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

Banoxantrone, AQ4N

1,4-双[2-(二甲氨基-N-氧化物)乙基氨基]-5,8-二羟基蒽-9,10-二酮Chemical Name: 1,4-Bis[2-(dimethylamino)ethylamino]-5,8-dihydroxyanthracene-9,10-dione di-N-oxide
CAS No. 136470-65-0
项目整合开发状态: Phase I
项目研究机构: De Mo...
参考文献标题:Anti-cancer cpds.
文献作者:Patterson,L.H.(National Research Development Corp.)
参考来源:US 5132327; WO 9105824

SB-204070

1,4-苯并二恶英-5-羧酸,8-氨基-7-氯-2,3-二氢,(1-丁基-4-哌啶基)甲酯Chemical Name: 8-Amino-7-chloro-1,4-benzodioxan-5-carboxylic acid 1-butylpiperidin-4-ylmethyl ester
CAS No. 148702-58-3
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Substituted 2,3-alkylenedioxybenzamides
文献作者:Bulteau,G.; Acher,J.; Thominet,M.; Collignon,C.(Ile de France)
参考来源:DE 2734270; FR 2360305; GB 1571278; GB 1571447; JP 53018570; US 4186135; US 4248885; US 4255580

Sitamaquine hydrochloride, Q45, WR-6026

1,6-己二胺,N1,N1-二乙基-N6-(6-甲氧基-4-甲基-8-喹啉)-,盐酸盐(1:2) 西罗莫斯 Chemical Name: 8-[6-(Diethylamino)hexylamino]-6-methoxy-4-methylquinoline dihydrochloride; 8-[6-(Diethylamino)hexylamino]-6-methoxyepidine dihydro...
参考文献标题:Process for production of 8-NHR quinolines
文献作者:Chen,E.H.; Saggiomo,A.J.; Nodiff,E.A.(Department of the Army)
参考来源:US 4167638

FK-453, FR-453, FR-113453

1-[(2R)-2-(2-羟基乙基)-1-哌啶基]-3-(2-苯基吡唑并[1,5-a]吡啶-3-基)-,(2E)-2-丙烯-1-酮Chemical Name: (+)-2(R)-(2-Hydroxyethyl)-1-[(E)-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)acryloyl]piperidine; [R-(E)]-1-[1-Oxo-3-(2-pheny...
参考文献标题:Pyrazolopyridine cpds.and processes for preparation thereof
文献作者:Shiokawa,Y.; Akahane,A.; Katayama,H.; Mitsunaga,T.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:AU 8817602; EP 0299209; JP 1989045385; US 4925849; US 4994453; US 5087629; US 5102878; US 5179103; US 5296490

Alkasar-18, NOAC

1-[(2R,3S,4S,5R)-3,4-二羟基-5-(羟基甲基)四氢呋喃-2-基]-4-(十八烷基氨基)嘧啶-2-酮Chemical Name: 1-(beta-D-Arabinofuranosyl)-4-(octadecylamino)-2(1H)-pyrimidinone; N4-Octadecyl-1-beta-D-arabinofuranosylcytosine
CAS No. 1...
参考文献标题:Treatment of L1210 murine leukemias with liposome-incorporated N4-hexadecyl-1-beta-D-arabinofuranosylcytosine
文献作者:Schwendener,R.A.; Schott,H.
参考来源:Int J Cancer 1992,51(3),466-9

SL-651498, SL-65.1498

1-[(6-氟-2,9-二氢-9-甲基-1-氧代-2-苯基-1H-吡啶并[3,4-b]吲哚-4-基)羰基]-吡咯烷Chemical Name: 6-Fluoro-9-methyl-2-phenyl-4-(pyrrolidin-1-ylcarbonyl)-2,9-dihydro-1H-pyrido[3,4-b]indole-1-one
CAS No. 205881-86-3
项目整合开发...
参考文献标题:1H-Pyrido[3,4-b]indole-4-carboxamide derivs.,preparation and application thereof in therapeutics
文献作者:Sevrin,M.; Maloizel,C.; Evanno,Y.; Legalloudec,O.; George,P.(Sanofi-Synthabo)
参考来源:FR 2754262; JP 2001508403; US 6075021; WO 9815552

NKT-343, SDZ-NKT-343

1-[[(2-硝基苯基)氨基]羰基]-l-丙基-N-甲基-3-(2-萘yl)-N-(苯基甲基)-l-丙氨酰胺Chemical Name: N-(2-Nitrophenyl)carbamoyl-L-prolyl-L-[3-(2-naphthyl)]alanine N-benzyl-N-methylamide
CAS No. 180046-99-5
项目整合开发状态: Phase I 参考文献标题:Process development of (2-nitrophenylcarbamoyl)-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N-methylamide (SDZ NKT343)
文献作者:Prashad,M.; et al.
参考来源:Org Process Res Dev 1999,3(6),409

Sunepitron hydrochloride, CP-93393-1, CP-93393(free base)

1-[[(7S,9aS)-2-嘧啶-2-基-1,3,4,6,7,8,9,9a-八氢吡啶并[1,6-a]吡嗪-7-基]甲基]吡咯烷-2,5-二酮盐酸盐 1-{[(7S,9aS)-2-(嘧啶-2-基)辛氢-2H-吡啶[1,2-a]吡嗪-7-基]甲基}吡咯里定-2,5-二酮 Chemical Name: (7S,9aS)-7-(2,5-Dioxopyrrolidin-1-ylmethyl)-2-(2-p...
参考文献标题:Bis-aza-bicyclic anxiolytic agents and antidepressants
文献作者:Desai,K.A.; Bright,G.M.(Pfizer Inc.)
参考来源:EP 0380217; JP 1990233681; US 5122525; WO 9008144; WO 9008148

TK-117

1-[1-(4-甲基苯基)丙基]哌啶盐酸Chemical Name: 3-(3',4'-Methylenedioxybenzoyl)-2'-deoxy-5-fluoro-uridine
CAS No. 74234-11-0
项目整合开发状态: Biological Testing
项目研究机构: Toyama (Originator)
合成路线:The acylation ...
参考文献标题:5-Fluoro-(beta-uridine or 2'-deoxy-beta-uridine) derivatives,a process for producing the same and a carcinostatic agent containing the same
文献作者:Terashima,N.; Kitayama,I.; Yamaguchi,T.; Hiraiwa,T.; Omori,M.; Senoura,M.; Yotsuji,M.; Kodama,T.; Kodama,Y.; Aoyama,H.(Toyama Chemical Co.,Ltd.)
参考来源:DE 2923368

AV-100

1-[1(S),2(R)-二(羟甲基)环丙基甲基]-5-[2(E)-溴乙烯基]尿苷Chemical Name: 1-[1(S),2(R)-Bis(hydroxymethyl)cyclopropylmethyl]-5-[2(E)-bromovinyl]uracil
CAS No. 164013-29-0
项目整合开发状态: Preclinical
项目研究机构: Ajinomoto...
参考文献标题:Bis(hydroxymethyl)cyclopropylmethyl pyrimidine derivs.,their preparation and their use as anti-viral agents
文献作者:Onishi,T.; Mukai,C.; Sekiyama,T.; Tsuji,T.; Iwayama,S.; Okunishi,M.(Ajinomoto Co.,Inc.)
参考来源:EP 0649840; JP 1995165731; US 5496824