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公开(公告)号：US5446130A
公开(公告)日：1995-08-29
申请号：US305799
申请日：1994-09-13
IPC分类号： A61K38/00 , C07K14/635
CPC分类号： C07K14/635 , A61K38/00
摘要： Peptide derivatives of the following general formula (I): ##STR1## wherein AAA is deletion or Ser, BBB is deletion or Glu, CCC is deletion, Ile, Phe, Leu, cyclohexylalanine, D-alle or Lys substituted at the .epsilon.-position by C.sub.6 --C.sub.18 alkylcarbonyl group, DDD is Gly or Gln, EEE is Leu, Nle or Phe, FFF is Met, Leu or Nle, GGG is Ala, Ser Leu, Asn, Asp or Gln, HHH is Leu, Glu or Lys, III is His, Lys or Arg, JJJ is His, Lys or Arg, Xaa is Ala modified at the carboxy terminal with an amino group, provided that CCC and DDD may independently be modified at the amino terminal by C.sub.2 --C.sub.18 alkylcarbonyl group, and that EEE is not Leu when FFF is Met, GGG is Asn, HHH is Leu, III and JJJ are His, and the salts thereof, which exhibit a potent inhibitory activity against hPTH and are useful as a therapeutic agent for treating dysbolism associated with calcium or phosphoric acid, such as hypercalcemia, osteoporosis, hyperparathyroidism, renal osteodystrophy, and the like, and other related diseases involving PTH or PTHrP.
摘要翻译： 下列通式（I）的肽衍生物：其中AAA是缺失或Ser，BBB是缺失或Glu，CCC是缺失，Ile，Phe，Leu，环己基丙氨酸，D- 通过C 6 -C 18烷基羰基在ε-位上取代的等位基或Lys，DDD是Gly或Gln，EEE是Leu，Nle或Phe，FFF是Met，Leu或Nle，GGG是Ala，Ser Leu，Asn，Asp或Gln ，HHH是Leu，Glu或Lys，III是His，Lys或Arg，JJJ是His，Lys或Arg，Xaa是在羧基末端用氨基修饰的Ala，条件是CCC和DDD可以独立地在氨基 末端为C2-C18烷基羰基，当FFF为Met时，EEE不为Leu，GGG为Asn，HHH为Leu，III和JJJ为His及其盐，对hPTH表现出有效的抑制活性，可用作 用于治疗与钙或磷酸相关的dysbolism的治疗剂，例如高钙血症，骨质疏松症，甲状旁腺功能亢进症，肾性骨营养不良等，以及其他 涉及PTH或PTHrP的相关疾病。
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公开(公告)号：US5229489A
公开(公告)日：1993-07-20
申请号：US684391
申请日：1991-04-12
IPC分类号： A61K38/00 , C07K14/635
CPC分类号： C07K14/635 , A61K38/00
摘要： Peptide derivatives of the following general formula (I): Seq. ID Nos. 1-6. ##STR1## wherein AAA is deletion or Ser, BBB is deletion or Glu, CCC is deletion, Ile, Phe, Leu, cyclohexylalanine, D-alle or Lys substituted at the .epsilon.-position by C.sub.6 -C.sub.18 alkylcarbonyl group, DDD is Gly or Gln, EEE is Leu, Nle or Phe, FFF is Met, Leu or Nle, GGG is Ala, Ser, Leu, Asn, Asp or Gln, HHH is Leu, Glu or Lys, III is His, Lys or Arg, JJJ is His, Lys or Arg, Xaa is Ala modified at the carboxy terminal with an amino group, provided that CCC and DDD may independently be modified at the amino terminal by C.sub.2 -C.sub.18 alkylcarbonyl group, and that EEE is not Leu when FFF is Met, GGG is Asn, HHH is Leu, III and JJJ are His, and the salts thereof, which exhibit a potent inhibitory activity against hPTH and are useful as a therapeutic agent for treating dysbolism associated with calcium or phosphoric acid, such as hypercalcemia, osteoporosis, hyperparathyroidism, renal osteodystrophy, and the like, and other related diseases involving PTH or PTHrP.
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