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1. 发明申请

WO2005108384A1 3- OR 4-MONOSUBSTITUTED PHENOL AND THIOPHENOL DERIVATIVES USEFUL AS H3 LIGANDS 审中-公开
标题翻译： 3-或4-单取代苯酚和噻吩酚衍生物有效用作H3配体
公开(公告)号：WO2005108384A1
公开(公告)日：2005-11-17
申请号：PCT/IB2005/001114
申请日：2005-04-19
申请人： WARNER-LAMBERT COMPANY LLC , BERNARDELLI, Patrick , CRONIN, Andrew, Michael , DENIS, Alexis , DENTON, Stephen, Martin , JACOBELLI, Henry , KEMP, Mark, Ian , LORTHIOIS, Edwige , ROUSSEAU, Fiona , SERRADEIL-CIVIT, Delphine , VERGNE, Fabrice
发明人： BERNARDELLI, Patrick , CRONIN, Andrew, Michael , DENIS, Alexis , DENTON, Stephen, Martin , JACOBELLI, Henry , KEMP, Mark, Ian , LORTHIOIS, Edwige , ROUSSEAU, Fiona , SERRADEIL-CIVIT, Delphine , VERGNE, Fabrice
IPC分类号： C07D309/06
CPC分类号： C07D309/06 , C07D207/08 , C07D207/12 , C07D213/82 , C07D295/088 , C07D295/12 , C07D295/135 , C07D295/155 , C07D295/26 , C07D309/08 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The invention relates to 3- or 4-monosubstituted phenol and thiophenol derivatives of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said 3- or 4-monosubstituted phenol and thiophenol derivatives are H 3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译：本发明涉及式（1）的3-或4-单取代的苯酚和苯硫酚衍生物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。所述3-或4-单取代的苯酚和苯硫酚衍生物是H3配体，可用于许多疾病，病症和病症，特别是炎性，过敏性和呼吸道疾病，病症和病症。

2. 发明申请

WO2002064595A1 TRIAZOLO COMPOUNDS AS MMP INHIBITORS 审中-公开
标题翻译： TRIAZOLO化合物作为MMP抑制剂
公开(公告)号：WO2002064595A1
公开(公告)日：2002-08-22
申请号：PCT/EP2002/001961
申请日：2002-02-11
申请人： WARNER-LAMBERT COMPANY , ANDRIANJARA, Charles , JACOBELLI, Henry , GAUDILLIERE, Bernard , BREUZARD, Francine
发明人： ANDRIANJARA, Charles , JACOBELLI, Henry , GAUDILLIERE, Bernard , BREUZARD, Francine
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound selected from those of formula (I): in which: W represents N or C-R 1 ; in which R 1 is as defined in the description, X represents N or C-R 2 in which R 2 is as defined in the description, Y represents a group selected from oxygen, sulfur, -NH, and -Nalkyl, Z represents a group selected from oxygen, sulphur, -NR 8 in which R 8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z 1 represents a group -CR 9 R 10 wherein R 9 and R 10 , are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R 4 is (are) as defined in the description, R 3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula (II): in which p, Z 2 , B, q, and R 13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of tpe-13 matrix mettaloprotease.
摘要翻译：选自式（I）的化合物：其中：W表示N或C-R 1; 其中R1如说明书中所定义，X表示N或C-R2，其中R2如说明书中所定义，Y表示选自氧，硫，-NH和-N烷基的基团，Z表示选自氧，硫，-NR 8，其中R8如说明书中所定义，可选地取决于Y的定义，n为0至8的整数，其中Z 1为基团-CR 9 R 10，其中R 9和R 10如描述，该组包含任选的多个键或杂原子，A表示环状基团，m是0至7的整数，包括端值，其中R 4是如在说明书中所定义的（是），R 3表示选自氢，烷基，烯基，炔基和式（II）基团：其中p，Z2，B，q和R13如说明书中所定义，任选地，其外消旋形式，异构体，N-氧化物，及其药学上可接受的盐和含有它们的药用产品可用作特定的物质 tpe-13基质蛋白酶的抑制剂。

