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

DV-7751a

Chemical Name: 10-[8(S)-Amino-6-azaspiro[3.4]octan-6-yl]-9-fluoro-3(S)-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid hemihydrate
CAS No. 151390-79-3, 129321-78-4 (n...
参考文献标题:Synthesis and antibacterial activity of novel pyridobenzoxazine analogues
文献作者:Kawakami,K.; Ararashi,S.; Kimura,Y.; Takemura,M.; Hayakawa,I.
参考来源:Chem Pharm Bull 1998,46(11),1710

YM-31472

Chemical Name: 2-Butyl-4-(3,N-dimethyl-2-butenamido)-1-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]imidazole-5-carboxylic acid 1-(ethoxycarbonyloxy)ethyl ester
CAS No. 149586-24-3
项目整合开发状态: Precli...
参考文献标题:Studies on nonpeptide angiotensin II receptor antagonists.IV.Synthesis and biological evaluation of 4-acrylamide-1H-imidazole derivatives
文献作者:Okazaki,T.; Watanabe,T.; Kikuchi,K.; Suga,A.; Shibasaki,M.; Fujimori,A.; Inagaki,O.; Yanagisawa,I.
参考来源:Chem Pharm Bull 1998,46(6),973

DX-9065a

Chemical Name: 3-(7-Amidino-2-naphthyl)-2(S)-[4-[1-(1-iminoethyl)pyrrolidin-3(S)-yloxy]phenyl]propionic acid hydrochloride pentahydrate; (2S)-2-[4-[[(3S)-1-Acetamidoyl-3-pyrrolidinyl]oxy]phenyl]-3-(7-...
参考文献标题:Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors
文献作者:Nagahara,T.; Yokoyama,Y.; Inamura,K.; Katakura,S.; Komoriya,S.; Yamaguchi,H.; Hara,T.; Iwamoto,M.
参考来源:J Med Chem 1994,37(8),1200-7

100240, M-100240, MDL-100240

Chemical Name: (4S,7S,12bR)-7-[2(S)-(Acetylsulfanyl)-3-phenylpropionamido]-6-oxo-1,2,3,4,6,7,8,12b-octahydropyrido[2,1-a][2]benzazepine-4-carboxylic acid
CAS No. 142695-08-7
项目整合开发状态: Phase II 参考文献标题:Novel mercaptoacetylamide derivs.useful as inhibitors of enkephalinase and ACE
文献作者:Flynn,G.A.; Warshawsky,A.M.; Mehdi,S.; Bey,P.; Beight,D.W.; Giroux,E.L.; Burkholder,T.P.(Merrell Pharmaceuticals,Inc.)
参考来源:EP 0481522; JP 1992282382; US 5430145

HA-188, BMD-188

Chemical Name: cis-1-Hydroxy-4-(1-naphthyl)-6-octylpiperidin-2-one
CAS No. 149082-42-8, 149082-43-9 (trans-isomer)
项目整合开发状态: Preclinical
项目研究机构: Vanderbilt University (Originator), Wayne Stat...
参考文献标题:Cyclic hydroxamic acids
文献作者:Honn,K.V.; Johnson,C.R.; Chen,Y.-F.; Shimoji,K.; Marnett,L.J.(Vanderbilt University; Wayne State University)
参考来源:US 5234933; WO 9308803

Emivirine, MKC-442, Coactinon

Chemical Name: 6-Benzyl-1-(ethoxymethyl)-5-isopropyluracil; 6-Benzyl-1-(ethoxymethyl)-5-isopropylpyrimidine-2,4(1H,3H)-dione
CAS No. 149950-60-7
项目整合开发状态: Phase III
项目研究机构: Mitsubishi Chemica...
参考文献标题:Antiviral combinations of 2',3'-dideoxyribonucleosides with 6-benzyl-1-ethoxymethyl-5-substd.uracil derivs.
文献作者:Ubasawa,M.; Yuasa,S.(Mitsubishi Chemical Corp.)
参考来源:EP 0631783; JP 1995097324

NNC-19-1228

Chemical Name: N-(Benzothiazol-6-yl)carbamic acid 3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]propyl ester
CAS No. 150396-84-2 (oxalate salt(1:1))
项目整合开发状态: Preclinical
项目研究机构: Novo N...
参考文献标题:Chemical cpds.,their preparation and use
文献作者:Hansen,J.B.; Jeppesen,L.; Gr鴑vald,F.C.(Novo Nordisk A/S)
参考来源:EP 0679085; JP 1995502268; US 5378714; WO 9310742

NC-1800

Chemical Name: (5RS,1'SR)-5-Benzyl-3-[3-(4-morpholinyl)-1-phenylpropyl]oxazolidin-2-one monofumarate
CAS No. 173273-43-3, 161214-65-9 (free base), 161214-64-8 (racemic, (R*,R*)-isomer, free base), ...
参考文献标题:Synthesis of optically active NC-1800,a therapeutic agent for urinary disturbance
文献作者:Yoshida,S.; Yamamoto,M.; Mochizuki,N.; Nohira,H.
参考来源:Chem Pharm Bull 1999,47(8),1154

Plevitrexed, BGC-9331, ZD-9331, Vamidex

Chemical Name: 2(S)-[4-[N-(2,7-Dimethyl-4-oxo-3,4-dihydroquinazolin-6-ylmethyl)-N-(2-propynyl)amino]-2-fluorobenzamido]-4-(1H-tetrazol-5-yl)butyric acid
CAS No. 153537-73-6, 153537-74-7 ((R)-isomer...
参考文献标题:Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors
文献作者:Marsham,P.R.; Wardleworth,M.; Boyle,F.T.; Hennequin,L.F.; Kimbell,R.; Brown,M.; Jackman,A.L.
参考来源:J Med Chem 1999,42(19),3809

FK-778, HMR-1715, X-920715, MNA-715

Chemical Name: 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]hepta-2-en-6-ynamide
CAS No. 152418-67-2
项目整合开发状态: Phase II
项目研究机构: Aventis Pharma (Originator), Fujisawa (Licensee)
合成路线:FK-7...
参考文献标题:Cyano-2-hydroxy-3-enamide derivs.,process for their preparation,their use as drugs,pharmaceutical compsns.containing them and intermediates obtained
文献作者:Bartlett,R.R.; Kay,D.P.; Kuo,E.A.; Schleyerbach,R.; Schwab,W.(Aventis Pharma SA)
参考来源:EP 0551230; JP 1993310672; US 5308865