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

L-796449

Chemical Name: 2-[3-Chloro-4-[3-(3-phenyl-7-propyl-1-benzofuran-6-yloxy)propylsulfanyl]phenyl]acetic acid
CAS No. 194608-80-5
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:Co...
参考文献标题:Antidiabetic agents
文献作者:Adams,A.L.; Berger,G.D.; Bergman,J.P.; Berger,J.P.; Han,W.; Leibowitz,M.D.; Moller,D.E.; Santini,C.; Sahoo,S.; Tolman,R.L.; Young,J.R.(Merck & Co.,Inc.)
参考来源:EP 0904079; JP 2002515865; US 5859051; WO 9727857

DK-507K

Chemical Name: 7-[7(S)-Amino-5-azaspiro[2.4]hept-5-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate
CAS No. 364069-13-6, 364...
参考文献标题:Quinolonecarboxylic acid deriv.
文献作者:Suzuki,T.; Takahashi,H.; Hayakawa,I.; Takemura,M.; Ohtani,T.; Kawakami,K.; Itoh,M.; Miyauchi,R.; Sekiguchi,M.(Daiichi Pharmaceutical Co.,Ltd.)
参考来源:WO 0172738

新产品编号:620653

Chemical Name: 5-Allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-benzopyrano[3,4-f]quinoline
CAS No. 239066-73-0, 239067-07-3 (R-isomer), 239067-08-4 (S-isomer)
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Glucocorticoid-selective anti-inflammatory agents
文献作者:Wang,A.X.; Kym,P.R.; Jones,T.K.; Kort,M.E.; Edwards,J.P.; Moore,J.L.; Elmore,S.W.; Coughlan,M.J.; Pratt,J.K.(Abbott Laboratories Inc.; Ligand Pharmaceuticals,Inc.)
参考来源:EP 1053239; WO 9941256

新产品编号:782017

Chemical Name: 1-[3-[2,3-Dichloro-4-(1-methyl-1H-indol-5-ylsulfanyl)phenyl]-2(E)-propenoyl]piperidine-4-carboxylic acid sodium salt
CAS No. 301178-64-3, 280752-02-5 (free base), 280753-09-5 (Li sal...
参考文献标题:Cell adhesion-inhibiting antiinflammatory and immune-suppressive cpds.
文献作者:Lynch,J.K.; Link,J.; Zhu,G.-D.; Boyd,S.A.; Winn,M.; Pei,Z.; Gunawardana,I.W.; Liu,G.; Xin,Z.; Jae,H.-S.; Freeman,J.C.; Von Geldern,T.; Staeger,M.A.(Abbott Laboratories Inc.)
参考来源:US 6110922; WO 0039081

SU-5614

Chemical Name: (Z)-5-Chloro-3-(3,5-dimethyl-1H-pyrrol-2-ylmethylene)-2,3-dihydro-1H-indol-2-one
CAS No. 186611-56-3
项目整合开发状态: Preclinical
项目研究机构: Sugen (Originator)
合成路线:Vilsmeier reaction...
参考文献标题:Indolinone cpds.for the treatment of disease
文献作者:Tang,P.C.; Sun,L.; McMahon,G.(Sugen,Inc.)
参考来源:EP 0769947; JP 2000026412; US 5780496; US 5792783; US 5880141; US 5883113; US 5883116; WO 9640116

GW-587270

Chemical Name: [1R-(1alpha,3abeta,4alpha,4abeta,7beta,7aalpha,8abeta)]-8a-[4-[2-(Fluoromethyl)-2-propenyl]-6(R)-methylmorpholin-2(R)-yloxymethyl]-4-formyl-3-isopropyl-7-methyl-1,3a,4,4a,5,6,7,7a,8,8a-...
参考文献标题:Morpholino ethers
文献作者:Bueno,J.M.; Chicharro Gonzalo,J.; Coteron,J.-M.; Cuevas,J.C.; Fiandor,J.M.; Mallo,A.(GlaxoSmithKline SA)
参考来源:EP 1077959; JP 2002514632; WO 9958512

RO-098246

Chemical Name: 2(R)-(2,4-Fluorophenyl)-3(R)-[3-[4-(1,2,3-thiadiazol-4-yl)phenyl]-1,2,4-thiadiazol-5-yl]-1-(1H-1,2,4-triazol-1-yl)butan-2-ol
CAS No. 368421-38-9
项目整合开发状态: Biological Testing
项目...
参考文献标题:Azole derivs.
文献作者:Shimma,N.; Tsukuda,T.; Komiyama,S.(Basilea Pharmaceutica AG)
参考来源:US 6319933; WO 0179196

DW-286a, DW-286

Chemical Name: 7-[3(R)-(Aminomethyl)-4(Z)-(methoxyimino)-3-methylpyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid hydrochloride
CAS No. 309762-48-9 ((-)...
参考文献标题:Optically active quinoline carboxylic acid derivs.having 7-pyrrolidine substitutes causing optical activity and a process for preparing thereof
文献作者:Yoon,S.J.; Chung,Y.H.; Lee,C.W.; Choi,D.R.; Lee,J.S.; Yang,W.Y.; Kim,N.D.; Jin,Y.H.; Song,W.J.; Kim,I.H.; Shin,J.H.(Dong-Wha Pharmaceuticals Industry Co.Ltd)
参考来源:WO 0071541

GI-448

Chemical Name: 4''-O-Acetylerythromycin A 9-[O-(3-cyclohexylpropyl)oxime]
CAS No. 301197-85-3
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The title erythromycin O-(phenoxypropyl...
参考文献标题:Erythromycin derivs.
文献作者:Yoshida,T.; Narita,K.; Kato,H.; Kado,N.; Nishimoto,A.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:EP 1167375; JP 2000351794; WO 0061593

A-217213

Chemical Name: 11-Amino-11-deoxy-3-des(hexopyranosyloxy)-3-oxo-6-O-[3-(3-quinolinyl)-2-propynyl]erythromycin A 11-N,12-O-cyclic carbamate
CAS No. 205111-68-8
项目整合开发状态: Preclinical
项目研究机构: Abb...
参考文献标题:6-O-Substd.ketolides having antibacterial activity
文献作者:Or,Y.S.; Ma,Z.; Clark,R.F.; Chu,D.T.; Plattner,J.J.(Abbott Laboratories Inc.)
参考来源:EP 0929563; US 5866549; WO 9809978