AR095308A1 - Compuesto de 2-piridona, composición farmacéutica que lo comprende y su uso para preparar un medicamento - Google Patents
Compuesto de 2-piridona, composición farmacéutica que lo comprende y su uso para preparar un medicamentoInfo
- Publication number
- AR095308A1 AR095308A1 ARP140101009A ARP140101009A AR095308A1 AR 095308 A1 AR095308 A1 AR 095308A1 AR P140101009 A ARP140101009 A AR P140101009A AR P140101009 A ARP140101009 A AR P140101009A AR 095308 A1 AR095308 A1 AR 095308A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cancer
- haloalkyl
- functional
- optionally substituted
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
-
- 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
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Compuestos de 2-piridona que son inhibidores de la quinasa Reorganizada Durante la Transfección (RET), representados por la fórmula (1) en donde: R¹ es hidrógeno, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₆, hidroxilo, alcoxi C₁₋₆, haloalcoxi C₁₋₆, cicloalcoxi C₃₋₆, amino, (alquil C₁₋₆)amino-, o (alquil C₁₋₆)(alquil C₁₋₆)amino-; cada R² se selecciona independientemente del grupo que consiste en halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₆, ciano, hidroxilo, alcoxi C₁₋₆, haloalcoxi C₁₋₆, cicloalcoxi C₃₋₆, amino, (alquil C₁₋₆)amino-, y (alquil C₁₋₆)(alquil C₁₋₆)amino-; R³ es fenilo o heteroarilo de 5 ó 6 miembros, cada uno de los cuales está sustituido opcionalmente con uno a tres sustituyentes seleccionados independientemente entre halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₆, ciano, heteroarilo de 5 ó 6 miembros, -OR⁴, y CONR⁵R⁶; en donde dicho alquilo C₁₋₆ está sustituido opcionalmente con ciano, hidroxilo, alcoxi C₁₋₄, haloalcoxi C₁₋₄, o -NR⁵R⁶; y en donde dicho sustituyente heteroarilo de 5 ó 6 miembros está sustituido opcionalmente con halógeno, alquilo C₁₋₄, o haloalquilo C₁₋₄; R⁴ es hidrógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₆, o heterocicloalquilo de 4 a 6 miembros; en donde dicho alquilo C₁₋₆ está sustituido opcionalmente con ciano, hidroxilo, alcoxi C₁₋₄, haloalcoxi C₁₋₄, o -NR⁵R⁶; y en donde dicho cicloalquilo C₃₋₆ está sustituido opcionalmente con uno o dos sustituyentes seleccionados independientemente entre alquilo C₁₋₄, haloalquilo C₁₋₄, hidroxilo, hidroxialquilo C₁₋₄, alcoxi C₁₋₄, y haloalcoxi C₁₋₄; y en donde dicho heterocicloalquilo de 4 a 6 miembros está sustituido opcionalmente con uno o dos sustituyentes seleccionados independientemente entre alquilo C₁₋₄ y haloalquilo C₁₋₄; R⁵ y R⁶ se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, alquilo C₁₋₄, y haloalquilo C₁₋₄; o R⁵ y R⁶ tomados junto con el nitrógeno al que están anclados representan un anillo saturado de 5 ó 6 miembros, que contiene opcionalmente un heteroátomo adicional seleccionado entre oxígeno, nitrógeno, y azufre, en donde dicho anillo está sustituido opcionalmente con halógeno, alquilo C₁₋₄, o haloalquilo C₁₋₄; y n es 0, 1, ó 2; o una de sus sales farmacéuticamente aceptables. Composiciones farmacéuticas que los contienen, procedimientos para su preparación, y a su uso en terapia, solos o combinados, para la normalización de la sensibilidad, la motilidad y/o la secreción gastrointestinal y/o trastornos o enfermedades abdominales y/o el tratamiento relacionado con enfermedades relacionadas con la disfunción de RET o en las que la modulación de la actividad de RET puede tener un beneficio terapéutico que incluye, pero no se limita a, todas las clasificaciones del síndrome del intestino irritable (SII) incluyendo diarrea predominante, estreñimiento predominante o un patrón de heces alternante, distensión abdominal funcional, estreñimiento funcional, diarrea funcional, trastorno intestinal funcional no especificado, síndrome de dolor abdominal funcional, estreñimiento idiopático crónico, trastornos esofágicos funcionales, trastornos gastroduodenales funcionales, dolor anorrectal funcional, enfermedad inflamatoria del intestino, enfermedades proliferativas tales como cáncer de pulmón de células no pequeñas, carcinoma hepatocelular, cáncer colorrectal, cáncer de tiroides medular, cáncer de tiroides folicular, cáncer de tiroides anaplásico, cáncer de tiroides papilar, tumores cerebrales, cáncer de la cavidad peritoneal, tumores sólidos, otro cáncer de pulmón, cáncer de cabeza y cuello, gliomas, neuroblastomas, Síndrome de Von Hippel-Lindau y tumores de riñón, cáncer de mama, cáncer de las trompas de falopio, cáncer de ovario, cáncer de células transicionales, cáncer de próstata, cáncer de esófago y de la unión gastroesofágica, cáncer biliar, adenocarcinoma, y cualquier tumor maligno con un incremento de la actividad quinasa RET.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013072683 | 2013-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR095308A1 true AR095308A1 (es) | 2015-10-07 |
