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

CB-300638

Chemical Name: 2(R)-[4(S)-Carboxy-4-[4-[N-(2-methyl-4-oxo-4,6,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(2-propynyl)amino]benzamido]butyramido]pentanedioic acid; N1-[4-[N-(2-Methyl-4-oxo-4,6,7...
参考文献标题:Tricyclic cpds.with pharmaceutical activity
文献作者:Boyle,F.; Crook,J.W.; Matusiak,Z.S.(AstraZeneca plc; BTG plc)
参考来源:EP 0667864; GB 2272217; JP 1996505838; US 5789417; WO 9411354

KF-58333

Chemical Name: (1aR,2Z,4E,6E,14R,15aR)-8-Chloro-9,11-dihydroxy-14-methyl-1a,14,15,15a-tetrahydro-6H-oxireno[e][2]benzoxacyclotetradecine-6,12(7H)-dione 6-[O-[2-(2-oxo-1-pyrrolidinyl)ethyl]oxime]; (3R,...
参考文献标题:Radicicol derivs.
文献作者:Ino,Y.; Shiotsu,Y.; Amishiro,N.; Miyata,M.; Murakata,C.; Ogawa,H.; Akiyama,T.; Akinaga,S.; Soga,S.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0889042; US 6239168; US 6316491; WO 9818780

VCP-11177, TH-1177

Chemical Name: 2(S)-[[(4-Chlorophenyl)(phenyl)methoxy]methyl]-1-[2-(4-methoxyphenyl)ethyl]pyrrolidine
CAS No. 266001-66-5
项目整合开发状态: Preclinical
项目研究机构: University of Virginia (Originator)
...
参考文献标题:Inhibition of human prostate cancer proliferation in vitro and in a mouse model by a compound synthesized to block Ca2+ entry
文献作者:Haverstick,D.M.; Heady,T.N.; MacDonald,T.L.; Gray,L.S.
参考来源:Cancer Res 2000,60(4),1002

新产品编号:668113

Chemical Name: Phosphoric acid 2-methoxy-5-(2,3,4,5,6-pentafluorophenylsulfonamido)phenyl mono ester; 2,3,4,5,6-Pentafluoro-N-[4-methoxy-3-(phosphonooxy)phenyl]benzenesulfonamide
CAS No. 253141-29-...
参考文献标题:Pentafluorobenzenesulfonamides and analogs
文献作者:Flygare,J.; Medina,J.; Shan,B.; Clark,D.; Rosen,T.(Tularik Inc.)
参考来源:EP 0939627; WO 9805315

DPC-083

Chemical Name: (E)-6-Chloro-4(S)-(2-cyclopropylvinyl)-4-(trifluoromethyl)-3,4-dihydro-1H-quinazolin-2-one
CAS No. 214287-99-7
项目整合开发状态: Phase II
项目研究机构: Bristol-Myers Squibb (Originator)
合...
参考文献标题:4,4-Disubstd.-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors
文献作者:Corbett,J.W.; Ko,S.S.(DuPont Pharmaceuticals Co.)
参考来源:US 6124302; WO 9845276

OT-7999

Chemical Name: 5-Butyl-8-[4-(trifluoromethyl)phenyl]-1H-[1,2,4]triazolo[5,1-i]purine
CAS No. 246031-23-2
项目整合开发状态: Preclinical
项目研究机构: Otsuka (Originator)
合成路线:The reaction of 4-amino-1H-i...
参考文献标题:Triazolopurine derivs,medicinal compsn.containing the derivs.,adenosine A3 receptor compatibilizing agent,and asthmatic remedy
文献作者:Kurogi,Y.; Nishikawa,H.; Okamura,T.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:EP 1069126; US 6288070; WO 9951606

J-113863

Chemical Name: 1-(1-Cycloocten-1-ylmethyl)-4-(2,7-dichloroxanthen-9-ylcarboxamido)-1-ethylpiperidinium iodide
CAS No. 202796-41-6 (cis-isomer), 202796-42-7 (trans-isomer)
项目整合开发状态: Preclinical 参考文献标题:Chemokine receptor antagonists
文献作者:Naya,A.; Owada,Y.; Saeki,T.; Ohwaki,K.; Iwasawa,Y.(Banyu Pharmaceutical Co.,Ltd.)
参考来源:EP 0916668; WO 9804554

新产品编号:535225

Chemical Name: 2-Ethoxy-3-[4-[2-(4-methyl-1-oxo-1,2-dihydro-2-phthalazinyl)ethoxy]phenyl]propionamide
CAS No. 221321-60-4
项目整合开发状态: Preclinical
项目研究机构: SSP (Originator)
合成路线:Debenzylation ...
参考文献标题:alpha-Substd.phenylpropionic acid deriv.and medicine containing the same
文献作者:Kotake,J.; Nagao,Y.; Konno,F.; Sato,S.; Honda,H.; Ishii,F.(SSP Co.,Ltd.)
参考来源:CA 2247772; EP 0903343; JP 1999158144

新产品编号:647547

Chemical Name: 2-[1-(2-Phenylethyl)piperidin-2-yl]acetic acid methyl ester
CAS No. 247259-34-3
项目整合开发状态: Preclinical
项目研究机构: Georgia Institute of Technology (Originator), Mercer University (O...
参考文献标题:Synthesis and pharmacology of site-specific cocaine abuse treatment agents: The role of the phenyl group in highly modified methylphenidate analogs as dopamine uptake inhibitors
文献作者:Dunn,T.; Deutsch,H.M.; Schweri,M.M.; Ye,X.
参考来源:Med Chem Res 1999,9(4),213

Ganstigmine hydrochloride, CHF-2819

Chemical Name: N-(2-Ethylphenyl)carbamic acid (4aS,9aS)-2,4a,9-trimethyl-2,3,4,4a,9,9a-hexahydro[1,2]oxazino[6,5-b]indol-6-yl ester hydrochloride; N-(2-Ethylphenyl)geneserine hydrochloride
CAS No. ...
参考文献标题:A process for the preparation of aminocarbonyl derivs.of geneseroline having selective brain anticholinesterase activity
文献作者:Ventura,P.; Pighi,R.; Servadio,V.; Pietra,C.; Amari,G.; Salsi,B.; Pivetti,F.; Delcanale,M.; Chiesi,P.; Villetti,G.(Chiesi Farmaceutici SpA)
参考来源:WO 9919329