RU2012129887A - Ингибиторы мк2 - Google Patents

Ингибиторы мк2 Download PDF

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Publication number
RU2012129887A
RU2012129887A RU2012129887/04A RU2012129887A RU2012129887A RU 2012129887 A RU2012129887 A RU 2012129887A RU 2012129887/04 A RU2012129887/04 A RU 2012129887/04A RU 2012129887 A RU2012129887 A RU 2012129887A RU 2012129887 A RU2012129887 A RU 2012129887A
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RU
Russia
Prior art keywords
alkyl
cycloalkyl
nr7r8
hydrogen
compound according
Prior art date
Application number
RU2012129887/04A
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English (en)
Russian (ru)
Inventor
Тьерд Андриес БАРФ
Артур АУБРИ
Карстен Шультц-Фадемрехт
Эдуард Виллем ЗВАРТ
Нильс ХОГЕНБОМ
ВИЛЬДЕ Сандер Мартейн ДЕ
Аллард КАПТЕЙН
Original Assignee
Мсд Осс Б.В.
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.)
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Application filed by Мсд Осс Б.В. filed Critical Мсд Осс Б.В.
Publication of RU2012129887A publication Critical patent/RU2012129887A/ru

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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
    • C07D471/20Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
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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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    • AHUMAN NECESSITIES
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    • A61P17/16Emollients or protectives, e.g. against radiation
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    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • 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
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
RU2012129887/04A 2009-12-14 2010-12-13 Ингибиторы мк2 RU2012129887A (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US28609109P 2009-12-14 2009-12-14
EP09179043 2009-12-14
EP09179043.6 2009-12-14
US61/286,091 2009-12-14
PCT/EP2010/069465 WO2011073119A1 (en) 2009-12-14 2010-12-13 Mk2 inhibitors

Publications (1)

Publication Number Publication Date
RU2012129887A true RU2012129887A (ru) 2014-01-27

Family

ID=41565893

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2012129887/04A RU2012129887A (ru) 2009-12-14 2010-12-13 Ингибиторы мк2

Country Status (13)

Country Link
US (3) US8772286B2 (enExample)
EP (1) EP2513111B1 (enExample)
JP (2) JP5859454B2 (enExample)
KR (1) KR20120104241A (enExample)
CN (2) CN102712641B (enExample)
AU (1) AU2010333024B2 (enExample)
BR (1) BR112012013199A8 (enExample)
CA (1) CA2780290C (enExample)
HK (1) HK1210159A1 (enExample)
IN (1) IN2012DN04978A (enExample)
MX (1) MX2012006778A (enExample)
RU (1) RU2012129887A (enExample)
WO (1) WO2011073119A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8772286B2 (en) * 2009-12-14 2014-07-08 Merck Sharp & Dohme B.V. MK2 inhibitors
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
CA2908098A1 (en) 2013-03-15 2014-09-25 Celgene Avilomics Research, Inc. Mk2 inhibitors and uses thereof
JP6552061B2 (ja) 2014-06-10 2019-07-31 サンフォード−バーンハム メディカル リサーチ インスティテュート 代謝型グルタミン酸受容体の負のアロステリックモジュレーター(nams)とその使用
CN108794496B (zh) * 2018-04-28 2020-04-24 北京施安泰医药技术开发有限公司 一类cdk抑制剂、其药物组合物、制备方法及用途
US11458124B2 (en) 2018-07-12 2022-10-04 UCBBiopharma Srl Spirocyclic indane analogues as IL-17 modulators
CN114105834B (zh) * 2022-01-26 2023-04-25 寿光诺盟化工有限公司 一种n,n,n,n-四烯丙基氧代双苯磺酰胺的制备方法
WO2024125464A1 (en) * 2022-12-11 2024-06-20 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Tetrahydroisoquinolin-one derivatives, preparation methods and medicinal uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1747949A (zh) * 2002-12-20 2006-03-15 法马西亚公司 无环吡唑化合物
BRPI0413438A (pt) * 2003-08-08 2006-10-17 Pharmacia Italia Spa derivados de pirimidilpirrol ativos como inibidores de cinase
US20050043346A1 (en) * 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
DK1951684T3 (en) * 2005-11-01 2016-10-24 Targegen Inc BIARYLMETAPYRIMIDIN kinase inhibitors
CA2693904A1 (en) * 2007-07-16 2009-01-22 Novartis Ag Heterocyclic compounds useful as mk2 inhibitors
US8772286B2 (en) * 2009-12-14 2014-07-08 Merck Sharp & Dohme B.V. MK2 inhibitors

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Publication number Publication date
US9102676B2 (en) 2015-08-11
US20140288109A1 (en) 2014-09-25
CA2780290A1 (en) 2011-06-23
HK1210159A1 (en) 2016-04-15
US20120245175A1 (en) 2012-09-27
BR112012013199A2 (pt) 2016-03-01
EP2513111A1 (en) 2012-10-24
JP2013513585A (ja) 2013-04-22
CN102712641B (zh) 2015-12-09
CN104710423A (zh) 2015-06-17
WO2011073119A1 (en) 2011-06-23
JP2016128412A (ja) 2016-07-14
US8772286B2 (en) 2014-07-08
AU2010333024A1 (en) 2012-06-14
JP5859454B2 (ja) 2016-02-10
AU2010333024B2 (en) 2014-09-18
BR112012013199A8 (pt) 2018-01-02
IN2012DN04978A (enExample) 2015-09-25
KR20120104241A (ko) 2012-09-20
CA2780290C (en) 2018-01-02
US20160159800A1 (en) 2016-06-09
MX2012006778A (es) 2012-07-23
EP2513111B1 (en) 2013-10-02
CN102712641A (zh) 2012-10-03

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FA94 Acknowledgement of application withdrawn (non-payment of fees)

Effective date: 20170519