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1. 发明授权

US06353006B1 Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents 有权
标题翻译：取代的2-芳基亚氨基杂环和含有它们的组合物，用作孕激素受体结合剂
公开(公告)号：US06353006B1
公开(公告)日：2002-03-05
申请号：US09453613
申请日：1999-12-03
申请人： Brian R. Dixon , Cedo M. Bagi , Catherine R. Brennan , David R. Brittelli , William H. Bullock , Jinshan Chen , William L. Collibee , Robert Dally , Jeffrey S. Johnson , Harold C. E. Kluender , William F. Lathrop , Peiying Liu , Carol Ann Mase , Anikó M. Redman , William J. Scott , Klaus Urbahns , Donald J. Wolanin
发明人： Brian R. Dixon , Cedo M. Bagi , Catherine R. Brennan , David R. Brittelli , William H. Bullock , Jinshan Chen , William L. Collibee , Robert Dally , Jeffrey S. Johnson , Harold C. E. Kluender , William F. Lathrop , Peiying Liu , Carol Ann Mase , Anikó M. Redman , William J. Scott , Klaus Urbahns , Donald J. Wolanin
IPC分类号： A01N4340
CPC分类号： C07D263/28 , C07D263/58 , C07D277/18 , C07D277/60 , C07D279/06 , C07D281/02 , C07D417/06 , C07D417/12 , C07D513/04 , C07D513/10
摘要： This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
摘要翻译：本发明涉及2-芳基亚氨基杂环，包括2-芳基亚氨基-1,3-噻唑烷，2-芳基亚氨基-2,3,4,5-四氢-1,3-噻嗪，2-芳基亚氨基-1,3-噻唑烷-2-酮， 4-芳基亚氨基-1,3-噻唑烷-5-酮和2-芳基亚氨基-1,3-恶唑烷，以及它们在调节孕酮受体介导的过程中的用途，以及用于这些疗法的药物组合物。

2. 发明授权

US06784167B2 17-beta-hydroxysteroid dehydrogenase-II inhibitors 失效
标题翻译： 17-β-羟基类固醇脱氢酶II抑制剂
公开(公告)号：US06784167B2
公开(公告)日：2004-08-31
申请号：US09967430
申请日：2001-09-28
申请人： Jill E. Wood , Jeremy L. Baryza , Catherine R. Brennan , Soongyu Choi , James H. Cook , Brian R. Dixon , Paul P. Ehrlich , David E. Gunn , Ian McAlexander , Peiying Liu , Derek B. Lowe , Anikó M. Redman , William J. Scott , Yamin Wang
发明人： Jill E. Wood , Jeremy L. Baryza , Catherine R. Brennan , Soongyu Choi , James H. Cook , Brian R. Dixon , Paul P. Ehrlich , David E. Gunn , Ian McAlexander , Peiying Liu , Derek B. Lowe , Anikó M. Redman , William J. Scott , Yamin Wang
IPC分类号： A61K3140
CPC分类号： C07D207/26 , C07D207/325 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D417/06
摘要： 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl. Pharmaceutically acceptable salts and N-oxides of these materials are also included. Also claimed are pharmaceutical compositions containing these materials and methods of using them.
摘要翻译：具有被标记为A的苯基的基团的结构式-17-β-羟基类固醇脱氢酶II抑制剂和基团-C（R 4）（R 6）Y取代为彼此顺式; W表示O或S; R 1表示-H或任选取代的 - （C 1 -C 4）烷基; n表示0或1-3的整数; 并且R 2代表环A上的任何取代基.R 4通常表示-H，但可以是在环A的邻位终止的键.Y表示氟，-OR 5或 - （C 1 -C 4）烷基，任选取代的 - 苯基，任选取代的（C 1 -C 4）烷基 - 苯基或任选取代的 - （C 1 -C 4）酰基。 R 6表示说明书和权利要求中定义的各种基团中的任何一种，包括杂芳基，芳基烷基，杂芳基烷基，芳基烯基，杂芳基烯基，炔基，芳基炔基，杂芳基炔基，芳基和吲哚基。也包括这些材料的药学上可接受的盐和N-氧化物。还要求保护的是含有这些材料的药物组合物和使用它们的方法。

