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51. 发明公开

EP3087217A1 CORROSION INHIBITING COMPOSITIONS INCLUDING BIS-IMIDAZOLINE COMPOUNDS DERIVED FROM ENRICHED LINEAR TETRAMINES 审中-公开
标题翻译：缓蚀丰富了组合物，直链四MINES衍生BIS咪唑啉CONNECTIONS
公开(公告)号：EP3087217A1
公开(公告)日：2016-11-02
申请号：EP14824272.0
申请日：2014-12-12
申请人： Dow Global Technologies LLC
发明人： GULABANI, Ritesh , KING, Stephen W. , TATAKE, Prashant
IPC分类号： C23F11/14 , C23F11/04 , C09K8/74 , C07D233/10 , C09K8/54 , C23F11/10
CPC分类号： C23F11/149 , C07D233/10 , C07D233/16 , C09D5/086 , C09D7/65 , C09K8/54 , C09K8/74 , C09K2208/32 , C23F11/04 , C23F11/10
摘要： The present invention provides corrosion inhibiting compositions that incorporate at least one bis-imidazoline compound. In the practice of the present invention, a tetramine admixture enriched with respect to linear tetramine is used to prepare the bis-imidazoline compound. “Enriched” means at least 70 weight percent and up to 100% of the tetramine species included in the admixture includes a linear tetramine such as L-TETA.
摘要翻译：本发明提供了腐蚀抑制组合物没有掺入至少一种双 - 咪唑啉化合物。在本发明的实践中，相对于直链甲基四胺中富集的甲基四胺的混合物被用于制备双咪唑啉化合物。包括在混合物中的四种类的“富集”是指至少70重量％和至多100％的包括线性四胺：如L-TETA。

52. 发明公开

EP2457896A1 Tripeptides as caspase modulators 审中-公开
标题翻译：四肽酶Caspase Modulatoren
公开(公告)号：EP2457896A1
公开(公告)日：2012-05-30
申请号：EP11184402.3
申请日：2005-07-12
申请人： Idun Pharmaceuticals, Inc.
发明人： Chao, Bin , Deckwerth, Thomas, L. , Furth, Paul, S. , Linton, Steven, D. , Spada, Alfred, P. , Ullman, Brett, R. , Weinhouse, Michael, I.
IPC分类号： C07D207/16 , C07D207/22 , C07D207/24 , C07D209/42 , C07D209/44 , C07D211/76 , C07D213/64 , C07D233/10 , C07D263/06 , C07D277/06 , C07D487/04 , C07D487/06 , C07D513/04 , C07K5/06 , C07K5/08 , C07K5/10 , C07D207/273 , A61K38/06 , A61P35/00
CPC分类号： C07D207/16 , A61K38/00 , C07D207/22 , C07D207/24 , C07D207/273 , C07D209/42 , C07D209/44 , C07D211/76 , C07D213/64 , C07D233/10 , C07D263/06 , C07D277/06 , C07D487/04 , C07D487/06 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/1008 , Y02A50/411 , Y02A50/414
摘要： Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.

or a pharmaceutically acceptable derivative thereof,
where:
M is CO, SO or SO 2 ;
R 1s and R 2s are selected as follows:
(i) R 1s is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyI; and R 2s is selected from hydrogen, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, OR 11 and NR 15 R 16 , or
(ii) R 1s and R 2s together with the nitrogen atom on which they are substituted form a heterocyclic or heteroaryl ring;
R 3s , R 4s and R 5s are each independently selected from (i) or (ii) as follows:
(i) R 3s is hydrogen or alkyl; R 4s is alkyl; and R 5s is selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroarylium, cycloalkyl, heterocyclyl and NR 15 R 16 ;
(ii )R 5s and R 3s or R 5s and R 4s together with the atoms on which they are substituted form heterocyclic or heteroaryl ring and the other of R 3s or R 4s is selected as (ii);
R 6s is hydrogen, lower alkyl, lower alkenyl or lower alkynyl;
R 7s is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl.
The other variables are as defined in the claims.
摘要翻译：提供了用于治疗过度增殖性疾病如癌症的化合物，组合物和方法。或其药学上可接受的衍生物，其中：M是CO，SO或SO 2; R 1和R 2选自如下：（i）R 1是氢，烷基，烯基，炔基，芳基，杂芳基，环烷基或杂环基; 和R 2选自氢，烯基，炔基，芳基，杂芳基，环烷基，杂环基，OR 11和NR 15 R 16，或（ii）R 1和R 2与它们所取代的氮原子一起形成杂环或杂芳基环; R 3，R 4和R 5各自独立地选自（i）或（ii）：（i）R 3是氢或烷基; R 4是烷基; R 5选自氢，烷基，烯基，炔基，芳基，杂芳基，杂芳基，环烷基，杂环基和NR 15 R 16; （ii）R 5和R 3或R 5和R 4与它们所取代的原子一起形成杂环或杂芳基环，R 3或R 4中的另一个选自（ii）; R 6是氢，低级烷基，低级烯基或低级炔基; R 7是氢，烷基，烯基，炔基，芳基，杂芳基，环烷基或杂环基。其他变量如权利要求中所定义。

