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-054264

Chemical Name: N-(Spiro[indene-1,4'-piperidin]-1'-ylcarbonyl)-D-tryptophan 3(S)-(aminomethyl)-1(R)-cyclohexylmethylamide; N-[2-[3(S)-(Aminomethyl)-1(R)-cyclohexylmethylamino]-1(R)-(1H-indol-3-ylmethyl...
参考文献标题:Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists
文献作者:Yang,L.; Guo,L..; Pasternak,A.; Mosley,R.; Rohrer,S.; Birzin,E.; Foor,F.; Cheng,K.; Schaeffer,J.; Patchett,A.A.
参考来源:J Med Chem 1998,41(13),2175

NSL-96184

Chemical Name: 1-[3-[2-Fluoro-4-(thiazolidin-3-ylcarboimidoyl)benzamido]-2,2-dimethylpentanoyl]piperidine-4-acetic acid ethyl ester
CAS No. 200490-65-9
项目整合开发状态: Preclinical
项目研究机构: Nippon St...
参考文献标题:Fibrinogen receptor antagonists and medicinal preparations containing the same as the active ingredient
文献作者:Hayashi,Y.; Harada,T.; Tachiki,A.; Katada,J.(Nippon Steel Corp.)
参考来源:EP 0852225; JP 1998017550; WO 9749682

新产品编号:396009

Chemical Name: N-(3,5-Diethyl-2-fluorobenzyl)-2-methyl-7H-pyrrolo[2,3-d]pyrimidine-4-amine
CAS No. 210414-79-2
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Aniline (I) w...
参考文献标题:Anxiolytic activity of analogues of 4-benzylamino-2-methyl-7H-pyrrolo[2,3-d]pyrimidines
文献作者:Meade,E.A.; et al.
参考来源:Eur J Med Chem 1998,33(5),363

DA-3934

Chemical Name: 2-[3-[3-[N-[2-(N-Methyl-N-phenylcarbamoylmethoxy)phenyl]-N-(N-methyl-N-phenylcarbamoylmethyl)carbamoylmethyl]ureido]phenyl]acetic acid
CAS No. 183176-50-3
项目整合开发状态: Preclinical 参考文献标题:Aminophenol derivs.
文献作者:Yokohama,S.; Kawagoe,K.; Takeda,Y.; Yokomizo,Y.; Yokomizo,A.(Daiichi Pharmaceutical Co.,Ltd.)
参考来源:EP 0985660; US 5919824; WO 9628416

新产品编号:414993

Chemical Name: 3-[4-(N2-Aminoamidino)phenyl]-N-cyclopentyl-N-methyl-2(S)-(6,7,8,9-tetrahydrobenzocyclohepten-2-ylsulfonamido)propionamide
CAS No. 213179-38-5
项目整合开发状态: Preclinical
项目研究机构: LG ...
参考文献标题:Structural modification of an orally active thrombin inhibitor,LB30057: Replacement of the D-pocket-binding napththyl moiety
文献作者:Lee,K.; Hwang,S.Y.; Hong,S.S.; Hong,C.Y.; Lee,C.S.; Shin,Y.; Kim,S.; Yun,M.; Yoo,Y.J.; Kang,M.; Oh,Y.S.
参考来源:Bioorg Med Chem 1998,6(6),869

L-784512

Chemical Name: 3-(3,4-Difluorophenoxy)-5(R)-methyl-4-[4-(methylsulfonyl)phenyl]-5-(2,2,2-trifluoroethyl)furan-2(5H)-one
CAS No. 189955-09-7, 189955-44-0 (undefined isomer)
项目整合开发状态: Preclinical<...
参考文献标题:(Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
文献作者:Belley,M.; Gauthier,J.Y.; Grimm,E.; Leblanc,Y.; Li,C.-S.; Therien,M.; Lau,C.-K.; Prasit,P.; Roy,P.(Merck Frosst Canada Inc.)
参考来源:EP 0863891; JP 1999500146; US 5981576; WO 9714691

YJA-20379-5

Chemical Name: 4,5-Dihydropyrido[1,2-a][1,3]thiazolo[5,4-g]benzimidazol-2-amine
CAS No. 187680-75-7
项目整合开发状态: Preclinical
项目研究机构: Yung-Jin (Originator)
合成路线:1,3-Cyclohexanedione (I) was br...
参考文献标题:Heterocycle-fused thiazole derivs.
文献作者:Yoo,H.Y.; Chung,K.J.; Chai,J.P.; Chang,M.S.; Kim,S.G.; Choi,W.S.; Kim,Y.H.; Chun,J.K.; Chung,Y.K.; Paek,J.H.; Seo,K.H.; Kang,D.P.(Yung-Jin Pharmaceutical Co.,Ltd.)
参考来源:EP 0843681; JP 1998508877; WO 9703076

新产品编号:66953

Chemical Name: (S)-(+)-4-[1-(4-tert-Butylphenyl)-2-oxo-4-pyrrolidinylmethoxy]benzoic acid
CAS No. 155730-91-9 ((R)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Taiho (Originator)
合成路线:Michael add...
参考文献标题:Optically active 1-phenylpyrrolidine derivative,intermediate for producing the same,and process for producing both
文献作者:Yano,S.; Ogawa,K.; Shirasaka,T.; Ohno,T.(Taiho Pharmaceutical Co.,Ltd.)
参考来源:WO 9406767

SU-4984

Chemical Name: (E)-4-[4-(2-Oxoindolin-3-ylidenemethyl)phenyl]piperazine-1-carbaldehyde
CAS No. 186610-89-9
项目整合开发状态: Biological Testing
项目研究机构: Sugen (Originator)
合成路线:Vilsmeier reaction b...
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

新产品编号:402337

Chemical Name: L-Tyrosine N-[6(S)-benzyl-1-methyl-5,8,11-trioxo-1,2,7,10-tetraazacyclotridecan-12(R)-yl]amide
CAS No. 210886-12-7
项目整合开发状态: Preclinical
项目研究机构: Adolor (Originator), University...
参考文献标题:Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): A new route to cyclic peptides and peptidomimetics
文献作者:Shreder,K.; Zhang,L.; Dang,T.; Yaksh,T.L.; Umeno,H.; DeHaven,R.; Daubert,J.; Goodman,M.
参考来源:J Med Chem 1998,41(14),2631