新项目精选

近年来，药物发现已从传统的小分子化药拓展至更多元的分子类型，这些新型API在项目整合中呈现出独特的开发范式：PROTAC/分子胶降解剂：通过诱导靶蛋白泛素化降解发挥作用，而非传统“占位驱动”抑制。这类分子的项目整合需要同时考量靶点配体、E3连接酶配体及连接子的三元复合物优化，临床前到临床的转化难度显著增加。多肽/环肽药物：介于小分子与生物制品之间，兼具高选择性与口服可用性潜力。项目整合中需重点解决稳定性、递送及生产工艺放大问题。抗体-药物偶联物（ADC）：作为“生物导弹”，ADC的项目整合涉及抗体、连接子、有效载荷三部分的协同优化，需要跨学科团队的深度整合。小核酸药物（siRNA/ASO）：通过基因沉默机制发挥作用，项目整合的核心挑战在于递送系统的设计与肝外靶向能力的突破。展望未来，新型API项目的整合将呈现以下趋势：第一，AI贯穿全链条。从靶点发现、分子优化到临床开发、上市后监测，AI将成为贯穿API全生命周期的核心工具。第二，数据资产化。临床研究数据和真实世界数据将从“辅助工具”升级为“核心资产”，数据驱动的决策将成为项目整合的标准范式。第三，开放整合生态。API经济的成熟正在推动制药企业从“封闭研发”走向“开放协作”，通过API接口与外部数据源、技术平台、CRO/CDMO实现无缝对接. 而API技术——无论是数据接口还是组织协作的“应用程序接口”——正成为支撑这一整合的核心基础设施。
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新项目整合精选

新产品编号:1367357

Chemical Name: (6R,8R,9R)-N-Acetyl-N'-[4-amino-9-(tert-butyldimethylsilyloxy)-6-(tert-butyldimethylsilyloxymethyl)-1,7-dioxa-2-thiaspiro[4.4]-3-nonen-8-yl]urea S,S-dioxide
项目整合开发状态: Biological Test...
参考文献标题:Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase
文献作者:Vel醶quez,S.; Chamorro,C.; Perez-Perez,M.J.; Alvarez,R.; Jimeno,M.L.; Martin-Domenech,A.; Perez,C.; Gago,F.; De Clercq,E.; Balzarini,J.; San-Felix,A.; Camarasa,M.J.
参考来源:J Med Chem 1998,41(23),4636

新产品编号:1368939

Chemical Name: (6R,8S,9R)-N-[4-Amino-9-(tert-butyldimethylsilyloxy)-6-(tert-butyldimethylsilyloxymethyl)-1,7-dioxa-2-thiaspiro[4.4]-3-nonen-8-y]-N'-phenylurea S,S-dioxide
项目整合开发状态: Biological Testi...
参考文献标题:Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase
文献作者:Vel醶quez,S.; Chamorro,C.; Perez-Perez,M.J.; Alvarez,R.; Jimeno,M.L.; Martin-Domenech,A.; Perez,C.; Gago,F.; De Clercq,E.; Balzarini,J.; San-Felix,A.; Camarasa,M.J.
参考来源:J Med Chem 1998,41(23),4636

新产品编号:1370521

Chemical Name: [4R-(4alpha,4aalpha,6abeta,7beta,9aalpha,9bbeta)]-5-[7-[1(R),5-dimethylhexyl]-4,6a-dimethyl-2-oxoperhydrocyclopenta[f][2]benzopyran-4-yl]-2(Z)-pentenenitrile
项目整合开发状态: Biological Tes...
参考文献标题:Novel CDC25A phosphatase inhibitors from pyrolysis of 3-alpha-azido-B-homo-6-oxa-4-cholesten-7-one on silica gel
文献作者:Peng,H.; Zalkow,L.H.; Abraham,R.T.; Powis,G.
参考来源:J Med Chem 1998,41(24),4677