53. 发明公开

EP2042506A4 SUBSTITUTED PHENYLETHYNYL GOLD-NITROGENATED HETEROCYCLIC CARBENE COMPLEX 有权
标题翻译：替代物苯乙烯 - 金 - 氮氧化物杂环化合物
公开(公告)号：EP2042506A4
公开(公告)日：2011-02-09
申请号：EP07744109
申请日：2007-05-25
申请人： UBE INDUSTRIES
发明人： FUJIMURA OSAMU , FUKUNAGA KENJI , HONMA TAKASHI , MACHIDA TOSHIKAZU
IPC分类号： C07F1/12 , C07D233/10 , C09K11/06 , H01L51/50
CPC分类号： C07F1/00 , C07D233/10 , C07F1/005 , C09K11/06 , C09K2211/1033 , C09K2211/1044 , C09K2211/188 , H01L51/0084 , H01L51/0091 , H01L51/5016 , H05B33/14

54. 发明公开

EP1773348A4 TETRAPEPTIDE ANALOGS 审中-公开
标题翻译： TETRAPEPTID-ANALOGA
公开(公告)号：EP1773348A4
公开(公告)日：2009-05-20
申请号：EP05771672
申请日：2005-07-12
申请人： IDUN PHARMACEUTICALS INC
发明人： CHAO BIN , DECKWERTH THOMAS L , FURTH PAUL S , LINTON STEVEN D , SPADA ALFRED P , ULLMAN BRETT R , WEINHOUSE MICHAEL I
IPC分类号： C07D207/00 , A01N43/64 , A61K31/4015 , A61K31/429 , A61K31/5517 , A61K38/00 , A61P35/00 , C07D207/16 , C07D207/22 , C07D207/24 , C07D207/273 , C07D209/42 , C07D209/44 , C07D211/76 , C07D213/64 , C07D233/10 , C07D263/06 , C07D277/06 , C07D487/04 , C07D487/06 , C07D513/04
CPC分类号： C07D207/16 , A61K38/00 , C07D207/22 , C07D207/24 , C07D207/273 , C07D209/42 , C07D209/44 , C07D211/76 , C07D213/64 , C07D233/10 , C07D263/06 , C07D277/06 , C07D487/04 , C07D487/06 , C07D513/04 , C07K5/06026 , C07K5/0806 , C07K5/1008
摘要： Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided. or a pharmaceutically acceptable derivative thereof, where: M is CO, SO or SO 2 ; R 1s and R 2s are selected as follows: (i) R 1s is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyI; and R 2s is selected from hydrogen, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, OR 11 and NR 15 R 16 , or (ii) R 1s and R 2s together with the nitrogen atom on which they are substituted form a heterocyclic or heteroaryl ring; R 3s , R 4s and R 5s are each independently selected from (i) or (ii) as follows: (i) R 3s is hydrogen or alkyl; R 4s is alkyl; and R 5s is selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroarylium, cycloalkyl, heterocyclyl and NR 15 R 16 ; (ii )R 5s and R 3s or R 5s and R 4s together with the atoms on which they are substituted form heterocyclic or heteroaryl ring and the other of R 3s or R 4s is selected as (ii); R 6s is hydrogen, lower alkyl, lower alkenyl or lower alkynyl; R 7s is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclyl. The other variables are as defined in the claims.

