AR088085A1 - Derivados heterociclicos nitrogenados y usos sobre el receptor de histamina - Google Patents
Derivados heterociclicos nitrogenados y usos sobre el receptor de histaminaInfo
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- AR088085A1 AR088085A1 ARP120103614A ARP120103614A AR088085A1 AR 088085 A1 AR088085 A1 AR 088085A1 AR P120103614 A ARP120103614 A AR P120103614A AR P120103614 A ARP120103614 A AR P120103614A AR 088085 A1 AR088085 A1 AR 088085A1
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- alkyl
- heterocyclyl
- heteroatoms
- carboxyl
- amino
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- C07D471/12—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 three hetero rings
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- 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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- 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
- A61K31/4196—1,2,4-Triazoles
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- 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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- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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Abstract
La presente se refiere a compuestos heterocíclicos que son de utilidad en la preparación de fármacos para el tratamiento de enfermedades asociadas con diversas funciones del receptor de histamina 4. En especial, los citados fármacos son de utilidad para el tratamiento de enfermedades inflamatorias, alergia, dolor, pólipos nasales, rinitis, sinusitis crónica, congestión nasal, prurito nasal, asma, enfermedad pulmonar obstructiva crónica, artritis reumatoide, dermatitis atópica, psoriasis, eczema, prurito, picazón de la piel, urticaria, urticaria idiopática crónica, escleroderma, conjuntivitis, queratoconjuntivitis, inflamación ocular, sequedad ocular, disfunción cardiaca, arritmia, ateroesclerosis, esclerosis múltiple, enfermedad intestinal inflamatoria (incluso colitis, enfermedad de Crohn, colitis ulcerante), dolor inflamatorio, dolor neuropático, dolor osteoartrítico, enfermedad tiroidea autoinmune, diabetes inmunomediada (también conocida como tipo I), lupus, adherencias posquirúrgicas, trastornos vestibulares y cáncer. Reivindicación 1: Un compuesto heterocíclico de la fórmula (1), o un racemato, un isómero o una sal farmacéuticamente aceptable del mismo, en el cual: cada uno de los siguientes: X¹, X², X³ y X⁴ es, independientemente, C ó N, con la condición de que al menos uno entre X¹, X², X³ y X⁴ sea N, R¹ es un mono- o poli-heterociclilo saturado o insaturado de 3 a 12 miembros, que contiene de 1 a 3 heteroátomos (con preferencia, heteroátomos seleccionados entre N, O y S), donde R¹ está insustituido o sustituido con 1 a 3 sustituyentes seleccionados entre -NR⁶R⁷, -alquil C₁₋₆-NR⁶R⁷ y R⁸; o R¹ se selecciona entre -H, -NR⁶R⁷ y R⁸; R², R³, R⁴ y R⁵ pueden ser iguales o diferentes; y cada uno de ellos se selecciona de un modo independiente entre -H; alquilo C₁₋₆; haloalquilo C₁₋₆; perhaloalquilo C₁₋₆; -amino-alquilo C₁₋₆; cicloalquilo C₃₋₈; -halógeno (-F, -Cl, -Br, -I); -CN; alcoxi C₁₋₆; haloalcoxi C₁₋₆; perhaloalcoxi C₁₋₆; alquenilo-C₂₋₇; alquinilo C₂₋₈; -amino; -amido; alquil C₁₋₆-carboxilo; -carboxilo (-COOH); -acilo C₁₋₆ -OH; -nitro (-NO₂) ; -arilo