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

S-23757

2-(2-氟-5-甲基苯基)-4,5-二氢-1H-咪唑Chemical Name: 2-(2-Fluoro-5-methylphenyl)-4,5-dihydro-1H-imidazole
CAS No. 208718-14-3
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:The title imidazo...
参考文献标题:New imidazoline derivs.having activity for the imidazoline receptor
文献作者:Payard,M.; Danoun,S.; Baziard-Mouysset,G.; Anastassiadou,M.; Caignard,D.-H.; Renard,P.; Manechez,D.; Scalbert,E.; Rettori,M.-C.(ADIR et Cie.)
参考来源:EP 0846688; JP 1998168065; US 5925665

Icoduline hydrochloride, CBS-113 A

2-(2-羟基-4-甲基苯基)氨基噻唑艾考度林 Chemical Name: 2-(2-Hydroxy-4-methylphenylamino)thiazole hydrochloride
CAS No. 110952-54-0, 138511-81-6 (free base)
项目整合开发状态: Phase II
项目研究机构: Chauvin (Originator) 参考文献标题:N-Substd.2-amino-thiazoles,process for their pre
文献作者:Alazet,A.; Bonne,C.; Coquelet,C.; Sincholle,D.(Chauvin Laboratories SA)
参考来源:EP 0202157; ES 8900045; FR 2581063; JP 1987077375; US 4785008

NSC-672121

2-(2-羟基乙基硫代)-3-甲基萘-1,4-二酮Chemical Name: 2-(2-Hydroxyethylsulfanyl)-3-methyl-1,4-naphthoquinone
CAS No. 59147-84-1
项目整合开发状态: Preclinical
项目研究机构: University of Pittsburgh (Originator)
合成路线:H...
参考文献标题:Antiproliferative naphthoquinones,derivs.,compsns.,and uses thereof
文献作者:Kerns,J.K.; Carr,B.I.; Wilcox,C.S.(University of Pittsburgh)
参考来源:WO 0008495

NS-1652

2-(3-(3-(三氟甲基)苯基)脲基)苯甲酸Chemical Name: 2-[3-[3-(Trifluoromethyl)phenyl]ureido]benzoic acid
CAS No. 1566-81-0
项目整合开发状态: Preclinical
项目研究机构: NeuroSearch (Originator)
合成路线:The title urea deriv...
参考文献标题:Phenyl derivs.containing an acidic group,their preparation and their use as chloridic channel blockers
文献作者:Christophersen,P.; Pedersen,O.(NeuroSearch A/S)
参考来源:EP 0906273; EP 0977741; JP 2000511167; WO 9745400; WO 9847879

ABT-963

2-(3,4-二氟苯基)-4-(3-羟基-3-甲基丁氧基)-5-(4-甲基磺酰基苯基)哒嗪-3-酮Chemical Name: 2-(3,4-Difluorophenyl)-4-(3-hydroxy-3-methylbutoxy)-5-[4-(methylsulfonyl)phenyl]-3(2H)-pyridazinone
CAS No. 266320-83-6, 444617-70-3 ...
参考文献标题:Prostaglandin endoperoxide H synthase biosynthesis inhibitors
文献作者:Stewart,A.O.; Black,L.A.; Basha,A.; Patel,M.V.; Kolasa,T.; Coghlan,M.J.; Liu,H.; Kort,M.E.; McCarty,C.M.; Rohde,J.J.(Abbott Laboratories Inc.)
参考来源:EP 1124804; JP 2003512292; WO 0024719

新产品编号:967111

2-(3,4-二氢异喹啉-2(1H)-基)吡啶-4-胺 2-(1,2,3,4-四氢异喹啉-2-基)吡啶-4-盐酸胺 Chemical Name: 2-(1,2,3,4-Tetrahydroisoquinolin-2-yl)pyridin-4-amine
CAS No. 524718-15-8, 524717-65-5 (monohydrochloride)
项目整合开发状态: Prec...
参考文献标题:2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists
文献作者:Btelman,B.; Alanine,A.; Bourson,A.; Gill,R.; Heitz,M.-P.; Mutel,V.; Pinard,E.; Trube,G.; Wyler,R.
参考来源:Bioorg Med Chem Lett 2003,13(5),829

KME-4

2(3H)-呋酮,3-[[3,5-双(1,1-二甲基乙基)-4-羟基苯]甲基]二氢-Chemical Name: alpha-(3,5-Di-tert-butyl-4-hydroxybenzylidene)-gamma-butyrolactone
CAS No. 83677-24-1
项目整合开发状态: Phase II
项目研究机构: Kaneka (Originator) 参考文献标题:3,5-di-Tert-butylstyrene derivatives,salts thereof and pharmaceutical compositions containing the same as an active ingredient
文献作者:Katsumi,I.; et al.(Kaneka Corp.)
参考来源:CA 1187505; EP 0057882; US 4431656

GP-7

2(3H)-硫代酰苯,3-乙基二氢-3-(1-甲基乙基)-(9CI)Chemical Name: 4-(2,2,6,6-Tetramethyl-1-oxylpiperidin-4-ylamino)-4'-demethylepipodophyllotoxin; 5alpha-(4-Hydroxy-3,5-dimethoxyphenyl)-9beta-(2,2,6,6-tetramethyl-1-ox...
参考文献标题:Anticancer drugs II.Synthesis and biological evaluation of spin labeled derivatives of podophyllotoxin
文献作者:Chen,Y.; Wang,Y.; Li,J.; Tian,X.; Jia,Z.; Zhang,P.
参考来源:Life Sci 1989,45(26),2569-75

2-MPPA, GPI-5693, NAAL-1

2-(3-巯基丙基)戊二酸Chemical Name: 2-(3-Sulfanylpropyl)pentanedioic acid
CAS No. 254737-29-6
项目整合开发状态: Discontinued
项目研究机构: Guilford Pharmaceuticals (Originator)
合成路线:Acylation of Meldrum's acid ...
参考文献标题:NAALADase inhibitors useful as pharmaceutical cpds.and compsns.
文献作者:Jackson,P.F.; Slusher,B.S.; Majer,P.; Maclin,K.M.; Wang,E.; Lapidus,R.S.(Guilford Pharmaceuticals Inc.)
参考来源:JP 2002519408; US 6395718; WO 0001668

MRS-1505

2-(3-氯苯基)-4,6-二乙基-5-(丙基磺酰羰基)吡啶-3-羧酸丙酯Chemical Name: 2-(3-Chlorophenyl)-4,6-diethyl-5-(propylsulfanylcarbonyl)pyridine-3-carboxylic acid propyl ester
CAS No. 212329-38-9
项目整合开发状态: Biological Test...
参考文献标题:Structure-activity relationships and molecular mod
文献作者:Li,A.-H.; Moro,S.; Melman,N.; Ji,X.D.; Jacobson,K.A.
参考来源:J Med Chem 1998,41(17),3186