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

TNK-6123

6-(环己基磺酰)-1-(乙氧基甲基)-5-异丙基-1,3-二氢嘧啶-2,4-二酮Chemical Name: 6-(Cyclohexylsulfanyl)-1-(ethoxymethyl)-5-isopropyl-1,3-dihydropyrimidine-2,4-dione; 6-(Cyclohexylsulfanyl)-1-(ethoxymethyl)-5-isopropyluracil 参考文献标题:Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants
文献作者:Hopkins,A.L.; Ren,J.; Tanaka,H.; Baba,M.; Okamoto,M.; Stuart,D.I.; Stammers,D.K.
参考来源:J Med Chem 1999,42(22),4500

CPDS

6,6'-二硫二烟酸Chemical Name: 6,6'-Dithiodinicotinic acid
CAS No. 15658-35-2
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi di Padova (Originator)
合成路线:6-Chloronicotinic acid (I) is...
参考文献标题:CPDS
文献作者:Grassetti,D.R.
参考来源:Drugs Fut 1986,11(7),559

Licostinel, CGP-63446, ACEA-1021

6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮Chemical Name: 6,7-Dichloro-5-nitroquinoxaline-2,3(1H,4H)-dione
CAS No. 153504-81-5
项目整合开发状态: Phase I
项目研究机构: CoCensys (Originator)
合成路线:Reaction of tetrabutyla...
参考文献标题:Synthesis of a C-11-labelled nitrated 1,4-dihydroquinoxaline-2,3-dione,the NMDA glycine receptor antagonist ACEA 1021 (Licostinel)
文献作者:Thorell,J.O.; et al.
参考来源:J Label Compd Radiopharm 1998,41(4),345-353

AG-1296

6,7-二甲氧基-2-苯基喹喔啉Chemical Name: 6,7-Dimethoxy-2-phenylquinoxaline
CAS No. 146535-11-7
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator)
合成路线:Leflunomide can be obtained by several r...
参考文献标题:Treatment of platelet derived growth factor related disorders such as cancers using inhibitors of platelet derived growth receptor
文献作者:Levitzki,A.; Mann,E.; Bajor,T.; Lammers,R.; Kabbinavar,F.F.; Hirth,K.P.; Orfi,L.; Slamon,D.J.; et al.(Max-Planck-Gesellschaft zur Fderung der Wissenschaften e.V.; Sugen,Inc.; The Hebrew University; Yissum Research Development Co.)
参考来源:EP 1000617; US 5700823; WO 9519169

PD-168787, CI-1018

6,8-二氧杂二环[3.2.1]辛烷,2-氟-1,5-二甲基-,(1R,2R,5R)-Chemical Name: N-[9-Methyl-4-oxo-1-phenyl-3,4,6,7-tetrahydropyrrolo[3,2,1-jk][1,4]benzodiazepin-3(R)-yl]pyridine-4-carboxamide
CAS No. 179024-48-7
项目整合...
参考文献标题:Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: Novel PDE4 inhibitors
文献作者:Pascal,Y.; Andrianjara,C.R.; Auclair,E.; Avenel,N.; Bertin,B.; Calvet,A.; Feru,F.; Lardon,S.; Moodley,I.; Ouagued,M.; Payne,A.; Pruniaux,M.P.; Szilagyi,C.
参考来源:Bioorg Med Chem Lett 2000,10(1),35

Michellamine B, NSC-661755, NSC-649324

6,8-异硝基二醇,5,5'-(1,1'-二羟基-8,8'-二甲氧基-6,6'-二甲基[2,2'-双苯二甲基]-4,4'-二甲基)双[1,2,3,4-四氢-1,3-二甲基-,(1R,1'R,3R,3'R,3'R,5R,5'S)-Chemical Name: (1S,1'R,3S,3'R)-2,2'-Bis[4-(6,8-dihydroxy-1,3-dimethyl-1,2,3,4-tetrahyd...
参考文献标题:Total synthesis of michellamines A-C,korupensamines A-D,and ancistrobrevine B
文献作者:Hoye,T.R.; et al.
参考来源:J Org Chem 1999,64(19),7184

NVP-728, DPP-728, NVP-DPP-728

6-[[[2-[[2-(2S)-2-氰基-1-吡咯烷基]-2-氧乙基]氨基]乙基]氨基-3-吡啶碳腈二盐酸盐Chemical Name: 6-[2-[2-[2(S)-Cyanopyrrolidin-1-yl]-2-oxoethylamino]ethylamino]pyridine-3-carbonitrile; 1-[2-[2-(5-Cyanopyridin-2-ylamino)ethylamin...
参考文献标题:N-Substd.2-cyanopyrrolidines
文献作者:Villhauer,E.B.(Novartis AG)
参考来源:JP 2000511559; WO 9819998

CHIR-99021

6-[[2-[[4-(2,4-二氯苯基)-5-(5-甲基-1H-咪唑-2-基)-2-嘧啶]氨基]乙基]氨基]-3-吡啶甲腈Chemical Name: 6-[2-[4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-ylamino]ethylamino]pyridine-3-carbonitrile
CAS No. ...
参考文献标题:Inhibitors of glycogen synthase kinase 3
文献作者:Brown,S.P.; Goff,D.; Ring,D.B.; Harrison,S.D.; Subramanian,S.; Nuss,J.M.; Boyce,R.S.; Johnson,K.; Pfister,K.B.; Ramurthy,S.; Renhowe,P.A.; Seely,L.; Wagman,A.S.; Zhou,X.A.(Chiron Corp.)
参考来源:EP 1087963; US 6417185; WO 9965897

CD-3127, LG-268, LG-100268

6-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)环丙基]-3-吡啶羧酸Chemical Name: 6-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid
CAS No. 153559-76-3
项目整合开发状态: P...
参考文献标题:Synthesis of novel retinoid X receptor-selective retinoids
文献作者:Faul,M.M.; Ratz,A.M.; Sullivan,K.A.; Trankle,W.G.; Winneroski,L.L.
参考来源:J Org Chem 2001,66(17),5772

WS-75624B

6-[2-(6-羟基-庚基)-噻唑-4-基]-4,5-二甲氧基-吡啶-2-羧酸Chemical Name: 6-[2-(6-Hydroxyheptyl)thiazol-4-yl]-4,5-dimethoxypyridine-2-carboxylic acid
CAS No. 188048-45-5
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (O...
参考文献标题:The total synthesis of the natural product endothelin converting enzyme (ECE) inhibitor,WS75624 B
文献作者:Massa,M.A.; et al.
参考来源:213th ACS Natl Meet (April 13-17,San Francisco) 1997,Abst MEDI 196