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

新产品编号:574775

Chemical Name: 12-(4-Hydroxyphenyl)-1,12-dicarba-closo-dodecaborane(12)-1-methanol
CAS No. 227183-66-6
项目整合开发状态: Biological Testing
项目研究机构: University of Tokyo (Originator)
合成路线:1,12-Dicar...
参考文献标题:Potent estrogenic agonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore
文献作者:Endo,Y.; Iijima,T.; Yamakoshi,Y.; Yamaguchi,M.; Fukasawa,H.; Shudo,K.
参考来源:J Med Chem 1999,42(9),1501

Crobenetine hydrochloride, BIII-890-CL

Chemical Name: (2R,6S)-3-[2(S)-Benzyloxypropyl]-6,11,11-trimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-10-ol hydrochloride
CAS No. 221018-88-8, 221019-25-6 (free base)
项目整合开发状态: Phase ...
参考文献标题:Substd.1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocine-10-oles,method for the production and use thereof as medicaments
文献作者:Weiser,T.; Bechtel,W.-D.; Palluk,R.; Pschorn,U.; Carter,A.; Grauert,M.(Boehringer Ingelheim Pharma KG)
参考来源:EP 1015433; WO 9914199

LAV-694, SDZ-LAV-694

Chemical Name: 6-[2-(2,5-Dimethoxyphenyl)ethyl]-4-ethylquinazoline
CAS No. 182878-97-3
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Palladium-catalyzed coupling between 4-ethyl...
参考文献标题:Trisubstd.phenyl derivs.
文献作者:Nussbaumer,P.(Novartis AG)
参考来源:US 5990116; WO 9628430

PNU-177864

Chemical Name: N-[4-[2-(Propylamino)ethyl]phenyl]-4-(trifluoromethoxy)benzenesulfonamide
CAS No. 250266-51-4
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:4-Nitrophenethylamine (I...
参考文献标题:Phenylsulfonamide-phenylethylamines useful as dopamine receptors
文献作者:Romero,A.G.; Leiby,J.A.(Pharmacia Corp.)
参考来源:EP 1077935; WO 9958499

UCL-1848

Chemical Name: 6,7,8,9,10,11,12,19,20,21,22,23-Dodecahydro-5,24:13,18-diethenodibenzo[b,m][1,5,11,15]tetraazacycloeicosine-18,24-diium bis(trifluoroacetate)
CAS No. 201147-53-7, 201147-52-6 (cation...
参考文献标题:Potassium channel blockers
文献作者:Campos-Rosa,J.; Dunn,P.M.; Galanakis,D.; Ganellin,C.R.; Jenkinson,D.H.; Yang,D.; Chen,J.(University College London)
参考来源:WO 9748705

SJ-749-1, SJ-749

Chemical Name: 3-[7-(Benzyloxycarbonyl)-8-(2-pyridinylaminomethyl)-1-oxa-2,7-diazaspiro[4.4]non-2-en-3-ylcarboxamido]-2(S)-(2,4,6-trimethylphenylsulfonylamino)propionic acid; 3-[N-[2(S)-Carboxy-2-(2,4...
参考文献标题:Spirocycle integrin inhibitors
文献作者:Jadhav,P.K.; Smallheer,J.M.(DuPont Pharmaceuticals Co.)
参考来源:EP 0888344; US 5760029; WO 9733887

新产品编号:443469

Chemical Name: 2(S)-[5-[2-Cyclohexyl-1(S)-(ethylsulfanylmethyl)ethylaminomethyl]-2'-methylbiphenyl-2-ylcarboxamido]-4-(methylsulfanyl)butyric acid; N-[5-[2-Cyclohexyl-1(S)-(ethylsulfanylmethyl)ethylam...
参考文献标题:PDB-093
文献作者:Henry,K.J.Jr.; Wasicak,J.; Tasker,A.S.; Cohen,J.; Ewing,P.; Mitten,M.; Larsen,J.J.; Kalvin,D.M.; Swenson,R.; Ng,S.C.; Saeed,B.; Cherian,S.; Sham,H.; Rosenberg,S.H.
参考来源:Drug Data Rep 1995,17(2),138

新产品编号:166619

Chemical Name: 2-[6-(4-Amidinobenzamido)-3,4-dihydro-2H-1-benzopyran-2-yl]acetic acid ethyl ester
CAS No. 181072-77-5, 181072-57-1 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: Lilly (Origina...
参考文献标题:Fused bicyclic Gly-Asp beta-turn mimics with specific affinity for GPIIb-IIIa
文献作者:Fisher,M.J.; Arfstan,A.E.; Giese,U.; Gunn,B.P.; Harms,C.S.; Khau,V.; Kinnick,M.D.; Lindstrom,T.D.; Martinelli,M.J.; Mest,H.J.; Mohr,M.; Morin,J.M.Jr.; Mullaney,J.T.; Nunes,A.; Paal,M.; Rapp,A.; Ruhter,G.; Ruterbories,K.J.; et al.
参考来源:J Med Chem 1999,42(23),4875

MC-002434

Chemical Name: L-Phenylalanyl-N2-methyl-L-ornithine (2-naphthyl)amide
CAS No. 233686-67-4, 233689-01-5 (trifluoroacetate)
项目整合开发状态: Preclinical
项目研究机构: Essential Therapeutics (Originator), Da...
参考文献标题:Efflux pump inhibitors
文献作者:Leger,R.; Zhang,Z.J.; She,M.; Lee,M.; Chamberland,S.; Renau,T.; Lee,V.J.(Microcide Pharmaceuticals,Inc.)
参考来源:WO 9937667

JTV-803

Chemical Name: 4-(2-Amidino-1,2,3,4-tetrahydroisoquinolin-7-yloxymethyl)-1-(4-pyridinyl)piperidine-4-carboxylic acid methanesulfonate trihydrate
CAS No. 247131-79-9 (anhydrous), 247131-06-2 (anhydr...
参考文献标题:Amidine cpds.
文献作者:Hayashi,M.; Yokota,K.; Katoh,S.(Japan Tobacco Inc.)
参考来源:EP 1070714; JP 2000136190; WO 9952895