C₆₋₁₀; -heterociclilo; y -O-alquil C₁₋₆-heterociclilo, donde el heterociclilo es un heterociclilo saturado o insaturado de 3 a 6 miembros, que contiene 1 a 3 heteroátomos (con preferencia, heteroátomos seleccionados entre N, O y S), con la condición de que cuando X¹ sea N, R² no exista; cuando X² sea N, R³ no exista; cuando X³ sea N, R⁴ no exista; y cuando X⁴ sea N, R⁵ no exista; cada uno de los siguientes: Y¹, Y², Y³, Y⁴ e Y⁵ es, independientemente, C o un heteroátomo (con preferencia, un heteroátomo seleccionado independientemente entre N, O y S), con la condición de que al menos uno de los siguientes: Y¹, Y², Y³, Y⁴ e Y⁵ sea un heteroátomo seleccionado independientemente entre N, O y S, cada uno de los siguientes: Y² e Y³ puede sustituirse de un modo independiente con R⁹, Y⁴ puede sustituirse con -H o alquilo C₁₋₆; cada R⁶ y R⁷ se selecciona, independientemente, entre -H; alquilo C₁₋₆ cicloalquilo C₃₋₈; -heterociclilo; -amino-mono- o di-alquilo C₁₋₆; alquil C₁₋₆-amino-mono- o di-alquil C₁₋₆; alquil C₁₋₆-heterociclilo; alquil C₁₋₆-carboxilo; -carboxilo (-COOH); y fenilo, donde el heterociclilo es un heterociclilo saturado o insaturado de 3 a 6 miembros, que contiene 1 a 3 heteroátomos (con preferencia, heteroátomos seleccionados entre N, O y S); R⁸ es alquilo C₁₋₆; alcoxi C₁₋₆; -OH; -amino; -alquil C₁₋₆-amino; cicloalquilo C₃₋₈; -S-alquil C₁₋₆-amino-mono- o di-alquil C₁₋₆; -S-alquil C₁₋₆-heterociclilo; -O-heterociclilo; o -O-alquil C₁₋₆-heterociclilo, donde el heterociclilo es un heterociclilo saturado o insaturado de 3 a 6 miembros, que contiene 1 a 3 heteroátomos (con preferencia, heteroátomos seleccionados entre N, O y S); y R⁹ se selecciona entre-H; -OH; alquilo C₁₋₆ haloalquilo C₁₋₆; perhaloalquilo C₁₋₆; -amino-mono- o di-alquilo C₁₋₆; cicloalquilo C₃₋₇; -heterociclilo; -arilo C₆₋₁₀; heteroarilo de 5 a 12 miembros; alcoxi C₁₋₆; haloalcoxi C₁₋₆; -halógeno (-F, -Cl, -Br, -I); -amino; -amido; -acilo C₁₋₆; -CN; -carboxilo (-COOH); alquil C₁₋₆-carboxilo; y -nitro (-NO₂), con la condición de que cuando Y⁴ sea N e Y¹, Y², Y³ e Y⁵ sea C, Y³ no esté sustituido con un sustituyente que tenga una parte -C(=O)-, donde cada uno de los siguientes grupos: alquilo, cicloalquilo, heterociclilo, alcoxi, alquenilo, alquinilo, acilo y arilo grupos pueden estar independientemente insustituidos o sustituidos con uno o más sustituyentes (por ejemplo, 1 - 3 sustituyentes) seleccionados del grupo que consiste en alquilo C₁₋₄, -halógeno (-F, -Cl, -Br, -I), -CN, alcoxi C₁₋₄, -amino, -amido, -carboxilo (-COOH), -acilo C₁₋₆, -OH, -nitro (-NO₂), heterociclilo y fenilo, donde el heterociclilo es un heterociclilo saturado o insaturado de 3 a 6 miembros, que contiene 1 a 3 heteroátomos (con preferencia, heteroátomos seleccionados entre N, O y S).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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KR20110100369 | 2011-09-30 | ||
KR20120033444 | 2012-03-30 |
Publications (1)
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AR088085A1 true AR088085A1 (es) | 2014-05-07 |
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ARP120103614A AR088085A1 (es) | 2011-09-30 | 2012-09-28 | Derivados heterociclicos nitrogenados y usos sobre el receptor de histamina |
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Country | Link |
