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

BIA-2-059

(R)-利卡西平乙酸酯Chemical Name: Acetic acid 5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10(R)-yl ester
CAS No. 186694-45-1, 186694-11-1 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Bial (Or...
参考文献标题:Substd.dihydrodibenzo[b,f]azepines,method of their preparation,their use in the treatment of some central nervous system disorders,and pharmaceutical compsns.containing them
文献作者:Benes,J.; Vieira Araujo Soares da Silva,P.M.(Portela & Ca.,SA)
参考来源:EP 0751129; US 5753646

(R)-Flurbiprofen, MPC-7869, E-7869, Flurizan

(R)-氟比洛芬(Tarenflurbil)Chemical Name: 2(R)-(2-Fluorobiphenyl-4-yl)propionic acid
CAS No. 51543-40-9
项目整合开发状态: Phase II/III
项目研究机构: Encore (Originator), Loma Linda University (Originator), Myri...
参考文献标题:Process for preparing substantially pure enantiomers of phenylpropionic acids
文献作者:Coe,P.F.; Hardy,R.; Hirst,A.; O'Donnell,H.O.(The Boots Company plc)
参考来源:WO 9412460

L-659699, F-244, Antibiotic 1233A, 1233A

(R,R)-半乳糖苷Chemical Name: 12-Hydroxy-13-hydroxymethyl-3,5,7-trimethyltetradeca-2,4-dien-1,14-dioic acid 12,14-lactone; 11-[3(R)-(Hydroxymethyl-4-oxooxetan-2(R)-yl]-3,5,7(R)-trimethyl-2(E),4(E)-undecadi...
参考文献标题:Total synthesis of the cholesterol biosynthesis inhibitor 1233A via a (Pi-allyl)tricarbonyliron lactone complex
文献作者:Bates,R.W.; et al.
参考来源:J Chem Soc - Perkins Trans I 1999,(14),1917

Sulpiride [L-(-)], Levosulpiride, RV-12309, Levopraid

(S)-(-)-舒必利Chemical Name: (S)-5-(Aminosulfonyl)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxybenzamide
CAS No. 23672-07-3, 77111-58-1 (HCl)
项目整合开发状态: Launched-1987
项目研究机构: Abbott (Originator),...
参考文献标题:Levosulpiride
文献作者:Forgione,A.
参考来源:Drugs Fut 1987,12(10),944

Esatenolol, (S)-Atenolol, TN-891

(S)-(-)-阿替洛尔Chemical Name: (S)-2-[4-[2-Hydroxy-3-(isopropylamino)propoxy]phenyl]acetamide
CAS No. 93379-54-5
项目整合开发状态: Phase III
项目研究机构: Taiyo (Originator)
合成路线:Condensation of acetamide (...
参考文献标题:Process for producing optically active atenolol and intermediate thereof
文献作者:Saragai,N.; Takehira,Y.; Kitaori,K.(Daiso Co.,Ltd.)
参考来源:EP 0435068

Dolastatin 10, NSC-376128, DLS-10

(S)-2-((S)-2-(二甲基氨基)-3-甲基丁酰氨基)-N-((3R,4S,5S)-3-甲氧基-1-((s)-2-((1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(((S)-2-苯基-1-(噻唑-2-基)乙基)氨基)丙基)吡咯烷-1-基)-5-甲基-1-氧代庚烷-4-基)-N,3-二甲基丁酰胺Chemical Name: N,N-Dimethylvalyl-N-[2(R)-methox...
参考文献标题:Synthesis of dolastatin 10
文献作者:Pettit,G.R.; Singh,S.B.(Arizona State University)
参考来源:US 4978744

SB-683698, TR-14035

(S)-2-(2,6-二氯苯酰胺)-3-(2,6-二甲氧基-[1,1-联苯]-4-基)丙酸Chemical Name: 2(S)-(2,6-Dichlorobenzamido)-3-(2',6'-dimethoxybiphenyl-4-yl)propionic acid; N-(2,6-Dichlorobenzoyl)-3-(2',6'-dimethoxybiphenyl-4-yl)-L-alan...
参考文献标题:Inhibitors of alpha4 mediated cell adhesion
文献作者:Gudmundsson,K.S.; Sircar,I.; Martin,R.(Tanabe Seiyaku Co.,Ltd.)
参考来源:WO 9936393

GS-7904, OSI-7904, GW-1843U89, GW-1843, BW-1843U89, 1843U89

(S)-2-(5-((3-甲基-1-氧基-1,2-二氢苯并喹啷-9-基)甲基)氨基)-1-氧异吹哆啰-2-基)戊二酸Chemical Name: 2(S)-[5-[3-Methyl-1-oxo-1,2-dihydrobenzo[f]quinazolin-9-ylmethylamino]-1-oxo-2,3-dihydro-1H-isoindol-2-yl]pentanedioic acid
...
参考文献标题:Pharmaceutically active benzoquinazoline cpds.
文献作者:Pendergast,W.; Dickerson,S.H.; Johnson,J.V.; Ferone,R.(GlaxoSmithKline plc)
参考来源:EP 0535034; EP 1199307; JP 1993507704; US 5405851; US 5663337; US 6306865; WO 9119700

Tanomastat, BAY-12-9566

(S)-4-(4’-氯联苯-4-基)-4-氧代-2-(苯硫基甲基)丁酸Chemical Name: 4-(4'-Chlorobiphenyl-4-yl)-4-oxo-2(S)-(phenylsulfanylmethyl)butyric acid
CAS No. 179545-77-8, 215258-80-3 (error), 179545-78-9 (R-isomer), 179545-7...
参考文献标题:Substd.4-biarylbutyric or 5-biarylpentanoic acids and derivs.as matrix metalloprotease inhibitors
文献作者:Kluender,H.C.E.; Benz,G.H.H.H.; Brittelli,D.R.; Bullock,W.H.; Combs,K.J.; Dixon,B.R.; Schneider,S.; Wood,J.E.; Vanzandt,M.C.; Wolanin,D.J.; Wilhelm,S.M.(Bayer AG)
参考来源:EP 0790974; JP 1998509146; US 5789434; US 5859047; WO 9615096

CTC-8

(S)-4-叔丁基二甲基硅氧基-2-环戊酮Chemical Name: (-)-4(S)-[tert-Butyl(dimethyl)silyloxy]-2-cyclopenten-1-one
CAS No. 61305-36-0
项目整合开发状态: Biological Testing
项目研究机构: Charterhouse Therapeutics (Originator)<...
参考文献标题:Highly enantioselective synthesis of (+) and (-)endo- tricyclo [5.2.1.02,6]deca-4,8-dien-3-one and (-)-4-t-butyldimethylsilyloxy-cyclopentenone by enzyme-catalyzed acetylation
文献作者:Liu,Z.-Y.; He,L.; Zheng,H.
参考来源:Tetrahedron Asymmetry 1993,4(11),2277