Family
ID=51529959
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140101009A AR095308A1 (es) | 2013-03-15 | 2014-03-14 | Compuesto de 2-piridona, composición farmacéutica que lo comprende y su uso para preparar un medicamento |
Country Status (3)
| Country | Link |
|---|---|
| US (2) | US8937071B2 (es) |
| AR (1) | AR095308A1 (es) |
| MA (1) | MA38394B1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| EP2571883B1 (en) | 2010-05-20 | 2015-01-07 | Array Biopharma, Inc. | Macrocyclic compounds as trk kinase inhibitors |
| CN103379564B (zh) * | 2012-04-20 | 2016-08-03 | 电信科学技术研究院 | 一种小区内切换方法及装置 |
| EP2848022A4 (en) * | 2012-05-07 | 2015-12-02 | Ericsson Telefon Ab L M | BASE STATION AND RELAY N UD MOBILITY METHOD |
| PL2970191T3 (pl) | 2013-03-15 | 2017-07-31 | Glaxosmithkline Intellectual Property Development Limited | Pochodne pirydyny jako inhibitory kinazy przebudowanej podczas transfekcji (RET) |
| US9879021B2 (en) | 2014-09-10 | 2018-01-30 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
| MX2017003114A (es) * | 2014-09-10 | 2017-11-15 | Glaxosmithkline Ip Dev Ltd | Derivados de piridona como inhibidores de cinasa ret (reorganizado durante la transfeccion). |
| RS64122B1 (sr) | 2014-11-16 | 2023-05-31 | Array Biopharma Inc | Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogensulfata |
| CA2992586A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| DK3439663T3 (da) | 2016-04-04 | 2024-08-26 | Loxo Oncology Inc | Fremgangsmåder til behandling af pædiatriske cancere |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| KR102400423B1 (ko) | 2016-04-04 | 2022-05-19 | 록쏘 온콜로지, 인코포레이티드 | (s)-n-(5-((r)-2-(2,5-디플루오로페닐)-피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-하이드록시피롤리딘-1-카복사미드의 액체 제형 |
| US20190142868A1 (en) | 2016-05-13 | 2019-05-16 | Instituto de Medicina Moleccular | Methods of treating diseases associated with ilc3 cells |
| LT3458456T (lt) | 2016-05-18 | 2021-02-25 | Loxo Oncology, Inc. | (s)-n-(5-((r)-2-(2,5-difluorfenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamido gavimas |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| CN111971286B (zh) | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| WO2019143991A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| CA3087972C (en) | 2018-01-18 | 2023-01-10 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| US11964988B2 (en) | 2018-09-10 | 2024-04-23 | Array Biopharma Inc. | Fused heterocyclic compounds as RET kinase inhibitors |
| CA3222177A1 (en) | 2021-06-03 | 2022-12-08 | Fundacao D. Anna De Sommer Champalimaud E Dr. Carlos Montez Champalimaud | Neuro-mesenchyme units control ilc2 and obesity via a brain-adipose circuit |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ517237A (en) | 1999-08-12 | 2004-02-27 | Pharmacia Italia S | 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| JP2004517840A (ja) | 2000-11-27 | 2004-06-17 | フアルマシア・イタリア・エツセ・ピー・アー | フェニルアセトアミド−ピラゾール誘導体およびそれの抗腫瘍薬としての使用 |
| DE10201764A1 (de) | 2002-01-18 | 2003-07-31 | Bayer Cropscience Ag | Substituierte 4-Aminopyridin-Derivate |
| US7968574B2 (en) | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| KR20090064602A (ko) | 2006-10-16 | 2009-06-19 | 노파르티스 아게 | 단백질 키나제 억제제로서 유용한 페닐아세트아미드 |
| PL2848610T3 (pl) | 2006-11-15 | 2018-01-31 | Ym Biosciences Australia Pty | Inhibitory aktywności kinazy |
| BR112012003661A2 (pt) | 2009-08-19 | 2017-04-25 | Ambit Biosciences Corp | "compostos de biarila e métodos de uso dos mesmos." |
| JP6097998B2 (ja) | 2010-12-16 | 2017-03-22 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ロイコトリエン生成のビアリールアミドインヒビター |
-
2014
- 2014-03-14 US US14/210,726 patent/US8937071B2/en not_active Expired - Fee Related
- 2014-03-14 AR ARP140101009A patent/AR095308A1/es unknown
- 2014-03-14 MA MA38394A patent/MA38394B1/fr unknown
- 2014-12-09 US US14/564,625 patent/US9035063B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US8937071B2 (en) | 2015-01-20 |
| US9035063B2 (en) | 2015-05-19 |
| US20150099762A1 (en) | 2015-04-09 |
| MA38394A1 (fr) | 2017-11-30 |
| MA38394B1 (fr) | 2018-04-30 |
| US20140275111A1 (en) | 2014-09-18 |
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