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

(S)-Bu-HIBO

Chemical Name: 2(S)-Amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid
CAS No. 204863-21-8
项目整合开发状态: Preclinical
项目研究机构: Lundbeck (Originator)
合成路线:Cyclization of oxoester (I) with aqu...
参考文献标题:Excitatory amino acid receptor ligands: Resolution,absolute stereochemistry,and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid
文献作者:Johansen,T.N.; Ebert,B.; Brauner-Osborne,H.; Didriksen,M.; Christensen,I.T.; Soby,K.K.; Madsen,U.; Krogsgaard-Larsen,P.; Brehm,L.
参考来源:J Med Chem 1998,41(6),930-939

PP1D-1

Chemical Name: N-(3-Chloro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)succinamic acid methyl ester
CAS No. 175090-76-3
项目整合开发状态: Preclinical
项目研究机构: China Medical College (Originator), National Tai...
参考文献标题:Synthesis and cytotoxicity of 1,2-disubstituted naphth[2,3-d]imidazole-4,9-diones and related compounds
文献作者:Kuo,S.-C.; Ibuka,T.; Huang,L.J.; Lien,J.C.; Yean,S.R.; Huang,S.C.; Lednicer,D.; Morris-Natschke,S.L.; Lee,K.H.
参考来源:J Med Chem 1996,39(7),1447-1451

LF-16.0335

Chemical Name: 4-[4-[1-[2,4-Dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)phenylsulfonyl]pyrrolidin-2(S)-ylcarbonyl]piperazin-1-ylcarbonyl]benzamidine dihydrochloride
CAS No. 202720-59-0, 202602-3...
参考文献标题:N-Benzenesulphonyl-L-proline derivs.as bradykinin B2 agonists
文献作者:Dodey,P.; Bondoux,M.; Houziaux,P.; Barth,M.; Ou,K.(Laboratoires Fournier SA)
参考来源:EP 0925295; US 6071917; WO 9803503

DR-4004

Chemical Name: 2a-[4-(4-Phenyl-1,2,3,6-tetrahydropyridin-1-yl)butyl]-1,2,2a,3,4,5-hexahydrobenz[cd]indol-2-one
CAS No. 201608-41-5
项目整合开发状态: Preclinical
项目研究机构: Meiji Seika (Originator)
合成...
参考文献标题:Tetrahydrobenzindoles: Selective antagonists of the 5-HT7 receptor
文献作者:Kikuchi,C.; Nagaso,H.; Hiranuma,T.; Koyama,M.
参考来源:J Med Chem 1999,42(4),533

YM-268

Chemical Name: 5,5'-Methylenebis(1,4-phenylene)bismethylenebis(thiazolidine-2,4-dione)
CAS No. 141716-96-3
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:Diazotization of 4,4'-...
参考文献标题:Bisheterocyclic cpd.
文献作者:Niigata,K.; Takahashi,T.; Iwaoka,K.; Yoneda,T.; Noshiro,O.; Koike,R.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0533933; JP 1992511153; WO 9200967

TP-1202

Chemical Name: 1-[4-[4-(Diphenylmethyl)piperazin-1-yl]-3(S)-(1H-indol-2-ylcarboxamido)-4-oxobutyl]-1,2,3-triazole-5-carboxylic acid
CAS No. 178612-35-6
项目整合开发状态: Preclinical
项目研究机构: Tobishi (...
参考文献标题:Amino acid deriv.having anti-CKK activity
文献作者:Ogawa,M.; Morita,T.; Matsuda,K.; Iibuchi,N.; Kidokoro,S.(Tobishi Pharmaceutical Co.)
参考来源:EP 0710661; JP 1996119940; JP 1996176144; US 5716958

Brostallicin hydrochloride, PNU-166196

Chemical Name: 2-[4-[4-[4-[4-(2-Bromo-2-propenamido)-1-methylpyrrol-2-ylcarboxamido]-1-methylpyrrol-2-ylcarboxamido]-1-methylpyrrol-2-ylcarboxamido]-1-methylpyrrol-2-ylcarboxamido]ethylguanidine hydro...
参考文献标题:Acryloyl substd.distamycin derivs.,process for preparing them,and their use as antitumor and antiviral agents
文献作者:Cozzi,P.; Beria,I.; Biasoli,G.; Caldarelli,M.; Capolongo,L.; Franzetti,C.(Pharmacia & Upjohn AB)
参考来源:WO 9804524

SK-1080, KR-31080

Chemical Name: 2-Butyl-5-methyl-6-(1-oxido-2-pyridinyl)-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-3H-imidazo[4,5-b]pyridine
CAS No. 174800-22-7
项目整合开发状态: Preclinical
项目研究机构: Korea Res. Ins...
参考文献标题:Pyridyl imidazole derivs.and processes for the preparation thereof
文献作者:Kim,N.J.; Seo,H.W.; Lee,S.H.; Shin,W.S.; Yi,K.Y.; Yoo,S.E.; Chan,O.J.; Jung,Y.S.; Lee,H.S.; Shin,Y.A.; Lee,B.H.; Kim,H.R.; Kim,S.J.; Suh,J.H.(Korea Research Institute of Chemical Technology)
参考来源:WO 9534564

新产品编号:291597

Chemical Name: 3-[2-(1-Piperidinyl)ethyl]-6-propylbenzothiazol-2(3H)-one
CAS No. 198056-28-9
项目整合开发状态: Preclinical
项目研究机构: National Institutes of Health (Originator), Universit?degli Studi di...
参考文献标题:Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives
文献作者:Ucar,H.; Van Derpoorten,K.; Cacciaguerra,S.; Spampinato,S.; Stables,J.P.; Depovere,P.; Isa,M.; Masereel,B.; Delarge,J.; Poupaert,J.H.
参考来源:J Med Chem 1998,41(7),1138

新产品编号:568447

Chemical Name: 1-(3-Bromo-4,5-dimethoxyphenyl)-5-chloro-3-[4-(2-hydroxyethyl)piperazin-1-ylcarbonyl]naphthalene-2-carboxylic acid methyl ester hydrochloride
CAS No. 225516-92-7
项目整合开发状态: Biologi...
参考文献标题:1-Arylnaphthalene lignan: A novel scaffold for type 5 phosphodiesterase inhibitor
文献作者:Ukita,T.; nakamura,Y.; Kubo,A.; Yamamoto,Y.; Takahashi,M.; Kotera,J.; Ikeo,T.
参考来源:J Med Chem 1999,42(7),1293