3. 发明授权

US5863915A Substituted 4-arylbutyric acid derivatives as matrix metalloprotease 失效
标题翻译：取代的4-芳基丁酸衍生物作为基质金属蛋白酶
公开(公告)号：US5863915A
公开(公告)日：1999-01-26
申请号：US857004
申请日：1997-05-15
申请人： Harold C. E. Kluender , Brian R. Dixon , David R. Brittelli
发明人： Harold C. E. Kluender , Brian R. Dixon , David R. Brittelli
IPC分类号： C07C59/90 , C07C69/84 , C07D209/48 , A61K31/19 , C07C59/84
CPC分类号： C07D209/48 , C07C59/90
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein R.sup.1 represents C.sub.6 -C.sub.12 alkyl; C.sub.5 -C.sub.12 alkoxy; C.sub.5 -C.sub.12 alkylthio; a polyether of formula R.sup.2 O(C.sub.2 H.sub.4 O).sub.a -- in which a is 1 or 2 and R.sup.2 is C.sub.1 -C.sub.5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R.sup.3 (CH.sub.2).sub.b --C.tbd.C--; in which b is 1-10 and R.sup.3 is H--, HO--, or R.sup.4 O-- in which R.sup.4 is C.sub.1 -C.sub.3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R.sup.1 may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R.sup.5 represents phenyl; imidoyl of 4-12 carbon atoms; (3H)-benzo-1,2,3-triazin-4-on-3-yl; N-saccharinyl; (2H)-phthalazin-1-on-2-yl; 2-benzoxazolin-2-on-3-yl; 5,5-dimethyloxazolidine-2,4-dion-3-yl; and thiazolidine-2,4-dion-3-yl; with the phenyl and benzo portions of R.sup.5 permissibly bearing at least one pharmaceutically-acceptable substituent. Pharmaceutically acceptable salts of these materials are also included.
摘要翻译：基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。本发明的化合物具有通式（I）其中R 1表示C 6 -C 12烷基; C5-C12烷氧基; C5-C12烷硫基; 苯基或苄基;式R2O（C2H4O）a-的聚醚，其中a为1或2，R2为C1-C5烷基，苯基或苄基; 和式R 3（CH 2）b -C 3的取代的炔基; 其中b为1-10，R3为H，HO-或R4O-，其中R4为C1-C3烷基，苯基或苄基。 R1的烷基，苯基和苄基部分可以具有至少一个药学上可接受的取代基。下标n为2-4。 R5表示苯基; 4-12个碳原子的亚氨基; （3H） - 苯并-1,2,3-三嗪-4-酮-3-基; N-糖精; （2H） - 酞嗪-1-酮-2-基; 2-苯并恶唑啉-2-酮-3-基; 5,5-二甲基恶唑烷-2,4-二酮-3-基; 和噻唑烷-2,4-二酮-3-基; 其中R 5的苯基和苯并部分容许具有至少一个药学上可接受的取代基。也包括这些材料的药学上可接受的盐。

4. 发明授权

US5932577A Substituted oxobutyric acids as matrix metalloprotease inhibitors 失效
标题翻译：取代的氧代丁酸作为基质金属蛋白酶抑制剂
公开(公告)号：US5932577A
公开(公告)日：1999-08-03
申请号：US857053
申请日：1997-05-15
申请人： Brian R. Dixon , Jinshan Chen , Michael C. VanZandt , David R. Brittelli
发明人： Brian R. Dixon , Jinshan Chen , Michael C. VanZandt , David R. Brittelli
IPC分类号： C07C59/90 , C07D209/48 , C07D253/08 , A61K31/53 , C07C65/32 , C07D251/00
CPC分类号： C07D209/48 , C07C59/90 , C07D253/08
摘要： The present invention provides pharmaceutical compositions and methods for treating certain conditions associated with matrix metalloproteases comprising administering an amount of a compound or composition of the invention which is effective to inhibit the activity of at least one matrix metalloprotease, resulting in achievement of the desired effect. The compounds of the present invention are either of the generalized formula: ##STR1## wherein y is 0, 2, or, 3, r is 0-6, Z is (CH.sub.2).sub.7 or (CH.sub.2).sub.e --C.sub.6 H.sub.4 --(CH.sub.2).sub.f, wherein e is 0-1 and f is 0-5, and R.sup.15 is --H, --Cl, --OMe or ##STR2## wherein n is 0-4, R.sup.17 is C.sub.2 H.sub.5, alkyl, benzyl, and R.sup.16 is ##STR3## wherein t is 0-2, x is 0-4, and R.sup.4 is one of the following: halide, alkyl of 1-6 carbons, OR, NR.sub.2, NO.sub.2 (R=H or alkyl of 1-6 carbons).
摘要翻译：本发明提供用于治疗与基质金属蛋白酶相关的某些病症的药物组合物和方法，其包括给予一定量的有效抑制至少一种基质金属蛋白酶活性的本发明化合物或组合物，从而达到预期的效果。本发明的化合物是以下通式：其中y是0,1或3，r是0-6，Z是（CH2）7或（CH2）e-C6H4-（CH2）f，其中 e为0-1，f为0-5，R15为-H，-Cl，-OMe或其中n为0-4，R17为C2H5，烷基，苄基，R16为其中t为0-2，x 是0-4，R4是以下之一：卤化物，1-6个碳的烷基，OR，NR2，NO2（R = H或1-6个碳原子的烷基）。

5. 发明授权

US06500847B2 Inhibition of matrix metalloproteases by substitued biaryl oxobutyric acids 失效
标题翻译：通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
公开(公告)号：US06500847B2
公开(公告)日：2002-12-31
申请号：US09845392
申请日：2001-04-30
申请人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
发明人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
IPC分类号： A61K3144
CPC分类号： C07D253/08 , A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抑制MMP的贡献，如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症反应的病症，MMP活性介导的骨质减少，下颌关节病，神经系统脱髓鞘疾病系统，肿瘤转移或创伤性关节损伤后的退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

