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

TAK-778-SR, TAK-778

(2R,4S)-(-)-N-[4-(二乙氧基磷基甲基)苯基]-4-甲基-7,8-(甲二氧基)-5-羰基-1,2,4,5-四氢-3-苯并噻庚英-2-甲酰胺Chemical Name: (2R,4S)-(-)-N-[4-(Diethoxyphosphorylmethyl)phenyl]-4-methyl-7,8-(methylenedioxy)-5-oxo-1,2,4,5-tetrahydro-3-b...
参考文献标题:Optically active benzothiepine deriv.,its preparation and use
文献作者:Sohda,T.; Taketomi,S.; Oda,T.(Takeda Chemical Industries,Ltd.)
参考来源:CA 2166152; EP 0719782; JP 1996231569; JP 1997183784

Lubeluzole, JK-8792, R-87926, Prosynap

(2S)-1-[4-(1,3-苯并噻唑-2-基-甲基氨基)哌啶-1-基]-3-(3,4-二氟苯氧基)丙-2-醇Chemical Name: (+)-(S)-1-[4-[N-(Benzothiazol-2-yl)-N-methylamino]piperidin-1-yl]-3-(3,4-difluorophenoxy)-2-propanol
CAS No. 144665-07-6
项目整...
参考文献标题:4-[(2-Benzothiazolyl)methylamino]-alpha-[(3,4-difluorophenoxy)methyl]-1-piperidineethanol
文献作者:Stokbroekx,R.A.; Grauwels,G.A.J.(Janssen Pharmaceutica NV)
参考来源:EP 0501552; EP 0573473; JP 1994505012; US 5434168; WO 9214731

Phortress, 5F-DF-203-L-lysinamide, NSC-710305

(2S)-2,6-二氨基-N-[4-(5-氟-1,3-苯并噻唑-2-基)-2-甲基苯基]己酰胺二盐酸盐Chemical Name: N1-[4-(5-Fluorobenzothiazol-2-yl)-2-methylphenyl]-L-lysinamide dihydrochloride
CAS No. 328087-38-3
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Substd.2-arylbenzazole cpds.and their use as antitumour agents
文献作者:Chua,M.-S.; Westwell,A.D.; Hutchinson,I.P.; Stevens,M.F.G.; Poole,T.D.(Cancer Research Campaign Technology Ltd.)
参考来源:WO 0114354

JTP-4819

(2S)-2-[(2S)-2-(2-羟基乙酰基)吡咯烷-1-羰基]-N-(苯基甲基)吡咯烷-1-甲酰胺Chemical Name: N-Benzyl-2(S)-[2(S)-(2-hydroxyacetyl)pyrrolidin-1-ylcarbonyl]pyrrolidine-1-carboxamide; N-Benzylcarbamoyl-L-prolyl-L-prolyl-methanol 参考文献标题:Cpd.with prolyl endopeptidase inhibitor activity and pharmaceutical use thereof
文献作者:Kobayashi,K.; Akamatsu,M.; Yata,S.; Abe,H.; Toide,K.; Kogayu,M.; Uchida,I.(Japan Tobacco Inc.; Welfide Corporation)
参考来源:EP 0670309; JP 1995512967; US 5536737; WO 9412474

CP-B, CMP-3

(2S)-2-[(3R)-3-羟基-4-[3-(三氟甲基)苯基]丁基]-5-氧代-1-吡咯烷庚酸Chemical Name: 7-[2(S)-[3(R)-Hydroxy-4-[3-(trifluoromethyl)phenyl]butyl]-5-oxopyrrolidin-1-yl]heptanoic acid
CAS No. 346672-61-5
项目整合开发状态: Preclin...
参考文献标题:EP4 receptor selective agonists in the treatment of osteoporosis
文献作者:Thompson,D.D.; Lefker,B.A.; Cameron,K.O.; Ke,H.Z.(Pfizer Products Inc.)
参考来源:EP 1110949; JP 2001181210; WO 0146140