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US (1) | US9586959B2 (es) |
EP (2) | EP3461825B1 (es) |
JP (1) | JP6031107B2 (es) |
KR (1) | KR101800749B1 (es) |
CN (1) | CN103889986B (es) |
AR (1) | AR088085A1 (es) |
AU (1) | AU2012316912B9 (es) |
BR (1) | BR112014007645A2 (es) |
CA (1) | CA2848154C (es) |
CY (1) | CY1121292T1 (es) |
DK (2) | DK3461825T3 (es) |
ES (2) | ES2687693T3 (es) |
FI (1) | FI3461825T3 (es) |
HR (2) | HRP20230893T1 (es) |
HU (2) | HUE040374T2 (es) |
LT (2) | LT2760865T (es) |
MX (1) | MX355795B (es) |
PL (2) | PL3461825T3 (es) |
PT (2) | PT2760865T (es) |
RS (2) | RS57854B1 (es) |
RU (1) | RU2628074C2 (es) |
SG (1) | SG11201400484RA (es) |
SI (2) | SI2760865T1 (es) |
TR (1) | TR201814710T4 (es) |
TW (1) | TWI551600B (es) |
WO (1) | WO2013048214A2 (es) |
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CA2917262A1 (en) | 2013-07-02 | 2015-01-08 | Syngenta Participations Ag | Pesticidally active bi- or tricyclic heterocycles with sulfur containing substituents |
CN103435561B (zh) * | 2013-08-19 | 2016-08-10 | 上海交通大学 | 一种新型d-氨基酸氧化酶抑制剂及其制备和应用 |
CN104016909B (zh) * | 2014-04-03 | 2016-04-20 | 定陶县友帮化工有限公司 | 一种2-氨基-3-溴-5-氯吡啶的合成方法 |
CN104016911A (zh) * | 2014-04-03 | 2014-09-03 | 定陶县友帮化工有限公司 | 一种2-氨基-3,5-二溴吡啶的合成方法 |
CN112010772A (zh) * | 2016-01-26 | 2020-12-01 | 赵鸣 | 5-氨基酮戊酸及其衍生物的盐化合物和应用 |
JP2019520379A (ja) | 2016-07-01 | 2019-07-18 | ジー1 セラピューティクス, インコーポレイテッド | ピリミジン系の抗増殖剤 |
US10905675B2 (en) | 2016-12-14 | 2021-02-02 | Sk Biopharmaceuticals Co., Ltd. | Use of carbamate compound for prevention, alleviation or treatment of pruritus |
WO2018139876A1 (ko) * | 2017-01-26 | 2018-08-02 | 동화약품주식회사 | 신규한 [1, 2, 4] 트리아졸로 [4, 3-a]퀴녹살린 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 bet 단백질 관련 질환의 예방 또는 치료용 약학적 조성물 |
RU2745035C1 (ru) * | 2017-02-27 | 2021-03-18 | Бетта Фармасьютикалз Ко., Лтд. | Ингибитор fgfr и его применение |
TW202021969A (zh) * | 2018-05-31 | 2020-06-16 | 南韓商C&C新藥研究所 | 雜環衍生物及其用途 |
GB2575490A (en) * | 2018-07-12 | 2020-01-15 | Recordati Ind Chimica E Farmaceutica Spa | P2X3 receptor antagonists |
US11718622B2 (en) | 2020-03-16 | 2023-08-08 | Exelixis Inc. | Heterocyclic adenosine receptor antagonists |
WO2021236650A1 (en) | 2020-05-19 | 2021-11-25 | G1 Therapeutics, Inc. | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
EP4067357A1 (en) * | 2021-03-30 | 2022-10-05 | JW Pharmaceutical Corporation | Novel crystalline form of 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-n-methylazetidin-3-amine hydrogen sulfate monohydrate |
TW202317568A (zh) * | 2021-06-22 | 2023-05-01 | 丹麥商理奧藥品公司 | 1-(8-溴化吡啶并[2,3-e][1,2,4]三唑并[4,3-a]吡嗪-4-基)-n-甲基吖丁啶-3-胺半琥珀酸鹽之新穎結晶形式 |
WO2024068851A1 (en) * | 2022-09-29 | 2024-04-04 | Jw Pharmaceutical Corporation | A process for the manufacture of salts and crystalline forms of 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-n-methylazetidin-3-amine and novel crystalline forms |
WO2024069577A1 (en) * | 2022-09-29 | 2024-04-04 | Jw Pharmaceutical Corporation | Novel crystalline form of 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-n-methylazetidin-3-amine |
WO2024069576A1 (en) * | 2022-09-30 | 2024-04-04 | Jw Pharmaceutical Corporation | Novel crystalline form of 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-n-methylazetidin-3-amine mono succinate |
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