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

EGIS-9377

Chemical Name: 2-(Methylsulfanyl)-N-[2-(4-morpholinyl)ethyl]-8,9-dihydro-7H-thiopyrano[3,2-d][1,2,4]triazolo[1,5-a]pyrimidin-5-amine dihydrochloride
CAS No. 144430-52-4 (free base)
项目整合开发状态: Pre...
参考文献标题:1,2,4-Triazolo[1,5-a]pyrimidine derivs.
文献作者:Reiter,J.; Berecz,G.; Zsila,G.; Petocz,L.; Gigler,G.; Fekete,M.; Sz隿sey,M.; Szirt,E.; Roh醕s,L.; Gg閚yl,F.; Csg? M.(Egis Pharmaceuticals Ltd.)
参考来源:EP 0500136; GB 2254611; JP 1993148267

Lys-Spm, ORI-1202

Chemical Name: L-Lysine N-[3-[4-(3-aminopropylamino)butylamino]propyl]amide
CAS No. 134951-06-7
项目整合开发状态: Preclinical
项目研究机构: MediQuest Therapeutics (Originator)
合成路线:Di-Boc-protected L-ly...
参考文献标题:Novel polyamine analogues as therapeutic and diagnostic agents
文献作者:Burns,M.R.; O'Day,C.L.; Bergstrom,D.E.; Webb,H.K.; Vermeulin,N.M.J.(Oridigm Corp.)
参考来源:EP 1085011

CKD-731

Chemical Name: 3-(3,4,5-Trimethoxyphenyl)-2(E)-propenoic acid (3R,4S,5S,6R)-4-[2(R)-methyl-3(R)-(3-methyl-2-butenyl)oxiran-2-yl]-5-methoxy-1-oxaspiro[2.5]oct-6-yl ester; 6-O-[3-(3,4,5-Trimethoxyphenyl...
参考文献标题:Fumagillol derivs.and processes for preparing the same
文献作者:Chun,H.S.; Choi,N.S.; Lee,S.J.; Han,C.K.; Hong,C.I.; Hong,R.K.; Kim,J.W.; Moon,S.K.; Ahn,S.K.(Chong Kun Dang Corp.)
参考来源:US 6063812; WO 9959986

Edaglitazone, BM-13.1258

Chemical Name: 5-[4-[2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy]benzothien-7-ylmethyl]thiazolidine-2,4-dione
CAS No. 213411-83-7
项目整合开发状态: Biological Testing
项目研究机构: Roche (Originator)
合成路线:An...
参考文献标题:Improved method for producing thiazolidinediones,and new thiazolidinediones
文献作者:K黨nle,H.-F.; Witte,E.-C.; Wolff,H.-P.(Roche Diagnostics GmbH)
参考来源:DE 19711616; EP 0970077; WO 9842704

Quinoxapeptin C

Chemical Name: Bis[N-(6-methoxyquinoxalin-2-ylcarbonyl)-D-seryl-[2,3,4,5-tetrahydro-4(S)-hydroxypyridazin-3(S)-ylcarbonyl]glycyl-N-methylglycyl-3-hydroxy-N-methyl-L-valine]-(5--1'),(5'--1)-dilactone 参考文献标题:Total synthesis and comparative evaluation of luzopeptin A - C and quinoxapeptin A - C
文献作者:Ledeboer,M.W.; Jin,Q.; Kume,M.; Searcey,M.; Boger,D.L.
参考来源:J Am Chem Soc 1999,121(49),11375

MCL-101

Chemical Name: (-)-N-(Cyclobutylmethyl)morphinan-3-ol (S)-mandelate
CAS No. 4163-26-2 (free base), 53448-67-2 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: Harvard Medical School (Originator)...
参考文献标题:N-Cyclopropylmethyl- and -cyclobutylmethyl-morphinans
文献作者:Gates,M.D.Jr.
参考来源:US 3285922

新产品编号:664949

Chemical Name: N1-[2-(Adenin-9-yl)ethyl]-N1'-[3-(6-chloro-2-methoxyacridin-9-ylamino)propyl]propane-1,3-diguanidine
CAS No. 252899-51-7
项目整合开发状态: Preclinical
项目研究机构: INSERM (Originator)
合成...
参考文献标题:Abasic site recognition in DNA as a new strategy to potentiate the action of anticancer alkylating drugs?
文献作者:Belmont,P.; Jourdan,M.; Demeunynck,M.; Constant,J.F.; Garcia,J.; Lhomme,J.; Carez,D.; Croisy,A.
参考来源:J Med Chem 1999,42(25),5153

E-4030, ER-40133

Chemical Name: (3R,6S,9R,9aR)-6-[2(S)-(Acetylsulfanyl)-3(S)-methylpentanamido]-9-methyl-5-oxooctahydrothiazolo[3,2-a]azepine-3-carboxylic acid
CAS No. 177566-02-8
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Substd.thiazolo[3,2-alpha]azepine deriv.
文献作者:Oinuma,H.; Suda,S.; Yoneda,N.; Kotake,M.; Mizuno,M.; Matsuhima,T.; Fukuda,Y.; Saito,M.; Matsuoka,T.; Adachi,H.; Namiki,M.; Sudo,T.; Miyake,K.; Okita,M.(Eisai Co.,Ltd.)
参考来源:EP 0719779; JP 1996027156; JP 1996059672; JP 1996165293; US 5789403; WO 9602549

BOM-1006

Chemical Name: 2,3,6-Trimethyl-4-[2-[2-[2-(4-methyl-1,4-perhydrodiazepin-1-yl)-1H-benzimidazol-1-yl]ethoxy]ethoxy]phenol difumarate
CAS No. 256366-95-7, 256366-84-4 (free base)
项目整合开发状态: Preclin...
参考文献标题:Synthesis of benzimidazole derivatives as antiallergic agents with 5-lipoxygenase inhibiting action
文献作者:Nakano,H.; Inoue,T.; Kawasaki,N.; Miyataka,H.; Matsumoto,H.; Taguchi,T.; Inagaki,N.; Nagai,H.; Satoh,T.
参考来源:Chem Pharm Bull 1999,47(11),1573

新产品编号:21075

Chemical Name: 7-[2(R)-Methyl-4(R)-[4-(phenyl)thiosemicarbazonomethyl]-1,3-dioxan-5(S)-yl]-5(Z)-heptenoic acid sodium salt
CAS No. 119216-66-9, 119216-65-8 (free acid)
项目整合开发状态: Preclinical
项...
参考文献标题:Oxygen-containing heterocyclic cpd.,processes for their preparation and pharmaceutical compsns.comprising them
文献作者:Setoi,H.; Kuroda,A.; Tanaka,H.; Hirai,H.; Marusawa,H.; Hashimoto,M.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0346511