3. 发明申请

WO2005040168A1 AZABENZODIAZEPINES AS PHOSPHODIESTERASE-4 INHIBITORS 审中-公开
标题翻译： AZABENZODIAZEPINES作为磷酸二酯酶-4抑制剂
公开(公告)号：WO2005040168A1
公开(公告)日：2005-05-06
申请号：PCT/IB2004/003406
申请日：2004-10-18
申请人： WARNER-LAMBERT COMPANY LLC , DEVILLERS, Ingrid , GAUDILLIERE, Bernard , JACOBELLI, Henry , PEVET, Isabelle
发明人： DEVILLERS, Ingrid , GAUDILLIERE, Bernard , JACOBELLI, Henry , PEVET, Isabelle
IPC分类号： C07D471/16
CPC分类号： C07D471/16
摘要： Compounds of formula (I): characterized in that: • R l represents a group selected from hydrogen atom, methyl, methoxy, hydroxy, amino, dimethylamino, acetamido, pyrrolidin-l-yl, and hydroxymethyl; • R 2 represent a group selected from phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, indolyl, pyrolyl, [1,2,3]-triazolyl, benzo[c]isoxazolyl, thienyl, pyrazolyl, isothiazolyl, imidazolyl, benzofuranyl, pyrazolo[5,1-c][1,2,4]triazyl each of these groups being optionally substituted from 1 to 3 groups, identical or different independently of each other, selected from halogen, trifluoromethyl, (C1-C4)alkyl, (C I -C4)alkoxy, hydroxy, amino, acetamido, tert-butyloxycarbonylamino, cycloalkylcarbonylamino, sulfonamide, nitro, acetylmethoxy, cyclopentyloxy; optionally, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and their use as active ingredient in pharmaceutical composition useful for treating diseases involving therapy by inhibition of PDE4.
摘要翻译：式（I）的化合物：其特征在于： R 1表示选自氢原子，甲基，甲氧基，羟基，氨基，二甲基氨基，乙酰氨基，吡咯烷-1-基和羟甲基的基团。。 R2代表选自苯基，吡啶基，嘧啶基，喹啉基，异喹啉基，吲哚基，焦油基，[1,2,3]三唑基，苯并[c]异恶唑基，噻吩基，吡唑基，异噻唑基，咪唑基，苯并呋喃基，吡唑并[ 1-c] [1,2,4]三氮烷，这些基团各自任选被1至3个彼此相同或不同的基团取代，所述基团选自卤素，三氟甲基，（C 1 -C 4）烷基，（C 1 -C 4））烷氧基，羟基，氨基，乙酰氨基，叔丁氧基羰基氨基，环烷基羰基氨基，磺酰胺，硝基，乙酰基甲氧基，环戊氧基; 任选的它们的光学异构体及其与药学上可接受的酸或碱的加成盐，以及它们作为药物组合物的有效成分的用途，可用于治疗涉及通过抑制PDE4治疗的疾病。

4. 发明申请

WO2003076417A2 OXO-AZABICYCLIC COMPOUNDS 审中-公开
标题翻译： OXO-AZABICYCLIC化合物
公开(公告)号：WO2003076417A2
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002277
申请日：2003-03-06
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
IPC分类号： C07D239/91
CPC分类号： C07D471/04 , C07D239/91
摘要： A compound selected from those of formula (1): ~',Xi Gi X 2 (7l) I ,N - R 1 (I) 11 - G 2 X3 wherein: 5 • X,, X2, and X3, represent N or -CR3 in which R3 is as described in the description, • G, represents a group selected from those of formulae (i/a) and (i/b): R4 R6 \ R4 N (i/a) (i/b) in which R4, R5, and R6 are as defined in the description, • G2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, 10 C=S, S(O) n , in which nl represents an integer from 0 to 2 inclusive, or a group of formula (i/c): 11-1y -r ( i/c ) Y 1 in which Y1 represents O, S, -NH or -Nalkyl, and Y2 represents O, S, -NH or -Nalkyl, • n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, 15 • Z, represents -CRgR,o, wherein R9 and R I O areas defined in the description, • A represents a ring system, • R, represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d) (G3)q~(Z2 )~ (i/d) 20 in which p, Z2, B, q and G3 are as defined in the description and optionally, its optical isomers , N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
摘要翻译：选自式（I）的化合物的化合物，其中：X 1，X 2和X 3表示N或-CR 3，其中R 3如描述中所述，G 1表示选自式（i / a）和（其中R 4，R 5和R 6如说明书中所定义，R 2表示选自碳 - 碳三键，-CH = C = CH-，C = O，C = S，S（O ）n1，其中n1表示0〜2的整数，或其中Y1表示O，S，-NH或-N烷基的式（i / c）基团，Y2表示O，S，-NH或-N烷基 n为0以上6以下的整数，m为0以上7以下的整数，Z1为-CR9R10，其中，R9和R10如说明书中所定义，A表示环系，R1表示选自 H，烷基，烯基，炔基，任选被取代的基团和其中p，Z2，B，q和G3如说明书中所定义的任选的其光学异构体，N-氧化物和加成其盐与药学上可接受的 le酸或碱，含有它们的药物可用作13型基质金属蛋白酶的特异性抑制剂。

