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: 1262036-50-9

LY2886721

中文名称:N-[3-[(4AS,7AS)-2-氨基-4A,5-二氢-4H-呋喃并[3,4-D][1,3]噻嗪-7A(7H)-基]-4-氟苯基]-5-氟-2-吡啶甲酰胺
CAS号:1262036-50-9
分子式: C18H16F2N4O2S 分子量: 390.41
产品形式: free base
研发状态: Completed
研发用途: Alzheimer Disease; Healthy Volunteers
研究机构: Eli Lilly and Company
研发日期: Mar-13
研发阶段: Phase 1
LY2886721 is a BACE inhibitor used for the treatment of Alzheimer's Disease. Phase 1/2.

CAS: 1260907-17-2

Molibresib (I-BET-762)

中文名称:(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-A][1,4]苯并二氮杂卓-4-乙酰胺
CAS号:1260907-17-2
分子式: C22H22ClN5O2 分子量: 423.90
产品形式: free base
研发状态: Withdrawn
研发用途: Solid Tumours
研究机构: GlaxoSmithKline
研发日期: November 27 2017
研发阶段: Phase 2
Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.

CAS: 1260251-31-7

Birinapant (TL32711)

中文名称:比瑞那帕
CAS号:1260251-31-7
分子式: C42H56F2N8O6 分子量: 806.94
产品形式: free base
研发状态: Terminated
研发用途: Epithelial Ovarian Cancer; Peritoneal Neoplasms; Fallopian Tube Neoplasms
研究机构: National Cancer Institute (NCI); National Institutes of Health Clinical Center (CC)
研发日期: August 15 2012
研发阶段: Phase 2
Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.

CAS: 1260141-27-2

Vonoprazan Fumarate (TAK-438)

中文名称:富马酸沃诺拉赞
CAS号:1260141-27-2
分子式: C17H16FN3O2S.C4H4O4 分子量: 461.46
产品形式: Fumarate
研发状态: Completed
研发用途: Japanese Healthy Adult Male
研究机构: Takeda
研发日期: January 30 2019
研发阶段: Phase 1
Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.

CAS: 1258861-20-9

Taladegib (LY2940680)

中文名称: 4-氟-N-甲基-N-[1-[4-(1-甲基-1H-吡唑-5-基)-1-酞嗪基]-4-哌啶基]-2-(三氟甲基)苯甲酰胺
CAS号:1258861-20-9
分子式: C26H24F4N6O 分子量: 512.50
产品形式: free base
研发状态: Completed
研发用途: Neoplasm Metastasis
研究机构: Eli Lilly and Company
研发日期: Aug-13
研发阶段: Phase 1
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

CAS: 1258453-75-6

ABX464

CAS号:1258453-75-6
分子式: C16H10ClF3N2O 分子量: 338.71
产品形式: free base
研发状态: Active not recruiting
研发用途: Ulcerative Colitis
研究机构: Abivax S.A.
研发日期: December 3 2021
研发阶段: Phase 2
ABX464 (SPL-464) is a novel anti-HIV molecule that inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) from 5 different donors with IC50 ranging between 0.1 μM and 0.5 μM.