m is an integer of from 2 to 5.

摘要翻译： 用于立体选择性生产（2S，4S）-2-AA（R） - 羟基（3R） - 环状胺-3-ylÜmethylÜpyrrolidine-4-硫醇或它的盐，其生产碳代青霉烯是有用的中间体，通过一种有效的方法 反应由通式（I）表示的化合物（其中，R <1>表示低级烷基磺酰基，任选取代的芳基磺酰基或烷基甲硅烷基;且R <2> darstellt氨基的保护基的）与由通式（II），worin表示的化合物 [R <3> darstellt OPTIONALLY substituiertem低级烷基或芳基; X darstellt氧或硫; ÿdarstellt叠氮基或硝基; 且m是从2至5的整数

公开(公告)号：EP1391451A1

公开(公告)日：2004-02-25

申请号：EP02724628.9

申请日：2002-04-19

申请人： Eisai Co., Ltd.

发明人： SUZUKI, Shuichi ,  KOTAKE, Makoto ,  MIYAMOTO, Mitsuaki ,  KAWAHARA, Tetsuya ,  KAJIWARA, Akiharu ,  HISHINUMA, Ieharu ,  OKANO, Kazuo ,  MIYAZAWA, Syuhei ,  CLARK, Richard ,  OZAKI, Fumihiro ,  SATO, Nobuaki ,  SHINODA, Masanobu ,  KAMADA, Atsushi ,  TSUKADA, Itaru ,  MATSUURA, Fumiyoshi ,  NAOE, Yoshimitsu ,  TERAUCHI, Taro ,  OOHASHI, Yoshiaki ,  ITO, Osamu ,  TANAKA, Hiroshi ,  MUSHA, Takashii ,  KOGUSHI, Motoji ,  KAWADA, Tsutomu ,  MATSUOKA, Toshiuyki ,  KOBAYASHI, Hiroko ,  CHIBA, Keni-ichi ,  KIMURA, Akifumi ,  ONO, Naoto

IPC分类号： C07D209/44

CPC分类号： C07D209/44

摘要： A 2-iminopyrrolidine derivative represented by the formula:
{wherein ring B represents a benzene ring, pyridine ring, etc.; R 101 - R 103 represent hydrogen, halogen, C 1-6 alkyl, etc.; R 5 represents hydrogen, C 1-6 alkyl, C 1-6 alkoxy-C 1-6 alkyl, etc.; R 6 represents hydrogen, C 1-6 alkyl, C 1-6 alkyloxycarbonyl, etc.; Y 1 represents a single bond, -CH 2 -, etc.; Y 2 represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula:
[wherein R 10 -R 14 represent hydrogen, C 1-6 alkyl, hydroxyl, C 1-6 alkoxy, etc.; and R 11 and R 12 or R 12 and R 13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.},
or a salt thereof.

摘要翻译： 由下式表示的2-亚氨基吡咯烷衍生物：环C表示苯环，吡啶环等; R 101 - R 103代表氢，卤素，C 1-6烷基等; R 5表示氢，C 1-6烷基，C 1-6烷氧基-C 1-6烷基等; R 6表示氢，C 1-6烷基，C 1-6烷氧基羰基等; Y 1表示单键，-CH 2 - 等; Y 2表示单键，-CO-等; 和Ar表示氢，由下式表示的基团：其中R 10 -R 14表示氢，C 1-6烷基，羟基，C 1-6烷氧基等; 并且R 11和R 12或R 12和R 13可以键合在一起形成5-至8-元杂环基等，或其盐。