55. 发明公开

EP2042506A1 SUBSTITUTED PHENYLETHYNYL GOLD-NITROGENATED HETEROCYCLIC CARBENE COMPLEX 有权
标题翻译：替代物苯乙烯 - 金 - 氮氧化物杂环化合物
公开(公告)号：EP2042506A1
公开(公告)日：2009-04-01
申请号：EP07744109.5
申请日：2007-05-25
申请人： Ube Industries, Ltd.
发明人： FUJIMURA, Osamu , FUKUNAGA, Kenji , HONMA, Takashi , MACHIDA, Toshikazu
IPC分类号： C07F1/12 , C07D233/10 , C09K11/06 , H01L51/50
CPC分类号： C07F1/00 , C07D233/10 , C07F1/005 , C09K11/06 , C09K2211/1033 , C09K2211/1044 , C09K2211/188 , H01L51/0084 , H01L51/0091 , H01L51/5016 , H05B33/14
摘要： The present invention is directed to a substituted phenylethynylgold-nitrogen-containing heterocyclic carbene complex represented by the formula (1) or (2):

wherein L represents a nitrogen-containing heterocyclic carbene ligand, and X represents an alkyl group, a cycloalkyl group, an aryl group, an aralkyl group, a heterocyclic group, an alkoxy group, an aryloxy group, an alkylmercapto group, an arylmercapto group or a substituted amino group; and one or a plural number of hydrogen atoms on the carbon atom(s) of X are independently optionally replaced by a halogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylmercapto group, an arylmercapto group or a substituted amino group.
摘要翻译：本发明涉及由式（1）或（2）表示的取代的苯基乙炔基金 - 含氮杂环卡宾络合物：其中L表示含氮杂环卡宾配体，X表示烷基，环烷基，芳基，芳烷基，杂环基，烷氧基，芳氧基，烷基巯基，芳基巯基或取代氨基; 并且X的碳原子上的一个或多个氢原子独立地任选被卤素原子，烷基，环烷基，烯基，芳基，芳烷基，烷氧基芳氧基，烷基巯基，芳基巯基或取代氨基。

56. 发明授权

EP1104407B1 COMPOUNDS AS SELECTIVE AGONISTS AT ALPHA 2B OR 2B/2C ADRENERGIC RECEPTORS 有权
标题翻译：化合物ALPHA 2B或作为选择性激动剂2B / 2C肾上腺素能受体
公开(公告)号：EP1104407B1
公开(公告)日：2004-12-01
申请号：EP00939699.5
申请日：2000-06-08
申请人： Allergan, Inc.
发明人： CHOW, Ken , GIL, Daniel, W. , BURKE, James, A. , HARCOURT, Dale, A. , GARST, Michael, E. , WHEELER, Larry, A. , MUNK, Stephen, A.
IPC分类号： C07D233/54 , A61K31/33 , A61P43/00 , C07D409/06 , C07D263/28 , C07D413/12 , C07D233/84 , C07D233/10 , C07D405/06 , C07D401/06 , C07D403/06 , C07D495/04
CPC分类号： C07D233/56 , C07D233/10 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
摘要： Compounds having adrenergic activity which are a selective agonists for one or both of the α2B and α2C adrenoceptor receptor subtypes in prefrence to the α2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having formula (I) wherein the dotted lines represent optional bonds; R is H or lower alkyl; X is S or C(H)R1, wherein R1 is H or lower alkyl, Y is O, N, S, (CR12)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y1CH2-, wherein Y1 is O, N or S.

57. 发明授权

EP0924209B1 Hypoglycemic imidazoline compounds 有权
标题翻译：低聚咪唑啉衍生物
公开(公告)号：EP0924209B1
公开(公告)日：2003-05-02
申请号：EP98310461.3
申请日：1998-12-18
申请人： ELI LILLY AND COMPANY
发明人： Jirousek, Michael Robert , Paal, Michael , Rühter, Gerd , Schotten, Theo , Stenzel, Wolfgang , Takeuchi, Kumiko
IPC分类号： C07D403/06 , A61K31/415 , C07D233/10 , C07D233/20 , C07D233/22 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/04 , A61K31/42
CPC分类号： C07D401/04 , C07D233/10 , C07D233/20 , C07D233/22 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/04 , Y02P20/55

58. 发明公开

EP1189891A1 TRIAZOLE COMPOUNDS AND COMBINATORIAL LIBRARIES THEREOF 审中-公开
标题翻译：三唑化合物和组合THEREOF图书馆
公开(公告)号：EP1189891A1
公开(公告)日：2002-03-27
申请号：EP00944744.2
申请日：2000-06-19
申请人： LION Bioscience AG
发明人： QI, Ming , HEBERT, R., Normand , KATRITZKY, Alan, R.
IPC分类号： C07D249/08 , C07D241/06 , C07D233/10 , C07D295/02 , C07F7/08 , A01N43/653
CPC分类号： C07D249/14 , A01N43/653
摘要： The present invention relates to novel triazole compounds of formula (A), wherein R1 to R5 have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing triazole compounds.

