AR085489A1 - Derivados de triazolopiridinas, composiciones farmaceuticas que los contienen, proceso para prepararlos, intermediarios de dicho proceso y uso de los mismos para el tratamiento de enfermedades autoinmunes e inflamatorias - Google Patents
Derivados de triazolopiridinas, composiciones farmaceuticas que los contienen, proceso para prepararlos, intermediarios de dicho proceso y uso de los mismos para el tratamiento de enfermedades autoinmunes e inflamatoriasInfo
- Publication number
- AR085489A1 AR085489A1 ARP120100626A ARP120100626A AR085489A1 AR 085489 A1 AR085489 A1 AR 085489A1 AR P120100626 A ARP120100626 A AR P120100626A AR P120100626 A ARP120100626 A AR P120100626A AR 085489 A1 AR085489 A1 AR 085489A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- optionally substituted
- ring
- halogen
- Prior art date
Links
Classifications
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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
- C07D471/04—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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
-
- 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
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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
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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
-
- 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- C07D487/10—Spiro-condensed systems
-
- 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
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Abstract
Reivindicación 1: Un compuesto de la fórmula general (1) y estereoisómeros, sales y solvatos farmacéuticamente aceptables de los mismos, donde: R1 es H, halógeno, CN, OH, alquilo C1-6, fluoroalquilo C1-6, difluoroalquilo C1-6, trifluoroalquilo C1-6, hidroxialquilo C1-6, cianoalquilo C1-6, (alcoxi C1-3)alquilo C1-6 (opcionalmente sustituido por hidroxi), di(alcoxi C1-3)alquilo C1-6, alcoxi C1-6, fluoroalcoxi C1-6, difluoroalcoxi C1-6, trifluoroalcoxi C1-6, hidroxialcoxi C2-6, cianoalcoxi C1-6, (alcoxi C1-3)alcoxi C2-6, di(alcoxi C1-3)alcoxi C2-6, (cicloalquil C3-6)metoxi, oxetanilmetoxi (opcionalmente sustituido por metilo), (alquilo C1-6)sulfanilo, -C(=O)NRaRb, -CH2C(=O)NRcRd o cicloalquilo C3-6 opcionalmente sustituido por -CH2OH o -CH2O(alquilo C1-4); Ra, Rb, Rc y Rd se seleccionan independientemente de H y alquilo C1-4; R2 es H, halógeno, CN, O, alquilo C1-6, fluoroalquilo C1-6, difluoroalquilo C1-6, trifluoroalquilo C1-6, hidroxialquilo C1-6, (alcoxi C1-3)alquilo C1-6, alcoxi C1-6 (opcionalmente sustituido por (alquilo C1-6)C(=O)O-, amino(alquilo C1-6)C(=O)O-, o fenil(C=O)O-), fluoroalcoxi C1-6, difluoroalcoxi C1-6, trifluoroalcoxi C1-6, hidroxialcoxi C2-6, (alcoxi C1-3)alcoxi C2-6, (cicloalquil C3-6)metoxi, cicloalcoxi C3-6 (opcionalmente sustituido por OH), oxetanilmetoxi (opcionalmente sustituido por metilo), tetrahidropiraniloxi, (alquil C1-6)sulfanilo, hidroxi(alquil C2-6)sulfanilo, (alquil C1-3sulfanil)alcoxi C2-6, -COOH, hetAr1, -C(=O)NReRf, -NReC(=O)Rf, oxetanilo o ciclopropilo opcionalmente sustituido por -CH2OH o -CH2O(alquilo C1-6); o R1 y R2 junto con los átomos a los que están unidos forman un anillo heterocíclico de 5 - 6 miembros que tiene 1 - 2 heteroátomos del anillo que se seleccionan independientemente de O y N donde dicho anillo se sustituye opcionalmente por alquilo C1-4; hetAr1 es un anillo heteroarilo de 5 - 6 miembros que tiene uno o dos átomos de nitrógeno del anillo y que está opcionalmente sustituido por uno o más grupos seleccionados de alquilo C1-6; Re y Rf son independientemente H, alquilo C1-6 o ciclopropilo opcionalmente sustituido por alquilo C1-4; R3 es H, halógeno o alquilo C1-6; R4 es un compuesto de fórmula (2); R5 es CF3, CH2F, CHF2, metilo o etilo; R5a es H o metilo; o R5 y R5a, junto con el átomo al cual están unidos forman un anillo ciclopropilo; R6 es H, NH2, OH, (alquilo C1-6)NH-, fluoro(alquilo C1-6)NH-, hidroxi(alquilo C1-6)NH-, (cicloalquilo C3-6)CH2NH-, (alquilo C1-6)C(=O)NH-, (alquilo C1-6)OC(=O)NH- (opcionalmente sustituido por 5-metil-2-oxo-1,3-dioxol-4-ilo) o aminoalquilo C1-6-; R7 es H, hidroxialquilo C1-6; o R6 y R7 junto con el átomo al que están unido forman un heterociclo espirocíclico de 5 - 6 miembros que tiene un átomo de nitrógeno en el anillo; R8 es H, halógeno, OH o alcoxi C1-6; o R6 y R8 junto con los átomos de carbono a los que están unidos forman un anillo ciclopropilo opcionalmente sustituido por NH2; R9 es H; o R6 y R9 juntos forman un grupo de enlace que tiene la fórmula -CH2NH- que une los átomos de carbono a los que están unidos; y R10 es H o halógeno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161446902P | 2011-02-25 | 2011-02-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR085489A1 true AR085489A1 (es) | 2013-10-09 |