5. 发明申请

WO2003076416A1 OXO AZABICYCLIC COMPOUNDS 审中-公开
标题翻译： OXO AZABICYCLIC化合物
公开(公告)号：WO2003076416A1
公开(公告)日：2003-09-18
申请号：PCT/EP2002/003240
申请日：2002-03-08
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
IPC分类号： C07D239/91
CPC分类号： C07D471/04 , C07D239/91
摘要： A compound selected from those of formula (I): formula (I) wherein: - X 1 , X 2 , and X 3 , represent N or CR 3 in which R 3 is as described in the description, - G 1 represents a group selected from those of formulae (i/a) and (i/b): formula (II) in which R 4 , R 5 , and R 6 are as defined in the description, - G 2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, C=S, S(O) nt in which n1 represents an integer from 0 to 2 inclusive, or a group of formula (i/c): formula (III) in which Y 1 represents O, S, -NH or Nalkyl, and Y 2 represents O, S, -NH or Nalkyl, - n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z 1 represents CR 9 R 10 , wherein R 9 and R 10 are as defined in the description, - A represents a ring system, - R 1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d): formula (IV) in which p, Z 2 , B, q and G 3 are as defined in the description and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
摘要翻译：选自式（I）的化合物：式（I）其中：-X 1，X 2和X 3表示其中R 3如描述中所述的N或CR 3，-G1表示选自式 I / a）和（i / b）：其中R 4，R 5和R 6如说明书中所定义的式（II），-G2表示选自碳 - 碳三键，-CH = C = CH- ，C = O，C = S，S（O）nt，其中n1表示0〜2的整数，或式（i / c）：式（III）的基团，其中Y1表示O，S， NH或N烷基，Y2表示O，S，-NH或N烷基，-n为0〜6的整数，m为0〜7的整数，Z1表示CR9R10，其中R9和R10如描述，-A表示环系，-R 1表示选自H，烷基，烯基，炔基，任选取代的基团和式（I / d）的基团：式（IV）其中p，Z2，B， q和G3如说明书中所定义，并且任选地，其光学异构体，和其药学上可接受的酸或碱的加成盐和含有它们的药物可用作13型基质金属蛋白酶的特异性抑制剂。

6. 发明申请

WO2004000322A1 THIAZINE AND OXAZINE DERIVATIVES AS MMP-13 INHIBITORS FOR TREATING ARTHRITIS 审中-公开
标题翻译：作为治疗ARTHRITIS的MMP-13抑制剂的噻嗪和氧化衍生物
公开(公告)号：WO2004000322A1
公开(公告)日：2003-12-31
申请号：PCT/EP2003/006601
申请日：2003-06-24
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry
IPC分类号： A61K31/536
CPC分类号： C07D265/26 , C07D279/08
摘要： A compound selected from those of formula (I): wherein: • X 1 , X 2 , and X 3 represent nitrogen or -CR 3 in which R 3 represents hydrogen, alkyl, amino, alkylamino, dialkylamino, hydroxy, alkoxy, or halogen, • G l represents oxygen or S(O) p in which p is from 0 to 2, • G 2 represents carbon-carbon triple bond, C=O, C=S, S(O) q in which q is from 0 to 2, or a group of formula (i/a): in which Y I and Y 2 are as defined in the description, • n is fromO to 6, Z l represents -CR 4 R 5 , wherein R 4 and R 5 are as defined in the description, • A represents 5- or 6-membered monocycle or bicycle aryl, heteroaryl, cycloalkyl, or heterocycloalkyl, • R I represents hydrogen, alkyl, alkenyl, alkynyl, (these groups may be optionally substituted as defined in the description) or the group of formula (i/b): in which s, Z 2 , B, t and G 3 are as defined in the description, and optionally, its optical isomers , N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease, for the treatment of i.a arthritis and cancer.
摘要翻译：选自式（I）的化合物：其中： X 1，X 2和X 3表示氮或-CR 3，其中R 3表示氢，烷基，氨基，烷基氨基，二烷基氨基，羟基，烷氧基或卤素。 G 1表示氧或S（O）p，其中p为0至2。 G2表示碳 - 碳三键，C = O，C = S，其中q为0至2的S（O）q，或式（i / a）的基团：其中YI和Y2如说明，。 n为0至6，Z 1表示-CR 4 R 5，其中R 4和R 5如说明书中所定义。 A表示5-或6-元单环或自由基芳基，杂芳基，环烷基或杂环烷基。 R 1表示氢，烷基，烯基，炔基（这些基团可以如说明书中所定义的任意取代）或式（i / b）的基团：其中s，Z2，B，t和G3如描述和任选的其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作13型基质金属蛋白酶的特异性抑制剂，用于治疗ia关节炎和癌症。

