公开(公告)号：US08110543B2

公开(公告)日：2012-02-07

申请号：US12871868

申请日：2010-08-30

Applicant: Andrew P. Mazar ,  Terrence R. Jones

Inventor： Andrew P. Mazar ,  Terrence R. Jones

IPC: A61K38/00 ,  A61K39/385

CPC classification number: C12N9/6462 ,  A61K38/00 ,  C12Y304/21073

Abstract: A peptide compound having the sequence Lys-Pro-Ser-Ser-Pro-Pro-Glu-Glu [SEQ ID NO:2] or a substitution variant, addition variant or other chemical derivative thereof inhibits cell invasion, endothelial tube formation or angiogenesis in vitro. A number of substitution variants and addition variants of this peptide, preferably capped at the N- and C-termini, as well as peptidomimetic derivates, are useful for treating diseases and conditions mediated by undesired and uncontrolled cell invasion and/or angiogenesis. Pharmaceutical compositions comprising the above peptides and derivatives are administered to subjects in need of such treatment in a dosage sufficient to inhibit invasion and/or angiogenesis. The disclosed compositions and methods are particularly useful for suppressing the growth and metastasis of tumors.

Abstract translation: 具有序列Lys-Pro-Ser-Ser-Pro-Pro-Glu-Glu [SEQ ID NO：2]或其取代变体，加成变体或其它化学衍生物的肽化合物抑制细胞侵袭，内皮细管形成或血管生成 体外。 该肽的多个取代变体和加成变体，优选在N-和C-末端封端，以及拟肽衍生物，可用于治疗由不期望的和不受控制的细胞侵袭和/或血管发生介导的疾病和病症。 将包含上述肽和衍生物的药物组合物以足以抑制侵袭和/或血管发生的剂量施用于需要这种治疗的受试者。 所公开的组合物和方法特别可用于抑制肿瘤的生长和转移。

公开(公告)号：US5885996A

公开(公告)日：1999-03-23

申请号：US923117

申请日：1997-09-04

Applicant: Stephen E. Webber ,  Ted M. Bleckman ,  John Attard ,  Terrence R. Jones ,  Michael D. Varney

Inventor： Stephen E. Webber ,  Ted M. Bleckman ,  John Attard ,  Terrence R. Jones ,  Michael D. Varney

IPC: A61K31/505 ,  A61K31/517 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  C07D239/88 ,  C07D239/90 ,  C07D239/91 ,  C07D239/93 ,  C07D239/95 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D417/12 ,  A61K31/54 ,  C07D403/02

CPC classification number: C07D401/12 ,  C07D239/90 ,  C07D239/93 ,  C07D239/95 ,  C07D403/06 ,  C07D403/12 ,  C07D417/12 ,  Y10S514/895 ,  Y10S514/896 ,  Y10S514/898

Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.

Abstract translation: 显示抗增殖活性的喹唑啉化合物，例如抗肿瘤活性，制备这些化合物的方法，含有这些化合物的药物组合物，以及这些化合物的用途。 这些化合物抑制细菌，酵母和真菌等高等生物和微生物细胞的生长和增殖。 优选的喹唑啉化合物能够抑制胸苷酸合酶的酶。 由抑制酶胸苷酸合酶导致的效果包括上述讨论。