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

Cangrelor sodium, AR-C69931MX

坎格雷洛Chemical Name: 5'-O-[[[Dichloro(phosphono)methyl](hydroxy)phosphoryloxy](hydroxy)phosphoryl]-N-[2-(methylsulfanyl)ethyl]-2-(3,3,3-trifluoropropylsulfanyl)adenosine tetrasodium salt
CAS No. 1637...
参考文献标题:N-Alkyl-2-substd.ATP analogues
文献作者:Ingall,A.H.; Cage,P.A.; Kindon,N.D.(Celltech Medeva plc)
参考来源:EP 0683789; JP 1996506335; US 5721219; WO 9418216

Candoxatril, UK-79300

坎沙曲坎沙曲 Chemical Name: (alphaS)-1-[(cis-4-Carboxycyclohexyl)carbamoyl]-alpha-[(2-methoxyethoxy)methyl]cyclopentanepropionic acid,alpha-5-indanyl ester; cis-4-[1-[(S)-2-(Indan-5-yloxycarbonyl)-3-(2-met...
参考文献标题:Enantiomeric glutaramide diuretic agents
文献作者:Williams,M.T.; Danilewicz,J.C.(Pfizer Inc.)
参考来源:EP 0342850

Tandutinib, MLN-518, CT-53518(former code name)

坦度替尼Chemical Name: N-(4-Isopropoxyphenyl)-4-[6-methoxy-7-[3-(1-piperidinyl)propoxy]quinazolin-4-yl]piperazine-1-carboxamide
CAS No. 387867-13-2, 387867-14-3 (sulfate)
项目整合开发状态: Phase I
项目研究机构...
参考文献标题:Quinazoline derivs.as kinase inhibitors
文献作者:Nomoto,Y.; Scarborough,R.M.; Ichimura,M.; Fujiwara,S.; Ide,S.; Oda,S.; Pandey,A.; Tsukuda,E.; Matsuno,K.; Irie,J.(Kyowa Hakko Kogyo Co.,Ltd.; Millennium Pharmaceuticals,Inc.)
参考来源:WO 0216351

NSC-704057, KOS-953, 17-AAG, CP-127374, NSC-330507D, NSC-330507

坦螺旋霉素Chemical Name: (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(Allylamino)-9-(carbamoyloxy)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaene-3,20,22-trio...
参考文献标题:Geldanamycin derivs.and antitumor drug
文献作者:Inoue,Y.; Sasaki,K.(Kaken Pharmaceutical Co.,Ltd.)
参考来源:US 4261989

(-)-Desoxyepothilone B, Epothilone D, Desoxyepothilone B, R-1492, KOS-862, dEpoB, NSC-703147

埃博霉素Chemical Name: (4S,7R,8S,9S,13Z,16S)-4,8-Dihydroxy-5,5,7,9,13-pentamethyl-16-[(E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-1-oxacyclohexadec-13-ene-2,6-dione
CAS No. 189453-10-9
项目整合开发状态: P...
参考文献标题:A process for the reduction of oxiranyl epothilones to olefinic epothilones
文献作者:Johnson,J.A.; Kim,S.-H.(Bristol-Myers Squibb Co.)
参考来源:WO 0071521

(-)-Desoxyepothilone A, Desoxyepothilone A, Epothilone C, dEpoA

埃博霉素 CChemical Name: (4S,7R,8S,9S,13Z,16S)-4,8-Dihydroxy-5,5,7,9-tetramethyl-16-[(E)-1-methyl-2-(methylthiazol-4-yl)vinyl]-1-oxacyclohexadec-13-ene-2,6-dione
CAS No. 186692-73-9
项目整合开发状态: Biolog...
参考文献标题:A process for the reduction of oxiranyl epothilones to olefinic epothilones
文献作者:Johnson,J.A.; Kim,S.-H.(Bristol-Myers Squibb Co.)
参考来源:WO 0071521

(-)-Epothilone E, Epothilone E

埃博霉素EChemical Name: [4S,7R,8S,9S,13R,14S,16S(E)]-13,14-Epoxy-4,8-dihydroxy-5,5,7,9-tetramethyl-16-[2-[2-(hydroxymethyl)thiazol-4-yl]-1-methylvinyl]-1-oxacyclohexadecane-2,6-dione; (1S,3S,7S,10R,11S,12...
参考文献标题:Epothilones with a modified side chain
文献作者:Sefkow,M.; H鰂le,G.(Gesellschaft f黵 Biotechnologische Forschung mbH)
参考来源:WO 9838192

Epithalon, Epitalon

埃皮塔隆Chemical Name: L-Alanyl-L-glutamyl-L-aspartyl-glycine
CAS No. 307297-39-8
项目整合开发状态: Phase II
项目研究机构: Russian Academy of Medical Sciences (Originator)
合成路线:The title compound was obtain...
参考文献标题:Tetrapeptide revealing geroprotective effect,pharmacological substance on its basis,and the method of its application
文献作者:Khavinson,V.K.
参考来源:WO 0068255

Pelrinone hydrochloride, AY-28768

培力农培力农 Chemical Name: 1,4-Dihydro-2-methyl-4-oxo-6-[(3-pyridinylmethyl)amino]-5-pyrimidinecarbonitrile monohydrochloride
CAS No. 89232-84-8, 94386-65-9 (free base)
项目整合开发状态: Phase II
项目研究机构...
参考文献标题:Amino-pyrimidine derivs.
文献作者:Bagli,J.F.(American Home Products Corp.)
参考来源:EP 0130735; ES 8602694; JP 1985025974; US 4505910

Perindopril, DW-7950(as erbumine), SED-9490(as erbumine), McN-A-2833, S-9490, Coverene Cor, Coverex, Aceon, Coversum, Coversyl

培哚普利Chemical Name: 1-[(2S)-2-[(1S)-1-Carbethoxybutylamino]-1-oxopropyl]-(2S,3aS,7aS)-perhydroindol-2-carboxylic acid
CAS No. 82834-16-0
项目整合开发状态: Launched-1988
项目研究机构: Servier (Originator), D...
参考文献标题:Asymmetric synthesis of pregabalin
文献作者:Mich,T.F.; Goel,O.P.; Mulhern,T.A.; Burk,M.J.; Hoekstra,M.S.; Ramsden,J.A.(Pfizer Inc.)
参考来源:WO 0155090