新产品编号:1372103

Chemical Name: (Z)-2-[5-(1-Methoxynaphthalen-2-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl]acetic acid
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:1-Methoxynaphthalene (I) was...
参考文献标题:Synthesis,activity,and molecular modeling of new 2,4-dioxo-5-(naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors
文献作者:Fresneau,P.; Cussac,M.; Morand,J.M.; Szymonski,B.; Tranqui,D.; Leclerc,G.
参考来源:J Med Chem 1998,41(24),4706

ORG-37476

Chemical Name: N-[1-(1-Amino-6-isoquinolinylmethyl)-2-oxo-2-(1-piperidinyl)ethyl]-3(S)-(4-methoxy-2,3,6-trimethylphenylsulfonamido)succinamic acid tert-butyl ester hydrochloride
项目整合开发状态: Preclinic...
参考文献标题:Heterocyclic derivs.and their use as antithrombotic agents
文献作者:Van Galen,P.J.M.; Rewinkel,J.B.M.; Van Boeckel,C.A.A.(Akzo Nobel N.V.)
参考来源:EP 0975600; WO 9847876

新产品编号:1373685

Chemical Name: N-[1-[4-Aminothieno[3,2-c]pyridin-2-ylmethyl]-2-(4-methyl-1-piperidinyl)-2-oxoethyl]-2-naphthalenesulfonamide hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Akzo Nobel (Originator) 参考文献标题:Heterocyclic derivs.and their use as antithrombotic agents
文献作者:Van Galen,P.J.M.; Rewinkel,J.B.M.; Van Boeckel,C.A.A.(Akzo Nobel N.V.)
参考来源:EP 0975600; WO 9847876

新产品编号:1375267

Chemical Name: N-[1-[4-Aminothieno[3,2-c]pyridin-2-ylmethyl]-2-(4-methyl-1-piperidinyl)-2-oxoethyl]-7-methoxy-2-naphthalenesulfonamide hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Akzo Nobel (Ori...
参考文献标题:Heterocyclic derivs.and their use as antithrombotic agents
文献作者:Van Galen,P.J.M.; Rewinkel,J.B.M.; Van Boeckel,C.A.A.(Akzo Nobel N.V.)
参考来源:EP 0975600; WO 9847876

新产品编号:1376849

Chemical Name: 1,8-Dihydroxy-10-[2-(4-methoxyphenyl)ethyl]anthracen-9(10H)-one
项目整合开发状态: Biological Testing
项目研究机构: Universit鋞 Regensburg (Originator), Westf鋖ische Wilhelms-Univ. M黱ster (Origina...
参考文献标题:10-omega-Phenylalkyl-9(10H)-anthracenones as inhibitors of keratinocyte growth with reduced membrane damaging properties
文献作者:M黮ler,K.; Breu,K.
参考来源:Bioorg Med Chem Lett 1998,8(22),3211

新产品编号:1378431

Chemical Name: 3-[4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-oxopyrrolidin-1-yl]-5-(3-methoxybenzyloxy)-N2,N2-dimethylbenzohydrazide
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Methy...
参考文献标题:N-Arylrolipram derivatives as potent and selective PDE4 inhibitors
文献作者:Bacher,E.; Boer,C.; Bray-French,K.; Demnitz,F.W.; Keller,T.H.; Mazzoni,L.; M黮ler,T.; Walker,C.
参考来源:Bioorg Med Chem Lett 1998,8(22),3229

新产品编号:1380013

Chemical Name: 3-[4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-oxopyrrolidin-1-yl]-5-(3-methoxybenzyloxy)benzoic acid
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Methyl 5-hydroxy-3-iod...
参考文献标题:N-Arylrolipram derivatives as potent and selective PDE4 inhibitors
文献作者:Bacher,E.; Boer,C.; Bray-French,K.; Demnitz,F.W.; Keller,T.H.; Mazzoni,L.; M黮ler,T.; Walker,C.
参考来源:Bioorg Med Chem Lett 1998,8(22),3229