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

CYC-682, CS-682

N-[1-[(2R,3S,4S,5R)-3-氰基-4-羟基-5-(羟甲基)氧杂环戊-2-基]-2-氧代嘧啶-4-基]十六酰胺Chemical Name: 2'-Cyano-2'-deoxy-1-(beta-D-arabinofuranosyl)-N4-palmitoylcytosine; N-[1-(2-Cyano-2-deoxy-beta-D-arabinofuranosyl)-1,2-dih...
参考文献标题:Pyrimidine nucleoside derivs.having anti-tumor activity,their preparation and use
文献作者:Kaneko,M.; Hotoda,H.; Shibata,T.; Kobayashi,T.; Mitsuhashi,Y.; Matsuda,A.; Sasaki,T.(Sankyo Co.,Ltd.)
参考来源:EP 0536936; JP 1993194497; US 5691319

Olcegepant, BIBN-4096, BIBN-4096BS

N-[2-[5-氨基-1(S)-[4-(4-吡啶基)哌嗪-1-甲酰基]戊基氨基]-1(R)-(3,5-二溴-4-羟基苄基)-2-氧代乙基]-4-(2-氧代-1,2,3,4-四氢喹唑啉-3-基)哌啶-1-甲酰胺Chemical Name: N-[2-[5-Amino-1(S)-[4-(4-pyridinyl)piperazin-1-ylcarbonyl]pentylamino]-1(R)-(3,5...
参考文献标题:Modified aminoacids,pharmaceuticals containing these cpds.and methods for their production
文献作者:Eberlein,W.; Wienen,W.; Doods,H.; Rudolf,K.; Entzeroth,M.; Pieper,H.; Engel,W.; Hallermayer,G.(Dr.Karl Thomae GmbH)
参考来源:JP 2000505100; WO 9811128

KRN-633

N-[2-氯-4-[(6,7-二甲氧基-4-喹唑啉基)氧基]苯基]-N'-丙基脲Chemical Name: N-[2-Chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl]-N'-propylurea
CAS No. 286370-15-8
项目整合开发状态: Preclinical
项目研究机构: Kirin Brewery (O...
参考文献标题:Quinoline derivs.and quinazoline derivs.
文献作者:Kubo,K.; Fujiwara,Y.; Isoe,T.(Kirin Brewery Co.,Ltd.)
参考来源:EP 1153920; WO 0043366

Targinine hydrochloride, L-NMMA.HCl, L-NMA.HCl, 546C88

Nω-单甲基-L-精氨酸乙酸酯 Nω-单甲基-L-精氨酸乙酸盐Chemical Name: Nomega-Methyl-L-arginine hydrochloride; N5-(Methylamidino)-L-ornithine hydrochloride
CAS No. 156706-47-7, 17035-90-4 (free base), 53308-83-1 (monoacet...
参考文献标题:NG-Monomethyl-L-arginine hydrochloride derivs.and their use in the treatment of septic shock
文献作者:Hodson,H.F.(Glaxo Wellcome plc)
参考来源:EP 0651741; JP 1995509239; US 5767312; WO 9402453

(+)-N-Desmethylzopiclone, (S)-DMZ, SEP-174559

N-去甲基异佐吡克隆盐酸盐 Chemical Name: (+)-6-(5-Chloro-2-pyridyl)-7(S)-(piperazin-1-ylcarbonyloxy)-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-5-one; Piperazine-1-carboxylic acid 6-(5-chloro-2-pyridyl)-7-oxo-6,7-dihy...
参考文献标题:Methods of making and using N-desmethylzopiclone
文献作者:Hong,Y.; Senanayake,C.H.; Jerussi,T.P.; Rubin,P.D.; Bakale,R.A.; Xiang,T.; McConville,F.A.(Sepracor Inc.)
参考来源:US 6339086; WO 0069442

P32/98

P32/98(半富马酸盐) Chemical Name: 2(S)-Amino-3(S)-methyl-1-(3-thiazolidinyl)pentan-1-one fumarate; 3-(L-Isoleucyl)thiazolidine fumarate; 3-[2(S)-Amino-3(S)-methylpentanoyl]thiazolidine fumarate
CAS No....
参考文献标题:Process for the preparation of new dipeptidyl peptidase IV inhibitors
文献作者:Faust,J.; Heins,J.; Rahfeld,J.U.; Demuth,H.-U.; Steinmetzer,T.; Born,I.; Barth,A.; Neubert,K.(Martin Luther Universit鋞 Halle-Wittenberg)
参考来源:DD 296075

Ruboxistaurin mesilate hydrate, LY-333531 mesylate hydrate

Ruboxistaurin甲磺酸盐鲁伯斯塔Chemical Name: 9(S)-(Dimethylaminomethyl)-6,7,10,11,19,20-hexahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20-dione monomethanes...
参考文献标题:Protein kinase C inhibitors
文献作者:Heath,W.F.Jr.; Jirousek,M.R.; McDonald,J.H.III; Rito,C.J.(Eli Lilly and Company)
参考来源:CA 2137203; EP 0657458; JP 1995238044; US 5624949

S-151276, S-15176

S-15176二富马酸盐盐 Chemical Name: 2,6-Di-tert-butyl-4-[3-[4-(2,3,4-trimethoxybenzyl)-1-piperazinyl]propylsulfanyl]phenol
CAS No. 148089-70-7, 148913-55-7 (fumarate)
项目整合开发状态: Preclinical
项目研究机构: ...
参考文献标题:Trimetazidine derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Regnier,G.; Vilaine,J.-P.; Villeneuve,N.; Bidouard,J.-P.; Iliou,J.-P.; Lenaers,A.(ADIR et Cie.)
参考来源:EP 0533579; FR 2681324; JP 1993194451; US 5283246

beta-Lapachone, ARQ-501, CO-501, R-1668

β-拉帕醌Chemical Name: 2,2-Dimethyl-3,4-dihydro-2H-benzo[h]-1-benzopyran-5,6-dione
CAS No. 4707-32-8
项目整合开发状态: Phase I
项目研究机构: ArQule (Proprietary), Cyclis Pharmaceuticals (Proprietary), Beth I...
参考文献标题:Novel synthesis and use of beta-lapachone analogs
文献作者:Boothman,D.A.; Frydman,B.J.; Witiak,D.T.(Wisconsin Alumni Research Foundation)
参考来源:US 5763625; WO 9633988

Centbucridine, CDRI-64/124

丁吖卡因 Chemical Name: N-(Butylamino)-1,2,3,4-tetrahydroacridine hydrochloride
CAS No. 34811-20-6, 316-15-4 (free base)
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:Anthranitic acid (I) is rea...
参考文献标题:Compounds acting on the central nervous system.IV.4-substituted 2,3-polymethylenequinolines
文献作者:Patnaik,G.K.; Vohra,M.M.; Bindra,J.S.; Garg,C.P.; Anand,N.
参考来源:J Med Chem 1966,9(4),483