59. 发明公开

EP0894003A4 N-FORMYL HYDROXYLAMINE CONTAINING COMPOUNDS USEFUL AS ACE INHIBITORS AND/OR NEP INHIBITORS 失效
标题翻译：含羟胺化合物作为ACE和/或NEP抑制剂N-甲酰基
公开(公告)号：EP0894003A4
公开(公告)日：2000-10-04
申请号：EP97917889
申请日：1997-04-07
申请人： SQUIBB BRISTOL MYERS CO
发明人： ROBL JEFFREY A
IPC分类号： C07D233/10 , A61K31/00 , A61K31/195 , A61K31/198 , A61K31/435 , A61K31/4353 , A61K31/4365 , A61K31/55 , A61K31/551 , A61K31/553 , A61K38/00 , A61P9/00 , A61P9/12 , A61P43/00 , C07C259/06 , C07D267/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D495/14 , C07D498/04 , C07D513/04 , C07K5/02 , C07K5/023 , A61K38/05
CPC分类号： C07K5/0202 , A61K38/00

60. 发明公开

EP0924209A1 Hypoglycemic imidazoline compounds 有权
标题翻译：低聚咪唑啉衍生物
公开(公告)号：EP0924209A1
公开(公告)日：1999-06-23
申请号：EP98310461.3
申请日：1998-12-18
申请人： ELI LILLY AND COMPANY
发明人： Jirousek, Michael Robert , Paal, Michael , Rühter, Gerd , Schotten, Theo , Stenzel, Wolfgang , Takeuchi, Kumiko
IPC分类号： C07D403/06 , A61K31/415 , C07D233/10 , C07D233/20 , C07D233/22 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/04 , A61K31/42
CPC分类号： C07D401/04 , C07D233/10 , C07D233/20 , C07D233/22 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/04 , Y02P20/55
摘要： This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.
The compounds have the following formula:
wherein

X is -O-, -S-, or -NR 5 -,
R 5 is hydrogen, C 1-8 alkyl, or an amino protecting group;
R 1 , R 1' , R 2 , and R 3 are independently hydrogen or C 1-8 alkyl;
R 1 and R 2 optionally together form a bond and R 1' and R 3 are independently hydrogen or C 1-8 alkyl;
R 1 and R 2 optionally combine together with the carbon atoms to which they are attached form a C 3-7 carbocyclic ring and R 1' and R 3 are independently hydrogen or C 1-8 alkyl;
R 1 and R 1' together with the carbon atom to which they are attached optionally combine to form a C 3-7 spirocarbocyclic ring and R 2 and R 3 are independently hydrogen or C 1-8 alkyl;
R 2 and R 3 together with the carbon atom to which they are attached optionally combine to form a C 3-7 spirocarbocyclic and R 1 and R 1' are independently hydrogen or C 1-8 alkyl;
n is 0, 1, or 2;
m is 0, 1 or 2;
m' is 0, 1, or 2;
q' is 0,1,2,3,4, or 5;
R 4 is

Y is -O-, -S-, or -NR 8 -;
Y' is -O- or -S-;
R 6 and R 7 are independently hydrogen, C 1-8 alkyl, C 3-7 cycloalkyl, C 1-8 alkoxy, C 1-8 alkylthio, halo C 1-8 alkylthio, C 1-8 alkylsulfinyl, C 1-8 alkylsulfonyl, C 3-7 cycloalkoxy, aryl-C 1-8 alkoxy, halo, halo-C 1-8 alkyl, halo- C 1-8 alkoxy, nitro, -NR 10 R 11 , -CONR 10 R 11 , aryl C 1-8 alkyl, optionally substituted heterocyclyl, optionally substituted phenyl, optionally substituted naphthyl, optionally halo substituted acylamino, cyano, hydroxy, COR 12 , halo C 1-8 alkylsulfinyl, or halo C 1-8 alkylsulfonyl, or alkoxyalkyl of the formula

