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

FP-21399

2,7-萘二硫尼酸,5-[(2,3-二氯苯酰)氨基]-3-[2-[4-[2-[8-[(2,4-二氯苯甲酰)氨基]-1-羟基-3,6-二硫-2-萘基]二唑基]-2,5-二甲氧基苯基]-4-羟基-,钠盐(1:4)Chemical Name: 5-(2,4-Dichlorobenzamido)-3-[2-[4-[2-[8-(2,3-dichlorobenzamido)-1-oxo-3,6-disulfo...
参考文献标题:Bisazo cpds.
文献作者:Mori,H.; Ogawa,T.; Yamazaki,S.; Satoh,H.; Kitaguchi,H.; Nishikawa,N.; Xu,H.; Izushi,T.(Fuji Photo Film Co.,Ltd.)
参考来源:EP 0747449; US 5717080; WO 9523189

N20C

2-[(3,3-二苯基丙基)氨基]-乙酰胺Chemical Name: N2-(3,3-Diphenylpropyl)glycinamide
CAS No. 76991-05-4
项目整合开发状态: Preclinical
项目研究机构: CSIC (Originator), Fundaci髇 Valenciana Invest Biom閐icas (Originator), U...
参考文献标题:Pharmaceutical for treatment of neurological and neuropsychiatric disorders
文献作者:Ognyanov,V.I.; Borden,L.; Bell,S.C.; Zhang,J.(NPS Allelix Corp.)
参考来源:EP 1014966; JP 2002515037; US 6191165; WO 9745115

Omiloxetine hydrochloride

2-[(3R,4S)-3-[(1,3-苯二氧并二氧醇-5-酰氧基)甲基]-4-(4-氟苯基)哌啶-1-基]-1-(4-氟苯尼)乙醇Chemical Name: trans-2-[3-(1,3-Benzodioxol-5-yloxymethyl)-4-(4-fluorophenyl)piperidin-1-yl]-1-(4-fluorophenyl)-1-ethanone hydrochloride...
参考文献标题:Process for preparing (-)-trans-N-p-fluorobenzoylmethyl-4-(p-fluorophenyl)-3-[[3,4-(methylenedioxy)phenoxy]methyl]piperidine
文献作者:Sacristan,A.; Ortiz,J.A.; Foguet,R.; Gubert,S.(Ferrer Internacional SA)
参考来源:US 5973155; WO 9731915

Exisulind, Aposulind, Sulindac sulfone, FGN-1, Aptosyn, FGN-1, Prevatac(former Brand Name)

2-[(3Z)-6-氟-2-甲基-3-[(4-甲基磺酰基苯基)亚甲基]茚-1-基]乙酸Chemical Name: (Z)-5-Fluoro-2-methyl-1-[4-(methylsulfonyl)benzylidene]-1H-indene-3-acetic acid
CAS No. 59973-80-7
项目整合开发状态: Phase III
项目研究机构: OSI (O...
参考文献标题:A method for treating patients with acne by administering a cyclic GMP PDE inhibitor
文献作者:Mayle,M.J.; Menander,K.B.(Cell Pathways,Inc.)
参考来源:WO 0044372

OCX-0191, OCX-191, 3-AP, Triapine

2-[(3-氨基吡啶-2-基)亚甲基]氨基硫脲Chemical Name: 3-Aminopyridine-2-carboxaldehyde thiosemicarbazone
CAS No. 143621-35-6
项目整合开发状态: Phase II
项目研究机构: Yale University (Originator), Pason (Licensee), Vion (L...
参考文献标题:2-Formylpyridine thiosemicarbazone derivs.,their preparation and their use as antitumor agents
文献作者:Sartorelli,A.C.; Lin,T.-S.(Yale University)
参考来源:EP 0570294; JP 1994128230; US 5281715; US 5721259

Unifiram, DM-232

2-[(4-氟苯基)磺酰基]六氢吡咯并[1,2-A]吡嗪-6(2H)-酮Chemical Name: (8aR)-2-(4-Fluorophenylsulfonyl)perhydropyrrolo[1,2-a]pyrazin-6-one
CAS No. 272786-64-8 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Uni...
参考文献标题:Design,synthesis,and preliminary pharmacological evaluation of 1,4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents
文献作者:Manetti,D.; Ghelardini,C.; Bartolini,A.; Bellucci,C.; Dei,S.; Galeotti,N.; Gualtieri,F.; Romanelli,M.N.; Scapecchi,S.; Teodori,E.
参考来源:J Med Chem 2000,43(10),1969

M-6434

2-[(5-氯-2-甲氧基苯基)氮杂]-1H-咪唑Chemical Name: 2-[(5-Chloro-2-methoxyphenyl)azo]-1H-imidazole
CAS No. 77636-92-1, 77636-84-1 (monoHCl)
项目整合开发状态: Phase II
项目研究机构: Mochida (Originator)
合成路线:The dia...
参考文献标题:Compsns.containing azo cpds.and use thereof for therapeutic treatment
文献作者:Mochida,E.; Suzuki,Y.; Onishi,H.; Kosuzume,H.(Mochida Pharmaceutical Co.,Ltd.)
参考来源:GB 2057874

Talopterin, NSC-712783(NH3 salt), NSC-633713, PT-523, Ndelta-Hemiphthaloyl-APA-Orn

2-[[(4S)-4-羧基-4-[[4-[(2,4-二氨基蝶啶-6-基)甲基氨基]苯甲酰基]氨基]丁基]氨基甲酰]苯甲酸Chemical Name: Nalpha-(4-Amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl-L-ornithine
CAS No. 113857-87-7
项目整合开发状态: Phase I
项目研究机构: Hudso...
参考文献标题:Methotrexate analogues.33.Ndelta-Acyl-Nalpha-(4-amino-4-deoxypteroyl)-L-ornithine derivatives: Synthesis and in vitro antitumor activity
文献作者:Rosowsky,A.; et al.
参考来源:J Med Chem 1988,311332-7

Meclinertant, Reminertant, SR-48692

2-[[[1-(7-氯-4-喹啉)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-三环[3.3.1.13,7]癸烷-2-羧酸Chemical Name: 2-[1-(7-Chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-ylcarboxamido]adamantane-2-carboxylic acid
CA...
参考文献标题:Amido-3-pyrazole derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Boigegrain,R.; Gully,D.; Jeanjean,F.; Molimard,J.-C.(Sanofi-Synthabo )
参考来源:EP 0477049; FR 2665898; JP 1992244065; US 5420141; US 5607958; US 5616592; US 5635526; US 5744491; US 5744493

Rafabegron, TAK-677, AJ-9677, AD-9677

2-[[3-[(2R)-2-[[(2R)-2-(3-氯苯基)-2-羟基-乙基]氨基]丙基]-1H-吲哚-7-基]氧基]乙酸Chemical Name: 2-[3-[2(R)-[2-(3-Chlorophenyl)-2(R)-hydroxyethylamino]propyl]-1H-indol-7-yloxy]acetic acid
CAS No. 244081-42-3, 179819-89...
参考文献标题:Indole derivs.
文献作者:Kato,S.; Harada,H.; Hirokawa,Y.; Yoshida,N.; Kawashima,H.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:EP 0801059; JP 1996231504; US 5817689; WO 9616938