Benzotript, CR-501

(2S)-2-[(4-氯苯基)甲酰氨基]-3-(1H-吲哚-3-基)丙酸 4-氯苯甲酰-L-色氨酸钙盐 N-(4-氯苯甲酰基)-L-色氨酸钠Chemical Name: N-(4-Chlorobenzoyl)-L-tryptophan
CAS No. 39544-74-6, 56116-62-2 (Ca salt (2:1)), 56116-64-4 (monoNa salt)
项目整...
参考文献标题:N-p-Chlorobenzoyl tryptophane salts and compsns.thereof
文献作者:Rovati,L.S.; Picciola,G.; Makovec,F.(Rotta Research Laboratorium SpA)
参考来源:US 4000297

Soblidotin, Auristatin PE, NSC-654663, TZT-1027

(2S)-2-[[(2S)-2-二甲基氨基-3-甲基丁酰基]氨基]-N-[(3R,4R,5S)-3-甲氧基-1-[(2S)-2-[(1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(2-苯基乙基氨基)丙基]吡咯烷-1-基]-5-甲基-1-氧代庚烷-4-基]-N,3-二甲基丁酰胺Chemical Name: 3(S)-[1-[4(S)-[N-(N,N-Dimethyl-L-valyl-L-valy...
参考文献标题:Novel tetrapeptide derivs.
文献作者:Sakakibara,K.; Gondo,M.; Miyazaki,K.(Teikoku Hormone Manufacturing Co.,Ltd.)
参考来源:EP 0598129; JP 1993503479; US 5654399; WO 9303054

Nepadutant, MEN-11420

(2S)-2-[[(3S,6S,9S,12S)-12-[[(2S)-4-[[(2R,3R,4R,5S,6R)-3-乙酰氨基-4,5-二羟基-6-(羟基甲基)四氢吡喃-2-基]氨基]-2-氨基-4-氧代丁酰基]氨基]-9-(1H-吲哚-3-基甲基)-5,8,11,14-四氧代-6-(苯基甲基)1,4,7,10-四氮杂环十四烷-3-羰基]氨基]-4-甲基戊酸Chemical Name: Cyclo[N...
参考文献标题:Bicyclic tachykinins antagonists,preparation thereof and their use in pharmaceutical compsn.
文献作者:Arcamone,F.; Maggi,C.A.; Quartara,L.; Giannotti,D.(Menarini Industrie Farma Riunite Srl)
参考来源:JP 1999501643; WO 9628467

BIO-5192

(2S)-2-[[[((2S)-1-[(3,5-二氯苯基)磺酰基]-2-吡咯烷基]羰基]氨基]-4-[[(2S)-4-甲基-2-[甲基[2-[4-[[[[((((2-(甲基苯基)氨基)羰基]氨基]苯基]乙酰基]氨基]-1-氧戊基]氨基]丁酸)Chemical Name: 2(S)-[1-(3,5-Dichlorophenylsulfonyl)-L-prolylamino]-4-[N-methyl-...
参考文献标题:Cell adhesion inhibitors
文献作者:Lee,W.-C.; Scott,D.; Cornebise,M.; Petter,R.(Biogen Idec Inc.)
参考来源:EP 1265606; JP 2003506491; US 6630503; WO 0112186

Wy-50295

(2S)-2-[6-(喹啉-2-基甲氧基)萘-2-基]丙酸Chemical Name: (+)-(S)-2-[6-(2-Quinolinylmethoxy)-2-naphthyl]propionic acid
CAS No. 123016-21-7
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator) 参考文献标题:Conversion of a cyclooxygenase (CO) inhibitor into a 5-lipoxygenase (LO) inhibitor - A general route to novel antiinflammatory and antiallergy drugs
文献作者:Kreft,A.F.; Failli,A.; Musser,J.H.; et al.
参考来源:Drugs Exp Clin Res 1991,17381-387