会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明申请
    • SUBSITUTE 4-ARYLBUTYRIC ACID DERIVATIVES AS MATRIX METALLOPROTEASE INHIBITORS
    • 作为基质金属蛋白酶抑制剂的4-ARYLBUTYRIC酸衍生物
    • WO1997043237A1
    • 1997-11-20
    • PCT/US1997007951
    • 1997-05-12
    • BAYER CORPORATIONKLUENDER, Harold, C., E.DIXON, Brian, R.BRITTELLI, David, R.
    • BAYER CORPORATION
    • C07C59/84
    • C07D209/48C07C59/84C07C59/90C07D237/32C07D253/04
    • 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 generalized formula (I) wherein R represents C6-C12 alkyl; C5-C12 alkoxy; C5-C12 alkylthio; a polyether of formula R O(C2H4O)a- in which a is 1 or 2 and R is C1-C5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R (CH2)b-CC-; in which b is 1-10 and R is H-, HO-, or R O- in which R is C1-C3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R 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 permissibly bearing at least one pharmaceutically-acceptable substituent. Pharmaceutically acceptable salts of these materials are also included.
    • 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; 式R 2 O(C 2 H 4 O)a - 的聚醚,其中a为1或2,R 2为C 1 -C 5烷基,苯基或苄基; 和取代的式R 3(CH 2)b-CC-的炔基; 其中b为1-10,R 3为H,HO-或R 4 O-,其中R 4为C 1 -C 3烷基,苯基或苄基。 R 1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。 R 5表示苯基; 4-12个碳原子的亚氨基; (3H) - 苯并-1,2,3-三嗪-4-上-3-基; 的N- saccharinyl; (2H)-2,3-二氮杂萘-1-酮-2-基; 2-苯并恶唑啉-2-酮-3-基; 5,5-二甲基唑烷-2,4-二酮-3-基; 和噻唑烷-2,4-二酮-3-基; 其中R 5的苯基和苯并部分允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。
    • 2. 发明申请
    • INHIBITION OF MATRIX METALLOPROTEASES BY 2-SUBSTITUTED-4-(4-SUBSTITUTEDPHENYL)-4-OXOBUTYRIC ACIDS
    • 通过取代的二异丁基氧化物抑制基质金属
    • WO1997043239A1
    • 1997-11-20
    • PCT/US1997007976
    • 1997-05-12
    • BAYER CORPORATIONVAN ZANDT, Michael, C.BRITTELLI, David, R.DIXON, Brian, R.
    • BAYER CORPORATION
    • C07C59/90
    • C07D263/44C07C59/90C07D237/32C07D243/24C07D253/04C07D263/58C07D275/04C07D277/34
    • Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have generalized formula (1) wherein r is 0-2, T is selected from (a) and (b) and R 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 of 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.
    • 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通式(1),其中r为0-2,T选自(a)和(b),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,由MMP活性介导的骨质减少,下颌关节疾病,神经系统脱髓鞘疾病,创伤性关节损伤后退行性软骨损失的肿瘤转移,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。
    • 3. 发明申请
    • SUBSTITUTED OXOBUTYRIC ACIDS AS MATRIX METALLOPROTEASE INHIBITORS
    • 作为基质金属蛋白酶抑制剂的取代的氧代酸
    • WO1997043238A1
    • 1997-11-20
    • PCT/US1997007975
    • 1997-05-12
    • BAYER CORPORATIONDIXON, Brian, R.CHEN, JinshanVAN ZANDT, MichaelBRITTELLI, David, R.
    • BAYER CORPORATION
    • C07C59/90
    • C07D209/48C07C59/90C07D253/08
    • The present invention provides pharmaceutical compositions and methods for treating certain conditions 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 generalized formula (I) wherein y is 0, 2, or 3, r is 0-6, Z is (CH2)7 or (CH2)e-C6H4-(CH2)f, wherein e is 0-1 and f is 1-6, and R is -H, -Cl, -OMe or (a), (b) wherein n is 0-4, R is C2H5, allyl, benzyl, and R is (c) wherein t is 0-1, x is 0-4, and R is one of the following: halide, alkyl of 1-6 carbons, OR, NR2, NO2 (R = H or alkyl of 1-6 carbons). 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 atherosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
    • 本发明提供用于治疗某些病症的药物组合物和方法,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。 本发明的化合物是通式(I),其中y是0,2或3,r是0-6,Z是(CH 2)7或(CH 2)e -C 6 H 4 - (CH 2)f,其中 e为0-1且f为1-6,R 15为-H,-Cl,-OMe或(a),(b)其中n为0-4,R 17为C 2 H 5,烯丙基, 苄基,R 16是(c)其中t是0-1,x是0-4,R 4是以下之一:卤素,1-6个碳的烷基,OR,NR 2,NO 2( R = H或1-6个碳的烷基)。 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,由MMP活性介导的骨质减少,颞下颌关节病,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。
    • 4. 发明申请
    • INHIBITION OF MATRIX METALLOPROTEASES BY ACETYLENE CONTAINING COMPOUNDS
    • 含乙烯基化合物对基质金属微球的抑制作用
    • WO1997043245A1
    • 1997-11-20
    • PCT/US1997007921
    • 1997-05-12
    • BAYER CORPORATIONDIXON, Brian, R.CHEN, Jinshan
    • BAYER CORPORATION
    • C07C229/34
    • C07D209/48C07C59/90C07C229/34
    • 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 formula (I) where R is selected from the group comprising: HOCH2, MeOCH2, (n-Pr)2NCH2, CH3CO2CH2, EtOCO2CH2, HO(CH2)2, CH3CO2(CH2)2, HO2C(CH2)2, OHC(CH2)3, HO(CH2)4, Ph, 3-HO-Ph, and PhCH2OCH2; and R is (a) or (b). 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 plate rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
    • 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通式(I),其中R 15选自HOCH 2,MeOCH 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 ,HO2C(CH2)2,OHC(CH2)3,HO(CH2)4,Ph,3-HO-Ph和PhCH2OCH2; R 16为(a)或(b)。 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,以及来自冠状动脉板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. 发明申请
    • INHIBITION OF MATRIX METALLOPROTEASES BY SUBSTITUTED PHENETHYL COMPOUNDS
    • 通过取代的苯乙烯化合物抑制基质金属
    • WO1997043247A1
    • 1997-11-20
    • PCT/US1997007919
    • 1997-05-12
    • BAYER CORPORATIONWOLANIN, Donald, J.
    • BAYER CORPORATION
    • C07C235/84
    • C07D295/192C07C17/16C07C45/46C07C59/88C07C69/738C07C235/84C07C25/02C07C49/813
    • Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have generalized formula (I), wherein R is a substituted phenylethyl moiety. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combatting 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.
    • 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通式(I),其中R 25是取代的苯乙基部分。 这些化合物可用于抑制基质金属蛋白酶,因此可用于促进MMP的作用,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。