PE20131164A1 - IMIDAZOPIRIDAZINAS SUSTITUIDAS COMO INHIBIDORES DE LA QUINASA Mps-1 - Google Patents
IMIDAZOPIRIDAZINAS SUSTITUIDAS COMO INHIBIDORES DE LA QUINASA Mps-1Info
- Publication number
- PE20131164A1 PE20131164A1 PE2013000392A PE2013000392A PE20131164A1 PE 20131164 A1 PE20131164 A1 PE 20131164A1 PE 2013000392 A PE2013000392 A PE 2013000392A PE 2013000392 A PE2013000392 A PE 2013000392A PE 20131164 A1 PE20131164 A1 PE 20131164A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- integer
- response
- cellular
- methylbenzamide
- Prior art date
Links
- 108091000080 Phosphotransferase Proteins 0.000 title abstract 2
- 150000005233 imidazopyridazines Chemical group 0.000 title abstract 2
- 102000020233 phosphotransferase Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- -1 2-HYDROXY-2-METHYLPROPYL Chemical class 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000024932 T cell mediated immunity Effects 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 230000001413 cellular effect Effects 0.000 abstract 1
- 230000036755 cellular response Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000004044 response Effects 0.000 abstract 1
- FDDDEECHVMSUSB-UHFFFAOYSA-N sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- 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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with 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
- A61K31/495—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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- 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
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hematology (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)
- Cosmetics (AREA)
- Paper (AREA)
Abstract
REFERIDA A DERIVADOS IMIDAZOPIRIDAZINAS DE FORMULA (I), DONDE A ES UN GRUPO (a), (b), (c) O (d); Z ES C(=O)N(H)R2, C(=S)N(H)R2, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, HALO-ALQUILO C1-C6, ENTRE OTROS; R3 ES ARIL-X O HETEROARIL-X; X ES O, NR6, S(=O)p, ENTRE OTROS; p ES UN ENTERO DE 0 A 2; n ES UN ENTERO DE 0 A 5; m ES UN ENTERO DE 0 A 6; R4a Y R4d SON H; R4b Y R4c SON H, HALO, CN, OH, ENTRE OTROS; R5 ES H, ALQUILO C1-C6, (CH2)n-ALQUENILO C2-C6, ENTRE OTROS; R6, R6 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-CICLOPROPIL-4-{6-[(2-METOXIFENIL)SULFANIL)]-8-[(3,3,3-TRIFLUOROPROPIL)AMINO]IMIDAZO[1,2-b]PIRIDAZIN-3-IL}-2-METILBENZAMIDA, N-CICLOPROPIL-4-{8-[(2-HIDROXI-2-METILPROPIL)AMINO]-6-[(4-HIDROXIFENIL)SULFANIL]-IMIDAZO[1,2-b]PIRIDAZIN-3-IL}-2-METILBENZAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN METODO DE PREPARACION. DICHOS COMPUESTOS INHIBEN LA QUINASA Mps-1 (DEL HUSO MONOPOLAR 1) Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES RELACIONADAS CON LA PROLIFERACION CELULAR DESCONTROLADA, CON UNA RESPUESTA INMUNE CELULAR INAPROPIADA, RESPUESTA INFLAMATORIA CELULAR INAPROPIADA, ENTRE OTRAS
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10176134 | 2010-09-10 | ||
| EP11075022 | 2011-02-04 | ||
| EP11170775 | 2011-06-21 | ||
| EP11170771 | 2011-06-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20131164A1 true PE20131164A1 (es) | 2013-10-30 |
Family
ID=44545741
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013000392A PE20131164A1 (es) | 2010-09-10 | 2011-09-06 | IMIDAZOPIRIDAZINAS SUSTITUIDAS COMO INHIBIDORES DE LA QUINASA Mps-1 |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US9255100B2 (es) |
| EP (1) | EP2614063B1 (es) |
| JP (1) | JP5824050B2 (es) |
| KR (1) | KR20140032337A (es) |
| CN (1) | CN103370318B (es) |
| AP (1) | AP3607A (es) |
| AR (1) | AR082946A1 (es) |
| AU (1) | AU2011298844B2 (es) |
| BR (1) | BR112013005679A2 (es) |
| CA (1) | CA2810755A1 (es) |
| CO (1) | CO6720961A2 (es) |
| CR (1) | CR20130102A (es) |
| CU (1) | CU24187B1 (es) |
| CY (1) | CY1117352T1 (es) |
| DK (1) | DK2614063T3 (es) |
| DO (1) | DOP2013000054A (es) |
| EA (1) | EA023420B1 (es) |
| EC (1) | ECSP13012752A (es) |
| ES (1) | ES2568220T3 (es) |
| HR (1) | HRP20160360T1 (es) |
| HU (1) | HUE028771T2 (es) |
| IL (1) | IL225058A (es) |
| MA (1) | MA34516B1 (es) |
| ME (1) | ME02389B (es) |
| MX (1) | MX2013002713A (es) |
| MY (1) | MY185139A (es) |
| NZ (1) | NZ607904A (es) |
| PE (1) | PE20131164A1 (es) |
| PH (1) | PH12013500454A1 (es) |
| PL (1) | PL2614063T3 (es) |
| RS (1) | RS54661B1 (es) |
| SA (1) | SA111320735B1 (es) |