6. 发明授权

US06225314B1 Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
标题翻译：通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
公开(公告)号：US06225314B1
公开(公告)日：2001-05-01
申请号：US09343142
申请日：1999-06-29
申请人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
发明人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
IPC分类号： A61K31495
CPC分类号： C07D253/08 , A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from arteriosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抑制MMP的贡献，如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症反应的病症，MMP活性介导的骨质减少，下颌关节病，神经系统脱髓鞘疾病系统，肿瘤转移或创伤性关节损伤后的退行性软骨损失，以及动脉硬化斑块破裂引起的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

7. 发明授权

US06762184B2 Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
标题翻译：通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
公开(公告)号：US06762184B2
公开(公告)日：2004-07-13
申请号：US09845379
申请日：2001-04-30
申请人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
发明人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
IPC分类号： A61K3153
CPC分类号： C07D253/08 , A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32
摘要： This application relates to matrix metalloprotease inhibitors having the generalized formula in which r is 0-2, T is selected from and R40 is a mono-or bi-heterocyclic structure. More particularly, the present application claims the various stereoisomeric forms of 4-(4′-choloro-biphenyl-4-yl)-4-oxo-2-[2-(4-oxo-4H-benzo[d][1,2,3]triazin-3-yl)ethyl]butyric acid, as well as their pharmaceutically acceptable salts. Pharmaceutical compositions containing these compounds, and methods for inhibiting matrix metalloprotease activity in mammals such as humans and for treating various conditions by administering such compounds are also claimed.
摘要翻译：本申请涉及具有广义结构的基质金属蛋白酶抑制剂，其r为0-2，T选自并且R 40为单或双杂环结构。更具体地说，本申请要求4-（4'-氯 - 联苯-4-基）-4-氧代-2- [2-（4-氧代-4H-苯并[d] [1,3] 2,3]三嗪-3-基）乙基]丁酸，以及它们的药学上可接受的盐。还要求保护含有这些化合物的药物组合物，以及用于抑制哺乳动物如人类中的基质金属蛋白酶活性的方法以及通过施用这些化合物来治疗各种病症。

8. 发明授权

US06911449B2 Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
标题翻译：通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
公开(公告)号：US06911449B2
公开(公告)日：2005-06-28
申请号：US10735040
申请日：2003-12-12
申请人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
发明人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
IPC分类号： A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32 , C07D253/08 , A61K31/519 , C07D239/72
CPC分类号： C07D253/08 , A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中r为0-2，T选自并且R 40是单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿性关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症反应，MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

9. 发明授权

US5925637A Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids 失效
标题翻译：通过取代的联芳基氧代丁酸抑制基质金属蛋白酶
公开(公告)号：US5925637A
公开(公告)日：1999-07-20
申请号：US856693
申请日：1997-05-15
申请人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
发明人： Michael C. VanZandt , David R. Brittelli , Brian R. Dixon
IPC分类号： A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32 , C07D253/08 , C07C63/64 , C07D253/10
CPC分类号： C07D253/08 , A61K31/425 , A61K31/426 , A61K31/4706 , A61K31/502 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/5513 , C07C62/38 , C07D237/32
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中r为0-2，选自T，R 40为单或双杂环结构。这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿关节炎，脓毒性关节炎，牙周病，溃疡性溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症反应，MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

10. 发明授权

US5968795A Biaryl acetylenes as inhibitors of matrix metalloproteases 失效
标题翻译：作为基质金属蛋白酶抑制剂的二芳基乙炔
公开(公告)号：US5968795A
公开(公告)日：1999-10-19
申请号：US856694
申请日：1997-05-15
申请人： Brian R. Dixon , Jinshan Chen
发明人： Brian R. Dixon , Jinshan Chen
IPC分类号： C07C59/84 , C07D209/48 , C12N9/99 , A01N37/10 , C07C63/00 , C12N9/50
CPC分类号： C07D209/48 , C07C59/84
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## where R.sup.15 is selected from the group comprising: HOCH.sub.2, (n--Pr).sub.2 NCH.sub.2, CH.sub.3 CO.sub.2 CH.sub.2, EtOCO.sub.2 CH.sub.2, HO(CH.sub.2).sub.2, CH.sub.3 CO.sub.2 (CH.sub.2).sub.2, HO.sub.2 C(CH.sub.2).sub.2, OHC(CH.sub.2).sub.3, HO(CH.sub.2).sub.4, 3--HO--Ph, and PhCH.sub.2 OCH.sub.2 ; and R.sup.16 is ##STR2## These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中R 15选自HOCH 2，（n-Pr）2 NCH 2，CH 3 CO 2 CH 2，EtOCO 2 CH 2，HO（CH 2）2，CH 3 CO 2（CH 2）2，HO 2 C（CH 2）2， OHC（CH 2）3，HO（CH 2）4，3-HO-Ph和PhCH 2 OCH 2; R16是这些化合物可用于抑制基质金属蛋白酶，因此可用于抑制MMP的贡献，如骨关节炎，类风湿性关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱性病变导致炎症反应，由MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

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