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

SB-204990

2-((3R,5S)-5-(6-(2,4-二氯苯基)己基)-3-羟基-2-氧代四氢呋喃-3-基)乙酸Chemical Name: (?-(3R*,5S*)-5-[6-(2,4-Dichlorophenyl)hexyl]-3-hydroxy-2-oxo-2,3,4,5-tetrahydrofuran-3-acetic acid
CAS No. 154566-12-8, 154566-58-2 ...
参考文献标题:Phenylderivate as inhibitors of ATP citrate lyase
文献作者:Gribble,A.D.; Groot,P.H.E.; Shaw,A.N.; Dolle,R.E.(SmithKline Beecham plc)
参考来源:EP 0639187; WO 9322304

ONO-AP-324

2-((5-(3-(苄基氨基)-3-氧代丙基)萘-1-基)氧基)乙酸Chemical Name: 2-[5-[2-[N-(Diphenylmethyl)carbamoyl]ethyl]naphthalen-1-yloxy]acetic acid
CAS No. 180197-87-9
项目整合开发状态: Preclinical
项目研究机构: Ono (Originator) 参考文献标题:Naphthyloxyacetic acid derivs.and their use as PGE2 agonists and antagonists
文献作者:Nagao,Y.; Torisu,K.; Maruyama,T.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 0719760; JP 1996239356

Indibulin, D-24851

2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺Chemical Name: 2-[1-(4-Chlorobenzyl)-1H-indol-3-yl]-2-oxo-N-(4-pyridyl)acetamide
CAS No. 204205-90-3
项目整合开发状态: Preclinical
项目研究机构: Baxter Oncology (O...
参考文献标题:N-Substd.indol-3-glyoxylamide with antiasthmatic,antiallergic and immunosuppressive/immunomodulating effect
文献作者:Lebaut,G.; Menciu,C.; Kutscher,B.; Emig,P.; Szelenyi,S.; Brune,K.(Asta Medica AG)
参考来源:DE 19636150; EP 0931063; JP 2000505098; US 6008231; WO 9809946

SCP-1

2-(1,1-二氧化二氧-3-氧-1,2-苯并噻唑-2(3h)-基)-n-(4-羟基苯L)乙酰胺Chemical Name: N-(4-Hydroxyphenyl)-2-(1,1,3-trioxo-2,3-dihydro-1,2-benzisothiazol-2-yl)acetamide
CAS No. 182502-68-7
项目整合开发状态: Phase I
项目研究机构: ...
参考文献标题:New N-acylated 4-hydroxyphenylamine derivs.with analgesic properties and pharmaceutical compsns.containing them
文献作者:Alvarez-Builla Gomez,J.; Bazan,N.G.(LSU Medical Center Foundation)
参考来源:JP 1999509520; US 5554636; WO 9632940

YM-31636

2-(1H-咪唑-4-基甲基)-8H-茚并[1,2-d]噻唑单富马酸酯Chemical Name: 2-(1H-Imidazol-4-ylmethyl)-8H-indeno[1,2-d]thiazole monofumarate
CAS No. 159081-22-8
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator) 参考文献标题:Novel condensed thiazole deriv.,process for producing the same,and pharmaceutical compsn.containing the same
文献作者:Iwaoka,K.; Koshio,H.; Ito,H.; Miyata,K.; Ohta,M.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0666263; JP 1995507965; US 5565479; WO 9406791

FR-194921

2-(1-甲基哌啶-4-基)-6-(2-苯基吡喃[1,5-a]吡啶-3-酰)吡啶嗪-3(2H)-1Chemical Name: 2-(1-Methylpiperidin-4-yl)-6-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)pyridazin-3(2H)-one
CAS No. 202646-80-8, 202646-82-0 (hydrochloride...
参考文献标题:Pyrazolopyridine cpd.and pharmaceutical use thereof
文献作者:Akahane,A.; Kuroda,S.; Itani,H.; Shimizu,Y.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0925299; JP 2000514821; US 6124456; WO 9803507

Centhaquin, Compound-7173

2-(2-(4-(3-甲基苯基)-1-哌嗪基)乙基)喹啉Chemical Name: 2-[2-[4-(3-Methylphenyl)-1-piperazinyl]ethyl]quinoline
CAS No. 57961-90-7
项目整合开发状态: Phase II
项目研究机构: Central Drug Research Institute (Originator) 参考文献标题:1-Substituted-4-(beta-2-quinolylethyl)piperazines and 1,2,3,4-tetrahydroquinolyl-ethyl analogues thereof
文献作者:Murthi,V.A.; et al.(Council of Scientific and Industrial Research)
参考来源:US 3983121

Detalliptinium, Datelliptium chloride, SR-95156B(monoHCl), NSC-311152, DTL

2-(2-二乙基氨基乙基)-5,11-二甲基-6H-吡啶并[4,3-b]咔唑-2-鎓-9-醇氯化物 2-[2-(二乙胺)乙基]-9-羟基-5,11-二甲基-6H-吡啶并[4,3-b]咔唑鎓乙酸盐 Chemical Name: 2-[2-(Diethylamino)ethyl]-9-hydroxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazolium chloride;...
参考文献标题:Hydrochlorides of 2-aminoalkyl-9-hydroxyellipticinium chloride derivs.and pharmaceutical compsns.containing them
文献作者:Gros,P.; Crisafulli,E.(CNRS (Centre National de la Recherche Scientifique); Sanofi-Synthabo)
参考来源:EP 0209511; FR 2584409; JP 1987010084; US 4897398

SCH-442416

2-(2-呋喃基)-7-[3-(4-甲氧基苯基)丙基]-7H-吡唑并[4,3-e][1,2,4]噻唑并[1,5-c]嘧啶-5-胺Chemical Name: 2-(2-Furyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine
CAS No. 316173-57...
参考文献标题:Design,radiosynthesis,and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using positron emission tomography
文献作者:Todde,S.; Moresco,R.M.; Simonelli,P.; Baraldi,P.G.; Cacciari,B.; Spalluto,G.; Varani,K.; Monopoli,A.; Matarrese,M.; Carpinelli,A.; Magni,F.; Kienle,M.G.; Fazio,F.
参考来源:J Med Chem 2000,43(23),4359

APHS

2-(2-庚炔-1-基硫代)-苯酚 1-乙酸酯Chemical Name: Acetic acid 2-(2-heptynylsulfanyl)phenyl ester
CAS No. 209125-28-0
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator), Vanderbilt University (Originator)<...
参考文献标题:Selective inhibitors of prostaglandin endoperoxide synthase-2
文献作者:Marnett,L.J.; Kalgutkar,A.S.(Vanderbilt University)
参考来源:US 5973191