zliming2004

Chemical Structures of Drugs in Clinical Pipeline:

Abametapir – Xeglyze

Chemical Structure of Xeglyze_Abametapir_Head Lice Treatment_Hatchtech Pty LtdTrade Name:Xeglyze
Generic Name:Abametapir
Chemical Name:5,5′-dimethyl-2,2′-bipyridinyl
CAS Number:1762-34-1
Indication:Head Lice Treatment
Drug Company:Hatchtech Pty Ltd.

Dasotraline – SEP-225289

Chemical Structure of Dasotraline_SEP-225289_Attention deficit hyperactivity disorder_Sunovion Pharmaceuticals

Generic Name:Dasotraline
Synonym: SEP-225289
Chemical Name:(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-amine
CAS Number:675126-05-3
Indication:Attention deficit hyperactivity disorder (ADHD)
Drug Company:Sunovion Pharmaceuticals. Inc.

Filgotinib – GLPG0634

Chemical Structure of Filgotinib_GLPG0634_rheumatoid arthritis_Galapagos NV_AbbVie  Galapagos公司类风湿关节炎新药Filgotinib的化学结构

Generic Name:Filgotinib
Synonym: GLPG0634; G146034
Chemical Name:N-(5-{4-[(1,1-dioxo-λ6-thiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide
CAS Number:1206161-97-8(Filgotinib),1540859-07-1(Filgotinib hydrochloride trihydrate)
Mechanims of Action:selective JAK1 (Janus kinase 1) inhibitor
Indication:rheumatoid arthritis,Crohn’s disease
Drug Company:Galapagos NV, AbbVie

通用名:Filgotinib
别名:GLPG0634; G146034
英文化学名:N-(5-{4-[(1,1-dioxo-λ6-thiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide
CAS 登录号:1206161-97-8(Filgotinib),1540859-07-1(Filgotinib盐酸盐)
作用机制:JAK1抑制剂
适应症:类风湿关节炎药
药物公司:Galapagos公司, 艾伯雄

Fostemsavir – BMS-663068

Chemical Structure of Fostemsavir_BMS-663068_Bristol-Myers Squibb  百时美施贵宝抗HIV新药Fostemsavir的化学结构

Generic Name:Fostemsavir
Synonym:BMS-663068
Chemical Name:{3-[2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl]-4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-1-yl}methyl dihydrogen phosphate
CAS Number:864953-29-7
Mechanims of Action:HIV-1 attachment inhibitor,a prodrug of the small-molecule inhibitor BMS-626529
Indication:HIV
Drug Company:Bristol-Myers Squibb

通用名:Fostemsavir
别名:BMS-663068
英文化学名:{3-[2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl]-4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-1-yl}methyl dihydrogen phosphate
CAS 登录号:864953-29-7
作用机制:HIV吸附抑制剂
适应症:HIV
药物公司:百时美施贵宝

BMS-663068的独特作用机制,该药是一种新颖的吸附抑制剂,能够阻止病毒最初吸附宿主CD4+T细胞并进入宿主免疫细胞。

Gilteritinib – ASP2215

Chemical Structure of Gilteritinib_ASP2215_FLT3-AXL inhibitor_acute myeloid leukemia_Astellas Pharma  安斯泰来急性骨髓性白血病新药Gilteritinib的化学结构

Generic Name:Gilteritinib
Synonym:ASP2215
Chemical Name:6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-[(tetrahydro-2H-pyran-4-yl)amino]pyrazine-2-carboxamide
CAS Number:1254053-43-4 (Gilteritinib), 1254053-84-3 (Gilteritinib hemifumarate)
Mechanims of Action:FLT3/AXL inhibitor
Indication:acute myeloid leukemia
Drug Company:Astellas Pharma

ASP2215 hemifumarate is a new chemical entity (NCE) discovered by Astellas Pharma Inc. in collaboration with Kotobuki Pharmaceutical Co., Ltd. ASP2215 has an inhibitory effect on tyrosine kinases, mainly FLT3, Axl and ALK.

