| 主权项 |
1.一种如下式胜或其制药容许盐: 式中 A1为Ser或Dap; A3为Ser或Aib; A5为Ile; A7为Leu或Cha; A8为Met或Nle; A11为Leu或Cha; A12为Gly或Aib; A15为Leu或Cha; A16为Asn或Aib; A17为Ser或Aib; A18为Met或Nle; A19为Glu或Aib; A21为Val; A23为Trp,Cha,或Leu; A24为Leu或Cha; A27为Lys,hArg,或Cha; A28为Leu或Cha; A30为Asp或Lys; A31为Nle,cha,Leu或删除; A32为His或删除; A33为Asn或删除; A34为Tyr,Aib或删除; R1及R2为H;及 R3为NH2; 但A7,A8,A11,A15,A23,A24,A27,A28及A31中至少一个为Cha或A3 ,A12,A16,A17,A19及A34中至少一个为Aib,且其中该胜 非为[Aib12]PTH(1-34)NH2。2.如申请专利范围第1项之胜 或其制药容许盐,其中 A3为Ser; A12为Gly; A17为Ser; A27为Lys,hArg或Cha; A31为Nle或Cha; A32为His; A33为Asn; A34为Tyr或Aib; R1为H; R2为H;及 R3为NH2。3.如申请专利范围第2项之胜或其制药 容许盐,[Cha7,11]hPTH(1-34)NH2,[Cha7,11,Nle8,18,Tyr34]hPTH(1- 34)NH2,[Cha7,11,15]hPTH(1-34)NH2;或[Cha7]hPTH(1-34)NH2。4.如 申请专利范围第2项之胜或其制药容许盐,其中 胜为[Cha23]hPTH(1-34)NH2,[Cha24]hPTH(1-34)NH2,[Nle8,18,Cha 27]hPTH(1-34)NH2,Cha28]hPTH(1-34)NH2,[Cha31]hPTH(1-34)NH2,[Cha24 ,28,31]hPTH(1-34)NH2;[Cha24,28,31,Lys30]hpTH(1-34)NH2;[Cha28,31] hPTH(1-34)NH2;或[Cha15]hPTM(1-34)NH2。5.如申请专利范围 第1项之胜或其制药容许盐,其中 A27为Lys,hArg或Cha; A31为Nle或Cha; A32为His; A33为Asn; A34为Tyr或Aib; R1为H; R2为H;及 R3为NH2。6.如申请专利范围第5项之胜或其制药 容许盐,其中胜为[Aib16]hPTH(1-34)NH2,[Aib19]hPTH(1-34) NH2,[Aib34]hPTH(1-34)NH2,[Aib16,19]hPTH(1-34)NH2,[Aib3]hPTH(1-34 )NH2,或[Aib17]hPTH(1-34)NH2。7.如申请专利范围第1项之 胜或其制药容许盐,其中胜为[Cha28,Nle8,18,Aib16, 19,Tyr34]hPTH(1-34)NH2,或[Cha28,Aib16,19]PTH(1-34)NH2。8.一 种如下式胜或其制药容许盐: 式中 A3为Ser或Aib; A5为Ile; A7为Leu或Cha; A8为Met或Nle; A11为Leu或Cha; A12为Gly或Aib; A15为Leu或Cha; A16为Asn或Aib; A17为Ser或Aib; A18为Met或Nle; A19为Glu或Aib; A21为Val; A23为Trp,Cha,Leu,Lys或Acc,其中Acc为选自-胺基环丙 烷羧酸,-胺基环丁烷羧酸,-胺基环戊烷羧酸, -胺基环己烷羧酸,-胺基环庚烷羧酸,-胺基 环辛烷羧酸及-胺基环壬烷羧酸之胺基酸; A24为Leu或Cha; A27为Lys,hArg,Acc或Cha,其中Acc的定义同上; A28为Leu或Cha; A30为Asp或Lys; A31为Nle,cha,Leu,Acc或删除,其中Acc的定义同上; A32为His或删除; A33为Asn或删除; A34为Tyr,Aib或删除; R1及R2各自为H,C1-6烷基,C2-6烯基,C7-12苯烷基,C11-16 烷基,C1-6羟烷基,C2-6羟烯基,C7-12羟苯烷基或C11-16羟 烷基;或R1及R2之一及只一为COE1而E1为C1-6烷基,C2- 6烯基,C7-12苯烷基,C11-16烷基,C1-6羟烷基,C2-6羟烯 基,C7-12羟苯烷基,或C11-16羟烷基;及 R3为OH,NH2,C1-6烷氧基,或NH-Y-CH2-Z而Y为C1-6烃部分及Z 为H,OH,CO2H或CONH2; 但至少A1为Dap,A27为hArg或A31为Nle。9.如申请专利范 围第8项之胜或其制药容许盐,其中 A1为Ser或Dap; A27为Lys,hArg或Cha; A31为Nle或Cha; A32为His; A33为Asn; A34为Tyr或Aib; R1为H; R2为H;及 R3为NH2。10.如申请专利范围第9项之胜或其制药 容许盐,其中胜为[Nle31]hPTH(1-34)NH2,[hArg27]hPTH(1-34) NH2,或[Dap1,Nle8,18,Tyr34]hPTH(1-34)NH2。11.一种化合物, 其具有[Glu22,25,Leu23,28,31,Aib29,Lys26,30]hPTHrP(1-34)NH2的 结构式。 |
