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

UK-240455, UK-212189(racemate)

Chemical Name: (aR)-N-(6,7-Dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-(2-hydroxyethyl)methanesulfonamide
CAS No. 178908-09-3 (undefined isomer)
项目整合开发状态: Phase I
项目研究机构: Pfizer (...
参考文献标题:Quinoxaline derivs.useful in therapy
文献作者:Stobie,A.; Mowbray,C.E.; Fray,M.J.(Pfizer Inc.)
参考来源:US 5852016; WO 9609295

L-838751

Chemical Name: 6-Fluoro-3-[4(R)-fluoropiperidin-3(R)-yl]-2-phenyl-1H-indole
CAS No. 244086-93-9 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Merck Sharp & Dohme (Originator)
合成路线:Conde...
参考文献标题:3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity,selective,and orally bioavailable h5-HT2A receptor antagonists
文献作者:Rowley,M.; Hallett,D.J.; Goodacre,S.; Moyes,C.R.; Crawforth,J.; Sparey,T.J.; Patel,S.; Marwood,R.; Thomas,S.; Hitzel,L.; O'Connor,D.; Szeto,N.; Castro,J.L.; Hutson,P.H.; MacLeod,A.M.
参考来源:J Med Chem 2001,44(10),1603

DY-9804

Chemical Name: 4(R)-[(1R,6S)-4-(2-Chlorobenzyl)-5-oxo-3,4-diazabicyclo[4.1.0]hept-2-en-2-yloxy]-3(S)-hydroxy-2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-6-carbonitrile
CAS No. 154186-97-7 (non-specifi...
参考文献标题:Diazabicycloalkene derivs.
文献作者:Mimura,T.; Kubo,H.(Daiichi Pharmaceutical Co.,Ltd.)
参考来源:EP 0571822; JP 1994025233; US 5418232

MBX-300, NMSO3

Chemical Name: 5-Acetamido-2-O-[2,2-bis(docosyloxymethyl)propyl]-3,5-dideoxy-4,7,8,9-tetra-O-sulfo-D-glycero-D-galacto-2-nonulopyranosuronic acid pentasodium salt; N-Acetyl-2-O-[3-(docosyloxy)-2-(doco...
参考文献标题:Novel cpds.having antiviral activity
文献作者:Numata,M.; Nunomura,S.; Terada,M.; Suzuki,K.; Sugimoto,M.; Fujita,S.(Nissin Food Products Co.,Ltd.)
参考来源:CA 2255070; EP 0957107; WO 9743296

新产品编号:68535

Chemical Name: 1,3,5-Trihexyl-2,4,6-triiodobenzene
CAS No. 155802-08-7
项目整合开发状态: Preclinical
项目研究机构: Amersham (Originator)
合成路线:Coupling of 1,3,5-trichlorobenzene (I) with n-hexylmagnesium...
参考文献标题:Compsns.of alkylbenzenes in film-forming materials for visualization of the gastrointestinal tract
文献作者:Josef,K.A.; Douty,B.D.; Bacon,E.R.; Illig,C.; Estep,K.G.(Sterling Winthrop Inc.)
参考来源:EP 0609589; JP 1994234664; US 5334370

NTP 15-5

Chemical Name: Dioxo[N,N,N-Triethyl-3-(1,4,7,10,13-pentaazacyclopentadecan-1-yl)-1-propanaminium-kappaN1,kappaN4,kappaN7,kappaN10]technecium(2+)-99Tc monobromide
CAS No. 280563-99-7
项目整合开发状态: Pr...
参考文献标题:Synthesis of N-quaternary ammonium [3H] and [99mTc]polyazamacrocycles,potential radiotracers for cartilage imaging
文献作者:Nicolas,C.; et al.
参考来源:J Label Compd Radiopharm 2000,43(6),585

DHET-PGE2

Chemical Name: (5Z,11alpha,,13E,15S)-15-Hydroxy-11-(2-hydroxyethylsulfanyl)-9-oxoprosta-5,13-dien-1-oic acid methyl ester; 11-Deoxy-11alpha-(2-hydroxyethylsulfanyl)prostaglandin E2
CAS No. 74412-44...
参考文献标题:11-(2-Hydroxyethylthio)prostenoic acid E{HD 2 {B series derivatives
文献作者:Weiss,M.J.; Siuta,G.J.(American Cyanamid Co.)
参考来源:US 4085272

ZD-4974

Chemical Name: 3-Cyano-N-[2(S)-(3,4-dichlorophenyl)-4-[4-[2-[(S)-methylsulfinyl]phenyl]piperidin-1-yl]butyl]-2-methoxy-N-methylnaphthalene-1-carboxamide citrate
CAS No. 263860-84-0, 263860-83-9 (fr...
参考文献标题:Naphthalenecarboxamides as tachykinin receptor antagonists
文献作者:Bernstein,P.R.; Russell,K.; Ohnmacht,C.J.; Dedinas,R.F.; Shewood,S.A.(AstraZeneca plc)
参考来源:EP 1119551; JP 2002526527; WO 0020389

ER-41666

Chemical Name: 4-[5-(5,8-Dimethyl-2H-1-benzopyran-3-yl)-1H-pyrrol-2-yl]benzoic acid
CAS No. 196518-58-8
项目整合开发状态: Biological Testing
项目研究机构: Eisai (Originator)
合成路线:The condensation of 7-e...
参考文献标题:Fused-ring carboxylic acid derivs.
文献作者:Tagami,K.; Yoshimura,H.; Nagai,M.; Hibi,S.; Kikuchi,K.; Sato,T.; Okita,M.; Okamoto,Y.; Nagasaka,Y.; Kobayashi,N.; Hida,T.; Tai,K.; Tokuhara,N.; Kobayashi,S.(Eisai Co.,Ltd.)
参考来源:EP 0889032; US 6110959; US 6121309; WO 9734869

T-0162

Chemical Name: N-[3-(tert-Butyl)-2-hydroxy-5-methoxyphenyl]-N'-(3-pyridylmethyl)urea hydrochloride
CAS No. 195312-36-8, 195315-01-6 (free base)
项目整合开发状态: Preclinical
项目研究机构: Tanabe Seiyaku (O...
参考文献标题:Phenol-derivs.having pharmaceutical activity and process for preparing the same
文献作者:Suzuki,T.; Ohmizu,H.; Hashimura,Y.; Kubota,H.; Tanaka,K.(Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0790240; JP 1998195037; US 5849732