MAINTENANCE AND OPERATION OF A SYNTHETIC PEPTIDE FACILITY

合成肽设施的维护和操作

• 批准号: 7946869
• 负责人: JEANICK PASCAL
• 金额: $ 64.42万
• 依托单位: NEOMPS, INC.
• 依托单位国家: 美国
• 财政年份: 2009
• 资助国家: 美国
• 起止时间: 2009-07-01 至 2010-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7946869
• 关键词: MAINTENANCE; OPERATION; SYNTHETIC; PEPTIDE; FACILITY

The Contraception and Reproductive Health Branch of the NICHD supports a Chemical Synthesis Facility (CSF) that provides services central to the Branch's programs to develop safe and effective contraceptive agents. This Facility provides the Government with drugs, chemicals, chemical intermediates, steroids, and optically pure and/or resolved unnatural amino acids possessing >99% enantipmeric excess, which are either commercially unavailable or unduly expensive, for further contraceptive development by the Government. Specific Aims: The areas of chemical synthesis include: 1) orally active steroids, including;{ estrogens without 17 -ethynyla1cohol, orally active and long ¿acting androgens, e.g., testosterone bucyclate and 7cm, 11 p..dimethyl-19~nortestosterone bucyclate & undecanoate, orally active 7&a-methyI-19¿nortestosterone (MENT) analogs, and progesterone receptor modulators (PRM),e.g., CDB-2914, 21-suhstituted analogs, e.g., CDB4124 (2nd generation) and novel derivatives (3rd generation) in combination of substititon at CllB-4-aryl and C17&a; 2) steroid haptens linked to bovine serum a1bumin as well as to histamine conjugates for the development of radioimmunoassay (RIA.); 3)radiolabeled compounds for RIA as tracers and for metabolism studies; 4) heterocyclic compounds including seconucleosides and hexahydroindenopyridine diastereomers ; and 5) alkylated iminosugars. The Contractor maintains and operate a Chemical Synthesis Facility (CSF) capable of (l) rapidly synthesizing laboratory scale quantities (1 to 5 grams) of specific chemical compounds required for initial contraceptive investigation in small animals, (2) synthesizing relatively larger quantities (up to <1 kg) of Some drugs for comprehensive antifertility testing by the Government, including preclinical and clinical studies under current Good Manufacturing Practices (cGMP); (3) synthesizing chemicals and/or chemical intermediates (up to < 1 kg) for use in other ongoing chemical. peptide and related contracts and other synthetic chemical contract programs; and (4) radiolabeled synthesis of compounds using 3H, I~C and 1251 for pharmacokinetics and metabolism studies.

NICHD的避孕和生殖健康处支持一个化学合成设施，该设施为该处开发安全有效的避孕药的方案提供核心服务。该基金向政府提供药品、化学品、化学中间体、类固醇和光学纯的和/或含有99%对映体过量的非天然氨基酸，这些都是商业上无法获得的或过于昂贵的，供政府进一步开发避孕药具。 具体目标： 化学合成领域包括：1)口服活性类固醇，包括：不含17-乙炔基醇的雌激素，口服活性和长效雄激素，例如四环睾丸酮和7 cm，11，p-二甲基-19去甲睾酮四环酸酯和十一酸，口服活性7-甲基-19去甲睾酮类似物，以及孕激素受体调节剂(PRM)，例如CDB-2914，21取代类似物，例如CDB4124(第二代)和C17&a取代的新衍生物(第三代)；2)与牛血清白蛋白以及组胺结合物相连的类固醇半抗原，用于发展放射免疫分析(RIA)；3)作为示踪剂和用于新陈代谢研究的放射性标记化合物；4)包括二次核苷和六氢吲哚并吡啶非对映异构体的杂环化合物；以及5)烷基化亚氨基糖。承包商维护和运营一家化学合成设施，该设施能够(L)在实验室范围内快速合成小动物首次避孕调查所需的特定化合物，(2)合成相对较大数量(不超过1公斤)的某些药物，供政府进行全面的抗生育测试，包括根据当前良好制造规范(CGMP)进行的临床前和临床研究；(3)合成化学品和/或化学中间体(不超过1公斤)，用于其他正在进行的化学品。多肽及相关合同和其他合成化学合同计划；以及(4)利用~3H、I~C和1251放射性标记化合物的合成，用于药代动力学和代谢研究。