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

HMN-214

(E)-4-[2-[2-[N-乙酰基-N-[(4-甲氧基苯基)磺酰]氨基]苯基]乙烯基]吡啶 1-氧化物Chemical Name: (E)-N-Acetyl-4-methoxy-N-[2-[2-(1-oxidopyridin-4-yl)vinyl]phenyl]benzenesulfonamide
CAS No. 173529-46-9
项目整合开发状态: Phase I
项目...
参考文献标题:Aminostilbazole derivs.and medicine
文献作者:Matsuura,A.; Matsuda,M.(Nippon Shinyaku Co.,Ltd.)
参考来源:EP 0754682; WO 9527699

LM-1484

(E)-8-[2-[4-(4-苯丁氧基)苯基]乙烯]-2-(1H-四唑-5-基)-4H-苯并吡喃-4-酮Chemical Name: (E)-8-[2-[4-(4-Phenylbutoxy)phenyl]vinyl]-2-(1H-tetrazol-5-yl)-4H-benzopyran-4-one
CAS No. 197506-02-8
项目整合开发状态: Preclinical 参考文献标题:Benzopyran derivs.having leukotriene-antagonistic action
文献作者:Carganico,G.; Mauleon Casellas,D.; Pascual Avellana,J.; Garcia Perez,M.L.; Palomer Benet,A.(Menarini Industrie Farma Riunite srl)
参考来源:EP 0888327; ES 2127106; JP 2000506878; US 5990142; WO 9734885

CGP-11112

(E)-N-[2-[4-[(3-环己基-2-亚胺基-1-吡氮基苯基)磺酰]苯基]乙基]-2-丁烯酰Chemical Name: (E)-N-[2-[4-[(3-Cyclohexyl-2-imino-1-imidazolidinyl)sulfonyl]phenyl]ethyl]-2-butenamide; trans-1-[[p-[2-(Crotonylamino)ethyl]phenyl]sulf...
参考文献标题:CGP-11112
文献作者:Serradell,M.N.; Castar,J.; Thorpe,P.J.
参考来源:Drugs Fut 1984,9(5),315

Dexniguldipine hydrochloride, (R)-Niguldipine hydrochloride, BY-935, B8509-035, B-844-39(racemate), B-859-34 [(-)-(S)-isomer], B-859-35

(R)-(-)-盐酸尼古地平 S-(+)-盐酸尼古地平 Chemical Name: (R)-2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-methyl 5-[3-(4,4-diphenyl-1-piperidinyl)propyl] diester hydrochloride
CAS N...
参考文献标题:1,4-Dihydropyridine enantiomers
文献作者:Amschler,H.; Flockerzi,D.; Klemm,K.; Kohl,B.; Eistetter,K.; Eltze,M.; Kolassa,N.; Sanders,K.; Schudt,C.(Byk Gulden Lomberg Chemische Fabrik GmbH)
参考来源:AU 8816264; EP 0296316; EP 0343193; WO 8807525

d-Thioctic acid, (R)-(+)-alpha-Lipoic acid, (R)-(+)-Thioctic acid, Dexlipotam

(R)-(+)-1,2-二硫戊环基-3-戊酸Chemical Name: (+)-5-[1,2-Dithiolan-3(R)-yl]pentanoic acid
CAS No. 1200-22-2
项目整合开发状态: Phase II
项目研究机构: Asta Medica (Originator), Aventis Pharma (Licensee)
合成路线:A syn...
参考文献标题:Method for producing lipoic acid and dihydrolipoic acid
文献作者:Paust,J.; Klatt,M.J.; Niebel,M.(BASF AG)
参考来源:WO 0210151

NKP-608

(R)-(+)-2-氨基-4-羟基丁酸Chemical Name: (2R,4S)-N-[1-[3,5-Bis(trifluoromethyl)benzoyl]-2-(4-chlorobenzyl)piperidin-4-yl]quinoline-4-carboxamide
CAS No. 177707-12-9
项目整合开发状态: Phase II
项目研究机构: Novart...
参考文献标题:Aroyl-piperidine derivs.
文献作者:Ofner,S.; Veenstra,S.J.; Schilling,W.(Novartis AG)
参考来源:CA 2160444; EP 0707006; JP 1996176145; US 5965562

L-772405

(R)-2-(4-氟苯基)-2-[1-[3-[5-(4H-1,2,4-三唑-4-基)-1H-吲哚-3-基]丙基]哌啶-4-酰胺]乙醇Chemical Name: (R)-2-(4-Fluorophenyl)-2-[1-[3-[5-(4H-1,2,4-triazol-4-yl)-1H-indol-3-yl]propyl]piperidin-4-ylamino]ethanol
CAS No. 1...
参考文献标题:Azetidine,pyrrolidine and piperidine derivs.
文献作者:Baker,R.; Bourrain,S.; Castro Pineiro,J.L.; Chambers,M.S.; Guiblin,A.R.; Hobbs,S.C.; Jelley,R.A.; Madin,A.; Matassa,V.G.; Reeve,A.J.; Russell,M.G.N.; Showell,G.A.; Sternfeld,F.; Street,L.J.; Van Niel,M.B.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0804434; JP 1998503768; US 5854268; WO 9604274

新产品编号:278941

(R)-2-氨基-N-苄基-3-甲氧基丙酰胺Chemical Name: 2(R)-Amino-N-benzyl-3-methoxypropionamide; N1-Benzyl-O-methyl-D-serinamide
CAS No. 196601-69-1
项目整合开发状态: Preclinical
项目研究机构: Research Corporation Technolo...
参考文献标题:Anticonvulsant enantiomeric amino acid derivs.
文献作者:Kohn,H.; Andurkar,S.V.(Research Corporation Technologies,Inc.)
参考来源:US 6048899; WO 0000463

BAY-38-7271

(R)-3-(2-(羟甲基)-2,3-二氢-1H-茚-4-氧基)苯基4,4,4-三氟丁烷-1-磺酸盐Chemical Name: (-)-4,4,4-Trifluorobutane-1-sulfonic acid 3-[2(R)-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy]phenyl ester
CAS No. 212188-60-8, 212...
参考文献标题:Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
文献作者:Raddatz,S.; De Vry,J.-M.-V.; Mohrs,K.-H.; Dressel,J.; Matzke,M.; Mittendorf,J.; Mauler,F.; Schuhmacher,J.; Friedl,A.; Horvath,E.; Jork,R.; Keldenich,J.; Franz,J.; Spreyer,P.; V鰄ringer,V.; Rock,M.-H.(Bayer AG)
参考来源:DE 19740785; EP 0966436; JP 2001515470; US 2002072529; US 6262112; US 6573278; WO 9837061

AZD-8129, AR-A2, AR-A2XX, AR-A000002

(R)-N-[5-甲基-8-(4-甲基哌嗪-1-基)-1,2,3,4-四氢-2-萘基]-4-甲苯甲酰胺Chemical Name: N-[5-Methyl-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2(R)-yl]-4-(4-morpholinyl)benzamide
CAS No. 220051-79-6, 220051...
参考文献标题:Substd.1,2,3,4-tetrahydronaphthalene derivs.
文献作者:Berg,S.; Ross,S.; Linderberg,M.; Thorberg,S.-O.; Ulff,B.(AstraZeneca plc)
参考来源:EP 1000048; JP 2001510837; US 6313118; WO 9905134