7. 发明申请

WO1997036905A1 DIAZEPINO-INDOLES AS PHOSPHODIESTERASE IV INHIBITORS 审中-公开
标题翻译： DIAZEPINO-INDOLES作为磷酸二酯酶IV抑制剂
公开(公告)号：WO1997036905A1
公开(公告)日：1997-10-09
申请号：PCT/FR1997000557
申请日：1997-03-27
申请人： INSTITUT DE RECHERCHE JOUVEINAL , PASCAL, Yves , JACOBELLI, Henry , CALVET, Alain , PAYNE, Adrian , DAHL, Svein, G.
发明人： INSTITUT DE RECHERCHE JOUVEINAL
IPC分类号： C07D487/06
CPC分类号： C07D487/06
摘要： Diazepino-indoles of formula (I), wherein A is mono- to trisubstituted aryl or heteroaryl, and B is an -OR1 or -NR2R3 group where R1, R2 and R3 are particularly hydrogen, and racemic forms, enantiomers and pharmaceutically acceptable salts thereof, as phosphodiesterase IV inhibitors, are disclosed.
摘要翻译：式（I）的二氮杂 - 吲哚，其中A是一至三取代的芳基或杂芳基，B是其中R 1，R 2和R 3特别是氢的-OR 1或-NR 2 R 3基团，外消旋形式，对映异构体和药学上可接受的盐，作为磷酸二酯酶IV抑制剂。

8. 发明申请

WO1995015948A1 NOVEL 2-ARYLALKENYL-AZACYCLOALKANE DERIVATIVES AS SIGMA RECEPTOR LIGANDS, PREPARATION METHOD THEREFOR AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译：新型2-亚甲基-L-缩水甘油衍生物作为SIGMA受体配体，其制备方法及其治疗用途
公开(公告)号：WO1995015948A1
公开(公告)日：1995-06-15
申请号：PCT/FR1994001439
申请日：1994-12-09
申请人： INSTITUT DE RECHERCHE JOUVEINAL , CALVET, Alain, Pierre , JACOBELLI, Henry , JUNIEN, Jean-Louis , RIVIERE, Pierre , ROMAN, François, Joseph
发明人： INSTITUT DE RECHERCHE JOUVEINAL
IPC分类号： C07D211/14
CPC分类号： C07D495/06 , C07D207/06 , C07D211/14
摘要： Novel 2-arylalkenyl-azacycloalkane derivatives as sigma receptor ligands, having formula (I), wherein Ar is optionally mono- or trisubstituted aryl or heteroaryl, m is 1 or 2, n is 1 to 3, and R is phenyl or C3-7 cycloalkyl; and isomers and addition salts thereof. Antipsychotic and gastroenterology drugs are also provided.
摘要翻译：具有式（I）的新型2-芳基烯基 - 氮杂环烷烃衍生物作为σ受体配体，其中Ar任选为单取代或三取代的芳基或杂芳基，m为1或2，n为1至3，R为苯基或C3-7 环烷基; 异构体及其加成盐。还提供了抗精神病药和胃肠病学药物。

