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

P-724

Chemical Name: 2(R)-(tert-Butoxycarbonylamino)-3-[3,7,11-trimethyl-2(E),6(E),10(E)-dodecatrienylthio]propyl-L-valyl-L-isoleucyl-L-methionine; tert-Butoxycarbonyl--L-(S-farnesyl)cysteinyl-psi(CH2NH)-L-...
参考文献标题:Cpds.for inhibition of proteolysis
文献作者:Rando,R.R.(Harvard College)
参考来源:WO 9401126

MEN-10700

Chemical Name: (+)-(5R,6S)-2-[N-(Carbamoylmethyl)-N-methylaminomethyl]-6-[1(R)-hydroxyethyl]-2-penem-3-carboxylic acid
CAS No. 156662-18-9, 156662-23-6 (monoNa salt)
项目整合开发状态: Preclinical
项目研...
参考文献标题:Penem derivs.,their preparation and pharmaceutical compsns.containing them
文献作者:Altamura,M.; Arcamone,F.M.; Perrotta,E.; Pestellini,V.; Sbraci,P.; Cascio,G.(Lusofarmaco; Menarini Industrie Farma Riunite Srl)
参考来源:EP 0660837; JP 1996501543; WO 9406803

SNAP-5150

Chemical Name: 2,6-Dimethyl-N3-[3-(4,4-diphenylpiperidin-1-yl)propyl]-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamide
CAS No. 166806-40-2, 166808-84-0 ((-)-enantiomer), 166808-83-9 ((+)-ena...
参考文献标题:Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate
文献作者:Cox,E.D.; Diaz-Arauzo,H.; Huang,Q.; Reddy,M.S.; Ma,C.; Harris,B.D.; McKernan,R.; Skolnick,P.; Cook,J.M.
参考来源:J Med Chem 1998,41(14),2643

KW-2170

Chemical Name: 5-(3-Aminopropylamino)-7,10-dihydroxy-2-(2-hydroxyethylaminomethyl)-6H-pyrazolo[4,5,1-de]acridin-6-one dihydrochloride
CAS No. 142853-45-0 (free base), 142853-70-1 (monoHCl)
项目整合开...
参考文献标题:Pyrazoloacridone derivs.
文献作者:Mimura,Y.; Shida,Y.; Kasai,M.; Ashizawa,T.; Gomi,K.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0487097; JP 1993001064; US 5220026

NSC-659687, NSC-D-659687, S-16020-2

Chemical Name: N-[2-(Dimethylamino)ethyl]-9-hydroxy-5,6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxamide dihydrochloride
CAS No. 156055-46-8 (free base)
项目整合开发状态: Phase II
项目研究机构: Servier (Or...
参考文献标题:Ellipticine derivs.with antitumor activity
文献作者:Bisagni,E.; Jasztold-Howorko,R.; Atassi,G.; Pierre,A.(ADIR et Cie.)
参考来源:EP 0591058; FR 2696465; JP 1994211852; US 5498611

Alatrofloxacin mesilate, CP-116517-27, CP-99219(L-Ala-L-Ala), L-Ala-L-Ala-CP-99219, CP-116517, Turvel, Trovan

Chemical Name: (alpha,alpha,alpha)-7-[6-(L-Alanyl-L-alanylamino)-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate
...
参考文献标题:Anti-bacterial azabicyclo quinolone carboxylic acids
文献作者:Brighty,K.E.(Pfizer Inc.)
参考来源:US 5229396

MDL-10222F(undefined isomer), MDL-101986

Chemical Name: (E)-N'-[4-(2-Chloro-1,2-diphenylvinyl)phenyl]-N,N-diethyl-1,2-ethanediamine citrate (1:1)
CAS No. 179552-06-8, 179552-05-7 (free base), 179552-10-4 (monoHCl), 155519-89-4 (undefined ...
参考文献标题:Non-metabolizable clomiphene analogs for treatment of tamoxifen-resistant tumors
文献作者:Bitonti,A.J.; Baumann,R.J.(Merrell Pharmaceuticals,Inc.)
参考来源:EP 0660821; JP 1997500863; WO 9406762

UK-147535

Chemical Name: 3-[3-[2-(4-Chlorophenylsulfonamido)ethyl]-5-(4-fluorobenzyl)phenyl]propionic acid
CAS No. 161777-76-0
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The reaction of ...
参考文献标题:Benzenealkanoic acids for cardiovascular diseases
文献作者:Dickinson,R.P.; Dack,K.N.; Steele,J.(Pfizer Inc.)
参考来源:EP 0662950; JP 1996502046; US 5618941; WO 9406761

Nortopixantrone hydrochloride, BBR-3438

Chemical Name: 2-[2-(2-Hydroxyethylamino)ethyl]-5-[2-(methylamino)ethylamino]indazolo[4,3-gh]isoquinolin-6(2H)-one dihydrochloride
CAS No. 156090-17-4 (free base)
项目整合开发状态: Phase II
项目研究机构: N...
参考文献标题:Synthesis and antitumor evaluation of 2,5-disubstituted-indazolo[4,3-gh]isoquinolin-6(2H)-ones (9-aza-anthrapyrazoles)
文献作者:Krapcho,A.P.; Menta,E.; Oliva,A.; Di Domenico,R.; Fiocchi,L.; Maresch,M.E.; Gallagher,C.E.; Hacker,M.P.; Beggiolin,G.; Giuliani,F.C.; Pezzoni,G.; Spinelli,S.
参考来源:J Med Chem 1998,41(27),5429

Topixantrone hydrochloride, BBR-3576, BBR-3409(dimaleate)

Chemical Name: 5-[2-(Dimethylamino)ethylamino]-2-[2-(2-hydroxyethylamino)ethyl]indazolo[4,3-gh]isoquinolin-6(2H)-one dihydrochloride
CAS No. 156090-18-5 (free base)
项目整合开发状态: Phase II
项目研究机构:...
参考文献标题:Synthesis and antitumor evaluation of 2,5-disubstituted-indazolo[4,3-gh]isoquinolin-6(2H)-ones (9-aza-anthrapyrazoles)
文献作者:Krapcho,A.P.; Menta,E.; Oliva,A.; Di Domenico,R.; Fiocchi,L.; Maresch,M.E.; Gallagher,C.E.; Hacker,M.P.; Beggiolin,G.; Giuliani,F.C.; Pezzoni,G.; Spinelli,S.
参考来源:J Med Chem 1998,41(27),5429