EA201500133A1 - Производные имидазопиразина в качестве модуляторов активности tnf - Google Patents
Производные имидазопиразина в качестве модуляторов активности tnfInfo
- Publication number
- EA201500133A1 EA201500133A1 EA201500133A EA201500133A EA201500133A1 EA 201500133 A1 EA201500133 A1 EA 201500133A1 EA 201500133 A EA201500133 A EA 201500133A EA 201500133 A EA201500133 A EA 201500133A EA 201500133 A1 EA201500133 A1 EA 201500133A1
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- Eurasian Patent Office
- Prior art keywords
- disorders
- derivatives
- imidazopirazine
- tnf activity
- activity modulators
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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 two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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 two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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- 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
- C07D471/02—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 two hetero rings
- C07D471/08—Bridged systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
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- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
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- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
В заявке описана серия производных имидазо[1,2-а]пиразина, которые являются активными модуляторами активности TNFα человека и поэтому полезны для лечения и/или предупреждения различных заболеваний человека, включая аутоиммунные и воспалительные нарушения; неврологические и нейродегенеративные нарушения; боль и ноцицептивные нарушения; сердечно-сосудистые нарушения; метаболические нарушения; глазные нарушения и онкологические нарушения.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1212513.4A GB201212513D0 (en) | 2012-07-13 | 2012-07-13 | Therapeutic agents |
PCT/EP2013/064332 WO2014009296A1 (en) | 2012-07-13 | 2013-07-05 | Imidazopyrazine derivatives as modulators of tnf activity |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201500133A1 true EA201500133A1 (ru) | 2015-07-30 |
EA028041B1 EA028041B1 (ru) | 2017-09-29 |
Family
ID=46799593
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201500133A EA028041B1 (ru) | 2012-07-13 | 2013-07-05 | Производные имидазопиразина в качестве модуляторов активности tnf |
Country Status (11)
Country | Link |
---|---|
US (1) | US9475820B2 (ru) |
EP (1) | EP2872511B1 (ru) |
JP (1) | JP6259824B2 (ru) |
CN (1) | CN104470924B (ru) |
BR (1) | BR112015000790B1 (ru) |
CA (1) | CA2877543C (ru) |
EA (1) | EA028041B1 (ru) |
ES (1) | ES2711131T3 (ru) |
GB (1) | GB201212513D0 (ru) |
TR (1) | TR201901652T4 (ru) |
WO (1) | WO2014009296A1 (ru) |
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GB201321737D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
GB201321744D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
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AU2020385113A1 (en) | 2019-11-11 | 2022-05-19 | Incyte Corporation | Salts and crystalline forms of a PD-1/PD-L1 inhibitor |
US11760756B2 (en) | 2020-11-06 | 2023-09-19 | Incyte Corporation | Crystalline form of a PD-1/PD-L1 inhibitor |
CR20230230A (es) | 2020-11-06 | 2023-07-27 | Incyte Corp | Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo |
US11780836B2 (en) | 2020-11-06 | 2023-10-10 | Incyte Corporation | Process of preparing a PD-1/PD-L1 inhibitor |
CN113967214A (zh) * | 2021-11-30 | 2022-01-25 | 广东药科大学 | 一种咪唑并吡嗪环丙烷甲酰胺类化合物的应用 |
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JP3648763B2 (ja) * | 1994-08-23 | 2005-05-18 | 日本油脂株式会社 | ウミホタルルシフェリン誘導体および糖加水分解酵素の定量方法 |
US7105550B2 (en) * | 2000-03-01 | 2006-09-12 | Christopher Love | 2,4-disubstituted thiazolyl derivatives |
JP2004532792A (ja) * | 2000-07-14 | 2004-10-28 | ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー | 神経障害を治療するためのイミダゾ[1,2−a]ピラジン |
US7186832B2 (en) * | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
US7157460B2 (en) * | 2003-02-20 | 2007-01-02 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
AU2006315718B2 (en) * | 2005-11-10 | 2012-10-04 | Merck Sharp & Dohme Corp. | Imidazopyrazines as protein kinase inhibitors |
EP2103614A1 (en) * | 2008-03-18 | 2009-09-23 | Santhera Pharmaceuticals (Schweiz) AG | Substituted imidazopyrimidine, imidazopyrazine and imidazopyridazine derivatives as melanocortin-4 receptor modulators |
AU2009273465A1 (en) * | 2008-07-24 | 2010-01-28 | Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. | Fluorescently or spin-labeled kinases for rapid screening and identification of novel kinase inhibitor scaffolds |
WO2010088518A2 (en) * | 2009-01-31 | 2010-08-05 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
CA2771532C (en) * | 2009-08-17 | 2021-03-23 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
CA2780922A1 (en) * | 2010-02-11 | 2011-08-18 | OSI Pharmaceuticals, LLC | 7-aminofuropyridine derivatives |
CN103429592A (zh) * | 2010-12-17 | 2013-12-04 | 拜耳知识产权有限责任公司 | 作为mps-1和tkk抑制剂用于治疗过度增殖性病症的6-取代的咪唑并吡嗪 |
WO2013033899A1 (en) * | 2011-09-08 | 2013-03-14 | Merck Sharp & Dohme Corp. | Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases |
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CN104470924A (zh) | 2015-03-25 |
CN104470924B (zh) | 2016-11-09 |
GB201212513D0 (en) | 2012-08-29 |
US9475820B2 (en) | 2016-10-25 |
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EA028041B1 (ru) | 2017-09-29 |
TR201901652T4 (tr) | 2019-02-21 |
CA2877543A1 (en) | 2014-01-16 |
WO2014009296A1 (en) | 2014-01-16 |
JP6259824B2 (ja) | 2018-01-10 |
BR112015000790A2 (pt) | 2017-06-27 |
EP2872511A1 (en) | 2015-05-20 |
CA2877543C (en) | 2020-09-22 |
US20150191482A1 (en) | 2015-07-09 |
ES2711131T3 (es) | 2019-04-30 |
JP2015525752A (ja) | 2015-09-07 |
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