项目整合精选

聚焦新型临床类新产品的整合与转化. 在创新药研发领域，传统的“单一产品、单打独斗”模式正在被一种更系统化的“项目整合”思维所取代。项目整合的核心，在于将散落在研发早期、中期的创新资产，通过资金、临床资源、产业生态等多维度要素的有机组合，实现从“科学发现”到“临床价值”，再到“商业成功”的跨越。研发与商业的战略整合：从“资产思维”到“组合思维”它要求我们超越单个分子的视野，拥抱一个由技术创新、临床需求、资本支持和商业洞察共同构成的复杂网络。在这个网络中，成功的标准不再是单一的“获批上市”，而是能否通过高效的整合，将科学上的突破，转化为临床上真正可及、商业上可持续、能够惠及患者的解决方案。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，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。
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项目整合精选

新产品编号:791509

Chemical Name: (2RS,3SR)-1,2-Dimethyl-3-(2-naphthyl)pyrrolidin-3-ol hydrochloride
CAS No. 302959-32-6
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:The target (rac)-(cis)...
参考文献标题:Synthesis and antinociceptive activity of pyrrolidinylnaphthalenes
文献作者:Collina,S.; Azzolina,O.; Vercesi,D.; Sbacchi,M.; Sheideler,M.A.; Barbieri,A.; Lanza,E.; Ghislandi,V.
参考来源:Bioorg Med Chem 2000,8(8),1925

新产品编号:127069

Chemical Name: (+)-N-(10-Amino-10-methyl-4-oxo-5,10-dihydro-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-8-yl)-N'-methylurea
CAS No. 173155-95-8, 173156-03-1 (undefined isomer), 173155-39-0 (undefined iso...
参考文献标题:Imidazo (1,2-a)-indeno (1,2-e) pyrazin-4-one derivs.and pharmaceutical compsns.containing same
文献作者:Genevois-Borella,A.; Aloup,J.-C.; Audiau,F.; Barreau,M.; Mignani,S.; Ribeill,Y.; Damour,D.; Jimonet,P.(Aventis Pharma SA)
参考来源:US 5807859; WO 9526350

DU-257

Chemical Name: (7bR,8aS)-2-[6-(2-Aminoethoxy)-5,7-dimethoxy-1H-indol-2-ylcarbonyl]-6-methyl-4-oxo-1,2,5,7a,8,8a-hexahydrocyclopropa[c]pyrrolo[3,2-e]indole-7-carboxylic acid methyl ester
CAS No. 185...
参考文献标题:Toxin conjugates
文献作者:Saito,H.; Nagamura,S.; Suzawa,T.; Yamasaki,M.; Ohta,S.; Hanai,N.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:US 6103236; WO 9635451

新产品编号:775689

Chemical Name: 6-Chloro-5-methyl-N-[6-(2-methylpyridin-3-yloxy)pyridazin-3-yl]indoline-1-carboxamide
CAS No. 300554-31-8
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合...
参考文献标题:1-[2-(Heteroaryloxy)heteroaryl]carbamoy]indolines: Novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents
文献作者:Bromidge,S.M.; Dabbs,S.; Davies,S.; Duckworth,D.M.; Forbes,I.T.; Jones,G.E.; Jones,J.; King,F.D.; Saunders,D.V.; Blackburn,T.P.; Holland,V.; Kennett,G.A.; Lightowler,S.; Middlemiss,D.N.; Riley,G.J.; Trail,B.; Wood,M.D.
参考来源:Bioorg Med Chem Lett 2000,10(16),1863

CP-654743

Chemical Name: 3-Des(hexopyranosyloxy)-9-deoxo-11-deoxy-2-fluoro-9-(methoxyimino)-6-O-methyl-3-oxo-11-[3-[4-(3-pyridyl)imidazol-1-yl]propylhydrazino]erythromycin A 11-N1,12-O-cyclic carbamate
CAS N...
参考文献标题:Ketolide antibiotics
文献作者:Kaneko,T.; McMillen,W.T.(Pfizer Inc.)
参考来源:WO 0044761

新产品编号:348549

Chemical Name: N-[1-(3,5-Dibromo-4-hydroxybenzyl)-2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-4-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidine-1-carboxamide
CAS No. 204695-47-6 (R-isomer)
项目整合开发状...
参考文献标题:Modified aminoacids,pharmaceuticals containing these cpds.and methods for their production
文献作者:Eberlein,W.; Wienen,W.; Doods,H.; Rudolf,K.; Entzeroth,M.; Pieper,H.; Engel,W.; Hallermayer,G.(Dr.Karl Thomae GmbH)
参考来源:JP 2000505100; WO 9811128

Imoproxifan

Chemical Name: 1-[4-[3-(1H-Imidazol-4-yl)propoxy]phenyl]ethan-1-one oxime
CAS No. 184025-69-2, 184025-70-5 (maleate salt (1:1))
项目整合开发状态: Preclinical
项目研究机构: Bioprojet (Originator), INSERM (O...
参考文献标题:Imidazole derivs.as histamine receptor H3 (ant)agonists
文献作者:Schwartz,J.-C.; Arrang,J.-M.; Garbarg,M.; Quemener,A.; Lecomte,J.-M.; Ligneau,X.; Schunack,W.G.; Stark,H.; Purand,K.; H黮s,A.; et al.(INSERM (Institut National de la Sante et de la Recherche Medicale; Societe Civile Bioprojet)
参考来源:EP 0760811; FR 2732017; JP 1998501001; WO 9629315

CGS-34225

Chemical Name: N-[1-[2(S)-(Acetylsulfanyl)pentanamido]cyclopent-1-ylcarbonyl]-4-phenyl-L-phenylalanine methyl ester
CAS No. 248262-98-8
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
...
参考文献标题:Certain thiol inhibitors of endothelin-converting enzyme
文献作者:Fink,C.A.; De Lombaert,S.; Hoyer,D.W.; Jeng,A.Y.; Firoozina,F.(Novartis AG; Novartis Pharma GmbH)
参考来源:WO 9955726

BMS-247243

Chemical Name: (6R,7R)-7-[2-[4-[3-(Carboxylatomethylamino)-3-oxo-1(E)-propenyl]-2,5-dichlorophenylsulfanyl]acetamido]-3-[2,6-dimethyl-1-[3-(4-methylmorpholin-4-iumyl)propyl]pyridinium-4-ylsulfanylmeth...
参考文献标题:Cephalosporin derivs.
文献作者:Springer,D.M.; Luh,B.Y.; D'Andrea,S.V.; Hudyma,T.W.; Kim,O.K.(Bristol-Myers Squibb Co.)
参考来源:EP 0966472; WO 9823621

TAK-456

Chemical Name: 1-[2(R)-(2,4-Difluorophenyl)-2-hydroxy-1(R)-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-3-[4-(1H-tetrazol-1-yl)phenyl]imidazolidin-2-one
CAS No. 181869-54-5
项目整合开发状态: Preclinical
项...
参考文献标题:Azole cpds.,their production and use
文献作者:Itoh,K.; Okonogi,K.; Tasaka,A.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0809640; JP 1997183769; WO 9625410