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

CI-844

3-苯氧基吡啶Chemical Name: 3-Phenoxypyridine sulfate
CAS No. 2176-45-6 (free base), 66066-82-8 (HBr salt), 66066-81-7 (HCl), 66066-84-0 (methanesulfonate)
项目整合开发状态: Phase II
项目研究机构: Pfizer (Origin...
参考文献标题:3-Phenoxypyridine monosulfate and a method for its production
文献作者:Butler,D.E.(Pfizer Inc.)
参考来源:BE 0861649; DE 2755016; ES 464922; FR 2392009; GB 1559918; JP 53077068; US 4128555

BIIL-260

4-((3-((4-(2-(4-(4-(4-(4-羟基苯)丙-2-基)苯氧基)甲基)苯甲基)氧)苯并咪酰胺Chemical Name: 4-[3-[4-[1-(4-Hydroxyphenyl)-1-methylethyl]phenoxy]methyl]benzyloxy]benzenecarboximidamide
CAS No. 204974-93-6
项目整合开发状态: Precl...
参考文献标题:Substd.benzamidines,their production and their use as medicaments
文献作者:Anderskewitz,R.; Schromm,K.; Renth,E.-O.; Birke,F.; F黦ner,A.; Heuer,H.; Meade,C.(Boehringer Ingelheim GmbH)
参考来源:DE 4424713; EP 0770059; JP 1998502645; US 5731332; WO 9602497

L-778123

4-((5-((4-(3-氯苯基)-3-氧代哌嗪-1-基)甲基)-1H-咪唑-1-基)甲基)苯甲腈 L-778123二盐酸盐 Chemical Name: 4-[5-[4-(3-Chlorophenyl)-3-oxopiperazin-1-ylmethyl]imidazol-1-ylmethyl]benzonitrile
CAS No. 183499-57-2, 183499-56-1 (d...
参考文献标题:Inhibitors of farnesyl-protein transferase
文献作者:Anthony,N.J.; Ciccarone,T.M.; Gomez,R.P.; Hutchinson,J.H.; Williams,T.M.; Dinsmore,C.J.; Stokker,G.E.(Merck & Co.,Inc.)
参考来源:EP 0820445; JP 1998511098; US 5856326; WO 9630343

RS-2232

4-((6,7-二氢-5H-环戊烯并嘧啶-4-基)氨基)苯甲腈Chemical Name: 4-[(6,7-Dihydro-5H-cyclopentapyrimidin-4-yl)amino]benzonitrile; 4-(4-Cyanophenyl)amino-6,7-dihydro-5H-cyclopentapyrimidine; 4-(4-Cyanoanilino)-6,7-dihydro...
参考文献标题:Pyrimidine derivatives and a pharmaceutical composition containing them
文献作者:Kamioka,T.; et al.(Sankyo Co.,Ltd.; Ube Industries,Ltd.)
参考来源:CA 1169861; EP 0067630; JP 57203072; US 4450162

AM-36

4-({4-[2-(4-氯苯基)-2-羟基乙基]-1-哌嗪基}甲基)-2,6-二(2-甲基-2-丙基)苯酚二盐酸盐Chemical Name: 4-[4-[2-(4-Chlorophenyl)-2-hydroxyethyl]piperazin-1-ylmethyl]-2,6-bis(tert-butyl)phenol
CAS No. 199467-52-2, 199467-53-3 (tar...
参考文献标题:Arylalkylpiperazine cpds.as antioxidants
文献作者:Collis,M.P.; Robertson,A.D.; Kenche,V.B.; Jackson,W.R.; Jarrott,B.; Beart,P.M.(Monash University)
参考来源:JP 2000510126; WO 9743259

Fadrozole hydrochloride, Fadrozole monohydrochloride, CGS-16949A, Afema, Arensin

4-(1,8-二氮腈环[4.3.0]nona-6,8-二烯-2-基)苯并腈盐酸盐法倔唑法倔唑盐酸盐Chemical Name: (?-4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile monohydrochloride
CAS No. 102676-96-0, 102676-47-1 (free base non-s...
参考文献标题:CGS-16949A
文献作者:Pento,J.T.; Prous,J.; Castar,J.
参考来源:Drugs Fut 1989,14(9),843

L1NAll

4(1H)-吡啶酮,3-羟基-2-甲基-1-(2-丙烯-1-基)-Chemical Name: 1-Allyl-2-methyl-3-hydroxypyridin-4(1H)-one
CAS No. 126055-15-0
项目整合开发状态: Preclinical
项目研究机构: Royal Free Hospital (Originator)
合成路线:By reflu...
参考文献标题:Process for producing pyrid-4-ones
文献作者:Kontoghiorghes,G.J.; Sheppard,L.N.(Royal Free Hospital)
参考来源:EP 0335745

M-17055

4(1H)-喹喴酮,7-氯-2,3-二氢-1-(2-甲基苯甲酰)-,O-磺胺,钾盐(1:1)Chemical Name: 7-Chloro-1-(2-methylbenzoyl)-1,2,3,4-tetrahydroquinolin-4-one O-sulfooxime potassium salt
CAS No. 114417-20-8
项目整合开发状态: Phase III
...
参考文献标题:1-Acyl-2,3-dihydro-4(1H)-quinolinone-4-oxime derivs.
文献作者:Uemura,A.; Mochida,E.; Haga,A.; Tokunaga,H.; Kato,K.(Mochida Pharmaceutical Co.,Ltd.)
参考来源:AU 9058618; EP 0243982; JP 1988239270; JP 1993262737; US 4739368; WO 8706580

NS-1, OCO-1112

4-(2-(4-异丙基苯并酰胺基)乙氧基)苯甲酸Chemical Name: 4-[2-(4-Isopropylbenzamido)ethoxy]benzoic acid
CAS No. 113079-40-6
项目整合开发状态: Phase II
项目研究机构: Nippon Shinyaku (Originator)
合成路线:The condensation of a...
参考文献标题:Benzoic acid derivs
文献作者:Yoshikuni,Y.; Choaki,S.; Ozaki,T.; Yoshida,H.(Nippon Shinyaku Co.,Ltd.)
参考来源:CH 674204; DE 3718765; FR 2600059; GB 2191487; JP 1987292754; JP 1988159359; US 4831055

AGZ-1067, AGI-1067

4-(2,6-二-叔丁基-4-(2-(3,5-二-叔丁基-4-羟基苯基硫代)丙烷-2-基硫代)苯氧基)-4-氧代丁酸Chemical Name: Succinic acid 2,6-di-tert-butyl-4-[1-(3,5-di-tert-butyl-4-hydroxyphenylsulfanyl)-1-methylethylsulfanyl]phenyl monoester
CAS ...
参考文献标题:Cpds.and methods for the inhibition of the expression of VCAM-1
文献作者:Medford,R.M.; Meng,C.Q.; Hoong,L.K.; Somers,P.K.(AtheroGenics,Inc.)
参考来源:JP 2002503227; US 6147250; WO 9851662