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11. 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。

12. 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。

13. 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。

14. 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。

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