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1. 发明申请

WO2008033757A3 2-(1-OXO-1H-ISOQUINOLIN-2-YL) ACETAMIDE DERIVATIVES 审中-公开
标题翻译： 2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物
公开(公告)号：WO2008033757A3
公开(公告)日：2008-12-11
申请号：PCT/US2007077999
申请日：2007-09-10
申请人： ORGANON NV , LETOURNEAU JEFFREY , CHAN JUI HSIANG , JOKIEL PATRICK , OHLMEYER MICHAEL , NEAGU IRINA , RIVIELLO CHRISTOPHER MARK , MORPHY JOHN RICHARD , NAPIER SUSAN ELIZABETH , HO KOC-KAN
发明人： LETOURNEAU JEFFREY , CHAN JUI HSIANG , JOKIEL PATRICK , OHLMEYER MICHAEL , NEAGU IRINA , RIVIELLO CHRISTOPHER MARK , MORPHY JOHN RICHARD , NAPIER SUSAN ELIZABETH , HO KOC-KAN
IPC分类号： C07D217/24 , A61K31/472
CPC分类号： C07D217/24 , C07D401/12
摘要： The present invention relates to a 2-(1-oxo-IH-isoquinolin-2-yl)acetamide derivative of formula (I).
摘要翻译：本发明涉及式（I）的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物。

2. 发明申请

WO2008020081A1 6-SUBSTITUTED ISOQUINOLINE DERIVATIVES AS ROCK-1 INHIBITORS 审中-公开
标题翻译： 6取代的异喹啉衍生物作为ROCK-1抑制剂
公开(公告)号：WO2008020081A1
公开(公告)日：2008-02-21
申请号：PCT/EP2007/058593
申请日：2007-08-17
申请人： N.V. ORGANON , RAY, Peter, Christopher , LAATS, Steven , MORPHY, John, Richard , SHERBORNE, Brad
发明人： RAY, Peter, Christopher , LAATS, Steven , MORPHY, John, Richard , SHERBORNE, Brad
IPC分类号： C07D217/22 , C07D217/24 , A61K31/472 , A61P9/10 , A61P27/06
CPC分类号： C07D217/22 , C07D217/24
摘要： The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH 2 ; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R 1 is H, when Y is NH 2 ; or R 1 is H, (C 1-4 )alk yl or halogen, when Y is OH; R 2 and R 3 are independently H, (C 1-4 )alkyl or halogen; R 4 is H or (C 1-6 )alkyl, optionally substituted with halogen, (C 3-7 )cycloalkyl, (C 6-10 )aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C 6-10 )aryl and heterocyclic ring being optionally substituted with (C 1-4 )alkyl, (C 1-4 )alkyloxy or halogen; R 5 is H or (C 1-4 )alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH, n is 0 and m+o =2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
摘要翻译：本发明涉及具有通式I的6-取代的异喹啉衍生物，其中X是O，S或NH; Y是OH或NH 2; m为0,1或2; n为0或1; o为0或1; R 1是H，当Y是NH 2时; 或者R 1是H，（C 1-4）烷基或卤素，当Y是OH时; R 2和R 3独立地是H，（C 1-4烷基）烷基或卤素; R 4是H或（C 1-6 - ）烷基，任选被卤素，（C 3-7）环烷基取代，（C 1 -C 6）（C 6-10）芳基或饱和的5-或6-元杂环，其包含1-3个独立地选自O，S和N的杂原子，芳基和杂环任选被（C 1-4烷基）烷基，（C 1-4-4烷基）烷氧基或卤素取代; R 5是H或（C 1-4烷基）烷基; 或其药学上可接受的盐，条件是其中X为O，Y为OH，n为0且m + o = 2的式I化合物排除于包含该化合物的药物组合物中，以及使用的所述6-取代的异喹啉衍生物用于制备用于治疗ROCK-1相关疾病如青光眼，高血压和动脉粥样硬化的药物。

