RU2012129887A - Ингибиторы мк2 - Google Patents
Ингибиторы мк2 Download PDFInfo
- 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
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- cycloalkyl
- nr7r8
- hydrogen
- compound according
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims abstract 19
- 150000001875 compounds Chemical class 0.000 claims abstract 17
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 17
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 17
- 239000001257 hydrogen Substances 0.000 claims abstract 17
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 17
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 11
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims abstract 8
- 229910052736 halogen Inorganic materials 0.000 claims abstract 8
- 125000005843 halogen group Chemical group 0.000 claims abstract 8
- 125000003118 aryl group Chemical group 0.000 claims abstract 6
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims abstract 4
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 229910052799 carbon Inorganic materials 0.000 claims abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims abstract 3
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims abstract 3
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 2
- 150000002825 nitriles Chemical class 0.000 claims abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 208000006386 Bone Resorption Diseases 0.000 claims 3
- 208000035473 Communicable disease Diseases 0.000 claims 3
- 230000001363 autoimmune Effects 0.000 claims 3
- 230000024279 bone resorption Effects 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 230000002526 effect on cardiovascular system Effects 0.000 claims 3
- 208000026278 immune system disease Diseases 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 230000000626 neurodegenerative effect Effects 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/12—Heterocyclic 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
- C07D471/20—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic 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
- C07D498/20—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against 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)
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)
| 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)
| 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 |
-
2010
- 2010-12-13 US US13/514,865 patent/US8772286B2/en active Active
- 2010-12-13 WO PCT/EP2010/069465 patent/WO2011073119A1/en not_active Ceased
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- 2010-12-13 CN CN201080056801.XA patent/CN102712641B/zh not_active Expired - Fee Related
- 2010-12-13 RU RU2012129887/04A patent/RU2012129887A/ru not_active Application Discontinuation
- 2010-12-13 CN CN201510037679.6A patent/CN104710423A/zh active Pending
- 2010-12-13 JP JP2012542575A patent/JP5859454B2/ja not_active Expired - Fee Related
- 2010-12-13 IN IN4978DEN2012 patent/IN2012DN04978A/en unknown
- 2010-12-13 AU AU2010333024A patent/AU2010333024B2/en not_active Ceased
- 2010-12-13 MX MX2012006778A patent/MX2012006778A/es not_active Application Discontinuation
- 2010-12-13 CA CA2780290A patent/CA2780290C/en not_active Expired - Fee Related
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2014
- 2014-06-05 US US14/297,167 patent/US9102676B2/en active Active
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2015
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- 2015-11-06 HK HK15110942.1A patent/HK1210159A1/xx unknown
- 2015-12-16 JP JP2015245246A patent/JP2016128412A/ja active Pending
Also Published As
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|---|---|
| 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) |
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