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

BE-6143, BDF-6143

2H-异哌多-2-胺,4-氯钼-(4,5-二氢-1H-吡达唑-2-基)-1,3-二氢,盐酸盐(1:1)Chemical Name: 4-Chloro-2-(2-imidazolin-2-ylamino)isoindoline hydrochloride
CAS No. 76727-72-5
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline...
参考文献标题:Hypotensive 2-heterocycloaminoimidazolines
文献作者:Cohnen,E.(Beiersdorf-Lilly GmbH)
参考来源:DE 2816627; DE 2905501; FR 2423491; GB 2021100; JP 79151990; US 4221798

LY-389795

2-Thia双环[3.1.0]己烷-4,6-二羧酸,4-氨基-, (1R,4S,5S,6S)-rel-Chemical Name: (1R,4R,5S,6R)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
CAS No. 191471-53-1 (stereoisomer)
项目整合开发状态: Preclinical<...
参考文献标题:Excitatory amino acid derivs.
文献作者:Massey,S.M.; Monn,J.A.; Valli,M.J.(Eli Lilly and Company)
参考来源:EP 0774461; JP 2000500748; WO 9718199

新产品编号:188767

2-丁基-N-(3,5-二氯吡啶-4-基)-7-甲氧基-1-苯并呋喃-4-甲酰胺Chemical Name: 2-Butyl-N-(3,5-dichloropyridin-4-yl)-7-methoxy-1-benzofuran-4-carboxamide
CAS No. 185400-42-4
项目整合开发状态: Preclinical
项目研究机构: Aventis Phar...
参考文献标题:Benzofuran based PDE4 inhibitors
文献作者:McGarry,D.G.; Regan,J.R.; Volz,F.A.; Hulme,C.; Moriarty,K.J.; Djuric,S.W.; Souness,J.E.; Miller,B.E.; Travis,J.J.; Sweeney,D.M.
参考来源:Bioorg Med Chem 1999,7(6),1131

AF-2785

2-丙戊酸,3-[1-[(2,4-二氯苯基)甲基]-1H-吲唑-3-基]-Chemical Name: 3-[1-(2,4-Dichlorobenzyl)-1H-indazol-3-yl]-2(E)-propenoic acid
CAS No. 252025-48-2
项目整合开发状态: Preclinical
项目研究机构: Angelini (Originator)
合...
参考文献标题:3-Substd.1-benzyl-1H-indazole derivs.as antifertility agents
文献作者:Cheng,C.Y.; Silvestrini,B.(Angelini Pharmaceuticals Inc.)
参考来源:US 6001865

Bornaprolol hydrochloride, FM-24

2-丙醇,1-(2-双环[2.2.1]庚-2-yl苯氧基)-3-[(1-甲基乙基)氨基]-,盐酸盐(1:1) 波那洛尔 Chemical Name: (?-1-(2-exo-Byciclo[2.2.1]hept-2-ylphenoxy)-3-[(1-methylethylamino]-2-propanol hydrochloride; (?-1-(Isopropylamino)-3-(o-2-ex...
参考文献标题:Bornaprolol hydrochloride
文献作者:Michaud,R.
参考来源:Drugs Fut 1982,7(2),91

91-454

2-丙醇酸,2-氰基-3-(3-甲氧基苯基)-,乙基酯Chemical Name: 2-Cyano-3-(3-methoxyphenyl)-2(Z)-propenoic acid ethyl ester
CAS No. 19098-69-2 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Central Drug Research...
参考文献标题:Synthesis and antileishmanial activity of alpha-cyano ethyl propenoates - A new class of antileishmanials
文献作者:Tiwari,S.; et al.
参考来源:Arzneim-Forsch Drug Res 1999,49(2),144

ZD-8731, ICI-D8731

2-乙基-4-((2'-(2H-四唑-5-基)(1,1'-双苯基)-4-基)甲氧基)喹啉盐酸盐Chemical Name: 2-Ethyl-4-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethoxy]quinoline hydrochloride
CAS No. 135015-84-8 (monoHCl)
项目整合开发状态: Phase II
项目研...
参考文献标题:Quinoline derivs.,process for their preparation and their use as medicaments
文献作者:Roberts,D.A.; Russell,S.T.; Pearce,R.J.(AstraZeneca plc)
参考来源:AU 9160955; EP 0412848; GB 2234748; JP 1991169863; US 5444071

Alvameline tartrate, LU-25-109(free base), LU-25-109T

2-乙基-5-(1-甲基-1,2,3,6-四氢吡啶-5-基)-2H-四唑L-(+)-酒石酸盐 2-乙基-5-(1-甲基-1,2,5,6-四氢-吡啶-3-基)-2H-四唑 Chemical Name: 2-Ethyl-5-(1-methyl-1,2,3,6-tetrahydropyridin-5-yl)-2H-tetrazole L-(+)-tartrate; 5-(2-Ethyltetrazol-...
参考文献标题:Bioisosteres of arecoline: 1,2,3,6-Tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles.Synthesis and muscarinic activity
文献作者:Moltzen,E.K.; Pedersen,H.; Bogeso,K.P.; Meier,E.; Frederiksen,K.S.; Sanchez,C.; Love Lembol,H.
参考来源:J Med Chem 1994,37(24),4085-99

Mexidol hydrochloride, Emoxipin Hydrochloride, 3-HP

2-乙基-6-甲基-3-羟基吡啶盐酸盐Chemical Name: 2-Ethyl-6-methyl-3-hydroxypyridine hydrochloride
CAS No. 13258-59-8
项目整合开发状态: Phase III
项目研究机构: All-Russian Chem.-Pharm. Res. Inst. (Originator)
合成路线:By r...
参考文献标题:Retino protector for treating intraocular hemorrhage,myopic,chlorioretinal dystrophies,congenital etinal dystrophies,retinal burns and prevention of injury in lasercoagulation
文献作者:Smirnov,L.D.; Emanuel,N.M.; Katsnelson,L.A.; Shvedova,A.A.; Spirina,L.V.(All-Russian Chemical-Pharmaceutical Research Institute; Inst.Khim.Fiz.Akad.Nauk; Nauchno-Issledovatelsky Institut)
参考来源:DE 3330053; JP 1985061526; US 4486440

Esonarimod, KE-298

2-乙酰基硫代甲基-3-(4-甲基苯甲酰)丙酸Chemical Name: (?-2-(Acetylsulfanylmethyl)-3-(4-methylbenzoyl)propionic acid; (?-2-(Acetylsulfanylmethyl)-4-(4-methylphenyl)-4-oxobutyric acid
CAS No. 101973-77-7
项目整合开发状态...
参考文献标题:Benzoylpropionic acid derivs.,their use and pharmaceutical compsns
文献作者:Tomisawa,K.; Kameo,K.; Matsunaga,T.; Saito,S.; Sota,K.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0164101; ES 8603818; JP 1985258160