3. 发明申请

WO2004071445A2 2-(AMINOMETHYL)ARYLAMIDE ANALGESICS 审中-公开
标题翻译： 2-（氨基甲基）丙酰胺解毒剂
公开(公告)号：WO2004071445A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/004017
申请日：2004-02-11
申请人： PHARMACOPEIA DRUG DISCOVERY, INC. , HO, Koc-Kan , BALDWIN, John, J. , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , MCDONALD, Edward , GUO, Tao , MORPHY, John, Richard , RANKOVIC, Zoran , HORLICK, Robert , APPELL, Kenneth, C.
发明人： HO, Koc-Kan , BALDWIN, John, J. , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , MCDONALD, Edward , GUO, Tao , MORPHY, John, Richard , RANKOVIC, Zoran , HORLICK, Robert , APPELL, Kenneth, C.
IPC分类号： A61K
CPC分类号： C07C237/30 , C07C237/32 , C07C311/08 , C07C311/37 , C07C323/42 , C07C2602/10 , C07C2602/12 , C07D207/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/81 , C07D217/04 , C07D223/16 , C07D295/155 , C07D401/06 , C07D401/12 , C07D471/04
摘要： A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed. The genus is represented by the Formula I: a representative example is:
摘要翻译：公开了可用作镇痛剂的2-（氨基甲基）芳基酰胺的化学属。该属由公式I表示：一个代表性的例子是：

4. 发明申请

WO2003010132A1 N-[(1-DIMETHYLAMINOCYCLOALKYL)METHYL]BENZAMIDE DERIVATIVES 审中-公开
标题翻译： N - [（1-二甲基氨基甲酰基）甲基]苯甲酰胺衍生物
公开(公告)号：WO2003010132A1
公开(公告)日：2003-02-06
申请号：PCT/EP2002/007892
申请日：2002-07-11
申请人： AKZO NOBEL N.V. , MORPHY, John, Richard , RANKOVIC, Zoran
发明人： MORPHY, John, Richard , RANKOVIC, Zoran
IPC分类号： C07C233/79
CPC分类号： C07D333/16 , C07C235/50 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18
摘要： The present invention relates to N-[(1-dimethylaminocycloalkyl)methyl]benzamide I derivatives having the general formula (I) wherein n is 0, 1, 2 or 3; R 1 and R 2 are independently H, (C 1-4 )alkyl or (C 1-4 )alkyloxy; R3 is (C 3-8 )alkyl, (C 4-7 )cycloalkyl, (C 4-7 )cycloalkyl (C 1-3 )alkyl, (C 6-12 )aryl(C 1-3 )alkyl (wherein the aryl moiety is optionailly substituted with 1-3 substituents selected from (C1-4)alkyl, (C 1-4 )alkyloxy, halogen, trifluoromethyl and methoxycarbonyl), or (C 4-9 )- heteroaryl(C 1-3 )alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives in the treatment of disorders or conditions which are responsive to inhibition of the GlyT-2 transporter, such as muscle spasticity, epilepsy and, particularly, acute, chronic and neuropathic pain.
摘要翻译：本发明涉及具有通式（I）的N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺I衍生物，其中n为0,1,2或3; R1和R2独立地为H，（C1-4）烷基或（C1-4）烷氧基; R3是（C3-8）烷基，（C4-7）环烷基，（C4-7）环烷基（C1-3）烷基，（C6-12）芳基（C1-3）烷基（其中芳基部分选择性地被 1-3个选自（C 1-4）烷基，（C 1-4）烷氧基，卤素，三氟甲基和甲氧基羰基的取代基）或（C 4-9） - 杂芳基（C 1-3）烷基; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物用于治疗对抑制GlyT-2转运蛋白有响应的病症或病症的用途，例如肌肉痉挛，癫痫，特别是急性，慢性和神经性疼痛。

