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

BD-1067

Chemical Name: N-[2-(3,4-Dichlorophenyl)ethyl]-N-ethyl-N-[2-(1-pyrrolidinyl)ethyl]amine
CAS No. 250777-45-8 (error)
项目整合开发状态: Preclinical
项目研究机构: National Institutes of Health (Originator), U...
参考文献标题:Synthesis,characterization,and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: Structural requirements and binding affinity at the sigma receptor
文献作者:de Costa,B.R.; Radesca,L..; Di Paolo,L.; Bowen,W.D.
参考来源:J Med Chem 1992,35(1),38

新产品编号:843715

Chemical Name: 4-(4-Bromo-3-thienylmethyl)-1H-imidazole fumarate
CAS No. 334917-95-2, 334917-94-1 (free base)
项目整合开发状态: Preclinical
项目研究机构: Johnson & Johnson (Originator)
合成路线:The reaction...
参考文献标题:alpha2 Adrenoceptor agonists as potential analgesic agents.3.Imidazolylmethylthiophenes
文献作者:Boyd,R.E.; Press,J.B.; Rasmussen,C.P.; Raffa,R.B.; Codd,E.E.; Connelly,C.D.; Li,Q.S.; Martinez,R.P.; Lewis,M.A.; Almond,H.R.; Reitz,A.B.
参考来源:J Med Chem 2001,44(6),863

新产品编号:302671

Chemical Name: 4-[2-[2(S)-Azetidinyl]ethoxy]-7-chloro-2-oxo-N-(4-pyrimidinyl)-3-(3,4,5-trimethylphenyl)-1,2-dihydroquinoline-6-carboxamide dihydrochloride
CAS No. 199861-41-1 (free base)
项目整合开发状...
参考文献标题:A potent,nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor
文献作者:DeVita,R.J.; Walsh,T.F.; Young,J.R.; Jiang,J.-D.; Ujjainwalla,F.; Toupence,R.B.; Parikh,M.; Huang,S.X.; Fair,J.A.; Goulet,M.T.; Wyvratt,M.J.; Lo,J.L.; Ren,N.; Yudkovitz,J.B.; Yang,Y.T.; Cheng,K.; Cui,J.; Mount,G.; Rohrer,S.P.; et al.
参考来源:J Med Chem 2001,44(6),917

新产品编号:180857

Chemical Name: 2-[5-Amino-2-(4-fluorophenyl)-6-oxo-1,6-dihydropyrimidin-1-yl]-N-(1-benzyl-3,3,3-trifluoro-2-oxopropyl)acetamide
CAS No. 184709-50-0
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Ph...
参考文献标题:Heterocyclic amide cpds.and medicinal use of the same
文献作者:Akahoshi,F.; Yoshimura,T.; Eda,M.; Ashimori,A.; Fukuyama,H.; Nakajima,M.; Imada,T.; Okunishi,H.; Miyazaki,M.(Welfide Corporation)
参考来源:EP 0826671; US 5948785; WO 9633974

新产品编号:13165

Chemical Name: 7,8-Dimethoxy-5-methyl-1-phenyl-3H-pyrazolo[3,4-c]isoquinoline
CAS No. 107879-55-0
项目整合开发状态: Biological Testing
项目研究机构: Daiichi Suntory Pharma (Originator)
合成路线:Conversion o...
参考文献标题:Synthesis of azolo(5,4-c) isoquinolines
文献作者:Nikolyukin,Y.A.; et al.
参考来源:Chem Heterocycl Compd 1990,26914

Y-40018

Chemical Name: 4-[5-Amino-2-(3-chlorophenyl)-6-oxo-1,6-dihydropyrimidin-1-ylacetamido]-N-benzyl-2,2-difluoro-3-oxo-5-phenylpentanamide
CAS No. 243462-36-4, 290814-60-7 (S-isomer)
项目整合开发状态: Precl...
参考文献标题:IgE antibody production inhibitors and autoimmune diseases inhibitors
文献作者:Kobayashi,F.; Naito,K.; Yoshikawa,T.; Kuwahara,S.; Imada,T.; Komorita,N.(Mitsubishi Pharma Corp.)
参考来源:EP 1062949; US 6528514; WO 9945928

CPTP

Chemical Name: N-[N-[2-[N-[1-(Cyclohexylmethyl)piperidin-3(R)-ylmethyl]carbamoyl]ethyl]carbamoylmethyl]-3,3,3-triphenylpropionamide
CAS No. 323181-78-8
项目整合开发状态: Preclinical
项目研究机构: Banyu (Or...
参考文献标题:Novel amide derivs.
文献作者:Kimura,T.; Noguchi,K.; Otake,N.; Uchiyama,M.; Naya,A.; Sagara,Y.; Numazawa,T.; Fujikawa,T.(Banyu Pharmaceutical Co.,Ltd.)
参考来源:EP 1213281; WO 0107406

新产品编号:138143

Chemical Name: 2-[3-[5-Methyl-2-[4-(trifluoromethoxy)phenyl]oxazol-4-ylmethoxy]benzyl]-1,2,4-oxadiazolidine-3,5-dione
CAS No. 174727-56-1
项目整合开发状态: Preclinical
项目研究机构: Amgen (Originator), Wye...
参考文献标题:Aralkyl-1,2,4-oxadiazolidine-3,5-diones as antihyperglycemic agents
文献作者:Malamas,M.S.; Palka,C.L.; Gunawan,I.(American Home Products Corp.)
参考来源:US 5480896

A-299620

Chemical Name: 2-Methoxy-5-[4-(3,4,5-trimethoxyphenyl)-1-methyl-1H-imidazol-5-yl]phenylamine hydrochloride
CAS No. 324519-48-4
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The co...
参考文献标题:Imidazole antiproliferative agents
文献作者:Wang,L.; Woods,K.W.; Li,Q.; Sham,H.L.(Abbott Laboratories Inc.)
参考来源:WO 0109103

KNI-694

Chemical Name: 3'-Azido-5'-O-[3-[N-[1(S)-benzyl-2(S)-[4(R)-[N-(2-methylbenzyl)carbamoyl]-5,5-dimethylthiazolidin-3-ylcarbonyl]-2-hydroxyethyl]carbamoyl]-2,2-dimethylpropionyl]-3'-deoxythymidine
CAS...
参考文献标题:Synthesis and biological evaluation of prodrug-type anti-HIV agents.Ester conjugates of carboxylic acid-containing dipeptide HIV protease inhibitors and a reverse transcriptase inhibitor
文献作者:Matsumoto,H.; Matsuda,T.; Nakata,S.; Mitoguchi,T.; Kimura,T.; Hayashi,Y.; Kiso,Y.
参考来源:Bioorg Med Chem 2001,9(2),417