通用名:Gilteritinib
别名:ASP2215
英文化学名:6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-[(tetrahydro-2H-pyran-4-yl)amino]pyrazine-2-carboxamide
CAS 登录号:1254053-43-4
作用机制:FLT3/AXL抑制剂
适应症: 急性骨髓性白血病(AML)
药物公司:安斯泰来制药

Glasdegib – PF-04449913

Chemical Structure of Glasdegib_PF-04449913_Hedgehog inhibitor_acute myeloid leukemia_Pfizer  辉瑞急性骨髓性白血病新药Glasdegib的化学结构

Generic Name:Glasdegib
Synonym:PF-04449913
Chemical Name:N-[(2R,4R)-2-(1H-benzimidazol-2-yl)-1-methylpiperidin-4-yl]-N’-(4-cyanophenyl)urea
CAS Number:1095173-27-5
Mechanims of Action:Hedgehog inhibitor
Indication:acute myeloid leukemia
Drug Company:Pfizer

通用名:Glasdegib
别名:PF-04449913
英文化学名:N-[(2R,4R)-2-(1H-benzimidazol-2-yl)-1-methylpiperidin-4-yl]-N’-(4-cyanophenyl)urea
CAS 登录号:1095173-27-5
作用机制:Hedgehog通路抑制剂
适应症: 急性骨髓性白血病(AML)
药物公司:辉瑞

Luminespib – AUY922

Chemical Structure of Luminespib_AUY922_HSP90 inhibitor_cancer treatment_Novartis  诺华抗癌药Luminespib的化学结构

Generic Name:Luminespib
Synonym:NVP-AUY922-NX,AUY922,VER-52296
Chemical Name:5-[2,4-dihydroxy-5-(1-methylethyl)phenyl]-N-ethyl-4-[4-(morpholin-4-ylmethyl)phenyl]isoxazole-3-carboxamide
CAS Number:747412-49-3 (Luminespib),1051919-26-6 (Luminespib mesylate)
Mechanims of Action:HSP90 inhibitor
Indication:cancer
Drug Company:Novartis Pharma AG

Luminespib (NVP-AUY922), an intravenous Hsp90 inhibitor, is an experimental drug candidate for the treatment of cancer. It was discovered through a collaboration between The Institute of Cancer Research and the pharmaceutical company Vernalis and licensed to Novartis. It is currently in Phase II clinical trials.

通用名:Luminespib
别名:NVP-AUY922,AUY922,VER-52296
英文化学名:5-[2,4-dihydroxy-5-(1-methylethyl)phenyl]-N-ethyl-4-[4-(morpholin-4-ylmethyl)phenyl]isoxazole-3-carboxamide
CAS 登录号:747412-49-3
作用机制:热休克蛋白(HSP)90抑制剂
适应症: 肿瘤
药物公司:诺华

Molidustat – BAY 85-3934

Chemical Structure of Molidustat_BAY 85-3934_HIF prolyl hydroxylase inhibitor_anemia_Bayer  拜耳贫血药Molidustat的化学结构

Generic Name:Molidustat
Synonym:BAY 85-3934
Chemical Name:2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one
CAS Number:1154028-82-6
Mechanims of Action:Hypoxia-inducible factor prolyl hydroxylase inhibitor
Indication:anemia associated with chronic kidney disease and/or end-stage renal disease
Drug Company:Bayer AG

通用名:Molidustat
别名:BAY 85-3934
英文化学名:2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one
CAS 登录号:1154028-82-6
作用机制:缺氧诱导因子(HIF)脯氨酰羟化酶(PH)抑制剂
适应症:慢性肾病和/或终末期肾病相关贫血
注册受理号码:JXHL1400077
注册药品名称:Molidustat钠包衣片
注册药品类型:化药
注册申请类型:进口
承办日期:2014-03-13
药物公司:拜耳

Molidustat(BAY 85-3934):是一种新颖的缺氧诱导因子(HIF)脯氨酰羟化酶(PH)抑制剂,目前正在慢性肾病和/或终末期肾病相关贫血患者中开展IIb期项目。I期临床研究表明,Molidustat抑制HIF-PH后,能够增加内源性促红细胞生成素(EPO)的生产。

Omipalisib – GSK2126458

 