5. 发明申请

WO1993024475A1 SULPHAMIDE DERIVATIVES AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：磺酰胺衍生物作为金属蛋白酶抑制剂
公开(公告)号：WO1993024475A1
公开(公告)日：1993-12-09
申请号：PCT/GB1993001185
申请日：1993-06-03
申请人： CELLTECH LIMITED , PORTER, John, Robert , MORPHY, John, Richard , MILLICAN, Thomas, Andrew , BEELEY, Nigel, Robert, Arnold
发明人： CELLTECH LIMITED
IPC分类号： C07D295/22
CPC分类号： C07D295/26 , C07C307/06 , C07C2601/14 , C07C2601/16
摘要： Compounds of formula (1) are described wherein R represents a -CONHOH, carboxyl (-CO2H), esterified carboxyl or -P(O)(X R )X R group, where X and X , which may be the same or different is each an oxygen or a sulphur atom, and R and R , which may be the same or different each represents a hydrogen atom or an optionally substituted alkyl, aryl or aralkyl group; R represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R represents an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkoxy, or aralkylthio group, or an amino (-NH2), substituted amino, carboxyl (-CO2H) or esterified carboxyl group; R represents a hydrogen atom or an alkyl group; R represents a hydrogen atom or an alkyl group; R represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms of -N(R )- groups, [where R is a hydrogen atom or a C1-6 alkyl group] or a group -(Alk)nR where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R )- groups, n is zero or an integer 1, and R is an optionally substituted cycloalkyl or cycloalkenyl group; X represents a group -NR R where R is a hydrogen atom or an optionally substituted alkyl, alkanoyl, aryl, aroyl, aralkyl or aralkanoyl group, and R is a straight or branched alkylaminosulphonylamino group wherein the alkyl portion is optionally interrupted by one or more -O- or -S- atoms or N(R )- or aminocarbonyloxy groups; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective inhibitory action against gelatinase and may be of use in the treatment of cancer to control the development of tumour metastases.
摘要翻译：描述式（1）化合物，其中R表示-CONHOH，羧基（-CO 2 H），酯化羧基或-P（O）（X 1 R 8）X 2 R 9基团，其中 X 1和X 2可以相同或不同，各自为氧或硫原子，R 8和R 9可以相同或不同，表示氢原子或任选取代的烷基，芳基或芳烷基; R 1表示氢原子或任选取代的烷基，烯基，芳基，芳烷基，杂芳烷基或杂芳硫基烷基; R 2表示任选取代的烷基，烯基，环烷基，环烷基烷基，芳基，芳烷基，芳烷氧基或芳烷硫基，或氨基（-NH 2），取代的氨基，羧基（-CO 2 H）或酯化羧基。 R 3表示氢原子或烷基; R 4表示氢原子或烷基; R 5表示任选被-N（R 7） - 基团的一个或多个-O-或-S-原子间隔的任意取代的烷基或链烯基，其中R 7是氢原子或 C 1-6烷基]或基团 - （Alk）n R 6，其中Alk是任选被一个或多个-O-或-S-或-N（R 7） - 基团间隔的烷基或烯基，n为0或整数1，R 6为任选取代的环烷基或环烯基; X表示-NR 10 R 11基团，其中R 10为氢原子或任选取代的烷基，烷酰基，芳基，芳酰基，芳烷基或芳烷酰基，R 11为直链或支链烷基氨基磺酰基氨基基团，其中烷基部分任选地被一个或多个-O-或-S-原子或N（R 7） - 或氨基羰基氧基中断; 及其盐，溶剂化物和水合物。化合物是金属蛋白酶抑制剂，特别是对明胶酶具有选择性抑制作用，并且可用于治疗癌症以控制肿瘤转移的发展。