CH 3 (CH 2 ) p -O-(CH 2 ) q -O-;

where
p is 0, 1, 2, 3, or 4; and
q is 1, 2, 3, 4, or 5;
R 12 is C 1-8 alkyl or optionally substituted phenyl;
R 8 is hydrogen, C 1-8 alkyl, halo-C 1 _ 8 alkyl, optionally substituted phenyl, optionally substituted heterocyclyl, COO C 1-8 alkyl, optionally substituted COaryl, COC 1-8 alkyl, SO 2 C 1-8 alkyl, optionally substituted SO 2 aryl, optionally substituted phenyl-C 1-8 alkyl, CH 3 (CH 2 ) p -O-(CH 2 ) q -O-;
R 9 is hydrogen, halo, C 1-8 alkyl, halo C 1-8 alkyl, C 1-8 alkylthio, halo C 1-8 alkylthio, C 3-7 cycloalkylthio, optionally substituted arylthio or heteroarylthio, C 1-8 alkoxy, C 3-7 cycloalkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, or optionally substituted aryl or heteroaryl, C 3-7 cycloalkyl, halo C 3-7 cycloalkyl, C 3-7 cycloalkenyl, cyano, COOR 10 ,CONR 10 R 11 or NR 10 R 11 , C 2-6 alkenyl, optionally substituted heterocyclyl, optionally substituted aryl C 1-8 alkyl, optionally substituted heteroaryl C 1-8 alkyl in which the alkyl group can be substituted by hydroxy, or C 1-8 alkyl substituted by hydroxy,
R 10 and R 11 are independently hydrogen, C 1-8 alkyl, optionally substituted aryl C 1-8 alkyl, optionally substituted phenyl, or R 10 and R 11 together with the nitrogen atom to which they are attached may combine to form a ring with up to six carbon atoms which optionally may be substituted with up to two C 1-8 alkyl groups or one carbon atom may be replaced by oxygen or sulfur;
R 14 and R 16 are independently hydrogen, halo, C 1-8 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkoxy, C 3-7 cycloalkylC 1-8 alkoxy, halo-C 1-8 alkyl, halo-C 1-8 alkoxy, C 1-8 alkoxy, carbo(C 1-8 )alkoxy, optionally substituted aryl, or optionally substituted heteroaryl;
R 15 and R 17 are independently hydrogen, halo, C 1-8 alkoxy, C 3-7 -cycloalkyl, C 3-7 cycloalkylC 1-8 alkoxy, C 1-8 alkyl, C 3-7 cycloalkoxy, hydroxy, halo C 1-8 alkoxy, carbo(C 1-8 )alkoxy, optionally substituted phenyl, optionally substituted phenyl-C 1-8 alkyl, optionally substituted phenyloxy, optionally substituted phenyl-C 1-8 alkoxy, (tetrahydropyran-2-yl)methoxy, C 1-8 alkyl-S(O) m -, optionally substituted aryl-C 1-8 alkyl-S(O) m' -, CH 3 (CH 2 ) p -Z 1 -(CH 2 ) q -Z 2 -, or Z 3 -(CH 2 )q'-Z 2 -;
Z 1 and Z 2 are independently a bond, O, S, SO, SO 2 , sulphoximino, or NR 10 ; and
