IL251777B - 5-(3-hydroxy-propyn-1-yl)-3-pyrazol-4-yl)-indole derivatives as nick inhibitors - Google Patents
5-(3-hydroxy-propyn-1-yl)-3-pyrazol-4-yl)-indole derivatives as nick inhibitorsInfo
- Publication number
- IL251777B IL251777B IL251777A IL25177717A IL251777B IL 251777 B IL251777 B IL 251777B IL 251777 A IL251777 A IL 251777A IL 25177717 A IL25177717 A IL 25177717A IL 251777 B IL251777 B IL 251777B
- Authority
- IL
- Israel
- Prior art keywords
- propyn
- pyrazol
- hydroxy
- indole derivatives
- nik inhibitors
- Prior art date
Links
- NLXABNCCPHDZEM-UHFFFAOYSA-N OCC#CC=1C=C2C(=CNC2=CC=1)C=1C=NNC=1 Chemical class OCC#CC=1C=C2C(=CNC2=CC=1)C=1C=NNC=1 NLXABNCCPHDZEM-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14190072 | 2014-10-23 | ||
| PCT/EP2015/074433 WO2016062791A1 (en) | 2014-10-23 | 2015-10-22 | New pyrazole derivatives as nik inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL251777A0 IL251777A0 (en) | 2017-06-29 |
| IL251777B true IL251777B (en) | 2021-09-30 |
Family
ID=51865980
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL251777A IL251777B (en) | 2014-10-23 | 2017-04-19 | 5-(3-hydroxy-propyn-1-yl)-3-pyrazol-4-yl)-indole derivatives as nick inhibitors |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9981962B2 (enExample) |
| EP (1) | EP3209654B1 (enExample) |
| JP (1) | JP6616411B2 (enExample) |
| KR (1) | KR102499862B1 (enExample) |
| CN (1) | CN107074818B (enExample) |
| AU (1) | AU2015334916B2 (enExample) |
| BR (1) | BR112017008039B1 (enExample) |
| CA (1) | CA2960335C (enExample) |
| EA (1) | EA033236B1 (enExample) |
| ES (1) | ES2704749T3 (enExample) |
| IL (1) | IL251777B (enExample) |
| MX (1) | MX371150B (enExample) |
| WO (1) | WO2016062791A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| TWI704146B (zh) | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物 |
| TWI627173B (zh) | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物 |
| EA033237B1 (ru) | 2014-10-23 | 2019-09-30 | Янссен Фармацевтика Нв | Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее |
| WO2016062792A1 (en) | 2014-10-23 | 2016-04-28 | Janssen Pharmaceutica Nv | New compounds as nik inhibitors |
| AU2015334914B2 (en) | 2014-10-23 | 2019-09-19 | Janssen Pharmaceutica Nv | New thienopyrimidine derivatives as NIK inhibitors |
| JP6616411B2 (ja) | 2014-10-23 | 2019-12-04 | ヤンセン ファーマシューティカ エヌ．ベー． | 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体 |
| CN122562777A (zh) * | 2015-12-02 | 2026-08-14 | 阿斯特来亚治疗有限责任公司 | 哌啶基痛敏肽受体化合物 |
| US10112924B2 (en) | 2015-12-02 | 2018-10-30 | Astraea Therapeutics, Inc. | Piperdinyl nociceptin receptor compounds |
| EP3405464B1 (en) * | 2016-01-22 | 2019-12-04 | Janssen Pharmaceutica NV | New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors |
| CR20210587A (es) | 2019-05-31 | 2022-02-11 | Janssen Pharmaceutica Nv | Inhibidores de molécula pequeña de quinasa inductora de nf-kb |
| TW202402269A (zh) * | 2022-05-26 | 2024-01-16 | 大陸商迪哲（江蘇）醫藥股份有限公司 | ＲＯＣＫ（Ｒｈｏ相關激酶）抑制劑及其用途 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0510319A (pt) | 2004-04-26 | 2007-10-16 | Pfizer | inibidores da enzima integrase de hiv |
| TW200736260A (en) | 2005-11-10 | 2007-10-01 | Smithkline Beecham Corp | Inhibitors of Akt activity |