6. 发明申请

WO1993014096A1 PHOSPHONO DERIVATIVES OF AMINO ACIDS AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：作为金属蛋白酶抑制剂的氨基酸的磷酸衍生物
公开(公告)号：WO1993014096A1
公开(公告)日：1993-07-22
申请号：PCT/GB1993000086
申请日：1993-01-15
申请人： CELLTECH LIMITED , BEELEY, Nigel, Robert, Arnold , MILLICAN, Thomas, Andrew , MORPHY, John, Richard
发明人： CELLTECH LIMITED
IPC分类号： C07F09/38
CPC分类号： C07F9/6533 , C07F9/3808 , C07F9/4006
摘要： Compounds of formula (I) are described wherein R represents a -P(O)(X R )X R group, where X and X , which may be the same of different, is each an oxygen or a sulphur atom, and R and R , which may be the same or different each represents a hydrogen atom or an optionally substituted alkyl, aryl, or aralkyl group; R represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R represents an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkoxy, or aralkylthio group, or an amino (-NH2), substituted amino, carboxyl (-CO2H) or esterified carboxyl group; R represents a hydrogen atom or an alkyl group; R represents a hydrogen atom or an alkyl group; R represents a group -[Alk]nR where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R )- groups [where R is a hydrogen atom or a C1-6alkyl group], n is zero or an integer 1, and R is an optionally substituted cycloalkyl or cycloalkenyl group; X represents an amino (-NH2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastasises.
摘要翻译：描述式（I）的化合物，其中R表示-P（O）（X 1 R 6）X 2 R 7基团，其中X 1和X 2可以是相同的，各自为氧或硫原子，R 6和R 7可以相同或不同，各自表示氢原子或任选取代的烷基，芳基或芳烷基; R 1表示氢原子或任选取代的烷基，烯基，芳基，芳烷基，杂芳烷基或杂芳硫基烷基; R 2表示任选取代的烷基，烯基，环烷基，环烷基烷基，芳基，芳烷基，芳烷氧基或芳烷硫基，或氨基（-NH 2），取代的氨基，羧基（-CO 2 H）或酯化羧基。 R 3表示氢原子或烷基; R 4表示氢原子或烷基; R 5表示基团 - [Alk] n R 8，其中Alk是任选被一个或多个-O-或-S-原子或-N（R 9） - 基团间隔的烷基或链烯基[其中 R 9为氢原子或C 1-6烷基]，n为0或整数1，R 8为任选取代的环烷基或环烯基; X表示氨基（-NH 2）或取代的氨基，羟基或取代的羟基; 及其盐，溶剂化物和水合物。化合物是金属蛋白酶抑制剂，特别是具有选择性明胶酶作用，并且可用于治疗癌症以控制肿瘤转移的发展。

7. 发明申请

WO1992009565A1 PEPTIDYL DERIVATIVES 审中-公开
标题翻译：肽衍生物
公开(公告)号：WO1992009565A1
公开(公告)日：1992-06-11
申请号：PCT/GB1991002143
申请日：1991-12-03
申请人： CELLTECH LIMITED , PORTER, John, Robert , MORPHY, John, Richard , MILLICAN, Thomas, Andrew , BEELEY, Nigel, Robert, Arnold
发明人： CELLTECH LIMITED
IPC分类号： C07C259/06
CPC分类号： C07C55/02 , A61K38/00 , C07C237/22 , C07C259/06 , C07C311/46 , C07C2601/14 , C07D209/20 , C07K5/06052 , C07K5/06113
摘要： Compounds of formula (I) are described wherein R represents a -CONHOH, carboxyl (-CO2H) or esterified carboxyl group; R1 represents an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R2 represents an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkoxy, or aralkylthio group, or an amino (-NH¿2?), substituted amino, carboxyl (-CO2H) or esterified carboxyl group; R?3¿ represents a hydrogen atom or an alkyl group; R4 represents a hydrogen atom or an alkyl group; R5 represents a group -[Alk]¿nR?6 where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R7)- groups [where R7 is a hydrogen atom or a C¿1-6?alkyl group], n is zero or an integer 1, and R?6¿ is an optionally substituted cycloalkyl or cycloalkenyl group; X represents an amino (-NH¿2?), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastases.
摘要翻译：其中R是-CONHOH，羧基（-CO2H）或酯化的羧基的式（I）化合物; R1代表任选取代的烷基，烯基，芳基，芳烷基，杂芳烷基或杂芳硫基烷基; R 2是烷基，链烯基，环烷基，环烷基烷基，芳基，芳烷基，芳烷氧基或芳烷硫基任选地被取代，或氨基（-NH 2），取代的氨基，羧基（-CO 2 H）或酯化的羧基; R3代表氢原子或烷基; R4代表氢原子或烷基; R 5表示的基团 - [ALK] NR 6，其中Alk为烷基或烯基任选地被一个或多个-O-或-S-原子或-N（R 7）中断 - [其中R 7是一个氢原子或一个 C 1-6烷基; n为0或整数1，并且R 6表示任选取代的环烷基或环烯基; 或取代的羟基; 和它们的盐，溶剂化物和水合物。这些化合物是金属蛋白酶的抑制剂，特别表现出选择性明胶酶活性，并可用于通过抵抗肿瘤转移的发展来治疗癌症。

