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

KT-8391, CEP-2563

化合物 T2Chemical Name: L-Lysyl-beta-alanine 9(S),12(R)-Epoxy-10(S)-methoxy-9-methyl-1-oxo-2,3,9,10,11,12-hexahydro-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-10-ylmethyl ester dih...
参考文献标题:Bis-staurosporine and K-252a derivs.
文献作者:Lewis,M.E.; Neff,N.; Roberts-Lewis,J.; Murakata,C.; Saito,H.; Matsuda,Y.; Kauer,J.C.(Cephalon,Inc.; Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0651754; EP 0768312; JP 1996501081; US 5461146; WO 9402488

ME-3221

化合物 T28009Chemical Name: 3-Methoxy-2,6-dimethyl-4-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethoxy]pyridine
CAS No. 139958-16-0
项目整合开发状态: Phase I
项目研究机构: Meiji Seika (Originator)
合成路线:The conden...
参考文献标题:Pyridine derivs.with angiotensin II antagonism
文献作者:Katano,K.; Ogino,H.; Shitara,E.; Watanabe,H.; Nagura,J.; Osada,N.; Ichimaru,Y.; Konno,F.; Machinami,T.; Tsuruoka,T.(Meiji Seika Kaisha,Ltd.)
参考来源:EP 0487745; US 5399566; WO 9119697

SB-235699, HEP-689

化合物 T28684Chemical Name: 4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]pyridine
CAS No. 180869-32-3
项目整合开发状态: Phase I
项目研究机构: GlaxoSmithKline (Originator), Leo (Licensee)
合成路线:B...
参考文献标题:Certain 1,4,5-tri-substd.imidazole cpds.useful as cytokine
文献作者:Adams,J.L.; Gallagher,T.F.; Garigipati,R.S.; Boehm,J.C.; Sisko,J.; Peng,Z.-Q.; Lee,J.C.-L.(SmithKline Beecham plc)
参考来源:EP 0809499; JP 1998512555; US 5593992; WO 9621452

TAK-187

化合物 T28914Chemical Name: 2-[2(R)-(2,4-Difluorophenyl)-2-hydroxy-1(R)-methyl-3-(1,2,4-triazol-1-yl)propyl]-4-[4-(2,2,3,3-tetrafluoropropoxy)phenyl]-3,4-dihydro-2H-1,2,4-triazol-3-one
CAS No. 155432-...
参考文献标题:Azole cpds.,their production and use
文献作者:Itoh,K.; Okonogi,K.; Tamura,N.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0567982; US 5371101

ABT-255

化合物 T29527Chemical Name: (1S,6S)-1-Cyclopropyl-8-(2,8-diazabicyclo[4.3.0]octan-8-yl)-7-fluoro-9-methyl-4-oxo-4H-quinolizine-3-carboxylic acid hydrochloride
CAS No. 186293-38-9 (free base)
项目整合开发...
参考文献标题:Quinolizinone type cpds.
文献作者:Chu,D.T.; Li,Q.; Cooper,C.S.; Fung,A.K.L.; Lee,C.M.; Plattner,J.J.; Ma,Z.; Wang,W.-B.(Abbott Laboratories Inc.)
参考来源:EP 0871628; JP 1999510478; WO 9639407

BMS-194449

化合物 T30502Chemical Name: N-[5-[2-[Bis[4-(difluoromethoxy)phenyl]methylamino]-1(R)-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide
CAS No. 170686-12-1, 170687-34-0 (trifluoroacetate salt)
项目整合开发...
参考文献标题:Catecholamine surrogates useful as B3 agonists
文献作者:Washburn,W.N.; Girotra,R.N.; Sher,P.M.; Mikkilineni,A.B.; Poss,K.M.; Mathur,A.; Gavai,A.; Bisacchi,G.S.(Bristol-Myers Squibb Co.)
参考来源:CA 2138675; EP 0659737; JP 1995206806; US 5776983

L-732531

化合物 T32504Chemical Name: [1R,9S,12S(1'R,3'R,4'R),13R,14S,17R,21S,23S,24R,25S,27R]-17-Ethyl-1,14-dihydroxy-12-[2-[4-[1-(2-hydroxyethyl)-1H-indol-5-yloxy]-3-methoxycyclohexyl]-1-methylvinyl]-23,25-dimet...
参考文献标题:O-Heteroaryl,O-alkylheteroaryl,O-alkenylheteroaryl and O-alkynylheteroaryl macrolides
文献作者:Sinclair,P.J.; Goulet,M.; Wong,F.; Parsons,W.H.; Goulet,J.; Wyvratt,M.J.(Merck & Co.,Inc.)
参考来源:EP 0532088; JP 1994116274; US 5252732; WO 9305058

Pivalopril, Pivopril, USV 3659(S), RHC 3659(S), REV 3659(S)

匹伏普利Chemical Name: (-)-(S)-N-Cyclopentyl-N-[3-(2,2-dimethyl-1-oxopropyl)thio]-2-methyl-1-oxopropyl]glycine
CAS No. 81045-50-3
项目整合开发状态: Clinical
项目研究机构: Revlon (Originator)
合成路线:The reacti...
参考文献标题:Pivopril
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1986,11(2),116

Pitavastatin calcium, Itavastatin calcium, Nisvastatin, NKS-104, NK-104, Livalo

匹伐他汀钙匹伐他汀匹伐他汀内酯Chemical Name: (3R,5S)-7-[2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxy-6(E)-heptenoic acid calcium salt (2:1)
CAS No. 147526-32-7, 147511-69-1 (free acid), 141750-6...
参考文献标题:Optically active ?*-diketo acid esters and their reduced forms
文献作者:Guntor,B.; Kaiyama,T.; Arai,K.; Minami,T.; Suzuki,M.; Kobara,Y.; Sakota,R.(Nissan Chemical Industry,Ltd.; Sagami Chemical Research Center)
参考来源:JP 1994025092

Pivagabine, Tonerg

匹伐加宾Chemical Name: 4-Pivalamidobutyric acid; 4-(2,2-Dimethylpropionamido)butanoic acid
CAS No. 69542-93-4
项目整合开发状态: Withdrawn
项目研究机构: Angelini (Originator)
合成路线:Pivagabine is prepared by r...
参考文献标题:Pivagabine
文献作者:Esposito,G.; Lazzarini,R.
参考来源:Drugs Fut 1998,23(4),390