Family
ID=46000320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120100626A AR085489A1 (es) | 2011-02-25 | 2012-02-24 | Derivados de triazolopiridinas, composiciones farmaceuticas que los contienen, proceso para prepararlos, intermediarios de dicho proceso y uso de los mismos para el tratamiento de enfermedades autoinmunes e inflamatorias |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US8889704B2 (es) |
| EP (1) | EP2678329B1 (es) |
| JP (2) | JP6039585B2 (es) |
| KR (1) | KR101940338B1 (es) |
| CN (1) | CN103492377B (es) |
| AR (1) | AR085489A1 (es) |
| AU (1) | AU2012254082B2 (es) |
| BR (1) | BR112013021675A2 (es) |
| CA (1) | CA2828269C (es) |
| CL (1) | CL2013002446A1 (es) |
| CO (1) | CO6771441A2 (es) |
| CR (1) | CR20130460A (es) |
| CY (1) | CY1117197T1 (es) |
| DK (1) | DK2678329T3 (es) |
| ES (1) | ES2563152T3 (es) |
| HK (1) | HK1190714A1 (es) |
| HR (1) | HRP20160134T1 (es) |
| HU (1) | HUE027675T2 (es) |
| IL (1) | IL228108A (es) |
| ME (1) | ME02365B (es) |
| MX (1) | MX339899B (es) |
| PL (1) | PL2678329T3 (es) |
| RS (1) | RS54586B1 (es) |
| RU (1) | RU2598846C2 (es) |
| SG (1) | SG192944A1 (es) |
| SI (1) | SI2678329T1 (es) |
| SM (1) | SMT201600052B (es) |
| TW (1) | TWI529170B (es) |
| UA (1) | UA111075C2 (es) |
| UY (1) | UY33924A (es) |
| WO (1) | WO2012154274A1 (es) |
| ZA (1) | ZA201306997B (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| PL3409278T3 (pl) | 2011-07-21 | 2021-02-22 | Sumitomo Pharma Oncology, Inc. | Heterocykliczne inhibitory kinazy białkowej |
| RU2014145806A (ru) * | 2012-04-25 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Способы производства (3,4-дихлорфенил)-((s)-3-пропил-пирролидин-3-ил)-метанонгидрохлорида |
| CA2897200C (en) | 2013-01-14 | 2021-07-06 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| US9200004B2 (en) | 2013-01-15 | 2015-12-01 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
| SG11201601259YA (en) | 2013-08-23 | 2016-03-30 | Incyte Corp | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| MA45122A (fr) * | 2016-05-24 | 2019-04-10 | Constellation Pharmaceuticals Inc | Inhibiteurs hétérocycliques de cbp/ep300 et leur utilisation dans le traitement du cancer |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| CA3095580A1 (en) | 2018-04-13 | 2019-10-17 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
| EP3825303A4 (en) | 2018-07-17 | 2022-07-06 | Nippon Chemiphar Co., Ltd. | T-CALCIUM CHANNEL BLOCKERS |
| CN108912032A (zh) * | 2018-08-13 | 2018-11-30 | 南通大学 | 一种（3s，4r）-4-甲基吡咯烷-3-基氨基甲醇叔丁酯盐酸盐的化学合成方法 |
| CN109053526A (zh) * | 2018-08-13 | 2018-12-21 | 南通大学 | 一种（3r，4s）-4-甲基吡咯烷-3-基氨基甲酸叔丁酯盐酸盐的化学合成方法 |
| US20220125777A1 (en) | 2019-02-01 | 2022-04-28 | Pfizer Inc. | Combination of a cdk inhibitor and a pim inhibitor |
| WO2020167990A1 (en) | 2019-02-12 | 2020-08-20 | Tolero Pharmaceuticals, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| US20220056043A1 (en) * | 2019-02-19 | 2022-02-24 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Nitrogen-containing fused cyclic compound, preparation method therefor and use thereof |
| US20220226299A1 (en) | 2019-03-29 | 2022-07-21 | Nippon Chemiphar Co., Ltd. | Use of t-type calcium channel blocker for treating pruritus |
| CN111171023B (zh) * | 2020-01-10 | 2021-12-21 | 中国药科大学 | 一种具有Pim1抑制活性的化合物及其制备方法与医药用途 |
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| JP2003513975A (ja) | 1999-11-12 | 2003-04-15 | ニューロゲン コーポレイション | 二環式および三環式のヘテロ芳香族化合物 |
| UA75055C2 (uk) * | 1999-11-30 | 2006-03-15 | Пфайзер Продактс Інк. | Похідні бензоімідазолу, що використовуються як антипроліферативний засіб, фармацевтична композиція на їх основі |
| CN1173975C (zh) | 2000-04-27 | 2004-11-03 | 山之内制药株式会社 | 咪唑并吡啶衍生物 |
| DE10038019A1 (de) | 2000-08-04 | 2002-02-14 | Bayer Ag | Substituierte Triazolopyrid(az)ine |
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| TWI496779B (zh) * | 2008-08-19 | 2015-08-21 | Array Biopharma Inc | 作為ｐｉｍ激酶抑制劑之三唑吡啶化合物 |
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2012
- 2012-02-24 JP JP2013555610A patent/JP6039585B2/ja not_active Expired - Fee Related
- 2012-02-24 SI SI201230453A patent/SI2678329T1/sl unknown
- 2012-02-24 AR ARP120100626A patent/AR085489A1/es active IP Right Grant
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