临床前CDMO研发筛选相关化合物

CDMO是Contract Development and Manufacturing Organization的缩写，即合同定制研发生产组织。它是一种为制药企业及生物技术公司提供医药（特别是创新药）工艺研发及制备、工艺优化、放大生产、注册和验证批生产以及商业化生产等定制服务的机构. 在传统代工基础上增加了研发和工艺优化能力，是高技术壁垒的工艺研发能力与规模生产能力的深度结合. 1, 工艺开发与优化：创新性合成路线设计、工艺参数优化. 2, 中试放大：实验室工艺向规模化生产的转化 3, 注册批生产：支持客户新药申报的验证批生产. 4, 商业化生产：药品上市后的大规模生产供应. 全球医药CDMO行业保持较高景气度。根据弗若斯特沙利文预测：2026年全球CDMO市场规模：预计达1,189亿美元 2033年全球CDMO市场规模：预计达3,385亿美元. CDMO作为医药产业链专业化分工的产物，已经从单纯的CMO代工模式升级为"研发+生产"一体化的高附加值服务。当前，在多肽、ADC、CGT等新型药物赛道的驱动下，全球及中国CDMO市场保持高速增长。中国CDMO企业凭借完整的供应链体系、工程师红利和一体化服务能力，全球市占率有望持续提升，行业正从"成本优势"竞争迈向"体系优势"竞争的新阶段。
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临床前CDMO研发化合物筛选

CAS: 1189767-28-9

BI-409306

CAS号:1189767-28-9
分子式: C16H17N5O2 分子量: 311.34
产品形式: Free Base
研发状态: Completed
研发用途: Healthy
研究机构: Boehringer Ingelheim
研发日期: April 27 2018
研发阶段: Phase 1
BI 409306 (SUB 166499) is a potent and selective inhibitor of human and rat PDE9A with mean IC50 of 65 nM and 168 nM, respectively. Treatment with BI 409306 increases brain cGMP levels, promotes long-term potentiation, and improves episodic and working memory performance in rodents.

CAS: 1187594-09-7

Baricitinib (INCB028050)

中文名称:巴瑞克替尼
CAS号:1187594-09-7
分子式: C16H17N7O2S 分子量: 371.42
产品形式: free base
研发状态: Not yet recruiting
研发用途: Hospital-acquired Pneumonia
研究机构: Nantes University Hospital
研发日期: July 1 2023
研发阶段: Phase 2 : Phase 3
Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.

CAS: 1187431-43-1

Trametinib DMSO solvate

中文名称: 曲美替尼二甲基亚砜
CAS号:1187431-43-1
分子式: C28H29FIN5O5S 分子量: 693.53
产品形式: Free Base
研发状态: Not yet recruiting
研发用途: Cancer; BRAF V600 Mutation; Melanoma; Colorectal Cancer; Thyroid Cancer; Nonsmall Cell Lung Cancer
研究机构: Xynomic Pharmaceuticals Inc.
研发日期: Dec-24
研发阶段: Phase 1 : Phase 2
Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.

CAS: 118-71-8

Maltol

中文名称:麦芽酚
CAS号:118-71-8
分子式: C6H6O3 分子量: 126.11
产品形式: Pyrone
研发状态: Recruiting
研发用途: Cancer Colon
研究机构: The Royal Wolverhampton Hospitals NHS Trust; Norgine
研发日期: May 30 2022
研发阶段: Phase 3
Maltol (Larixinic acid, Palatone, Veltol) is a naturally occurring organic compound that is flavour enhancer and flavouring agent.

CAS: 1186486-62-3

Evacetrapib (LY2484595)

中文名称:反式-4-[[(5S)-5-[[[3,5-双(三氟甲基)苯基]甲基](2-甲基-2H-四氮唑-5-基)氨基]-2,3,4,5-四氢-7,9-二甲基-1H-1-苯并氮杂卓-1-基]甲基]环己烷羧酸
CAS号:1186486-62-3
分子式: C31H36F6N6O2 分子量: 638.65
产品形式: free base
研发状态: Completed
研发用途: Healthy
研究机构: Eli Lilly and Company
研发日期: Jul-15
研发阶段: Phase 1
Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.

CAS: 1185-53-1

Trometamol hydrochloride

中文名称:三羟甲基氨基甲烷盐酸盐
CAS号:1185-53-1
分子式: C4H12ClNO3 分子量: 157.60
产品形式: Hydrochloride
研发状态: Completed
研发用途: Healthy Subjects
研究机构: Egalet Ltd
研发日期: Feb-07
研发阶段: Phase 1
Trometamol (THAM, Tromethamine, TRIS-HCL) hydrochloride, a proton acceptor, is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol rapidly restores pH and acid-base regulation in acidaemia.