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

ER-38930

Chemical Name: 4-[5-(1,5-Diisopropylpyrazol-3-yl)-1H-pyrrol-2-yl]benzoic acid
CAS No. 187402-44-4
项目整合开发状态: Biological Testing
项目研究机构: Eisai (Originator)
合成路线:Condensation of 3-methyl-2-bu...
参考文献标题:Novel retinoic acid receptor alpha agonists: Syntheses and evaluation of pyrazole derivatives
文献作者:Kikuchi,K.; Hibi,S.; Yoshimura,H.; Tai,K.; Hida,T.; Tokuhara,N.; Yamauchi,T.; Nagai,M.
参考来源:Bioorg Med Chem Lett 2000,10(7),619

ME-3229

Chemical Name: 2,2'-[4-[2-(4,5,6,7-Tetrahydrothieno[3,2-c]pyridin-2-ylcarboxamido)acetyl]-1,2-phenylene]bis(oxy)bis(acetic acid) dibutyl ester
CAS No. 165949-40-6, 165949-41-7 (monotrifluoroacetate...
参考文献标题:Novel cpd.with platelet aggregation inhibitor activity
文献作者:Katano,K.; Ohugichi,S.; Shitara,E.; Shimizu,M.; Yaegashi,K.; Miura,T.; Isomura,Y.; Iida,H.; Ishikawa,M.; Asai,K.; Hatsushiba,E.; Kawaguchi,M.; Tsuruoka,T.(Meiji Seika Kaisha,Ltd.)
参考来源:JP 1995520876; US 5594004; US 5698692; WO 9421599

KB-R9032, KBR-9032

Chemical Name: N2-(4-Isopropyl-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-ylcarbonyl)guanidine methanesulfonate
CAS No. 179950-68-6
项目整合开发状态: Preclinical
项目研究机构: Kanebo (Originator) 参考文献标题:Synthesis and quantitative structure-activity relationships of N-(3-oxo-3,4-dihydro-2H-benzo[1,4]oxazine-6-carbonyl)guanidines as Na/H exchange inhibitors
文献作者:Yamamoto,T.; Hori,M.; Watanabe,I.; Tsutsui,H.; Harada,K.; Ikeda,S.; Maruo,J.; Morita,T.; Ohtaka,H.
参考来源:Chem Pharm Bull 1998,46(11),1716

FR-183998

Chemical Name: N-(Diaminomethylene)-4-(2,5-dichlorothiophen-3-yl)-N'-[2-(dimethylamino)ethyl]isophthalamide dihydrochloride; 2-[5-(2,5-Dichlorothiophen-3-yl)-3-[N-[2-(dimethylamino)ethyl]carbamoyl]ben...
参考文献标题:Benzoylguanidine derivs.as medicaments
文献作者:Kuno,A.; Mizuno,H.; Yamasaki,K.; Inoue,Y.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:JP 1998503770; WO 9604241

H-2545, A-2545

Chemical Name: 2,2,5,5-Tetramethyl-N-(3-phthalimidopropyl)-2,5-dihydro-1H-pyrrole-3-carboxamide hydrochloride
CAS No. 93799-37-2 (free base)
项目整合开发状态: Preclinical
项目研究机构: Alkaloida (Originato...
参考文献标题:New alkyl diamine derivatives
文献作者:Bodi,I.; Csak,J.; Frank,L.; Hankovszky,O.H.; Hideg,K.(Alkaloida Chemical Co.Ltd.)
参考来源:EP 0134225; JP 1985500669; US 4703056; US 5028609; US 5032600; WO 8402907

MS-180

Chemical Name: (-)-2-[6-[4-(4-Morpholinylcarbonimidoyl)benzamido]-3,4-dihydro-2H-1-benzopyran-3(S)-yl]acetic acid ethyl ester hydrochloride
CAS No. 188350-51-8, 188349-93-1 (undefined isomer)
项目...
参考文献标题:New platelet fibrinogen receptor glycoprotein IIb-
文献作者:Okumura,K.; Shimazaki,T.; Aoki,Y.; Yamashita,H.; Tanaka,E.; Banba,S.; Yazawa,K.; Kibayashi,K.; Banno,H.
参考来源:J Med Chem 1998,41(21),4036

FR-167344

Chemical Name: (E)-N-[N-[3-(3-Bromo-2-methylimidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichlorophenyl]-N-methylcarbamoylmethyl]-4-(N,N-dimethylcarbamoyl)cinnamamide hydrochloride
CAS No. 188550-14-3,...
参考文献标题:A novel class of orally active non-peptide bradykinin B2 receptor antagonists.2.Overcoming the species difference between guinea pig and man
文献作者:Abe,Y.; Kayakiri,H.; Satoh,S.; Inoue,T.; Sawada,Y.; Inamura,N.; Asano,M.; Hatori,C.; Sawai,H.; Oku,T.; Tanaka,H.
参考来源:J Med Chem 1998,41(21),4053

RB-360-II

Chemical Name: [3(R)-(1H-Indol-3-ylmethyl)-3-methyl-2,5-dioxo-1,3-diazacyclotridec-13(S)-ylcarbonyl]-L-aspartyl-L-phenylalaninamide
CAS No. 187454-95-1
项目整合开发状态: Preclinical
项目研究机构: INSERM (O...
参考文献标题:Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor
文献作者:Blommaert,A.G.S.; Dhotel,H.; Ducos,B.; Durieux,C.; Goudreau,N.; Bado,A.; Garbay,C.; Roques,B.P.
参考来源:J Med Chem 1997,40(5),647-658

ISA-13-1

Chemical Name: 2-(2-Aminopyrimidinium-1-yl)ethylidenediphosphonic acid inner salt
CAS No. 188246-51-7
项目整合开发状态: Preclinical
项目研究机构: Yissum (Originator)
合成路线:The title compound was synthesi...
参考文献标题:Synthesis and preclinical pharmacology of 2-(2-aminopyrimidino) ethylidene-1,1-bisphosphonic acid betaine (ISA-13-1) - A novel biphosphonate
文献作者:Cohen,H.; Alferiev,I.S.; Monkkonen,J.; Seibel,M.J.; Pinto,T.; Ezra,A.; Solomon,V.; Stepensky,D.; Sagi,H.; Ornoy,A.; Patlas,N.; Hagele,G.; Hoffman,A.; Breuer,E.; Golomb,G.
参考来源:Pharm Res 1999,16(9),1399

XQ-443, DMP-851

Chemical Name: (4R,5S,6S,7R)-1-(3-Amino-1H-indazol-5-ylmethyl)-4,7-dibenzyl-3-butyl-5,6-dihydroxyperhydro-1,3-diazepin-2-one
CAS No. 188978-02-1
项目整合开发状态: Phase I
项目研究机构: Bristol-Myers Squibb...
参考文献标题:Design and selection of DMP 850 and DMP 851: The next generation of cyclic urea HIV protease inhibitors
文献作者:Rodgers,J.D.; Lam,P.Y.S.; Johnson,B.L.; Wang,H.; Li,R.; Ru,Y.; Ko,S.S.; Seitz,S.P.; Trainor,G.L.; Anderson,P.S.; Klabe,R.M.; Bacheler,L.T.; Cordova,B.; Garber,S.; Reid,C.; Wright,M.R.; Chang,C.-H.; Erickson-Viitanen,S.
参考来源:Chem Biol 1998,5(10),597