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

S-17834

Chemical Name: 6,8-Diallyl-2-(2-allyl-3-hydroxy-4-methoxyphenyl)-5,7-dihydroxy-4H-1-benzopyran-4-one
CAS No. 178367-40-3
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:The alkylat...
参考文献标题:Diosmetin derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Wierzbicki,M.; Boussard,M.-F.; Verbeuren,T.; Vallez,M.-O.; Canet,E.; Rolland,Y.(ADIR et Cie.)
参考来源:CA 2161297; EP 0709383; FR 2726273; JP 1996225563; US 5629339

Implitapide, BAY-13-9952

Chemical Name: 2(S)-Cyclopentyl-2-[4-(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-ylmethyl)phenyl]-N-[2-hydroxy-1(R)-phenylethyl]acetamide
CAS No. 177469-96-4
项目整合开发状态: Phase II
项目研究机构: Bayer (Origi...
参考文献标题:Cycloalkano-indole- and -azaindole derivs.
文献作者:M黮ler,U.; Connell,R.; Goldmann,S.; Grzmann,R.; Beuck,M.; Bischoff,H.; Denzer,D.; Domdey-Bette,A.; Wohlfeil,S.(Bayer AG)
参考来源:CA 2159546; DE 4435477; EP 0705831; JP 1996225526; US 5684014

NPC-17731

Chemical Name: D-Arginyl-L-arginyl-L-prolyl-L-(trans-4-hydroxy)prolyl-glycyl-L-phenylalanyl-L-seryl-D-(trans-4-propoxy)prolyl-L-[(2alpha,3abeta,7abeta)octahydroindol-2-ylcarbonyl]-L-arginine
CAS No...
参考文献标题:Bradykinin antagonist peptides
文献作者:Kyle,D.J.; Hiner,R.N.(Scios Inc.)
参考来源:JP 1995504155; US 5385889

NSC-651016

Chemical Name: 4,4'-Carbonylbis(1H-pyrrol-4,2-diyl)bis(carbonylimino)bis(1-methylpyrrol-4,2-diyl)bis(carbonylimino)bis(naphthalene-1,7-disulfonic acid disodium salt)
CAS No. 208576-37-8 (error)
...
参考文献标题:New ureido derivs.of poly-4-amino-2-carboxy-1-methyl cpds.
文献作者:Mongelli,N.; Biasoli,G.; Paio,A.; Grandi,M.; Ciomei,M.(Pharmacia Corp.)
参考来源:EP 0462258; JP 1992504426; US 5260329; US 5420296; WO 9110649

PD-123497, RSD-921

Chemical Name: (+)-(1R,2R)-N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzo[b]thiophene-4-acetamide
CAS No. 114419-77-1
项目整合开发状态: Phase II
项目研究机构: Pfizer (Originator), Cardiome (Licensee), Chem...
参考文献标题:Aminocyclohexylamides for antiarrhythmic and anaesthetic uses
文献作者:MacLeod,B.A.; Walker,M.J.A.; Wall,R.A.(University of British Columbia)
参考来源:EP 0632806; JP 1995505151; US 5506257; WO 9319056

Mivotilate, YH-439

Chemical Name: 2-(1,3-Dithietan-2-ylidene)-2-[N-(4-methylthiazol-2-yl)carbamoyl]acetic acid isopropyl ester
CAS No. 130112-42-4
项目整合开发状态: Discontinued
项目研究机构: Yuhan (Originator), Grelan (Lice...
参考文献标题:Pharmaceutically active dithioketene derivs.
文献作者:Kim,C.S.; Chae,J.S.; Yoo,H.S.; Park,J.G.; Lee,J.W.(Yuhan Corp.)
参考来源:EP 0366614

F4CC-1104

Chemical Name: (?-3-(3,4-Dimethoxyphenyl)-3-(4,5,6,7-tetrafluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)propionic acid methyl ester
CAS No. 179033-27-3
项目整合开发状态: Preclinical
项目研究机构: Massachus...
参考文献标题:Thalidomide analogs and PDE4 inhibition
文献作者:Muller,G.W.; Shire,M.G.; Wong,L.M.; Corral,L.G.; Patterson,R.T.; Chen,Y.; Stirling,D.I.
参考来源:Bioorg Med Chem Lett 1998,8(19),2669

DZ-3358

Chemical Name: 1-(3-Chlorophenyl)-4-[3-[5-methyl-1-(2-pyrimidinyl)pyrazol-4-yl]-1(E)-propenyl]piperazine hydrochloride
CAS No. 178927-85-0, 258824-19-0 (undefined isomer)
项目整合开发状态: Preclinical 参考文献标题:Pyrimidinylpyrazole deriv.
文献作者:Ejima,A.; Sugimori,M.; Mitsui,I.(Daiichi Pharmaceutical Co.,Ltd.)
参考来源:EP 0784055; JP 1997048776; US 5852019; WO 9610024

NVP-VID-400

Chemical Name: (R)-4'-Chloro-N-[2-(1-imidazolyl)-2-phenylethyl]biphenyl-4-carboxamide
CAS No. 174262-10-3, 174262-09-0 ((S)-isomer), 174262-13-6 (racemate)
项目整合开发状态: Preclinical
项目研究机构: Novar...
参考文献标题:Acylated aminoalkanimidazoles and -triazoles
文献作者:Schuster,I.; Egger,H.(Novartis AG; Novartis Deutschland GmbH)
参考来源:CA 2149459; EP 0683156; JP 1996053422; US 5622982

AR-0510

Chemical Name: trans-2-[4-(5-Amidino-1-benzofuran-2-ylcarboxamido)cyclohexyloxy]acetic acid ethyl ester
CAS No. 174774-03-9, 174774-04-0 (monomethanesufonate salt)
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Novel fused-ring carboxylic acid cpds.or salt thereof,and medicinal use thereof
文献作者:Ono,S.; Yoshida,T.; Ashimori,A.; Kosaka,K.; Okada,T.; Maeda,K.; Eda,M.; Mori,F.; Inoue,Y.; Ebisu,H.; Imada,T.; Ikegawa,R.; Wang,F.; Nakamura,N.(Welfide Corporation)
参考来源:EP 0712844; JP 1996053398; JP 1996231548; US 5635527; US 5753670; WO 9533720