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

RPR-117820A

Chemical Name: (+)-2(S)-[2-Cyano-5-(4-pyridylmethoxy)phenoxy]-2-(2-methylphenyl)acetic acid sodium salt
CAS No. 181038-01-7
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator)
合成路线:T...
参考文献标题:Substd.phenyl cpds.as endothelin antagonists
文献作者:Porter,B.; Astles,P.C.; Bridge,A.W.; McLay,I.M.; Van Sickle,A.P.; Walsh,R.J.A.; McCarthy,C.; Morley,A.D.; Halley,F.; Harris,N.V.; Majid,T.N.; Smith,C.(Rh鬾e-Poulenc Rorer Ltd.)
参考来源:US 6048893; US 6124343; WO 9622978

新产品编号:682351

Chemical Name: 4'-Amidino-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-2'-methylbiphenyl-4-carboxamide
CAS No. 256227-71-1
项目整合开发状态: Preclinical
项目研究机构: Merck KGaA (Originator)
合成路线:Coup...
参考文献标题:Biphenyl derivs.
文献作者:Van Amsterdam,C.; Harting,J.; Wikstr鰉,H.V.; Liao,Y.; B鰐tcher,H.(Merck Patent GmbH)
参考来源:WO 0005225

新产品编号:104921

Chemical Name: 1-Methyl-2(S)-[2-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]ethyl]pyrrolidine hydrochloride
CAS No. 167144-72-1, 167144-74-3 (enantiomer), 167144-71-0 (free base)
项目整合开发状态: Biological T...
参考文献标题:Phenoxyalkylamines,-pyrrolidines and -piperidines for the treatment and prevention of circulatory diseases and psychosis
文献作者:Fujimoto,K.; Tanaka,N.; Asai,F.; Ito,T.; Koike,H.(Sankyo Co.,Ltd.)
参考来源:EP 0600717; JP 1994234736; JP 1994306025; US 5556864

AG-5507

Chemical Name: 4-(3,5-Dimethoxyphenyl)-13-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]-4,7,13-triazatricyclo[7.3.1.0(2,7)]tridec-2-ene-5,8-dione; 2-(3,5-Dimethoxyphenyl)-12-[2-oxo-2-(3,4,5-trimethoxypheny...
参考文献标题:Cpds.,compsns.,and methods for stimulating neuronal growth and elongation
文献作者:Tada,H.; Kalish,V.; Kato,S.; Villafranca,J.E.; Tatlock,J.H.; Linton,M.A.; Kawakami,H.(Agouron Pharmaceuticals,Inc.)
参考来源:WO 0004020

Bradyzide

Chemical Name: N-[2-[N-[2-(Dimethylamino)ethyl]-N-methylamino]ethyl]-1-[4-[4-(diphenylmethyl)thiosemicarbazido]-3-nitrophenylsulfonyl]pyrrolidine-2(S)-carboxamide
CAS No. 263011-13-8
项目整合开发状态: P...
参考文献标题:1-(2-Nitrophenyl)thiosemicarbazides: A novel class of potent,orally active non-peptide antagonist for the bradykinin B2 receptor
文献作者:Dziadulewicz,E.K.; Ritchie,T.J.; Hallett,A.; Snell,C.R.; Ko,S.Y.; Hughes,G.A.; Dunstan,A.R.; Bloomfield,G.C.; Drake,G.S.; Brown,M.C.; Lee,W.; Burgess,G.M.; Davis,C.; Yaqoob,M.; Perkins,M.N.; Campbell,E.A.; Davis,A.J.; Rang,H.P.
参考来源:J Med Chem 2000,43(5),769

BIIE-0246

Chemical Name: N-[1-[2-[4-(6-Oxo-6,11-dihydro-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]cyclopentyl]acetyl]-L-arginine N-[2-(3,5-dioxo-1,2-diphenyl-1,2,3,4-tetrahydro-1,2,4-triazol-4-yl]ethylamide
...
参考文献标题:Novel substd.amino acid derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Gaida,W.; Schnorrenberg,G.; Dollinger,H.; Doods,H.N.; Esser,F.; Rudolf,K.; Mihm,G.(Boehringer Ingelheim Pharma KG)
参考来源:DE 19816929

Z-15370A

Chemical Name: 1-(3,5-Dichloropyridin-4-ylmethyl)-6-methoxy-4-(1H-1,2,4-triazol-1-yl)phthalazine
CAS No. 256443-12-6
项目整合开发状态: Preclinical
项目研究机构: Zambon (Originator)
合成路线:Friedel-Crafts h...
参考文献标题:Phthalazine derivs.phosphodiesterase 4 inhibitors
文献作者:Norcini,G.; Morazzoni,G.; Leali,G.M.; Napoletano,M.; Grancini,G.; Pellacini,F.(Zambon Group SpA)
参考来源:EP 1097142; US 6329370; WO 0005218

新产品编号:712409

Chemical Name: N-[trans-4-(cis-7-Hydroxy-3a,4,5,9b-tetrahydro-1H-benzo[e]indol-2-ylaminomethyl)cyclohexylmethyl]benzenesulfonamide
CAS No. 263843-88-5 (mono HCl salt)
项目整合开发状态: Biological Testin...
参考文献标题:3a,4,5,9b-Tetrahydro-1H-benz[e]indol-2-yl amine-derived neuropeptide Y receptor ligands useful in the treatment of obesity and other disorders
文献作者:Dax,S.; McNally,J.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:WO 0068197

新产品编号:713991

Chemical Name: N-[3-(1,2,3,4-Tetrahydroquinolin-1-ylsulfonyl)phenyl]-N,N-bis(1H-imidazol-5-ylmethyl)amine; 1-[3-[Bis(1H-imidazol-5-ylmethyl)amino]phenylsulfonyl]-1,2,3,4-tetrahydroquinoline
CAS No....
参考文献标题:3-Imidazolylmethylaminophenylsulfonyltetrahydroquinolines,a novel series of farnesyltransferase inhibitors
文献作者:Ding,C.Z.; Hunt,J.T.; Ricca,C.; Manne,V.
参考来源:Bioorg Med Chem Lett 2000,10(3),273

新产品编号:430813

Chemical Name: (2,3,5,6,8,9,11,12-Octahydro-1,4,7,10,13-benzopentaoxacyclopentadecin-15-ylcarbonyloxy)(triphenyl)stannane; Triphenyltin 4-carboxybenzo-15-crown-5
CAS No. 215233-49-1
项目整合开发状态: Bi...
参考文献标题:Tin polyoxaalkanecarboxylates and compsns.containing them
文献作者:De Vos,D.; Kemmer,M.; Biesemans,M.; Willem,R.; Gielen,M.(Pharmachemie BV)
参考来源:WO 0006583