Chemical Structure of Omipalisib_GSK2126458_PI3Kα-mTOR inhibitor_idiopathic pulmonary fibrosis_GlaxoSmithKline    葛兰素史克特发性肺纤维化药物Omipalisib的化学结构

Generic Name:Omipalisib
Synonym:GSK2126458
Chemical Name:2,4-difluoro-N-{2-methoxy-5-[4-(pyridazin-4-yl)quinolin-6-yl]pyridin-3-yl}benzenesulfonamide
CAS Number:1086062-66-9
Mechanims of Action:PI3Kα/mTOR inhibitor
Indication:idiopathic pulmonary fibrosis (IPF)
Drug Company:GlaxoSmithKline

Steven D. Knight et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.ACS Med. Chem. Lett., 2010, 1 (1), pp 39–43
通用名:Omipalisib
别名:GSK2126458
英文化学名:2,4-difluoro-N-{2-methoxy-5-[4-(pyridazin-4-yl)quinolin-6-yl]pyridin-3-yl}benzenesulfonamide
CAS 登录号:1086062-66-9
作用机制:双靶点PI3K/mTOR抑制剂
适应症:特发性肺纤维化
药物公司:葛兰素史克

Onalespib – AT13387

Chemical Structure of Onalespib_AT13387_Hsp90 inhibitor_NSCLC_Melanoma_Astex  抗癌药Onalespib的化学结构

Generic Name:Onalespib
Synonym:AT13387,ATI13387X
Chemical Name:{5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydro-2H-isoindol-2-yl}[2,4-dihydroxy-5-(1-methylethyl)phenyl]methanone
CAS Number:912999-49-6
Mechanims of Action:Hsp90 inhibitor
Indication:non-small cell lung cancer,B-Raf melanoma
Drug Company:Astex Pharmaceuticals, Inc.

Onalespib (AT13387) is currently being evaluated by Astex Pharmaceuticals in a Phase 2 clinical study in combination with Xalkori® (crizotinib) in the treatment of ALK+  non-small cell lung cancer, and via a CRADA with the US National Cancer Institute (NCI) in combination with Tafinlar® (dabrafenib) and Mekinist® (trametinib) in the treatment of B-Raf melanoma.

通用名:Onalespib
别名:AT13387,ATI13387X
英文化学名:{5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydro-2H-isoindol-2-yl}[2,4-dihydroxy-5-(1-methylethyl)phenyl]methanone
CAS 登录号:912999-49-6
作用机制:Hsp90抑制剂
适应症:抗癌药
药物公司:Astex Pharmaceuticals

Peficitinb – ASP015K – JNJ-54781532 

Chemical Structure of Peficitinib_ASP015K_JAK inhibitor_Rheumatoid arthritis_Astellas  安斯泰来类风湿性关节炎新药Peficitinib的化学结构

Generic Name:Peficitinb
Synonym:ASP015K,JNJ-54781532
Chemical Name:4-{[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
CAS Number:944118-01-8
Mechanims of Action:JAK inhibitor
Indication:Rheumatoid arthritis,ulcerative colitis
Drug Company:Astellas Pharma, Johnson & Johnson

通用名:Peficitinib
别名:ASP015K,JNJ-54781532
英文化学名:4-{[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
CAS 登录号:944118-01-8
作用机制:Janus激酶(JAK)抑制剂
适应症:类风湿性关节炎,溃疡性结肠炎
药物公司:安斯泰来,强生公司

Solcitinib – GSK2586184 – GLPG0778  (Discontinued)

Chemical Structure of Solcitinib_GSK2586184_GLPG0778_JAK1 inhibitor_Immunologic disorders_GlaxoSmithKline  葛兰素史克抗炎药物Solcitinib的化学结构

Generic Name:Solcitinib
Synonym:GSK2586184, G154578, GLPG0778
Chemical Name:N-(5-{4-[(3,3-dimethylazetidin-1-yl)carbonyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide
CAS Number:1206163-45-2
Mechanims of Action:Janus kinase 1 (JAK1) inhibitor
Indication:psoriasis,systemic lupus erythematosus, ulcerative colitis
Drug Company:GlaxoSmithKline,Galapagos
Development Status:Discontinued as August 2014

GlaxoSmithKline obtained rights of Solcitinib (GSK2586184,GLPG0778) from Galapagos in February 2012 asa treatment for systemic lupus erythematosus, chronic plaque psoriasis, and ulcerative colitis. GlaxoSmithKline halted in August 2014 to develop Galapagos’ GSK2586184 for chronic anti-inflammatory disorders, six months after it began generating disappointing results in Phase II studies for systemic lupus erythematosus.

