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AR067535A1 - Derivados de lactama tetraciclicos - Google Patents

Derivados de lactama tetraciclicos

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Publication number
AR067535A1
AR067535A1 ARP080103021A ARP080103021A AR067535A1 AR 067535 A1 AR067535 A1 AR 067535A1 AR P080103021 A ARP080103021 A AR P080103021A AR P080103021 A ARP080103021 A AR P080103021A AR 067535 A1 AR067535 A1 AR 067535A1
Authority
AR
Argentina
Prior art keywords
carbon atoms
unsubstituted
alkyl
substituted
hydrogen
Prior art date
Application number
ARP080103021A
Other languages
English (en)
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR067535A1 publication Critical patent/AR067535A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
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    • A61P35/00Antineoplastic agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
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  • Rheumatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • AIDS & HIV (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Obesity (AREA)
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Abstract

Su uso en el tratamiento de ciertas enfermedades, por ejemplo, dependientes de la actividad de MK-2 o TNF, y sus formas de fabricacion. Reivindicacion 1: Un compuesto de la formula (lA) o (IB): en donde: R es hidrogeno, halogeno, -Y-cicloalquilo de 3 a 7 átomos de carbono, arilo insustituido o sustituido, heterociclilo insustituido o sustituido, aril-alquenilo de 2 a 7 átomos de carbono insustituido o sustituido, mono- o di-(alquilo de 1 a 7 átomos de carbono insustituido o sustituido)-amino, o aril-amino insustituido o sustituido; A es -CH2-, -CH2-CH2-, -CH2-CH2-CH2- o -CH=CH-; D es un enlace entre el átomo de carbono y el átomo de nitrogeno con los que está enlazado, o es C(R4R5); R2 y R3 son hidrogeno o forman juntos un puente de etileno o trimetileno, en cada uno de los cuales, uno de los átomos de carbono puede ser reemplazado con O, S o NR6; R3 y R4 son hidrogeno o alquilo de 1 a 4 átomos de carbono, o forman juntos un puente de etileno o trimetileno, en cada uno de los cuales, uno de los átomos de carbono puede ser reemplazado con O, S o NR6; o uno de R2 y R3 es hidrogeno, y uno de R4 y R5 es hidrogeno, mientras que el otro de R2 y R3 junto con el otro de R4 y R5 forman un etileno, en donde uno de los átomos de carbono puede ser reemplazado con O, S o NR6, o un puente de metileno, con la condicion de que cuando menos uno de los puentes mencionados debe estar presente en un compuesto de la formula (lA) o (IB) y se forma por R2 y R3, por R4 y R5, o por R2 o R3 y R4 o R5, de tal manera que no más de dos de R2, R3, R4 y R5 son hidrogeno o alquilo de 1 a 4 átomos de carbono; R6 es hidrogeno, alquilo, alquilo de 1 a 7 átomos de carbono, halo-alquilo de 1 a 7 átomos de carbono, hidroxi-alquilo de 1 a 7 átomos de carbono, aril-alquilo de 1 a 7 átomos de carbono insustituido o sustituido, o acilo, X es CH o N; e Y es O, S o NR7, en donde R7 es hidrogeno, alquilo insustituido o sustituido, cicloalquilo insustituido o sustituido, aril alquilo de 1 a 7 átomos de carbono insustituido o sustituido, heterociclilo saturado insustituido o sustituido, o heterociclil-alquilo de 1 a 7 átomos de carbono insustituido o sustituido; un éster o amida disociable y farmacéuticamente aceptable del mismo, y/o una sal farmacéuticamente aceptable del mismo.
ARP080103021A 2007-07-16 2008-07-14 Derivados de lactama tetraciclicos AR067535A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07112549 2007-07-16

Publications (1)

Publication Number Publication Date
AR067535A1 true AR067535A1 (es) 2009-10-14

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ID=38792023

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080103021A AR067535A1 (es) 2007-07-16 2008-07-14 Derivados de lactama tetraciclicos

Country Status (15)

Country Link
US (2) US7838674B2 (es)
EP (1) EP2178874A1 (es)
JP (1) JP2010533674A (es)
KR (1) KR20100031619A (es)
CN (1) CN101687869A (es)
AR (1) AR067535A1 (es)
AU (1) AU2008277676A1 (es)
BR (1) BRPI0814426A2 (es)
CA (1) CA2693904A1 (es)
CL (1) CL2008002073A1 (es)
EA (1) EA201000100A1 (es)
MX (1) MX2009014247A (es)
PE (1) PE20090480A1 (es)
TW (1) TW200904818A (es)
WO (1) WO2009010488A1 (es)

