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。
如有产品相关项目调研推广服务, 请致函联系我们

客户展示

新项目整合精选

R-96544

Chemical Name: 2(R)-[2-[2-[2-(3-Methoxyphenyl)ethyl]phenoxy]ethyl]-1-methylpyrrolidin-4(R)-ol hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Sankyo (Originator)
合成路线:Synthesis of intermediate (V...
参考文献标题:Phenoxyalkylamines,-pyrrolidines and -piperidines for the treatment and prevention of circulatory diseases and psychosis
文献作者:Fujimoto,K.; Tanaka,N.; Asai,F.; Ito,T.; Koike,H.(Sankyo Co.,Ltd.)
参考来源:EP 0600717; JP 1994234736; JP 1994306025; US 5556864

新产品编号:1033555

Chemical Name: (2aR,4S,4aS,9S,11S,12S,12aR,12bS)-12b-Acetoxy-9-[3(S)-benzamido-2(R)-hydroxy-3-phenylpropionyloxy]-12-benzoyloxy-4,11-dihydroxy-4a,8,13,13-tetramethyl-2a,3,4,4a,5,6,9,10,11,12,12a,12b-d...
参考文献标题:Process for the preparation of taxane derivs.,novel taxanes so obtained and antitumour and antileukaemia compsns.containing same
文献作者:Bourzat,J.-D.; Commer鏾n,A.; Deprez,D.; Pulicani,J.-P.(Aventis Pharma SA)
参考来源:JP 1996503261; WO 9411547

FR-86521

Chemical Name: (6R,7R)-7-[2-(5-Amino-1,2,4-thiadiazol-3-yl)-2(Z)-(ethoxyimino)acetamido]-3-[3-amino-2-(2-hydroxyethyl)pyrazolium-1-ylmethyl]-3-cephem-4-carboxylic acid chloride
项目整合开发状态: Preclinica...
参考文献标题:Synthesis and biological properties of a novel cephalosporin FR86521 having potent activity against methicilin-resistant Staphylococcus aureus (MRSA)
文献作者:Kishi,K.; Ohki,H.; Okuda,S.; Kawabata,K.; Sakane,K.; Matsumoto,Y.; Matsumoto,S.; Tawara,S.
参考来源:J Antibiot 1999,52(12),1152

新产品编号:1035137

Chemical Name: 2-[2-Methyl-6-nitro-2-(nitrooxymethyl)-3,4-dihydro-2H-1,4-benzoxazin-4-yl]pyridine 1-oxide
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:Treatment of 2-amino-4-nit...
参考文献标题:Novel potassium channel activators.III.Synthesis and pharmacological evaluation of 3,4-dihydro-2H-1,4-benzoxazine derivatives: Modification at the 2 position
文献作者:Matsumoto,Y.; Uchida,W.; Nakahara,H.; Yanagisawa,I.; Shibanuma,T.; Nohira,H.
参考来源:Chem Pharm Bull 2000,48(3),428

Altorhyrtin C, Spongistatin 2

Chemical Name: (1S,3S,5R,9R,10R,11R,13R,14S,15R,17S,18R,19R,23Z,25R,27S,29S,31S,33S,36S,37S,38R,41S,43S,49S)-3,37-Diacetoxy-11-[4(S)-hydroxy-2-methylene-5(E),7-octadienyl]-10,14,15,17,27,43-hexahydrox...
参考文献标题:The spongistatins: Architecturally complex natural products - Part one: A formal synthesis of (+)-spongistatin 1 by construction of an advanced ABCD fragment
文献作者:Smith,A.B.; et al.
参考来源:Angew Chem.Int Ed Engl 2001,40(1),191

W4R

Chemical Name: 7-Amino-6-chloro-10-[2-(diethylamino)ethyl]-1-hydroxy-3-methoxyacridin-9(10H)-one
项目整合开发状态: Biological Testing
项目研究机构: Mediolanum (Originator), Universit?degli Studi di Perugia (O...
参考文献标题:Design and synthesis of modified quinolones as antitumoral acridones1
文献作者:Tabarrini,O.; Cecchetti,V.; Fravolini,A.; Nocentini,G.; Barzi,A.; Sabatini,S.; Miao,H.; Sissi,C.
参考来源:J Med Chem 1999,42(12),2136

(R)-(+)-XK-469, NSC-698215(free acid), XB-947

Chemical Name: (+)-2(R)-[4-(7-Chloroquinoxalin-2-yloxy)phenoxy]propionic acid sodium salt
项目整合开发状态: Phase I
项目研究机构: Bristol-Myers Squibb (Originator), National Cancer Institute (Not Determined)<...
参考文献标题:(2-Quinoxalinyloxy)phenoxypropanoic acids and related derivs.as anticancer agents
文献作者:Behrens,C.H.; Dusak,B.A.; Harrison,B.A.; Orwat,M.J.(Bristol-Myers Squibb Co.)
参考来源:WO 9413647

DPP-NH[psi]

Chemical Name: 2,6-Dimethyltyrosyl-(1,2,3,4-tetrahydroisoquinolin-3-ylmethyl)-phenylalanyl-phenylalaninamide
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:The condensation of re...
参考文献标题:New peptides
文献作者:Schiller,P.(AstraZeneca plc)
参考来源:EP 0678099; JP 1996505386; WO 9415959

FR-167653

Chemical Name: 7-(4-Fluorophenyl)-2-(phenylglyoxyloyl)-8-(4-pyridyl)-1,2,3,4-tetrahydropyrazolo[5,1-c][1,2,4]triazine sulfate; 1-[7-(4-Fluorophenyl)-8-(4-pyridyl)-1,2,3,4-tetrahydropyrazolo[5,1-c][1,2...
参考文献标题:Pyrazolitriazines with interleukin-1 and tumour necrosis factor inhibitory activity
文献作者:Kawai,Y.; Yamazaki,H.; Tanaka,H.; Oku,T.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0686156; JP 1996507056; WO 9419350

新产品编号:1036719

Chemical Name: 7-[2-(2-Aminothiazol-4-yl)-2(Z)-[1(S)-carboxyethoxyimino]acetamido]-3-(5-methylthiazolo[4,5-c]pyridinium-2-ylsulfanylmethyl)-3-cephem-4-carboxylate sodium salt
项目整合开发状态: Preclinical<...
参考文献标题:Novel cephalosporin derivatives possessing a bicyclic heterocycle at the 3-position.Part II: Synthesis and antibacterial activity of 3-(5-methylthiazolo[4,5-c]pyridinium-2-yl)thiomethylcephalosporin derivatives and related compounds
文献作者:Tsushima,M.; Kano,Y.; Umemura,E.; Iwamatsu,K.; Tamura,A.; Shibahara,S.
参考来源:Bioorg Med Chem 1998,6(9),1641