| DE102008005493A1 (de) | 2008-01-22 | 2009-07-23 | Merck Patent Gmbh | 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate |
| AU2009263037B2 (en) * | 2008-06-26 | 2011-10-06 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| CA2728559A1 (en) | 2008-07-03 | 2010-01-07 | Exelixis Inc. | Cdk modulators |
| WO2010042337A1 (en) | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| CN101723936B (zh) | 2008-10-27 | 2014-01-15 | 上海睿星基因技术有限公司 | 激酶抑制剂及其在药学中的用途 |
| WO2011050245A1 (en) | 2009-10-23 | 2011-04-28 | Yangbo Feng | Bicyclic heteroaryls as kinase inhibitors |
| AR085908A1 (es) * | 2011-03-16 | 2013-11-06 | Hoffmann La Roche | DERIVADOS DE 3-BUTIN-2-OL Y DE CARBONITRILO CON ACTIVIDAD INHIBIDORA DE LA QUINASA INDUCTORA DE NF-kB (NIK) |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| TWI704146B (zh) | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物 |
| TWI627173B (zh) * | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物 |
| WO2016062792A1 (en) | 2014-10-23 | 2016-04-28 | Janssen Pharmaceutica Nv | New compounds as nik inhibitors |
| EA033237B1 (ru) | 2014-10-23 | 2019-09-30 | Янссен Фармацевтика Нв | Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее |
| AU2015334914B2 (en) | 2014-10-23 | 2019-09-19 | Janssen Pharmaceutica Nv | New thienopyrimidine derivatives as NIK inhibitors |
| JP6616411B2 (ja) | 2014-10-23 | 2019-12-04 | ヤンセン ファーマシューティカ エヌ．ベー． | 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体 |
-
2015
- 2015-10-22 JP JP2017522072A patent/JP6616411B2/ja not_active Expired - Fee Related
- 2015-10-22 US US15/520,342 patent/US9981962B2/en not_active Expired - Fee Related
- 2015-10-22 ES ES15784360T patent/ES2704749T3/es active Active
- 2015-10-22 CN CN201580057462.XA patent/CN107074818B/zh not_active Expired - Fee Related
- 2015-10-22 MX MX2017005283A patent/MX371150B/es active IP Right Grant
- 2015-10-22 EA EA201790904A patent/EA033236B1/ru not_active IP Right Cessation
- 2015-10-22 EP EP15784360.8A patent/EP3209654B1/en active Active
- 2015-10-22 AU AU2015334916A patent/AU2015334916B2/en not_active Ceased
- 2015-10-22 WO PCT/EP2015/074433 patent/WO2016062791A1/en not_active Ceased
- 2015-10-22 BR BR112017008039-7A patent/BR112017008039B1/pt not_active IP Right Cessation
- 2015-10-22 KR KR1020177010800A patent/KR102499862B1/ko active Active
- 2015-10-22 CA CA2960335A patent/CA2960335C/en active Active
-
2017
- 2017-04-19 IL IL251777A patent/IL251777B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR102499862B1 (ko) | 2023-02-13 |
| US9981962B2 (en) | 2018-05-29 |
| CN107074818B (zh) | 2020-04-17 |
| AU2015334916B2 (en) | 2020-02-06 |
| JP6616411B2 (ja) | 2019-12-04 |
| EA201790904A1 (ru) | 2017-08-31 |
| WO2016062791A1 (en) | 2016-04-28 |
| MX2017005283A (es) | 2017-08-15 |
| AU2015334916A1 (en) | 2017-03-23 |
| EP3209654B1 (en) | 2018-10-03 |
| ES2704749T3 (es) | 2019-03-19 |
| KR20170068488A (ko) | 2017-06-19 |
| US20170334900A1 (en) | 2017-11-23 |
| EA033236B1 (ru) | 2019-09-30 |
| JP2017531677A (ja) | 2017-10-26 |
| EP3209654A1 (en) | 2017-08-30 |
| CA2960335C (en) | 2023-09-19 |
| CN107074818A (zh) | 2017-08-18 |
| MX371150B (es) | 2020-01-20 |
| IL251777A0 (en) | 2017-06-29 |
| CA2960335A1 (en) | 2016-04-28 |
| BR112017008039A2 (pt) | 2017-12-19 |
| BR112017008039B1 (pt) | 2023-04-11 |
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