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

ACEA-762, ACEA-0762

7-氯-4-羟基-3-(3-苯氧基苯基)-1,5-二氮杂萘-2(1H)-酮Chemical Name: 7-Chloro-4-hydroxy-3-(3-phenoxyphenyl)-1,5-naphthyridin-2(1H)-one
CAS No. 181122-94-1
项目整合开发状态: Preclinical
项目研究机构: CoCensys (Originator) 参考文献标题:Aza and aza (N-oxy) analogs of glycine/NMDA receptor antagonists
文献作者:Keana,J.F.W.; Cai,S.X.; Martin,V.V.; Zhou,Z.-L.; Navratil,J.M.(Oregon Health Sciences University)
参考来源:EP 0805809; US 5801183; WO 9622990

ACEA-1416

7-氯-6-甲基-5-硝基-1,4-二氢喹喔啉-2,3-二酮Chemical Name: 7-Chloro-6-methyl-5-nitroquinoxaline-2,3(1H,4H)-dione
CAS No. 167415-33-0
项目整合开发状态: Preclinical
项目研究机构: Acea (Originator), Oregon Health and Scien...
参考文献标题:Alkyl,azido,alkoxy,and fluoro-substd.and fused quinoxalinediones and the use thereof as glycine receptor antagonists
文献作者:Cai,S.X.; Weber,E.; Keana,J.F.W.; Kher,S.(Acea Pharmaceuticals; Oregon Health Sciences University; University of California,Oakland)
参考来源:EP 0732942; JP 1997504794; WO 9512417

Compound 73/602, CDRI-73/602

7-甲氧基-2,3-二氢吡咯并[2,1-b]喹唑啉-9(1H)-酮Chemical Name: 7-Methoxy-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazolin-9-one; 7-Methoxydeoxyvasicinone
CAS No. 60811-32-7
项目整合开发状态: Phase II
项目研究机构: Central Drug...
参考文献标题:Synthetic analogs of Peganum alkaloids.1.Synthesis of methoxy- and hydroxysubstituted desoxyvasicinones and desocypeganines
文献作者:Karimov,A.; Yunusov,S.; Telezhenetskaya,M.V.
参考来源:Khim Prir Soedin 1982,(4),498-504

7-Methoxytacrine, 7-MEOTA

7-甲氧基他克林Chemical Name: 9-Amino-7-methoxy-1,2,3,4-tetrahydroacridine; 7-Methoxy-1,2,3,4-tetrahydro-9-acridinamine
CAS No. 5778-80-3, 65239-02-3 (lactate)
项目整合开发状态: Phase III
项目研究机构: Purkyne Me...
参考文献标题:7,8,9,10-Tetrahalo-6H-cyclohepta[b]quinolines
文献作者:Sigal,M.V.Jr.; Brent,B.J.; Marchini,P.
参考来源:US 3232945

Salcaprozic acid sodium salt, E414(free acid), SNAC, P414

8-(2-羟基苯甲酰氨基)辛酸Chemical Name: 8-(2-Hydroxybenzamido)octanoic acid sodium salt
CAS No. 183990-46-7 (free acid)
项目整合开发状态: Phase III
项目研究机构: Emisphere (Originator)
合成路线:Full protection of 8-a...
参考文献标题:Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin
文献作者:Paton,D.R.; Leone-Bay,A.; Freeman,J.; Lercara,C.; O'Toole,D.; Gschneidner,D.; Wang,E.; Harris,E.; Rosado,C.; Rivera,T.; DeVincent,A.; Tai,M.; Mercogliano,F.; Agarwal,R.; Leipold,H.; Baughman,R.A.
参考来源:J Med Chem 1998,41(7),1163

TMB-8

8-(二乙基氨基)辛基3,4,5-三甲氧基苯甲酸酯Chemical Name: 8-(N,N-Diethylamino)octyl 3,4,5-trimethoxybenzoate hydrochloride; 3,4,5-Trimethoxybenzoic acid 8-(diethylamino)octyl ester hydrochloride
CAS No. 57818-92-5 (...
参考文献标题:TMB-8
文献作者:Murer,E.H.
参考来源:Drugs Fut 1983,8(11),940

新产品编号:35313

8-(苯基甲氧基)-8-氮杂螺[4.4]壬烷-7,9-二酮Chemical Name: N-Benzyloxy-2-azaspiro[4.4]nonane-1,3-dione
CAS No. 131042-61-0
项目整合开发状态: Preclinical
项目研究机构: Howard University (Originator)
合成路线:This compound ...
参考文献标题:Imidooxy anticonvulsants: Structural analogs with special emphasis on N-(benzyloxy)-2-azaspiro[4,4]nonane-1,3-dione
文献作者:Scott,K.R.; Nicholson,J.M.; Edafiogho,I.O.; Farrar,V.A.; Hinko,C.N.; Moore,J.A.
参考来源:Drugs Fut 1992,17(5),395

KF-21213

8-[(E)-2-(2,3-二甲基-4-甲氧苯基)乙烯基]-1,3,7-三甲基-3,7-二氢-1H-嘌呤-2,6-二酮Chemical Name: 8-[(E)-2-(2,3-Dimethyl-4-methoxyphenyl)vinyl]-1,3,7-trimethyl-3,7-dihydro-1H-purine-2,6-dione
CAS No. 155271-17-3
项目整合开发...
参考文献标题:Antidepressant
文献作者:Suzuki,F.; Shimada,J.; Ishii,A.; Nakamura,J.; Ichikawa,S.; Kitamura,S.; Koike,N.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0628311; JP 1994502746; WO 9401114

FR-236924

8-{2-[(2-戊基环丙基)甲基]环丙基}辛酸Chemical Name: 8-[2-(2-Pentylcyclopropylmethyl)cyclopropyl]octanoic acid
CAS No. 28399-31-7
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:Cyclopropanatio...
参考文献标题:Carboxylic acid cpd.having cyclopropane ring
文献作者:Tanaka,A.; Nishizaki,T.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 1343746; WO 0250013

Tiaspirone hydrochloride, Tiospirone hydrochloride, BMY-13859, MJ-138591, MJ-13859(free base)

8-{4-[4-(1,2-苯并噻唑-3-基)-1-哌嗪基]丁基}-8-氮杂螺[4.5]癸烷-7,9-二酮替螺酮 Chemical Name: 8-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione hydrochloride
CAS No. 87691-92-7, 8769...
参考文献标题:BMY-13859
文献作者:Eison,M.S.; Taylor,D.P.; New,J.S.; Minielli,J.L.
参考来源:Drugs Fut 1985,10(9),731