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CN102712641B (zh) * 2009-12-14 2015-12-09 默沙东有限责任公司 Mk2抑制剂
AU2014277711B2 (en) * 2009-12-14 2016-10-27 Merck Sharp & Dohme B.V. MK2 inhibitors
US20120065195A1 (en) 2010-03-31 2012-03-15 Clark Christopher T Compounds for treating neurodegenerative diseases
EP2619181A1 (en) 2010-09-23 2013-07-31 Syngenta Participations AG Novel microbiocides
WO2012101029A1 (en) * 2011-01-26 2012-08-02 Nerviano Medical Sciences S.R.L. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
EP2668190B1 (en) * 2011-01-26 2016-08-17 Nerviano Medical Sciences S.r.l. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
WO2012117021A2 (en) 2011-03-03 2012-09-07 Syngenta Participations Ag Novel microbiocidal oxime ethers
WO2012152741A1 (de) 2011-05-10 2012-11-15 Bayer Intellectual Property Gmbh Bicyclische (thio)carbonylamidine
WO2013092460A1 (en) 2011-12-20 2013-06-27 Syngenta Participations Ag Cyclic bisoxime microbicides
EP2641901A1 (en) 2012-03-22 2013-09-25 Syngenta Participations AG. Novel microbiocides
KR101561330B1 (ko) 2012-09-19 2015-10-16 주식회사 두산 인돌로인돌계 유기 발광 화합물 및 이를 이용한 유기 전계 발광 소자
CN102936216B (zh) * 2012-12-05 2015-03-04 南京药石药物研发有限公司 7,9-二氧代-2,6-氮杂-螺[3.5]壬-2-甲酸叔丁酯及其中间体的制备方法
ES2656012T3 (es) 2013-02-06 2018-02-22 Bayer Cropscience Aktiengesellschaft Derivados de pirazol sustituidos con halógeno como pesticidas
KR20150133172A (ko) 2013-03-15 2015-11-27 셀진 아빌로믹스 리서치, 인코포레이티드 Mk2 억제제 및 이의 용도
SG10201902326XA (en) 2014-09-17 2019-04-29 Celgene Car Llc Mk2 inhibitors and uses thereof
CN105348263B (zh) * 2015-12-15 2018-03-23 乐普药业股份有限公司 一种达比加群酯中间体的制备方法
CN110035661B (zh) * 2016-10-05 2021-09-10 结核病药物开发全球联盟公司 用于治疗分枝杆菌感染的杂芳基三氟硼酸盐化合物
CA3054826A1 (en) 2017-03-16 2018-09-20 Celgene Car Llc Mk2 inhibitors, synthesis thereof, and intermediates thereto
JP2020514361A (ja) 2017-03-16 2020-05-21 セルジーン シーエーアール エルエルシー 9,10,11,12−テトラヒドロ−8h−[1,4]ジアゼピノ[5’,6’:4,5]チエノ[3,2−f]キノリン−8−オン化合物およびその使用
US11124525B2 (en) 2017-03-16 2021-09-21 Celgene Car Llc Heteroaryl compounds useful as MK2 inhibitors
CN110678178B (zh) 2017-03-16 2023-10-03 百时美施贵宝公司 Mk2抑制剂的形式和组合物
JP2020511468A (ja) 2017-03-16 2020-04-16 セルジーン シーエーアール エルエルシー Mk2阻害剤の重水素化アナログおよびその使用
CN107383026B (zh) * 2017-06-29 2019-04-30 武汉药明康德新药开发有限公司 一种7-羟甲基-2,5-二氮杂螺[3,4]辛烷-2-甲酸叔丁酯的合成方法
CN109336890B (zh) * 2018-11-17 2020-03-20 重庆文理学院 一种吲唑类衍生物的合成方法及抗肿瘤应用
CN109678879A (zh) * 2019-02-27 2019-04-26 陕西科技大学 一种苯并噻吩并吡喃酮类化合物及其合成方法
CN109678878A (zh) * 2019-02-27 2019-04-26 陕西科技大学 一种苯并噻吩并香豆素类化合物及其合成方法
CN110563726A (zh) * 2019-07-23 2019-12-13 上海合全药业股份有限公司 叔丁基-7,9-二氧亚基-2,6-二氮杂螺[4.5]癸烷-2-甲酸基酯的制备方法
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US7838674B2 (en) 2010-11-23
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CA2693904A1 (en) 2009-01-22
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