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

NBI-30545

Chemical Name: N-[3-(2,4-Dimethoxyphenyl)-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-yl]-N-(2-methoxyethyl)-N-propylamine hydrochloride
CAS No. 195054-99-0 (free base)
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Pyrazolopyrimidines as CRF receptor antagonists
文献作者:Chen,C.; Webb,T.R.; McCarthy,J.R.; Moran,T.J.; Wilcoxen,K.M.(Janssen Pharmaceutica NV; Neurocrine Biosciences Inc.)
参考来源:EP 0880523; JP 2000503661; WO 9729109

DPC-696, SK-696, DMP-696

Chemical Name: 8-(2,4-Dichlorophenyl)-N-[2-methoxy-1-(methoxymethyl)ethyl]-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
CAS No. 202578-52-7
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Sq...
参考文献标题:Azolo triazines and pyrimidines
文献作者:Arvanitis,A.G.; Chorvat,R.J.(DuPont Pharmaceuticals Co.)
参考来源:US 6124289; WO 9803510

L-376062

Chemical Name: 2-[3-(Benzylsulfonamido)-6-methyl-2-oxo-1,2-dihydropyridin-1-yl]-N-[1-(N-tert-butylcarbamoylmethyl)-4-methyl-1H-imidazol-5-ylmethyl]acetamide
CAS No. 214152-91-7
项目整合开发状态: Preclin...
参考文献标题:Thrombin inhibitors
文献作者:Naylor-Olsen,A.M.; Newton,C.L.; Isaacs,R.C.A.; Dorsey,B.D.(Merck & Co.,Inc.)
参考来源:EP 0969840; US 5932606; WO 9842342

SN-429

Chemical Name: 1-(3-Amidinophenyl)-N-[2'-(sulfamoyl)biphenyl-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoroacetate
CAS No. 209954-53-0, 209954-52-9 (free base)
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Nitrogen containing heteroaromatics as factor Xa inhibitors
文献作者:Orwat,M.J.; Cacciola,J.; Han,Q.; Fevig,J.M.; Pinto,D.J.P.; Rossi,K.A.; Pruitt,J.R.; Quan,M.L.(DuPont Pharmaceuticals Co.)
参考来源:EP 0946508; WO 9828269

SN-116

Chemical Name: 1-(3-Amidinophenyl)-N-[5-[2-(sulfamoyl)phenyl]-2-pyrimidinyl]-3-methyl-1H-pyrazole-5-carboxamide
CAS No. 209954-79-0, 209955-63-5 (monotrifluoroacetate)
项目整合开发状态: Preclinical
项...
参考文献标题:Nitrogen containing heteroaromatics as factor Xa inhibitors
文献作者:Orwat,M.J.; Cacciola,J.; Han,Q.; Fevig,J.M.; Pinto,D.J.P.; Rossi,K.A.; Pruitt,J.R.; Quan,M.L.(DuPont Pharmaceuticals Co.)
参考来源:EP 0946508; WO 9828269

新产品编号:304253

Chemical Name: N-[1(S)-(4-Aminobenzyl)-2-(4-ethyl-1-piperidinyl)-2-oxoethyl]-4-[1(S)-benzyl-2-(2-hydroxyethoxy)ethylamino]pyridine-3-sulfonamide
CAS No. 200269-57-4
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Thrombin inhibitors
文献作者:Brundish,D.E.; Brown,L.N.; Le Grand,D.M.; Menear,K.A.; Smith,G.P.; Allen,M.C.; Butler,P.I.; Cockroft,X.-L.; Matthews,I.T.W.; Walker,C.V.; Wathey,W.B.(Novartis AG)
参考来源:WO 9746553

新产品编号:343803

Chemical Name: 4-[2,2-Dimethyl-4-(4-methylphenyl)-2H-naphtho[2,3-b]thiopyran-7-yl]benzoic acid
CAS No. 204449-02-5
项目整合开发状态: Preclinical
项目研究机构: Allergan (Originator)
合成路线:Condensation of ...
参考文献标题:Benzo[1,2-g]-chrom-3-ene and benzo[1,2-g]-thiochrom-3-ene derivatives
文献作者:Johnson,A.T.; Chandraratna,R.A.; Vuligonda,V.(Allergan,Inc.)
参考来源:EP 0948478; WO 9825875

L-766892

Chemical Name: 4-[3-(3-Cyclopentylpropyl)-2-oxo-1-imidazolidinyl]-N-[4-[2-[2(R)-hydroxy-2-(3-pyridinyl)ethylamino]ethyl]phenyl]benzenesulfonamide
CAS No. 173901-71-8, 173900-80-6 (undefined isomer)...
参考文献标题:Substd.sulfonamides as selective beta3 agonists for the treatment of diabetes and obesity
文献作者:Fisher,M.H.; Naylor,E.M.; Ok,D.; Weber,A.E.; Shih,T.; Ok,H.(Merck & Co.,Inc.)
参考来源:EP 0757674; JP 1997512275; US 5541197; US 5561142; WO 9529159

新产品编号:263121

Chemical Name: trans-3-[3-Methoxy-4-[2-(1-pyrrolidinyl)cyclohexyloxy]benzyl]-2-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]benzo[b]thiophen-6-ol
CAS No. 193961-76-1
项目整合开发状态: Biological Testing
项目研究机...
参考文献标题:Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4.SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[b]thiophenes
文献作者:Takeuchi,K.; Kohn,T.J.; Sall,D.J.; Denney,M.L.; McCowan,J.R.; Smith,G.F.; Gifford-Moore,D.S.
参考来源:Bioorg Med Chem Lett 1999,9(5),759

Dihydrocalanolide A-(+), (+)-Dihydrocalanolide A, NSC-678323

Chemical Name: (10R,11S,12S)-12-Hydroxy-6,6,10,11-tetramethyl-4-propyl-7,8,11,12-tetrahydro-2H,6H,10H-benzo[1,2-b:3,4-b':5,6-b'']tripyran-2-one
CAS No. 183904-53-2
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Calanolide antiviral cpds.,compsns.and uses ther
文献作者:Boyd,M.R.; Cardellina,J.H.II; Gustafson,K.R.; McMahon,J.B.; Fuller,R.W.; Cragg,G.M.; Kashman,Y.(US Department of Health & Human Services)
参考来源:EP 0633887; JP 1996502948; JP 1996507311; US 5591770; WO 9320082; WO 9428000