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

BF-388

Chemical Name: 1-(3,5-Di-tert-butyl-4-hydroxyphenyl)pyrrolidin-2-one
CAS No. 129464-78-4
项目整合开发状态: Preclinical
项目研究机构: Biofor (Originator)
合成路线:The 2,6-di-tert-butylphenol (I) was nitrated...
参考文献标题:BF-388
文献作者:Naismith,R.W.; Frierson,M.R.III,Wong,S.; Lee,S.J.
参考来源:Drugs Fut 1992,17(10),871

BMS-181101

Chemical Name: 1-[3-(5-Fluoro-1H-indol-3-yl)propyl]-4-(5-methoxypyrimidin-4-yl)piperazine; 5-Fluoro-3-[3-[4-(5-methoxypyrimidin-4-yl)piperazin-1-yl]propyl]-1H-indole
CAS No. 141071-67-2
项目整合开发状态...
参考文献标题:Process development of 5-fluoro-3[3-[4-(5-methoxy-4-pyrimidinyl)-1-piperazinyl]propyl]-1H-indole dihydrochloride
文献作者:Anderson,N.G.; et al.
参考来源:Org Process Res Dev 1997,1(4),300

PA-1806, BMS-180680

Chemical Name: (3S,4R)-3-[2-(2-Aminothiazol-4-yl)-2(Z)-(3-carboxy-6,7-dihydroxyquinoxalin-2-ylmethoxyimino)acetamido]-4-methyl-2-oxoazetidine-1-sulfonic acid; (3S,4R)-3-[(Z)-1-(2-Aminothiazol-4-yl)-2-...
参考文献标题:Heteroaroyl derivs.of monocyclic beta-lactam antibiotics
文献作者:Koster,W.H.; Sundeen,J.E.; Straub,H.; Ermann,P.H.; Treuner,U.(Bristol-Myers Squibb Co.)
参考来源:EP 0484881; JP 1992283579

E-1101

Chemical Name: 7-[2-(2-Aminothiazol-4-yl)-2(Z)-(hydroxyimino)acetamido]-3-(N,N-dimethylcarbamoyloxymethyl)-3-cephem-4-carboxylic acid 1-(isopropoxycarbonyloxy)ethyl ester
CAS No. 142494-87-9 ([6R-(...
参考文献标题:7-Acyl-3-(substd.carbamoyloxy)cephem cpds.,use thereof and process for their preparation
文献作者:Negi,S.; Yamanaka,M.; Katsu,K.; Sugiyama,I.; Komatu,Y.; Kamata,A.; Tsuruoka,A.; Machida,Y.(Eisai Co.,Ltd.)
参考来源:EP 0484966; EP 0761671; JP 1992178392; JP 1992282388; JP 1993311173; JP 1993311174; JP 1994092969; JP 1998067784; US 5559225; US 5587473; US 5604217

LU-29-066

Chemical Name: 3-(4-Fluorophenyl)-2,5-dimethyl)-1-[1-[2-(2-oxoimidazolidin-1-yl)ethyl]piperidin-4-yl]-1H-indole
CAS No. 141307-07-5
项目整合开发状态: Biological Testing
项目研究机构: Lundbeck (Originator)<...
参考文献标题:Synthesis of [11C]LU 29-066,a 5-HT2 receptor antagonist
文献作者:Amokhtari,M.; et al.
参考来源:J Label Compd Radiopharm 1999,42(5),437

NLA-1

Chemical Name: N-[3-(2-Nitro-1H-imidazol-1-yl)propyl]acridine-9-amine hydrochloride
CAS No. 140448-36-8
项目整合开发状态: Preclinical
项目研究机构: Stanford University (Originator), University of Auckland ...
参考文献标题:Bis(nitro-1-imidazolyl alkylamine) platinum complexes useful in radiotheraphy or chemotherapy
文献作者:Adams,G.E.; Ahmed,I.; Stratford,I.J.(Gerald Edward Adams; Ian James Stratford; Israr Ahmed)
参考来源:GB 2131020

SS-212

Chemical Name: 11-(1-Methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine-8-carbonitrile fumarate
CAS No. 143540-37-8 (free base)
项目整合开发状态: Preclinical
项目研究机构: SSP (...
参考文献标题:Novel benzo[5,6]cyclohepta[1,2-b]pyridine derivs.and antiallergic agents comprising same
文献作者:Honda,H.; Mizuno,H.; Mogi,K.; Ito,Y.; Kaneko,Y.; Taido,N.; Sato,S.; Kuraishi,T.(SSP Co.,Ltd.)
参考来源:EP 0495484; JP 1993059040; US 5231101

Rofleponide palmitate

Chemical Name: 16alpha,17alpha-[(R)-Butylidenedioxy]-6alpha,9alpha-difluoro-21-(hexadecanoyloxy)-11beta-hydroxypregn-4-ene-3,20-dione
CAS No. 144653-57-6
项目整合开发状态: Discontinued
项目研究机构: AstraZ...
参考文献标题:Novel steroids
文献作者:Andersson,P.; Axelsson,B.; Brattssand,R.; Thalen,A.(AstraZeneca plc)
参考来源:JP 1994505232; US 5674861; US 5939409; WO 9213872

BOF-4272

Chemical Name: (?-8-[3-Methoxy-4-(phenylsulfinyl)phenyl]pyrazolo[1,5-a]-1,3,5-triazin-4-ol sodium salt hydrate
CAS No. 134395-51-0 ((-)-enantiomer, anhydrous), 134395-58-7 ((-)-enantiomer, Ca salt,...
参考文献标题:Pyrazolotriazine cpds
文献作者:Fujii,S.; Kawamura,H.; Kiyokawa,H.; Yamada,S.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:EP 0269859; JP 1989079184; JP 1994316578; US 4824834

FR-115906, FK-906

Chemical Name: N-Methyl-N-[2(S)-[N-methyl-N-[2-[N-methyl-N-(4-morpholinylcarbonyl)amino]ethyl]carbamoyloxy]-3-phenylpropionyl]-L-histidine 1(S)-(cyclohexylmethyl)-2(S)-hydroxy-5-methylhexylamide hydro...
参考文献标题:New amino acid derivs.processes for the preparation thereof and pharmaceutical compsns.containing the same
文献作者:Hemmi,K.; Neya,M.; Marusawa,H.; Imai,K.; Kayakiri,N.; Hashimoto,M.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:AU 8818190; EP 0300189; JP 1989019071; US 4921855; US 5223489