公开(公告)号：US5252560A

公开(公告)日：1993-10-12

申请号：US905933

申请日：1992-06-29

申请人： Peter L. Myers ,  Andrew B. McElroy ,  Michael Gregson ,  Peter J. Brown ,  Howard G. Davies ,  David H. Drewry ,  Michael A. Foley

发明人： Peter L. Myers ,  Andrew B. McElroy ,  Michael Gregson ,  Peter J. Brown ,  Howard G. Davies ,  David H. Drewry ,  Michael A. Foley

IPC分类号： A61K38/55 ,  A61K38/00 ,  A61P1/02 ,  A61P17/00 ,  A61P19/10 ,  A61P25/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D209/48 ,  C07D209/66 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  A61K37/02 ,  C07D413/12

CPC分类号： C07K5/0222 ,  A61K38/00

摘要： Compounds are described of the formula ##STR1## wherein: R.sup.1 is C.sub.3-6 alkyl or C.sub.1-3 alkylthioC.sub.1-3 alkyl;R.sup.2 is an optionally substituted C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, aryl, heteroaryl, arylC.sub.1-4 alkyl, heteroarylC.sub.1-4 alkyl or a side-chain of a natural .alpha.-amino acid;R.sup.3 is hydrogen, C.sub.1-6 alkyl, CHR.sup.4 COR.sup.5 (where R.sup.4 is a side-chain of a natural .alpha.-amino acid and R.sup.5 is hydroxyl, C.sub.1-6 alkoxy or NHR.sup.6 where R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group) or a group (CH.sub.2).sub.n X (where n is 1 to 6 and X is hydroxyl, C.sub.1-4 alkoxy, heteroaryl or a group NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-6 alkyl or the group NR.sup.7 R.sup.8 forms a 5 to 7 membered cyclic amine); andHet is an optionally substituted cyclic imide where the cyclic imide ring system has the formula (i), (ii) or (iii) ##STR2## in which A, B, C and D are each CH or 1 or 2 of A, B, C and D represents N and the others represent CH, and E and F may each independently represent CH or N; and physiologically acceptable salts and solvates thereof.These compounds inhibit metalloproteases involved in tissue degradation. Compounds of the invention may be formulated for use in a variety of conditions involving tissue degradation including arthropathy, dermatological conditions, bone resorption, inflammatory diseases, tumour invasion and multiple sclerosis and related diseases involving myelin degradation, and in the promotion of wound healing.

公开(公告)号：US5326760A

公开(公告)日：1994-07-05

申请号：US31439

申请日：1993-03-15

申请人： Andrew B. McElroy ,  Peter J. Brown ,  David H. Drewry ,  James M. Salovich ,  Frank J. Schoenen

发明人： Andrew B. McElroy ,  Peter J. Brown ,  David H. Drewry ,  James M. Salovich ,  Frank J. Schoenen

IPC分类号： C07C237/06 ,  C07D209/48 ,  C07D209/66 ,  C07D213/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D453/02 ,  C07D487/04 ,  C07F7/18 ,  A61K31/395 ,  A61K31/40

CPC分类号： C07D209/48 ,  C07C237/06 ,  C07D209/66 ,  C07D213/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D453/02 ,  C07D487/04 ,  C07F7/1852 ,  C07F7/1856

摘要： Aminobutanoic acids of the following formula (I): ##STR1## where R.sup.1 -R.sup.5 are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases, demyelinating diseases, and tumor metastasis, methods for such treatment and processes for preparing compounds of formula (I).

摘要翻译： 下式（I）的氨基丁酸：其中R1-R5是多种取代基，新型中间体，用于治疗炎性疾病，脱髓鞘疾病和肿瘤转移的药物组合物，其用于治疗和治疗的方法 用于制备式（I）的化合物。