| SG (1) | SG188417A1 (es) |
| SI (1) | SI2614063T1 (es) |
| TW (1) | TWI541243B (es) |
| UY (1) | UY33598A (es) |
| WO (1) | WO2012032031A1 (es) |
| ZA (1) | ZA201301756B (es) |
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|---|---|---|---|---|
| TWI541243B (zh) | 2010-09-10 | 2016-07-11 | 拜耳知識產權公司 | 經取代咪唑并嗒 |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| US9416132B2 (en) * | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| JP6166289B2 (ja) * | 2012-03-14 | 2017-07-19 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 置換イミダゾピリダジン |
| UA125503C2 (uk) | 2012-06-13 | 2022-04-13 | Інсайт Холдинґс Корпорейшн | Заміщені трициклічні сполуки як інгібітори fgfr |
| WO2014020041A1 (en) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer |
| WO2014020043A1 (en) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9573954B2 (en) | 2012-11-16 | 2017-02-21 | University Health Network | Pyrazolopyrimidine compounds |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| TW201437211A (zh) * | 2013-03-01 | 2014-10-01 | Bayer Pharma AG | 經取代咪唑并嗒□ |
| WO2014172644A2 (en) | 2013-04-19 | 2014-10-23 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
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| AU2014280224A1 (en) * | 2013-06-13 | 2016-01-07 | Bayer Pharma Aktiengesellschaft | Combination of a imidazopyridazine derivative and a mitotic agent for the treatment of cancer |
| CN103360399B (zh) * | 2013-08-02 | 2016-03-02 | 北京大学 | 6-芳基取代-咪唑-[1,2-b]哒嗪类衍生物，其制备方法及用途 |
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| WO2015157955A1 (en) | 2014-04-17 | 2015-10-22 | Abbvie Inc. | Heterocyclic btk inhibit ors |
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| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| UA121669C2 (uk) | 2015-02-20 | 2020-07-10 | Інсайт Корпорейшн | Біциклічні гетероцикли як інгібітори fgfr |
| CN114592061A (zh) | 2015-04-17 | 2022-06-07 | 荷兰转化研究中心有限责任公司 | 用于ttk抑制剂化疗的预后生物标记 |
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| BR112018010271A2 (pt) * | 2015-12-04 | 2018-11-27 | Exxonmobil Research And Engineering Company | material cristalino sintético emm-28, sua preparação e uso |
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| KR102700233B1 (ko) * | 2016-07-18 | 2024-08-28 | 유니버시티 헬스 네트워크 | 고체 형태의 ttk 억제제 |
| WO2018189185A1 (en) * | 2017-04-11 | 2018-10-18 | Straumann Holding Ag | Dental implant |
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| SI3788047T1 (sl) | 2018-05-04 | 2024-11-29 | Incyte Corporation | Trdne oblike inhibitorja fgfr in postopki priprave le-teh |
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| FI3792260T3 (fi) | 2018-05-08 | 2024-10-01 | Nippon Shinyaku Co Ltd | Atsabentsimidatsoliyhdisteitä ja lääkkeitä |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
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| CN111978325B (zh) * | 2019-05-22 | 2023-11-17 | 中国药科大学 | 咪唑并哒嗪类mnk1/mnk2激酶抑制剂及其制备方法和应用 |
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| WO2024155844A1 (en) * | 2023-01-19 | 2024-07-25 | Skyhawk Therapeutics, Inc. | Compositions useful for modulating splicing |
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| EP2576560B1 (en) | 2010-06-01 | 2015-09-30 | Bayer Intellectual Property GmbH | Substituted imidazopyrazines |
| TWI541243B (zh) | 2010-09-10 | 2016-07-11 | 拜耳知識產權公司 | 經取代咪唑并嗒 |
| US20140135319A1 (en) | 2010-12-17 | 2014-05-15 | Bayer Intellectual Property Gmbh | 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| JP2013545776A (ja) | 2010-12-17 | 2013-12-26 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 過剰増殖性障害の治療におけるｍｐｓ−１およびｔｋｋ阻害剤として使用するための６置換イミダゾピラジン |
| US9284317B2 (en) | 2010-12-17 | 2016-03-15 | Bayer Intellectual Property Gmbh | Substituted imidazo[1,2-a]pyrazines as MPS-1 inhibitors |
| EP2651946B1 (en) | 2010-12-17 | 2015-05-27 | Bayer Intellectual Property GmbH | 2-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| ES2530802T3 (es) | 2010-12-17 | 2015-03-06 | Bayer Ip Gmbh | Imidazopirazinas 6-tiosustituidas para uso como inhibidores de MPS-1 y TKK en el tratamiento de trastornos hiperproliferativos |
| WO2012080229A1 (en) | 2010-12-17 | 2012-06-21 | Bayer Pharma Aktiengesellschaft | Imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment hyperproliferative disorders |
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