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

BPDZ-216, NNC-55-9216

Chemical Name: 3-(Isopropylamine)-7-methoxy-4H-1,2,4-benzothiadiazine 1,1-dioxide
CAS No. 201224-35-3
项目整合开发状态: Biological Testing
项目研究机构: Novo Nordisk (Originator)
合成路线:The target thiadia...
参考文献标题:1,2,4-Benzothiadiazine derivs.their preparation and use
文献作者:Pirotte,B.; Lebrun,P.; De Tullio,P.; Somers,F.; Delarge,J.; Hansen,J.B.; Nielsen,F.E.; Hansen,H.C.; Mogensen,J.P.; Tagmose,T.M.(Novo Nordisk A/S)
参考来源:EP 0906297; JP 2000512641; US 6242443; WO 9749692

INS-48848

Chemical Name: N-(1-Oxo-2,3,4,9-tetrahydro-1H-beta-carbolin-6-yl)carbamic acid methyl ester; N-(1-Oxo-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-6-yl)carbamic acid methyl ester
CAS No. 393835-84-2 参考文献标题:Method for reducing intraocular pressure using indole derivs.
文献作者:Yerxa,B.R.; Peterson,W.M.; Pintor,J.J.; Peral,M.A.; Plourde,R.Jr.; Brown,E.G.(Inspire Pharmaceuticals,Inc.; Universidad Complutense de Madrid)
参考来源:WO 0209702

RO-3202904

Chemical Name: 4-[4-[N-[1(S)-Methyl-2-[4-(methylsulfonyl)phenyl]ethyl]-N-propylamino]butyl]perhydrodiazepin-5-one
CAS No. 376579-95-2 (diHCl)
项目整合开发状态: Preclinical
项目研究机构: Amgen (Originator),...
参考文献标题:Substd.1-aminoalkyl-lactams and their use as muscarinic receptor antagonists
文献作者:Maag,H.; Fisher,L.E.; Prince,A.; Repke,D.B.; Dvorak,C.A.; Harris,R.N.III; Green,K.L.; Stabler,R.S.(F.Hoffmann-La Roche AG)
参考来源:JP 2003534330; US 2002004501; US 6667301; WO 0190081

RG-1103

Chemical Name: 1-(4-Benzylpiperidin-1-yl)-1-(6-hydroxy-1H-benzimidazol-2-yl)methanone
CAS No. 420136-91-0
项目整合开发状态: Preclinical
项目研究机构: Gedeon Richter (Originator)
合成路线:Treatment of the N-...
参考文献标题:Amine derivs.as NMDA receptor antagonists
文献作者:Nagy,J.; Domany,G.; Farkas,S.; Borza,I.; Horvath,C.; Bartane Szalai,G.; Kolok,S.(Gedeon Richter Ltd.)
参考来源:WO 0234718

BGC-20-1178, RS-1178

Chemical Name: 5-Methyl-8-(1-phenylethyl)-7,8-dihydro-6H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-a]pyrimidine
CAS No. 62052-82-8
项目整合开发状态: Preclinical
项目研究机构: BTG (Proprietary), Sankyo (Originator)...
参考文献标题:Pyrrolotriazolopyrimidine derivs.and process for the preparation thereof
文献作者:Takagi,H.; Sato,Y.; Shimoji,Y.; Kumakura,S.(Sankyo Co.,Ltd.)
参考来源:US 4007189

S-34176, S-34176-1

Chemical Name: N-tert-Butyl-N-[(Z)-2-[4-(trifluoromethyl)phenyl]-1H-imidazol-4-ylmethylene]amine N-oxide; N-tert-Butyl-alpha-[2-[4-(trifluoromethyl)phenyl]-1H-imidazol-4-yl]nitrone
CAS No. 252988-2...
参考文献标题:Nitrone derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Dhainaut,A.; Lestage,P.; Lockhart,B.; Tizot,A.; Goldstein,S.(ADIR et Cie.)
参考来源:CA 2274621; EP 0967207; FR 2780404; JP 2000026428; US 6034250

(-)-cis-MR-22, (-)-MR-22

Chemical Name: (-)-cis-2-[N-(1-Adamantyl)-N-methylaminomethyl]-1-phenylcyclopropanecarboxylic acid methyl ester
CAS No. 290342-29-9
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Cata...
参考文献标题:Substituted 1-phenyl-2-cyclopropylmethylamines with high affinity and selectively for sigma sites
文献作者:Ronsisvalle,G.; Marrazzo,A.; Prezzavento,O.; Pasquinucci,L.; Falcucci,B.; Di Toro,R.D.; Spampinato,S.
参考来源:Bioorg Med Chem 2000,8(6),1503

A-349821

Chemical Name: 1-[4'-[3-[2(R),5(R)-Dimethylpyrrolidin-1-yl]propoxy]biphenyl-4-yl]-1-(4-morpholinyl)methanone
CAS No. 372513-99-0
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Fisc...
参考文献标题:Aminoalkoxybiphenyl carboxamides as histamine-3 receptor ligands and their therapeutic applications
文献作者:Faghih,R.; Bennani,Y.L.(Abbott Laboratories Inc.)
参考来源:US 6316475; WO 0240461

S-35836-1

Chemical Name: N,N-Dimethylcarbamic acid 2-[1-(dimethylamino)cyclopropyl]ethyl ester fumarate
CAS No. 387844-54-4, 387844-53-3 (free base)
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator) 参考文献标题:1,1- And 1,2-disubstd.cyclopropanes,process for their preparation and pharmaceutical compsns.thereof
文献作者:Guillonneau,C.; Lestage,P.; Charton,Y.; Lockhart,B.; Goldstein,S.(Servier Laboratoires)
参考来源:EP 1170281; FR 2810664; JP 2002069046; US 2002022643

新产品编号:258375

Chemical Name: 16alpha,17alpha-[(R)-Butylidenedioxy]-6alpha,9-difluoro-11beta-hydroxy-21-[2-oxotetrahydrofuran-3(S)-ylsulfanyl]pregn-4-ene-3,20-dione
CAS No. 193408-42-3
项目整合开发状态: Biological Tes...
参考文献标题:21-(2-Oxo-tetrahydrofuran)-thio pregnane derivs.,a process for their production and pharmaceutical compsns.containing them
文献作者:Farrell,R.M.; Biggadike,K.(Glaxo Wellcome Inc.)
参考来源:US 6013244; WO 9724367