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

CP-533536

2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸Chemical Name: 2-[3-[N-(4-tert-Butylbenzyl)-N-(pyridin-3-ylsulfonyl)aminomethyl]phenoxy]acetic acid
CAS No. 223488-57-1, 223490-49-1 (Na salt)
项目整合开发状态:...
参考文献标题:Prostaglandin agonists and their use to treat bone disorders
文献作者:Rosati,R.L.; Lefker,B.A.; Cameron,K.O.(Pfizer Inc.)
参考来源:EP 1021410; JP 2001519414; US 6498172; WO 9919300

AVP-13358

2-[4-(金刚烷-1-基甲酰氨基)苯基]-N-(2-吡啶基)-1H-苯并咪唑-5-甲酰胺Chemical Name: 2-[4-(Adamantan-1-ylcarboxamido)phenyl]-N-(2-pyridyl)-1H-benzimidazole-5-carboxamide
CAS No. 459805-03-9
项目整合开发状态: Phase I
项目研究机构: ...
参考文献标题:Benzimidazole cpds.for modulating IgE and inhibiting cellular proliferation
文献作者:Sircar,J.C.; Richards,M.L.; Major,M.W.(Avanir Pharmaceuticals)
参考来源:EP 1368028; WO 0272090

TAK-024

2-[4-[2-(4-鸟苷苯甲胺)乙酰]-3(S)-[3-(4-胍苯甲酰胺)丙基]-2-氧哌嗪-1-酰基]醋酸Chemical Name: 2-[4-[2-(4-Guanidinobenzamido)acetyl]-3(S)-[3-(4-guanidinobenzamido)propyl]-2-oxopiperazin-1-yl]acetic acid
CAS No. 186971-69-7...
参考文献标题:Piperazinones useful as inhibitors of platelet aggregation
文献作者:Fukushi,H.; Naka,T.; Terashita,Z.; Miyawaki,T.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0822931; JP 1997316059; US 5935963; US 6020334; WO 9633982

CP-331684

2-[4-[2-[2(R)-(6-氨基-3-吡啶基)-2-羟基乙基氨基]乙氧基]苯基]醋酸Chemical Name: 2-[4-[2-[2(R)-(6-Amino-3-pyridinyl)-2-hydroxyethylamino]ethoxy]phenyl]acetic acid
CAS No. 207922-70-1
项目整合开发状态: Phase I
项目研究机构: Pfi...
参考文献标题:Novel beta-adrenergic agonists
文献作者:Fisher,M.H.; Wyvratt,M.J.(Merck & Co.,Inc.)
参考来源:AU 9047392; EP 0377488; JP 1990231486; US 5030640

GW-9820

2-[4-[2-[N3-(4-氟苯基)-N1-(七基)脲啶]乙基苯氧基]-2-甲基丙酸Chemical Name: 2-[4-[2-[N3-(4-Fluorophenyl)-N1-(heptyl)ureido]ethyl]phenoxy]-2-methylpropionic acid
CAS No. 195131-60-3
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Use of agonists of the peroxisome proliferator activated receptor alpha for treating obesity
文献作者:Willson,T.M.(Glaxo Group Ltd.)
参考来源:WO 9736579

LY-674, LY-518674

2-[4-[3-[2,5-二氢-1-[(4-甲基苯基)甲基]-5-氧代-1H-1,2,4-T噻唑-3-基]丙基]苯氧基]-2-甲基-丙酸Chemical Name: 2-Methyl-2-[4-[3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl]propyl]phenoxy]propionic acid
CAS No....
参考文献标题:Perixosome proliferator activated receptor alpha agonists
文献作者:Mantlo,N.B.; Martinelli,M.J.; Thompson,R.C.; Mayhugh,D.R.; Wang,X.; Vicenzi,J.T.; Dominianni,S.J.; Schmid,C.R.; Collado Cano,I.; Xu,Y.; Letourneau,M.E.; Garcia-Paredes,C.; Etgen,G.J.Jr.; et al.(Eli Lilly and Company)
参考来源:WO 0238553

Clomoxir ethyl(Rec INNM), B-80727(free acid Na salt), B-80706, CPOC, POCA

2-[5-(4-氯苯基)戊基]环氧乙烷-2-羧酸乙酯克罗米芬 2-[5-(4-氯苯基)戊基]环氧乙烷-2-羧酸钠Chemical Name: Ethyl 2-[5-(4-chlorophenyl)pentyl]oxirane-2-carboxylate; 2-[5-(4-Chlorophenyl)pentyl]oxiranecarboxylic acid ethyl ester
CAS N...
参考文献标题:Substd.oxiranecarboxylic acids,their use and medicaments containing them
文献作者:Eistetter,K.; Rapp,E.(Byk Gulden Lomberg Chemische Fabrik GmbH)
参考来源:US 4324796

FR-181877

2-[6(S)-[3-(二苯甲基)-6-羰基-1,6-二氢哒嗪-1-基甲基]-5,6,7,8-四氢-1-萘氧基]乙酸Chemical Name: 2-[6(S)-[3-(Diphenylmethyl)-6-oxo-1,6-dihydropyridazin-1-ylmethyl]-5,6,7,8-tetrahydro-1-naphthyloxy]acetic acid
CAS No. 1729...
参考文献标题:Naphthalene derivs.as prostaglandin I2 agonists
文献作者:Taniguchi,K.; Nagano,M.; Hattori,K.; Tsubaki,K.; Okitsu,O.; Tabuchi,S.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0749424; JP 1997509958; US 5763489; WO 9524393

WAY-151693

2-[N-(4-甲氧基苯基磺酰)-N-(3-吡啶甲基)氨基]-3-甲基苯并羟胺酸盐酸Chemical Name: 2-[N-(4-Methoxyphenylsulfonyl)-N-(3-pyridinylmethyl)amino]-3-methylbenzohydroxamic acid hydrochloride
CAS No. 206551-25-9, 206547-44-6 (free...
参考文献标题:Preparation and use of orthosulfonamido aryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors
文献作者:Gu,Y.; Nelson,F.C.; Zask,A.; Du,M.T.; Levin,J.I.; Venkatesan,M.(American Cyanamid Co.)
参考来源:US 5929097

FAUC-213

2-{[4-(4-氯苯基)-1-哌嗪基]甲基}吡唑并[1,5-a]吡啶Chemical Name: 2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine
CAS No. 337972-47-1
项目整合开发状态: Preclinical
项目研究机构: Friedrich-Alexander-Unive...
参考文献标题:Rationally based efficacy tuning of selective dopamine D4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl) piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213)
文献作者:L鯾er,S.; Hubner,H.; Utz,W.; Gmeiner,P.
参考来源:J Med Chem 2001,44(17),2691