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

MLD-987, SDZ-MLD-987

Chemical Name: (1R,9S,12S(1'R,3'R,4'R),13R,14S,17R,21S,23S,24R,25S,27R)-17-Allyl-1,14-dihydroxy-23,25-dimethoxy-12-[2-[3-methoxy-4-[N-[4-(2-methoxy-2-oxoethyl)phenyl]carbamoyloxy]cyclohexyl]-1(E)-meth...
参考文献标题:Ascomycins
文献作者:Naef,R.; Hersperger,R.(Novartis AG; Novartis Deutschland GmbH)
参考来源:JP 2000505044; US 5925649; WO 9631514

新产品编号:117577

Chemical Name: 3-Chloro-4-[1-(4-phenoxybenzyl)-1H-indol-5-yloxy]benzoic acid
CAS No. 170146-86-8
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:The N-benzyl indole derivative (...
参考文献标题:A novel class of inhibitors for human steroid 5alpha-reductase: Synthesis and biological evaluation of indole derivatives.II
文献作者:Igarashi,S.; Inami,H.; Hara,H.; Fujii,M.; Koutoku,H.; Oritani,H.; Mase,T.
参考来源:Chem Pharm Bull 2000,48(3),382

RC-552C, RC-552

Chemical Name: 2-Deoxy-6-O-[2-deoxy-4-O-phosphono-3-O-[3(R)-(tetradecanoyloxy)tetradecanoyl]-2-[3(R)-(octadecanoyloxy)tetradecanamido]-beta-D-glucopyranosyl]-2-[3(R)-(hexadecanoyloxy)tetradecanamido]-...
参考文献标题:Phosphoglycolipid and methods for its use
文献作者:Sowell,C.G.; Weber,P.A.; Elliott,G.T.(Corixa Corp.)
参考来源:WO 0011010

MGS-0028

Chemical Name: (1R,2S,5S,6S)-2-Amino-6-fluoro-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
CAS No. 260353-67-1
项目整合开发状态: Preclinical
项目研究机构: Taisho (Originator)
合成路线:Coupling of ethyl p...
参考文献标题:6-Fluorobicyclo[3.1.0]hexane derivs.
文献作者:Kumagai,T.; Sakagami,K.; Nakazato,A.; Tomisawa,K.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 1110943; JP 2000336071; WO 0012464

OM-99-1

Chemical Name: L-Valyl-L-asparaginyl-L-leucyl-psi[(S)-CH(OH)CH2]-L-alanyl-L-alanyl-L-glutamyl-L-phenylalanine; L-Valyl-L-asparaginyl-(2R,4S,5S)-5-amino-4-hydroxy-2,7-dimethyloctanoyl-L-alanyl-L-glutam...
参考文献标题:Design of potent inhibitors for human brain memapsin 2 (beta-secretase)
文献作者:Lin,X.; Shin,D.; Downs,D.; Tang,J.; Koelsch,G.; Ghosh,A.K.; Ermolieff,J.
参考来源:J Am Chem Soc 2000,122(14),3522

Y-34959

Chemical Name: N-[5-[4-(4-Amino-5-chloro-2-methoxybenzamidomethyl)piperidin-1-yl]pentyl]-1-methyl-1H-indole-3-carboxamide hydrochloride
CAS No. 173339-89-4 (free base)
项目整合开发状态: Preclinical
项...
参考文献标题:Benzoic acid cpd.and use thereof as medicine
文献作者:Kawakita,T.; Hakira,H.; Haga,K.; Murozono,T.; Kuroita,T.(Welfide Corporation)
参考来源:EP 0774460; WO 9526953

新产品编号:301089

Chemical Name: 5-(Acetamido)-N-[2-[1-(chloromethyl)-5-hydroxy-1,2-dihydro-3H-benzo[e]indol-3-ylcarbonyl]-1H-indol-5-yl]-1H-indole-2-carboxamide
CAS No. 199806-33-2
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:DNA-binding indole derivs.,their prodrugs and immunoconjugates as anticancer agents
文献作者:Larrick,J.W.; Wright,S.C.; Wang,Y.(Panorama Research,Inc.)
参考来源:WO 9744000

PNU-109849

Chemical Name: 2(S)-[3(S)-[2-(Hydroxyamino)-2-oxoethyl]-3-isobutyl-2-oxopyrrolidinyl]-N-methyl-3-phenylpropionamide
CAS No. 196950-05-7, 196949-86-7 (undefined isomer)
项目整合开发状态: Preclinical
项...
参考文献标题:Hydroxamic acid derivs.for use with the treatment of diseases related to connective tissue degradation
文献作者:Jacobsen,E.J.(Pharmacia & Upjohn AB)
参考来源:EP 0898562; JP 2000506163; US 5712300; WO 9732846

OC-060-062

Chemical Name: 3,3'-[2-[4-(Diethylamino)phenyl-1H-imidazole-4,5-diyl]di-4,1-phenylene]bis[2(E)-propenoic acid]
CAS No. 207867-66-1, 207867-67-2 (trifluoroacetate)
项目整合开发状态: Biological Testing 参考文献标题:Modulators of proteins with phosphotyrosine recognition units
文献作者:Mjalli,A.; Sarshar,S.; Cao,X.; Bakir,F.(Ontogen Corp.)
参考来源:US 5753687; US 5770620

Becampanel, AMP-397, AMP-397A

Chemical Name: (7-Nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-ylmethylaminomethyl)phosphonic acid
CAS No. 188696-80-2
项目整合开发状态: Phase II
项目研究机构: Novartis (Originator)
合成路线:The reaction ...
参考文献标题:Substd.aminoalkane phosphonic acids
文献作者:Acklin,P.; Allgeier,H.; Auberson,Y.; Ofner,S.; Veenstra,S.J.(Novartis AG)
参考来源:EP 0934326; US 6117873; WO 9817672