8. 发明申请

WO2006095014A1 2- (4-0X0-4H-QUINAZ0LIN-3-YL) ACETAMIDES AND THEIR USE AS VASOPRESSIN V3 ANTAGONISTS 审中-公开
标题翻译： 2-（4-0X0-4H-喹喔啉-3-基）乙酰胺及其作为VASOPRESSIN V3拮抗剂的用途
公开(公告)号：WO2006095014A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060612
申请日：2006-03-10
申请人： AKZO NOBEL N.V. , PHARMACOPEIA DRUG DISCOVERY, INC. , LETOURNEAU, Jeffrey , RIVIELLO, Christopher , HO, Koc-Kan , CHAN, Jui-Hsiang , OHLMEYER, Michael , JOKIEL, Patrick , NEAGU, Irina , MORPHY, John, Richard , NAPIER, Susan, Elizabeth
发明人： LETOURNEAU, Jeffrey , RIVIELLO, Christopher , HO, Koc-Kan , CHAN, Jui-Hsiang , OHLMEYER, Michael , JOKIEL, Patrick , NEAGU, Irina , MORPHY, John, Richard , NAPIER, Susan, Elizabeth
IPC分类号： C07D239/91 , C07D403/10 , A61K31/517 , C07D403/04 , A61P25/24 , C07D409/04 , C07D401/12 , C07D401/10 , C07D401/04 , C07D405/04
CPC分类号： C07D409/04 , C07D239/91 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04
摘要： The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
摘要翻译：本发明涉及式（I）的2-（4-氧代-4-喹唑啉-3-基）乙酰胺衍生物及其作为加压素V3拮抗剂的用途，特别是用于治疗抑郁症。

9. 发明申请

WO2002100861A1 1-(3-PHENYLOXYPROPYL)PIPERIDINE DERIVATIVES 审中-公开
标题翻译： 1-（3-苯基丙基）哌啶衍生物
公开(公告)号：WO2002100861A1
公开(公告)日：2002-12-19
申请号：PCT/EP2002/006313
申请日：2002-06-07
申请人： AKZO NOBEL N.V. , COWLEY, Phillip, Martin , COTTNEY, Jean , BARN, David, Raeburn , MORPHY, John, Richard , PALIN, Ronald , GROVE, Simon, James, Anthony
发明人： COWLEY, Phillip, Martin , COTTNEY, Jean , BARN, David, Raeburn , MORPHY, John, Richard , PALIN, Ronald , GROVE, Simon, James, Anthony
IPC分类号： C07D471/10
CPC分类号： C07D401/04 , C07D471/10
摘要： The present invention relates to 1(3-phenyloxypropyl)-piperidine derivative having general Formula (I), wherein R1 is (C 1-6 )alkyl or (C 4-8 )cycloalkyl or phenyl, optionally substituted with (C 1-6 )alkyl, (C 1-6 )alkyloxy or halogen; R2 is H or (C 1-6 )alkyl; or R1 and R2 form together with the carbon atom to which they are bound (C 4-8 )cycloalkyl, optionally substitutes with (C 1-6 )alkyloxy or halogen; R3 is H, OH, (C 1-6 )alkyloxy or (C 1-6 )alkylcarbonyloxy; R4 represents 1-5 substituents independently selected from H, (C 1-6 )alkyl, (C 1-6 )alkyloxy and halogen; Y represents (a), (b) and Z is H; or Y and Z together with the carbon atom to which they are bound represent the spiro atom in the spiro atom in the spiro system formed with (c) *represents the spiro carbon atom; R6 is H, (C 1-6 )alkyl or (CO)n-(CH 2 )m-R12; n is 0 or 1; m is 1-4; R8 and R10 are independently H or(C 1-6 )alkyl; R7, R9 and R11 are independently H, (C 1-6 )alkyl, (C 1-6 )alkyloxy or halogen; R12 is hydroxy, (C 1-4 )alkyloxy, (C 1-4 )alkylthio, (C 1-4 )alkyloxycarbonyl, (C 1-4 )alkylcarbonyloxy, 2-tetrahydrofuranyl, 4-morpholinyl or di(C 1-4 )alkylamino; or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 1-(3-phenyloxypropyl)-piperidine derivatives in therapy.
摘要翻译：本发明涉及具有通式（I）的1（3-苯氧基丙基） - 哌啶衍生物，其中R 1为（C 1-6）烷基或（C 4-8）环烷基或任选被（C 1-6）烷基取代的苯基，（C 1-6）烷氧基或卤素; R2是H或（C1-6）烷基; 或R 1和R 2与它们所连接的碳原子一起形成（C 4-8）环烷基，任选地与（C 1-6）烷氧基或卤素取代; R3是H，OH，（C1-6）烷氧基或（C1-6）烷基羰基氧基; R 4表示独立地选自H，（C 1-6）烷基，（C 1-6）烷氧基和卤素的1-5个取代基; Y表示（a），（b），Z表示H; 或者Y和Z与它们所连接的碳原子一起表示在（c）中形成的螺系中的螺原子中的螺原子*代表螺
碳原子; R6是H，（C1-6）烷基或（CO）n-（CH2）m-R12; n为0或1; m为1-4; R 8和R 10独立地为H或（C 1-6）烷基; R 7，R 9和R 11独立地为H，（C 1-6）烷基，（C 1-6）烷氧基或卤素; R 12是羟基，（C 1-4）烷氧基，（C 1-4）烷硫基，（C 1-4）烷氧基羰基，（C 1-4）烷基羰基氧基，2-四氢呋喃基，4-吗啉基或二（C 1-4）烷基氨基; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些1-（3-苯氧基丙基） - 哌啶衍生物在治疗中的用途。

