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

R-107500

Chemical Name: (+)-N,N-Dimethyl-N-[(2R,3aR)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepin-2-ylmethyl]amine L-malate
CAS No. 179602-48-3 (free base), 179796-92-0 (oxalate)
项目整合开发状态: Precl...
参考文献标题:Substd.tetracyclic azepine derivs.which have affinity for 5-HT2 receptors
文献作者:Sipido,V.K.; Fernandez-Gadea,F.J.; Andres-Gil,J.I.; Meert,T.F.; Gil-Lopetegui,P.(Janssen Pharmaceutica NV)
参考来源:EP 0789701; JP 1998508308; US 5552399; WO 9614320

ELB-176, AWD-34-176

Chemical Name: 5-(2,6-Difluorobenzyl)-2-methyl-4,5-dihydro-2H-pyrazolo[3,4-d]pyrimidin-4-one
CAS No. 402570-60-9
项目整合开发状态: Preclinical
项目研究机构: elbion (Originator)
合成路线:Benzaldehyde (I) is ...
参考文献标题:2,5-Dihydro-pyrazolo[3,4-d]pyrimidin-4-ones with an anticonvulsive action and methods for producing the same
文献作者:Lankau,H.-J.; Unverferth,K.; Tober,C.; Rundfeldt,C.; Arnold,T.; Dost,R.; Gasparic,A.; Bernter,K.(AWD.pharma GmbH & Co.KG)
参考来源:WO 0218387

新产品编号:184021

Chemical Name: 2-[8-[2(R)-(2-Amino-2-methylpropionylamino)-5-phenylpentanoyl]-8-azabicyclo[3.2.1]oct-3exo-yl]-N-ethylbenzamide
CAS No. 185099-60-9, 185099-56-3 (monoHCl)
项目整合开发状态: Preclinical 参考文献标题:Bridged piperidines promote release of growth hormone
文献作者:Patchett,A.A.; Tata,J.R.; Lu,Z.(Merck & Co.,Inc.)
参考来源:US 5731317

TAK-810

Chemical Name: N-[4-[3-(N-Benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-5-isobutyryl-4-oxo-4,7-dihydrothieno[2,3-b]pyridin-2-yl]phenyl]-1-hydroxycyclopropanecarboxamide
CAS No. 253433-89-5, 25...
参考文献标题:Thienopyridine cpds.,their production and use
文献作者:Suzuki,N.; Furuya,S.; Choh,N.; Imada,T.(Takeda Chemical Industries,Ltd.)
参考来源:EP 1090010; JP 2000219690; JP 2000219691; US 6262267; US 6329388; WO 0000493

新产品编号:454543

Chemical Name: 2-(4-Chlorophenoxy)-1-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]ethanone
CAS No. 217646-35-0, 217645-39-1 ((S)-isomer), 217645-38-0 (undefined isomer)
项目整合开发状态: Preclinical 参考文献标题:Piperazine derivs.and their use as anti-inflammatory agents
文献作者:Monahan,S.D.; Xu,W.; Morissey,M.M.; Bauman,J.G.; Ng,H.P.; Hesselgesser,J.E.; Liang,M.; Zheng,W.; Islam,I.; May,K.B.; Ghannam,A.F.; Buckman,B.O.; Horuk,R.; Wei,G.P.(Schering AG)
参考来源:US 6207665; WO 9856771

新产品编号:699753

Chemical Name: 6-Fluoro-2-[4-(methylsulfonyl)phenyl]-3-(3-pyridyl)-4H-1-benzopyran-4-one
CAS No. 259680-30-3
项目整合开发状态: Preclinical
项目研究机构: AmorePacific (Originator)
合成路线:Aldol condensation...
参考文献标题:Diarylbenzopyran derivs.as cyclooxygenase-2 inhibitors
文献作者:Kim,J.K.; Choi,J.K.; Lee,C.H.; Joo,Y.H.; Noh,M.-S.; Ha,J.-Y.; Lim,K.M.; Kang,S.-H.(Pacific Corp.)
参考来源:EP 1105384; JP 2002523410; US 6340694; WO 0010993

新产品编号:571611

Chemical Name: 3endo-[1-(3,5-Dichlorophenylsulfonyl)pyrrolidin-2(S)-ylcarboxamido]bicyclo[2.2.1]heptane-2exo-carboxylic acid; N-(2exo-Carboxybicyclo[2.2.1]heptan-3endo-yl)-1-(3,5-dichlorophenylsulfony...
参考文献标题:Cyclic amino acid derivs.as cell adhesion inhibitors
文献作者:Hagmann,W.K.; MacCoss,M.; Chang,L.(Merck & Co.,Inc.)
参考来源:JP 2001523711; US 6271252; WO 9926615

R-278995, CRA-0450

Chemical Name: 1-[8-(2,4-Dichlorophenyl)-2-methylquinolin-4-yl]-1,2,3,6-tetrahydropyridine-4-carboxamide benzenesulfonate
CAS No. 388122-48-3 (free base)
项目整合开发状态: Preclinical
项目研究机构: Johnson...
参考文献标题:Tetrahydropyridino or piperidino heterocyclic derivs.
文献作者:Kameo,K.; Kumagai,T.; Nakazato,A.; Okubo,T.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 1299378; WO 0202549

Genz-34940

Chemical Name: 2-[4-(4-Chlorophenoxy)-3,5-dimethyl-1H-pyrazol-1-yl]-4-(2-pyridyl)pyrimidine
CAS No. 374080-71-4
项目整合开发状态: Preclinical
项目研究机构: Genzyme (Originator)
合成路线:2,2-Diphenylethylami...
参考文献标题:Modulators of TNF-alpha signaling
文献作者:Hirth,B.H.; Sneddon,S.F.; Kane,J.L.; Vinick,F.; Qiao,S.; Nahill,S.R.(Genzyme Corp.)
参考来源:WO 0187849

UCB-62045

Chemical Name: N-[4-[4-[4-[4-[Bis(4-fluorophenyl)methyl]piperazin-1-yl]butoxy]phenyl]-3-butynyl]-N-hydroxyurea
CAS No. 299461-07-7
项目整合开发状态: Preclinical
项目研究机构: UCB (Originator)
合成路线:4-Iod...
参考文献标题:Cpds.and methods for treatment of asthma,allergy and inflammatory disorders
文献作者:Chatelain,P.; Differding,E.; Cai,X.; Hussoin,S.; Grewal,G.; Young,M.; Lewis,T.; Toy-Palmer,A.; Scannel,R.; Ellis,J.; Lassoie,M.-A.(UCB SA)
参考来源:JP 2002540198; US 6451801; WO 0058295