Z 3 is hydroxy, protected hydroxy, NR 10 R 11 , protected amino, SH or protected SH;
provided that when R 1 , R 1' , R 2 and R 3 are all hydrogen; n is 0; R 4 is naphthyl; and R 14 , R 15 and R 16 , or R 15 , R 16 and R 17 are all hydrogen, then R 17 or R 14 , respectively, is other than halo, methoxy, or C1-6 alkyl.
or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及某些新的咪唑啉化合物及其类似物，其用于治疗糖尿病，糖尿病并发症，代谢紊乱或其中存在葡萄糖处置受损的相关疾病，其包含它们的药物组合物及其制备方法。该化合物具有下式：其中X是-O - ， - S-或-NR 5 - ，R 5是氢，C 1-8烷基或氨基保护基的 R 1，R 1，R 2和R 3独立地是氢或C 1-8烷基; R 1和R 2任选地一起形成键，R 1和R 3独立地是氢或C 1-8烷基; R 1和R 2任选地与它们所连接的碳原子一起形成C 3-7碳环，R 1和R 3独立地是氢或C 1-8烷基; R 1和R 1与它们所连接的碳原子一起任选地结合形成C 3-7螺环碳环，R 2和R 3独立地是氢或C 1-8烷基; R 2和R 3与它们所连接的碳原子一起任选地结合形成C 3-7螺环碳环，R 1和R 1独立地是氢或C 1-8烷基; n为0,1或2; m为0,1或2; m'为0,1或2; q'为0,1,2,3,4或5; R 4是 CHEM，Y是-O - ， - S-或-NR 8 - 。 Y'为-O-或-S-; R 6和R 7独立地是氢，C 1-8烷基，C 3-7环烷基，C 1-8烷氧基，C 1-8烷硫基，卤代C 1-8烷硫基，C 1-8烷基亚磺酰基，C 1-8烷基磺酰基，C 3 -7环烷氧基，芳基-C 1-8烷氧基，卤素，卤代-C 1-8烷基，卤代-C 1-8烷氧基，硝基，-NR 10 R 11，-CONR 10 R 11，芳基 C 1-8烷基，任选取代的杂环基，任选取代的苯基，任选取代的萘基，任选的卤素取代的酰基氨基，氰基，羟基，COR 12，卤代C 1-8烷基亚磺酰基或卤代C 1-8烷基磺酰基，或式CH 3的烷氧基烷基（CH2）PO-（CH2）qO-; 其中p为0,1,2,3或4; q为1,2,3,4或5; R 12是C 1-8烷基或任选取代的苯基; R 8是氢，C 1-8烷基，卤代-C 1-8烷基，任选取代的苯基，任选取代的杂环基，COO C 1-8烷基，任选取代的芳基，COC 1-8烷基，SO 2 C 1-8烷基，任选取代的SO 2芳基，任选取代的苯基-C 1-8烷基，CH 3（CH 2）p O-（CH 2）q O-; R 9是氢，卤素，C 1-8烷基，卤代C 1-8烷基，C 1-8烷硫基，卤代C 1-8烷硫基，C 3-7环烷硫基，任选取代的芳硫基或杂芳硫基，C 1-8烷氧基，C 3-7 环烷氧基，任选取代的芳氧基，任选取代的杂芳氧基或任选取代的芳基或杂芳基，C 3-7环烷基，卤素C 3-7环烷基，C 3-7环烯基，氰基，COOR 10，CONR 10 R 11或NR 任选取代的芳基C 1-8烷基，任选取代的杂芳基C 1-8烷基，其中烷基可以被羟基取代，或被C 1-8烷基取代的C 1-8烷基，羟基，R 10和R 11独立地是氢，C 1-8烷基，任选取代的芳基C 1-8烷基，任选取代的苯基，或R 10和R 11与它们的氮原子一起可以结合形成具有多达六个碳原子的环，其任选地可以被至多两个C 1-8烷基取代，或者一个碳原子可以是由氧或硫置换; R 14和R 16独立地是氢，卤素，C 1-8烷基，C 3-7环烷基，C 3-7环烷氧基，C 3-7环烷基C 1-8烷氧基，卤代-C 1-8烷基，卤代-C 1-8 烷氧基，C 1-8烷氧基，碳（C 1-8）烷氧基，任选取代的芳基或任选取代的杂芳基; R 15和R 17独立地是氢，卤素，C 1-8烷氧基，C 3-7 - 环烷基，C 3-7环烷基C 1-8烷氧基，C 1-8烷基，C 3-7环烷氧基，羟基，卤代C 1-8 烷氧基，碳（C 1-8）烷氧基，任选取代的苯基，任选取代的苯基-C 1-8烷基，任选取代的苯氧基，任选取代的苯基-C 1-8烷氧基，（四氢吡喃-2-基）甲氧基，C 1-8烷基 - S（O）m - ，任选取代的芳基-C 1-8烷基-S（O）m'-，CH 3（CH 2）pZ 1 - （CH 2）q Z 2 - 或Z 3 - （CH 2 ）Q'-Z <2> - ; Z 1和Z 2独立地是键，O，S，SO，SO 2，亚肟基或NR 10; Z 3为羟基，被保护的羟基，NR 10 R 11，保护的氨基，SH或被保护的SH; 条件是当R 1，R 1'，R 2和R 3都是氢时; n为0; R 4是萘基; R 14，R 15和R 16或R 15，R 16和R 17均为氢，则R 17或R 14分别为其它比卤代，甲氧基或C 1-6烷基。或其药学上可接受的盐或酯。

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