10. 发明申请

WO1993024449A1 PEPTIDYL DERIVATIVES AND THEIR USE AS METALLOPROTEINASES INHIBITORS 审中-公开
标题翻译：肽衍生物及其作为金属蛋白酶抑制剂的用途
公开(公告)号：WO1993024449A1
公开(公告)日：1993-12-09
申请号：PCT/GB1993001186
申请日：1993-06-03
申请人： CELLTECH LIMITED , PORTER, John, Robert , MORPHY, John, Richard , MILLICAN, Thomas, Andrew , BEELEY, Nigel, Robert, Arnold
发明人： CELLTECH LIMITED
IPC分类号： C07C237/22
CPC分类号： C07C259/06 , C07C237/22 , C07C2601/14 , C07D213/56
摘要： Compounds of formula (1) are described wherein R represents a -CONHOH, carboxyl (-CO2H), esterified carboxyl or -P(O)(X R )X R group, where X and X , which may be the same or different is each an oxygen or a sulphur atom, and R and R , which may be the same or different each represents a hydrogen atom or an optionally substituted alkyl, aryl or aralkyl group; R represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R represents an optionally substituted aryloxy, arylthio, aryloxyalkyl, arylthioalkyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl or heteroarylthioalkyl group; R represents a hydrogen atom or an alkyl group; R represents a hydrogen atom or an alkyl group; R represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R ) groups, [where R is a hydrogen atom or a C1-6 alkyl group] or a group -[Alk]nR where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R ) groups, n is zero or an integer 1 and R is an optionally substituted cycloalkyl or cycloalkenyl group; X represents an amino (-NH2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular are selective inhibitors of the action of gelatinase, and may be of use in the treatment of cancer to control the development of tumour metastases.
摘要翻译：描述式（1）化合物，其中R表示-CONHOH，羧基（-CO 2 H），酯化羧基或-P（O）（X 1 R 8）X 2 R 9基团，其中 X 1和X 2可以相同或不同，各自为氧或硫原子，R 8和R 9可以相同或不同，表示氢原子或任选取代的烷基，芳基或芳烷基; R 1表示氢原子或任选取代的烷基，烯基，芳基，芳烷基，杂芳烷基或杂芳硫基烷基; R 2表示任选取代的芳氧基，芳硫基，芳氧基烷基，芳硫基烷基，杂芳基，杂芳烷基，杂芳氧基，杂芳硫基，杂芳氧基烷基或杂芳硫基烷基; R 3表示氢原子或烷基; R 4表示氢原子或烷基; R 5表示任选被一个或多个-O-或-S-或-N（R 7）基团间隔的任选取代的烷基或烯基，其中R 7是氢原子或C1 -6烷基]或基团 - [Alk] nR 6，其中Alk是任选地被一个或多个-O-或-S-或-N（R 7）基团间隔的烷基或烯基，n 为零或整数1，R 6为任选取代的环烷基或环烯基; X表示氨基（-NH 2）或取代的氨基，羟基或取代的羟基; 及其盐，溶剂化物和水合物。化合物是金属蛋白酶抑制剂，特别是明胶酶作用的选择性抑制剂，并且可用于治疗癌症以控制肿瘤转移的发展。

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