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

Repinotan hydrochloride, X-3702, Bay-x-3702, Branosyn

1,2-苄异噻唑-3(2H)-1,2-[4-[[[[(2R)-3,4-二氢-2H-1-苯并吡喃-2-基]甲基]丁基,1,1-二氧化物Chemical Name: (-)-(R)-2-[4-[(3,4-Dihydro-2H-1-benzopyran-2-yl)methylamino]butyl]-1,2-benzisothiazol-3(2H)-one 1,1-dioxide monohydroch...
参考文献标题:Substd.amino methyl tetralines,and their heterocyclic analogous cpds
文献作者:Junge,B.; Schohe,R.; Seidel,P.-R.; Glaser,T.; Traber,J.; Benz,U.; Schuurman,T.; De Vry,J.-M.-V.(Bayer AG)
参考来源:EP 0352613; JP 1990096552; US 5137901; US 5506246

Arbutamine hydrochloride, GP-2-121-3, GenESA

1,2-苯二醇,4-[(1R)-1-羟基-2-[[4-(4-羟基苯基)丁基]氨基]乙基]-,盐酸盐(1:1) 阿布他明 Chemical Name: (R)-(-)-1-(3,4-Dihydroxyphenyl)-2-[4-(4-hydroxyphenyl)butylamino]ethanol hydrochloride
CAS No. 125251-66-3, 128470-16-6 (f...
参考文献标题:Diagnosis,evaluation & treatment of coronary artery disease by exercise simulation using closed loop drug delivery of an exercise simulating agent beta agonist
文献作者:Tuttle,R.R.; Browne III,C.E.(Sicor Inc.)
参考来源:EP 0329464; JP 1998276991; US 5108363

NSC-32122, SOAz

1,3,3,5,5-五氮丙啶基-1-硫杂-2,4,6-三氮杂-3,5-二膦咛-1-氧化物Chemical Name: 1,3,3,5,5-Pentaziridino-1-thia-2,4,6-triaza-3,5-diphosphorine 1-oxide; 1,3,3,5,5-Pentakis(1-aziridinyl)-3,3,5,5-tetrahydro-1H-1,2,4,6,3,5-thi...
参考文献标题:Inorganocyclic cpds.usable as medicaments and a process for their preparation
文献作者:Labarre,J.F.; Sournies,F.; Van der Grampel,J.; Van der Huizen,A.(ANVAR (Agence Natl.Valor.Rech.))
参考来源:EP 0022407

Neramexane hydrochloride, MRZ-2/279, MRZ-2/579

1,3,3,5,5-五甲基环己-1-胺盐酸盐Chemical Name: 1,3,3,5,5-Pentamethylcyclohexylamine hydrochloride
CAS No. 209185-99-9
项目整合开发状态: Phase III
项目研究机构: Merz (Originator), Forest (Licensee)
合成路线:Addition o...
参考文献标题:1-Amino-alkylcyclohexane NMDA receptor antagonists
文献作者:Kalvinsh,I.; Gold,M.; Parsons,C.G.R.; Jirgensons,A.; Klauss,V.(Merz Pharmaceuticals GmbH)
参考来源:JP 2002511873; WO 9901416

HMR-4902, KW-3902

1,3-二丙基-8-(3-正金刚烷基)黄嘌呤Chemical Name: 8-(Octahydro-2,5-methanopentalen-3a-yl)-1,3-dipropylxanthine; 1,3-Dipropyl-8-(2-nor-1-adamantyl)xanthine
CAS No. 136199-02-5
项目整合开发状态: Phase II
项目研究机构: Ky...
参考文献标题:Xanthine derivs
文献作者:Suzuki,F.; Shimada,J.; Kubo,K.; Ohno,T.; Karasawa,A.; Ishii,A.; Hiromi,N.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0386675; JP 1991173888; US 5068236

PD-116948, DPCPX, CPX

1,3-二丙基-8-环戊基黄嘌呤Chemical Name: 8-Cyclopentyl-1,3-dipropylxanthine; 8-Cyclopentyl-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione
CAS No. 102146-07-6
项目整合开发状态: Phase II
项目研究机构: SciClone (Orphan D...
参考文献标题:8-Aryl- and 8-cycloalkyl-1,3-dipropylxanthines: Further potent and selective antagonists for A1-adenosine receptors
文献作者:Shamim,M.T.; Ukena,D.; Padgett,W.L.; Hong,O.; Daly,J.W.
参考来源:J Med Chem 1988,31(3),613

Semaxanib, Semoxind, TSU-16, NSC-696819, SU-5416

1,3-二氢-3-[(3,5-二甲基-1H-吡咯-2-基)亚甲基]-2H-吲哚-2-酮Chemical Name: (Z)-3-(3,5-Dimethylpyrrol-2-ylmethylene)indolin-2-one
CAS No. 204005-46-9
项目整合开发状态: Phase II
项目研究机构: Sugen (Originator), Esteve (Lice...
参考文献标题:Indolinone cpds.for the treatment of disease
文献作者:Tang,P.C.; Sun,L.; McMahon,G.(Sugen,Inc.)
参考来源:EP 0769947; JP 2000026412; US 5780496; US 5792783; US 5880141; US 5883113; US 5883116; WO 9640116

CH-170, Chinoin-170

1,3-二甲基-7-[(5-甲基-1,2,4-恶二唑-3-基)甲基]-3,7-二氢-1H-嘌呤-2,6-二酮Chemical Name: 3-[(1,3-Dimethylxanthin-7-yl)methyl]-5-methyl-1,2,4-oxadiazole; 3,7-Dihydro-1,3-dimethyl-7-[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]-...
参考文献标题:Theophyllinyl-alkyl-oxadiazoles,process for the preparation thereof and pharmaceutical compositions containing same
文献作者:Korbonits,D.; et al.(Chinoin Pharmaceutical and Chemical Works Co.,Ltd.)
参考来源:EP 0089028; JP 59010586; US 4565817

K-7174

1,4-bis5-(3,4,5-三甲氧基苯)戊-4-烯-1-基-1,4-di氮杂庚烷Chemical Name: 1,4-Bis[5-(3,4,5-trimethoxyphenyl)-4(E)-pentenyl]hexahydro-1H-1,4-diazepine
CAS No. 191089-59-5, 191089-60-8 (diHCl)
项目整合开发状态: Preclinica...
参考文献标题:Cell adhesion inhibitor
文献作者:Nakao,H.; Umetani,M.; Suda,M.; Nagoya,T.(Kowa Co.,Ltd.)
参考来源:EP 0774257; JP 1997143075; US 5723465

Bay-k-8644

1,4-二氢-2,6-二甲基-5-硝基-4-(2-[三氟甲基]苯基)吡啶-3-羧酸甲酯Chemical Name: Methyl 2,6-dimethyl-3-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-5-carboxylate; 1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-(trifluorom...
参考文献标题:Dihydropyridines having a positive inotropic effect,novel compounds,their use in medicaments,and processes for their preparation
文献作者:Bossert,F.; Franckowiak,G.; Boeshagen,H.; Goldmann,S.; Schramm,M.; Thomas,G.; Meyer,H.; Towart,R.; Wehinger,E.(Bayer AG)
参考来源:BE 0893984; DE 3130041; ZA 8205456