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

Sch-37370

N-乙酰基地氯雷他定Chemical Name: 11-(1-Acetyl-4-piperidylidene)-8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridine
CAS No. 117796-52-8
项目整合开发状态: Phase II
项目研究机构: Schering-Plough (Originator...
参考文献标题:Dual antagonists of platelet activating factor and histamine.Identification of structural requirements for dual activity of N-acyl-4-(5,6-dihydro-11H-benzo[5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines
文献作者:Piwinski,J.J.; Wong,J.K.; Green,M.J.; Ganguly,A.K.; Billah,M.M.; West,R.E.Jr.; Kreutner,W.
参考来源:J Med Chem 1991,34(1),457

N-Acetylprocainamide hydrochloride, Acecainide hydrochloride, ASL-601, NAPA, NAPA

N-乙酰普鲁卡因胺盐酸盐乙酰普卡胺 Chemical Name: 4-Acetamido-N-[2-(diethylamino)ethyl]benzamide hydrochloride; N-[4-[N-[2-(Diethylamino)ethyl]carbamoyl]phenyl]acetamide hydrochloride
CAS No. 34118-92-8, 32795-44...
参考文献标题:p-Acetamido-N-2-diethylaminoethylbenzamide and its salts
文献作者:Schreiber,E.C.(Bristol-Myers Squibb Co.)
参考来源:CA 977366; CH 520107; DE 2062978; FR 2081421; GB 1319980

beta-Alethine, Beta LT, Betathine

N-巯基乙基-3-氨基丙酰胺二硫化物Chemical Name: N,N'-(Dithio-di-2,1-ethanediyl)bis[3-aminopropionamide]
CAS No. 646-08-2
项目整合开发状态: Phase I/II
项目研究机构: Dovetail (Orphan Drug), University of New Mexico (Origin...
参考文献标题:Novel disulfides and thiol cpds.
文献作者:Lednicer,D.; Murray,C.K.; Daughenbaugh,R.J.; Taub,F.E.(Dovetail Technologies Inc.)
参考来源:JP 2002503700; US 2001008933; US 6414114; WO 9942097; WO 9942116

PNU-83757, U-83757, P-1075

N-氰基-N'-(1,1-二甲基丙基)-N''-3-吡啶基胍Chemical Name: 1-Cyano-2-(1,1-dimethylpropyl)-3-(3-pyridyl)guanidine
CAS No. 60559-98-0
项目整合开发状态: Phase II
项目研究机构: Leo (Originator), Pfizer (Not Determined)
合...
参考文献标题:Antihypertensive pyridylguanidine compounds
文献作者:Petersen,H.J.(Leo Pharmaceutical Products Ltd.A/S)
参考来源:DE 2557438; FR 2294703; GB 1489879; JP 51086474; US 4057636

KRN-2391

N-氰基-N'-(2-硝氧乙基)-3-吡啶甲脒甲烷磺酸盐Chemical Name: N-Cyano-N'-(2-nitrooxyethyl)-3-pyridinecarboxamidine monomethanesulfonate; N-Cyano-N'-(2-nitrooxyethyl)nicotiamidine monomethanesulfonate; N-Cyano-N'-(2-nitr...
参考文献标题:KRN2391
文献作者:Ogawa,N.; Izawa,T.
参考来源:Drugs Fut 1994,19(6),546

Etintidine hydrochloride, BL-5641A

N-氰基-N'-[2-[[(5-甲基-1H-咪唑-4-基)甲基]硫代]乙基]-N''-2-丙炔基胍盐酸盐依汀替丁 Chemical Name: 2-Cyano-1-[2-[[(5-methylimidazol-4-yl)methyl]thio]ethyl]-3-(2-propynyl)guanidine hydrochloride; N-Cyano-N'-[2-[(5-methyl-4-imid...
参考文献标题:Imidazolylmethylthioethyl alkynyl guanidines
文献作者:Crenshaw,R.R.; Luke,G.M.(Bristol-Myers Squibb Co.)
参考来源:US 4112234

(-)-SK&F-10047, SK&F-10047

N-烯丙去甲间唑新Chemical Name: (-)-2'-Hydroxy-5,9-dimethyl-2-allyl-6,7-benzomorphan; (-)-(2R,6R,11R)-1,2,3,4,5,6-Hexahydro-6,11-dimethyl-3-(2-propenyl)-2,6-methano-3-benzazocin-8-ol
CAS No. 14198-28-8, 74...
参考文献标题:Novel N-allyl and N-propargyl benzmorphan derivs.
文献作者:Gordon,M.; Lafferty,J.J.(SmithKline Beecham Corp.)
参考来源:US 4048178

(S)-Fluoxetine

N-甲基-3-(4-三氟甲基苯氧基)-3-(苯基)丙胺Chemical Name: (S)-N-Methyl-gamma-[4-(trifluoromethyl)phenoxy]benzenepropanamine; (S)-N-Methyl-3-phenyl-3-[(alpha,alpha,alpha-trifluoro-p-tolyl)oxy]propylamine
CAS No. 10...
参考文献标题:Fluoxetine process from benzoylacetonitrile
文献作者:Jurgens,A.R.; Hilborn,J.W.(Sepracor Inc.)
参考来源:WO 0007976

Efegatran sulfate hydrate, LY-294468, GYKI-14766

N-甲基-D-苯丙氨酸-L-脯氨基-L-精氨酸硫酸盐水合物依非加群Chemical Name: N-Methyl-D-phenylalanyl-L-prolyl-L-arginal sulfate hydrate; N-Methyl-D-phenylalanyl-N-[4-guanidino-1(S)-formylbutyl]-L-prolinamide sulfate hydrate
CA...
参考文献标题:Highly active and selective anticoagulants: D-Phe-Pro-Arg-H,a free tripeptide aldehyde prone to spontaneous inactivation and its stable N-methyl derivative,D-MePhe-Pro-Arg-H
文献作者:Szl,E.; Bagdy,D.; Bajusz,S.; et al.
参考来源:J Med Chem 1990,33(6),1729-35

Milameline hydrochloride, Miramelin, CI-979, RU-35926, PD-129409

N-甲氧基-1-(1-甲基-5,6-二氢-2H-吡啶-3-基)甲烷亚胺盐酸盐米拉美林 Chemical Name: (E)-1-Methyl-1,2,5,6-tetrahydropyridine-3-carboxaldehyde O-methyloxime monohydrochloride
CAS No. 139886-04-7, 139886-32-1 (free base), 114...
参考文献标题:1,2,5,6-Tetrahydropyridine-3-carboxaldehyde oxime derivs.,process for their preparation,their application as medicaments and compsns.containing them
文献作者:Galliani,G.; Barzaghi,F.; Butti,A.; Bonetti,C.; Toja,E.(Aventis Pharma SA)
参考来源:EP 0239445; JP 1987252767; US 5219872