通用名:Solcitinib
别名:GSK2586184, G154578, GLPG0778
英文化学名:N-(5-{4-[(3,3-dimethylazetidin-1-yl)carbonyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide
CAS 登录号:1206163-45-2
作用机制:Janus激酶(JAK)抑制剂
适应症:银屑病,红斑狼疮,溃疡性结肠炎
药物公司:葛兰素史克
开发进展:2014年8月开发已终止

Solcitinib(GSK2586184,曾用名GLPG0778)是一种选择性的JAK1抑制剂,是由Galapagos和葛兰素史克联合开发。2012年2月,葛兰素史克获得了该化合物的全球开发及商业权利。Galapagos于2014年2月份曾披露其合作伙伴葛兰素史克因缺乏有效性而停止GSK2586184用于红斑狼疮的一项2期临床研究,葛兰素史克2014年8月放弃了Solcitinib(GSK2586184,曾用名GLPG0778)用于治疗银屑病,红斑狼疮,溃疡性结肠炎的研究。

Taselisib – GDC-0032

Chemical Structure of Taselisib_RG7604_PI3K-Alpha Inhibitor_solid tumors_Roche  罗氏抗肿瘤药物Taselisib的化学结构

Generic Name:Taselisib
Synonym:GDC-0032; RG7604
Chemical Name:2-methyl-2-(4-{2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl}-1H-pyrazole-1-yl)propanamide
CAS Number:1282512-48-4
Mechanims of Action:PI3K-Alpha Inhibitor
Indication:solid tumors
Drug Company:Roche

通用名:Taselisib
别名:GDC-0032; RG-7604, RG7604
英文化学名:2-methyl-2-(4-{2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl}-1H-pyrazole-1-yl)propanamide
CAS 登录号:1282512-48-4
作用机制:磷脂酰肌醇-3-激酶(PI3K)α抑制剂
适应症: 抗肿瘤药
药物公司:罗氏

Temsavir –  BMS-626529

Chemical Structure of Temsavir (BMS-626529), Active Component of BMS-663068_Fostemsavir_HIV-1 attachment inhibitor_Bristol-Myers Squibb
Generic Name:Temsavir
Synonym:BMS-626529
Chemical Name:1-(4-benzoylpiperazin-1-yl)-2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]ethane-1,2-dione
CAS Number:701213-36-7
Mechanims of Action:HIV-1 attachment inhibitor, active component of BMS-663068 (Fostemsavir)
Indication:HIV Treatment
Drug Company:Bristol-Myers Squibb

通用名:Temsavir
别名:BMS-626529
英文化学名:1-(4-benzoylpiperazin-1-yl)-2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]ethane-1,2-dione
CAS 登录号:701213-36-7
作用机制:HIV吸附抑制剂
适应症: 抗HIV药
药物公司:百时美施贵宝

Uprosertib – GSK2141795

Chemical Structure of Uprosertib_GSK21417954_Akt inhibitor_cancer treatment_GlaxoSmithKline 葛兰素史克抗肿瘤药物Uprosertib的化学结构

Generic Name:Uprosertib
Synonym:GSK2141795,GSK795
Chemical Name:N-[(1S)-1-(aminomethyl)-2-(3,4-difluorophenyl)ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide
CAS Number:1047634-65-0
Mechanims of Action:Akt inhibitor
Indication:Cancer Treatment
Drug Company:GlaxoSmithKline

通用名:Uprosertib
别名:GSK2141795,GSK795
英文化学名:N-[(1S)-1-(aminomethyl)-2-(3,4-difluorophenyl)ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide
CAS 登录号:1047634-65-0
作用机制:Akt抑制剂
适应症: 抗肿瘤药
药物公司:葛兰素史克公司

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