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

新产品编号:426067

Chemical Name: N-(2-Butylthieno[3,2-d]pyrimidin-4-yl)-N-cyclohexylamine hydrochloride
CAS No. 214416-93-0
项目整合开发状态: Preclinical
项目研究机构: Almirall Prodesfarma (Originator)
合成路线:This compound...
参考文献标题:Design,synthesis,and biological activities of new thieno[3,2-d]pyrimidines as selective type 4 phosphodiesterase inhibitors
文献作者:Crespo,M.I.; Pages,L.; Vega,A.; Segarra,V.; Lopez,M.; Domenech,T.; Miralpeix,M.; Beleta,J.; Ryder,H.; Palacios,J.M.
参考来源:J Med Chem 1998,41(21),4021

新产品编号:176111

Chemical Name: 4-[3-(4-Ethynylphenoxy)propyl]-1H-imidazole maleate
CAS No. 184027-09-6, 184027-08-5 (free base)
项目整合开发状态: Preclinical
项目研究机构: Bioprojet (Originator), INSERM (Originator)
合成...
参考文献标题:4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity
文献作者:Krause,M.; Ligneau,X.; Stark,H.; Garbarg,M.; Schwartz,J.C.; Schunack,W.
参考来源:J Med Chem 1998,41(21),4171

CGP-68730A

Chemical Name: 2-[9-Bromo-5,6-dioxo-2,3,6,7-tetrahydro-5H-[1,4]thiazino[4,3,2-de]quinoxalin-3(R)-yl]acetic acid sodium salt
CAS No. 177537-85-8 (free acid), 177537-84-7 (free acid, (S)-isomer), 177...
参考文献标题:Quinoxaline-2,3-diones with an oxa or thiaheterocyclic fused ring
文献作者:Moretti,R.; Zimmermann,K.(Novartis AG)
参考来源:CA 2157231; EP 0705835; JP 1996109185

SL-88.0338

Chemical Name: 2-[1-(3-Ethoxybenzoyl)piperidin-4-ylmethyl]-5,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline
CAS No. 214693-17-1
项目整合开发状态: Preclinical
项目研究机构: Sanofi-Aventis (Originator)
合成路线:R...
参考文献标题:Derivs.of 2-[(4-piperidinyl)methyl]-1,2,3,4-tetrahydroisoquinoline,their use in therapy
文献作者:George,P.; Sevrin,M.; Maloizel,C.; Tixidre,A.; Froissant,J.(Sanofi-Synthabo )
参考来源:AU 8929617; EP 0351255; JP 1990025481; US 4925850

BSF-190555, BTS-79018

Chemical Name: N-[7-Chloro-1,4-benzodioxan-2(S)-ylmethyl]-N-[1-(2-methoxyphenyl)piperidin-4-ylmethyl]amine
CAS No. 170353-17-0 (undefined isomer), 170352-95-1 (undefined isomer, HCl salt)
项目整合开发...
参考文献标题:Bicyclic aromatic cpds.as therapeutic agents
文献作者:Kerrigan,F.; Heal,D.J.; Martin,K.F.(The Boots Company plc)
参考来源:EP 0717739; JP 1997502431; US 5767116; WO 9507274

PD-161989

Chemical Name: 6-Methyl-7-nitro-5-(pyrrolidin-1-ylmethyl)quinoxaline-2,3(1H,4H)-dione
CAS No. 186268-07-5
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:2-Amino-6-methylbenzoic aci...
参考文献标题:Cyclic amine derivs.of substd.quinoxaline 2,3-diones as glutamate receptor antagonists
文献作者:Kornberg,B.E.; Nikam,S.; Rafferty,M.F.; Yuen,P.-W.(Pfizer Inc.)
参考来源:JP 1999506724; US 5874426; WO 9640650

ER-62899, E-2100

Chemical Name: N-[1-[1-[2-(4-Fluorophenyl)ethyl]piperidin-4-yl]indolin-6-ylmethyl]acetamide
CAS No. 214611-53-7
项目整合开发状态: Preclinical
项目研究机构: Eisai (Originator)
合成路线:Addition of methyl acr...
参考文献标题:1,4-Substd.cyclic amine derivs.
文献作者:Kimura,T.; Takahashi,K.; Matsunaga,M.; Kawano,K.; Kubota,A.; Kitazawa,N.; Okabe,T.; Ueno,K.; Komatsu,M.; Sasaki,A.(Eisai Co.,Ltd.)
参考来源:EP 0976732; WO 9843956

Gantacurium chloride, AV-430A, GW-0430, GW-280430A

Chemical Name: (Z)-2-Chlorofumaric acid 1-[3-[6,7-dimethoxy-2(S)-methyl-1(R)-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinolinium-2-yl]propyl] 4-[3-[6,7-dimethoxy-2(R)-methyl-1(S)-(3,4,5-trimetho...
参考文献标题:Bis- and mixed-tetrahydroisoquinolinium chlorofumarates: New ultra-short-acting nondepolarizing neuromuscular blockers
文献作者:Boros,E.E.; Bigham,E.C.; Boswell,G.E.; Mook,R.A.Jr.; Patel,S.S.; Savarese,J.J.; Ray,J.A.; Thompson,J.B.; Hashim,M.A.; Wisowaty,J.C.; Feldman,P.L.; Samano,V.
参考来源:J Med Chem 1999,42(2),206

A-177430

Chemical Name: (7S,8R,11S)-8-Isobutyl-N7-hydroxy-N11-methyl-9-oxo-2-oxa-10-azabicyclo[11.2.2]heptadeca-1(15),13,16-triene-7,11-dicarboxamide
CAS No. 210483-49-1
项目整合开发状态: Preclinical
项目研究机构: ...
参考文献标题:Macrocyclic inhibitors of matrix metalloproteinases and TNFalpha secretion
文献作者:Sheppard,G.S.; Guo,Y.; Siummers,J.B.; Holms,J.H.; Steinman,D.H.; Michaelides,M.R.; Florjancic,A.S.; Xu,L.; Davidsen,S.K.(Abbott Laboratories Inc.)
参考来源:EP 1021423; WO 9830551

MBX-36, SHU-9119

Chemical Name: N-Acetyl-L-norleucyl-L-aspartyl-L-histidyl-3-(2-naphthyl)-D-alanyl-L-arginyl-L-tryptophyl-L-lysinamide cyclic C-4.2-N-6.7-amide
CAS No. 168482-23-3
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Peptides having potent antagonist and agonist bioactivities at melanocortin receptors
文献作者:Hadley,M.E.; Hruby,V.J.; Sharma,S.D.(University of Arizona)
参考来源:US 5731408