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

IPdR

1-(2-脱氧-beta-呋喃核糖基)-5-碘-2-嘧啶酮Chemical Name: 1-(2-Deoxy-beta-D-ribofuramosyl)-5-iodo-2-pyrimidinone
CAS No. 93265-81-7
项目整合开发状态: Phase I
项目研究机构: State University of New York, Albany (Originato...
参考文献标题:Improved stereoselective synthesis of the beta-anomer of 1-[3,5-bis-O-(p-chlorobenzoyl)-2-deoxy-D-ribofuranosyl]-5-iodo-2-pyrimidinone
文献作者:Schure,R.; et al.
参考来源:Org Process Res Dev 1999,3(2),135

OPC-14523

1-(3-(4-(3-氯苯基)-1-哌嗪基)丙基)-5-甲氧基-3,4-二氢-2-喹啉酮 2(1H)-喹啉酮,1-[3-[4-(3-氯苯基)-1-哌嗪基]丙基]-3,4-二氢-5-甲氧基-,盐酸盐 Chemical Name: 1-[3-[4-(3-Chlorophenyl)piperazin-1-yl]propyl]-5-methoxy-1,2,3,4-tetrahydroquinolin-2-...
参考文献标题:3,4-Dihydro-2(1H)-quinolinone as a novel antidepressant drug: Synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4-dihydro-5-methoxy-2(1H)-quinolinone and its derivatives
文献作者:Oshiro,Y.; Sakurai,Y.; Sato,S.; Kurahashi,N.; Tanaka,T.; Kikuchi,T.; Tottori,K.; Uwahodo,Y.; Miwa,T.; Nishi,T.
参考来源:J Med Chem 2000,43(2),177

Aptiganel, CNS-1102, Cerestat(former Brand Name)

1-(3-乙基苯基)-1-甲基-2-萘-1-基胍Chemical Name: N1-(3-Ethylphenyl)-N1-methyl-N3-(1-naphthyl)guanidine
CAS No. 137159-92-3, 137160-11-3 (monoHCl)
项目整合开发状态: Discontinued
项目研究机构: CeNeS (Originator)
合成...
参考文献标题:Tri- and tetra-substd.guanidines and their use as excitatory amino acid antagonists
文献作者:Weber,E.; Keana,J.F.W.(University of Oregon)
参考来源:JP 2002020361; US 5262568; WO 9112797

MY-5445

1-(3-氯苯胺基)-4-苯基酞嗪Chemical Name: 1-(3-Chloroanilino)-4-phenylphthalazine; N-(3-Chlorophenyl)-4-phenyl-1-phthalazinamine
CAS No. 78351-75-4
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Chemical (Or...
参考文献标题:4-Phenylphthalazine derivs.
文献作者:Hayashi,E.; Oishi,E.; Marinaka,Y.; Mori,M.; Kanayama,T.(Mitsubishi Chemical Corp.)
参考来源:GB 2063249

SJ-3366

1-(3-环戊烯-1-甲基)-6-(3,5-二甲基苯甲酰)-5-乙基嘧啶-2,4(1H,3H)-二酮Chemical Name: 1-(3-Cyclopenten-1-ylmethyl)-6-(3,5-dimethylbenzoyl)-5-ethylpyrimidine-2,4(1H,3H)-dione
CAS No. 195720-26-4
项目整合开发状态: Preclinical...
参考文献标题:New antiviral substd.pyrimidinedione homocarbocyclic nucleoside derivs.and methods for the preparation thereof and compsns.containing the same as active ingredients
文献作者:Cho,E.-H.; Chung,S.-G.; Kim,J.-Y.; Kwon,H.-S.; Lee,S.-H.; Lee,J.-E.; Joo,J.-H.; Kim,B.-C.; Kang,D.-W.(Samjin Pharmaceutical Co.,Ltd.)
参考来源:EP 0827498; JP 1998507780; US 5922727; WO 9730979

FE-999011

1-(3-甲基-L-戊酸)吡咯利丁-2(S)-碳腈Chemical Name: 1-(3-Methyl-L-valyl)pyrrolidine-2(S)-carbonitrile
CAS No. 171092-64-1, 341997-80-6 (mono HCl salt)
项目整合开发状态: Preclinical
项目研究机构: Ferring (Originator) 参考文献标题:Compsns.for improving fertility
文献作者:Broqua,P.(Ferring BV Group Holding)
参考来源:WO 0056296

Iobenguane[131I], MIBG, PheoMIBG-I(131) Injection

1-(3-碘苄基)胍 3-碘苄基-胍半硫酸盐硫酸碘苄胍EP标准品Chemical Name: m-131-Iodobenzylguanidine; [(3-Iodo-[131I])phenyl]methylguanidine
CAS No. 77679-27-7, 139755-80-9 (123I-labeled sulfate(2:1)), 87862-25-7 (non-labele...
参考文献标题:Iobenguane (131I)
文献作者:Eastland,G.Jr.
参考来源:Drugs Fut 1989,14(5),427

SK&F-100330A

1-(4,4-二苯基-3-丁烯基)-1,2,5,6-四氢-3-吡啶羧酸Chemical Name: N-(4,4-Diphenyl-3-butenyl)guvacine hydrochloride; 1-(4,4-Diphenyl-3-butenyl)-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride
CAS No. 853...
参考文献标题:SK&F-100330-A
文献作者:Lcher,W.
参考来源:Drugs Fut 1986,11(1),39

Indometacin farnesil, Indomethacin farnesil, E-0710, Infree

1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1-吲哚-3-乙酸3,7,11-三甲基-2,6,10-十二碳三烯酯Chemical Name: 2-[1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid 3,7,11-trimethyl-2,6,10-dodecatrienyl ester
CAS No. 85801-...
参考文献标题:Polyprenyl esters of acemethacins and anti-inflammatory method of use thereof
文献作者:Yamatsu,I.; Abe,S.; Inai,Y.; Suzuki,T.; Kinoshita,K.; Mishima,M.; Katoh,Y.; Kobayashi,S.; Murakami,M.; Yamada,K.(Eisai Co.,Ltd.)
参考来源:DE 3226687; FR 2510107; GB 2104513; JP 8315940

CI-933

1-(4-甲氧基苯甲酰基)-5-氧代-2-吡咯烷丙酸Chemical Name: 1-(4-Methoxybenzoyl)-5-oxopyrrolidine-2-propionic acid; 3-[1-(4-Methoxybenzoyl)-5-oxopyrrolidin-2-yl]propionic acid
CAS No. 91829-95-7
项目整合开发状态: Phase II...
参考文献标题:1-Aroyl-5-oxo-2-pyrrolidinepropanoic acid derivs.
文献作者:(Pfizer Inc.)
参考来源:EP 0110575; ES 8600238