9. 发明申请

WO2004007469A1 NEW ALKYNYLATED QUINAZOLIN COMPOUNDS AS MMP-13 INHIBITORS 审中-公开
标题翻译：新的烷基喹唑啉化合物作为MMP-13抑制剂
公开(公告)号：WO2004007469A1
公开(公告)日：2004-01-22
申请号：PCT/EP2002/008475
申请日：2002-07-12
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
IPC分类号： C07D239/96
CPC分类号： C07D231/12 , C07D233/56 , C07D239/96 , C07D249/08 , C07D403/06 , C07D471/04 , C07D487/04 , C07F7/1856
摘要： A compound selected from those of formula (I) wherein W¿1? represents O, S, or -NR¿3? in which R¿3? represents hydrogen, alkyl, OH or CN; W¿2? represents a group selected from hydrogen, CF¿3?, NH¿2?, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W¿1? and W¿2? form together a group of formula -N=X¿4?-W¿3?- as defined in the description, X¿1?, X¿2? and X¿3? represent N or C optionally substituted, n is 0 to 8, Z represents -CR¿12?R¿13?, wherein R¿12? and R¿13? are as defined in the description, A represents a ring system, the groups R¿2? represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R¿1? represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物，其中W 1表示O，S或-NR 3，其中R？3？表示氢，烷基，OH或CN; W¿2？表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳烷基，环烷基烷基，杂环，这些基团任选取代的基团，或W 1 和W？2？形成一组式-N = X-4'-W 3' - 如说明书中所定义的X 1，X 2，和X？3？表示N或C任选取代，n为0至8，Z表示-CR 12 R 13，其中R 12，和R ?? 13？如在描述中所定义的，A代表一个环系，R = 表示如描述中定义的氢或各种化学基团，q为0至7; R¿1？代表氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作特异性抑制剂 13型基质金属蛋白酶。

10. 发明申请

WO2004000321A1 THIAZINE AND OXAZINE DERIVATIVES AS MMP-13 INHIBITORS FOR TREATING ARTHRITIS 审中-公开
标题翻译：作为治疗ARTHRITIS的MMP-13抑制剂的噻嗪和氧化衍生物
公开(公告)号：WO2004000321A1
公开(公告)日：2003-12-31
申请号：PCT/EP2002/008062
申请日：2002-06-25
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry
IPC分类号： A61K31/536
CPC分类号： C07D265/26 , C07D279/08
摘要： A compound selected from those of formula (I) wherein: X 1 , X 2 and X 3 represent nitrogen or -CR 3 in which R 3 represents hydrogen, alkyl, amino, alkylamino, dialkylamino, hydroxy, alkoxy, or halogen, G 1 represents oxygen or S(O) p in which p is from 0 to 2, G 2 represents carbon-carbon triple bond, C=O, C=S, S(O) q in which q is from 0 to 2, or a group of formula (i/a) in which Y 1 and Y 2 are as defined in the description, n is from 0 to 6, Z 1 represents CR 4 R 5 . wherein R 4 and R 5 are as defined in the description, A represents 5- or 6-membered monocycle or bicycle aryl, heteroaryl, cycloalkyl, or heterocycloalkyl, R 1 represents hydrogen, alkyl, alkenyl, alkynyl, (these groups may be optionally substituted as defined in the description) or the group of formula (i/b) in which s, Z 2 , B, t and G 3 are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease, for the treatment of i.a arthritis and cancer.
摘要翻译：选自式（I）的化合物，其中：X> 1 <，X> 2 <和X> 3代表氮或-CR 3，其中R 3表示氢，烷基，氨基，烷基氨基，二烷基氨基，羟基，烷氧基或卤素，G> 1 <代表氧或S（O）> p 2 <表示碳 - 碳三键，C = O，C = 其中q为0至2的S（O）q>或其中Y> 1 <和Y> 2 <如描述中所定义的式（i / a）的基团，n为0至6 ，Z> 1 4 <5>。 A表示5-或6-元单环或自由基芳基，杂芳基，环烷基或杂环烷基，R 1表示氢，烷基，烯基，炔基，（这些基团可以如说明书中定义的任选取代）或其中s，Z> 2 <，B，T和G> 3 <如说明书中所定义的式（i / b）的基团，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和含有它们的药物可用作13型基质金属蛋白酶的特异性抑制剂，用于治疗关节炎和癌症。

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