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

N-89

Chemical Name: 1,2,6,7-Tetraoxaspiro[7.11]nonadecane
CAS No. 229323-98-2
项目整合开发状态: Preclinical
项目研究机构: Okayama University (Originator), Osaka University (Originator)
合成路线:Bishydroperoxide ...
参考文献标题:Synthesis,crystal structure and anti-malarial activity of novel spiro-1,2,4,5-tetraoxacycloalkanes
文献作者:Tsuchiya,K.; et al.
参考来源:Tetrahedron Lett 1999,40(21),4077

alpha-TEA

Chemical Name: 2-[2(R),5,7,8-Tetramethyl-2-[4(R),8(R),12-trimethyltridecyl]-3,4-dihydro-2H-1-benzopyran-6-yloxy]acetic acid
CAS No. 261929-52-6, 261929-63-9 (undefined isomer)
项目整合开发状态: Preclini...
参考文献标题:Tocopherols,tocotrienols,other chroman and side chain derivs.and uses thereof
文献作者:Liu,S.; Kline,K.; Sanders,B.G.; Hurley,L.; Gardner,R.; Menchaca,M.; Yu,W.; Ramanan,P.N.; Israel,K.(Research Development Foundation )
参考来源:EP 1115398; JP 2002526446; US 6417223; WO 0016772

新产品编号:391263

Chemical Name: N-[2(S)-(3-Chlorophenyl)-4-[1-oxospiro[benzothiophene-3(2H),4'-piperidin]-1'-yl]butyl]-N-methylbenzenesulfonamide
CAS No. 209349-02-0
项目整合开发状态: Biological Testing
项目研究机构: Merck...
参考文献标题:Spiro-substd.azacycles as modulators of chemokine receptor activity
文献作者:Mills,S.G.; MacCoss,M.; Springer,M.S.(Merck & Co.,Inc.)
参考来源:US 5962462; WO 9825605

新产品编号:459289

Chemical Name: N-[5-(Aminosulfonyl)-1,3,4-thiadiazol-2-yl]-beta-alanine trifluoroacetate
CAS No. 217972-52-6
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Firenze (Originator)
合成路...
参考文献标题:Carbonic anhydrase inhibitors: Synthesis of water-soluble,aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route
文献作者:Scozzafava,A.; Briganti,F.; Mincione,G.; Menabuoni,L.; Mincione,F.; Supuran,C.T.
参考来源:J Med Chem 1999,42(18),3690

Sabiporide mesilate

Chemical Name: N-[4-[4-(1H-Pyrrol-2-ylcarbonyl)piperazin-1-yl]-3-(trifluoromethyl)benzoyl]guanidine methanesulfonate
CAS No. 261505-80-0 (free base)
项目整合开发状态: Phase I
项目研究机构: Boehringer Ingel...
参考文献标题:Benzoylguanidine derivs.with advantageous properties,method for producing them and their use in the production of medicaments
文献作者:Roos,O.; Eickmeier,C.; Blech,S.-M.; B鷕ger,E.(Boehringer Ingelheim Pharma GmbH & Co.KG)
参考来源:DE 19843489; JP 2002538077; US 6323207; WO 0017176

新产品编号:729811

Chemical Name: 2-[4-[8-Hydroxy-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-3-yl]butyl]-2-[3-(trifluoromethyl)benzyl]malonic acid triethylamine salt hydrate
CAS No. 273224-16-1 (anhydrous), 273224...
参考文献标题:AMP deaminase inhibitors.4.Further N3-substituted coformycin aglycon analogues: N3-alkylmalonates as ribose 5'-monophosphate mimetics
文献作者:Bookser,B.C.; Kasibhatla,S.R.; Erion,M.D.
参考来源:J Med Chem 2000,43(8),1519

新产品编号:43223

Chemical Name: N,N-Dimethyl-N-[2-[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethylperhydro-3,12-epoxypyrano[4,3-j]-1,2-benzodioxepin-10-yloxy]ethyl]amine oxalate; 10beta-[2-(N,N-Dimethylamino)ethyl]-10...
参考文献标题:Synthesis and antimalarial activity of artemisinin derivatives containing an amino group
文献作者:Li,Y.; Zhu,Y.M.; Jiang,H.J.; Pan,J.P.; Wu,G.S.; Wu,J.M.; Shi,Y.L.; Yang,J.D.; Wu,B.A.
参考来源:J Med Chem 2000,43(9),1635

新产品编号:369115

Chemical Name: 1-[5'-O-[Hydroxy(tetradecyloxy)phosphoryl]-beta-D-arabinofuranosyl]-2-thiocytosine sodium salt
CAS No. 205826-63-7 (free acid), 205826-62-6 (Li salt)
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Enzymatic reactivity and anti-tumor activity of 1-(beta-D-arabinofuranosyl)-2-thiocytosine derivatives
文献作者:Kawaguchi,T.; Ichikawa,T.; Hasegawa,T.; Saneyoshi,M.; Wakayama,T.; Kato,H.; Yukita,A.; Nagata,T.
参考来源:Chem Pharm Bull 2000,48(4),454

CB-126229

Chemical Name: (3'R*,3'aR*,6'aS*)-5'-(3,4-Dichlorophenyl)-3'-phenylspiro[indane-2,1'-perhydrofuro[3,4-c]pyrrole]-1,3,4',6'-tetraone
CAS No. 262847-89-2, 262847-99-4 (undefined stereochem.)
项目整合开...
参考文献标题:Condensed imidazolidinones as tRNA synthetase inhibitors
文献作者:Wang,Z.; Hill,J.; Finn,J.; Yu,X.Y.; Keith,D.; Gallant,P.; Wendler,P.(Cubist Pharmaceuticals,Inc.)
参考来源:WO 0018772

CB-102930

Chemical Name: (3'R*,3'aS*,6'aR*)-5'-(3,4-Dichlorophenyl)-3'-phenylspiro[indane-2,1'-perhydrofuro[3,4-c]pyrrole]-1,3,4',6'-tetraone
CAS No. 262847-90-5, 262847-99-4 (undefined stereochem.)
项目整合开...
参考文献标题:Condensed imidazolidinones as tRNA synthetase inhibitors
文献作者:Wang,Z.; Hill,J.; Finn,J.; Yu,X.Y.; Keith,D.; Gallant,P.; Wendler,P.(Cubist Pharmaceuticals,Inc.)
参考来源:WO 0018772