AR090994A1 - Uracilos sustituidos biciclicamente y uso de los mismos - Google Patents
Uracilos sustituidos biciclicamente y uso de los mismosInfo
- Publication number
- AR090994A1 AR090994A1 ARP130101600A ARP130101600A AR090994A1 AR 090994 A1 AR090994 A1 AR 090994A1 AR P130101600 A ARP130101600 A AR P130101600A AR P130101600 A ARP130101600 A AR P130101600A AR 090994 A1 AR090994 A1 AR 090994A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- halogen
- difluoromethyl
- trifluoromethyl
- Prior art date
Links
Classifications
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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
- A61K31/495—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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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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
- A61K31/495—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
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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
- A61K31/535—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
- A61K31/536—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 ortho- or peri-condensed with carbocyclic ring 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
- A61K31/535—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
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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- 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
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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
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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
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
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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
Abstract
La presente solicitud se refiere a derivados de uracilo sustituidos bicíclicamente, a procedimientos de preparación de los mismos, al uso de los mismos solos o en combinaciones para el tratamiento y/o la prevención de enfermedades y al uso de los mismos para la producción de medicamentos para el tratamiento y/o la prevención de enfermedades. Reivindicación 1: Compuesto de la fórmula (1) en la que R¹ es hidrógeno o alquilo C₁₋₄; R² es un grupo de la fórmula (2), (3) ó (4) en la que * es el sitio de unión al átomo de nitrógeno del uracilo; A es -CH₂-, -CH₂-CH₂-, -O-CH₂-## u oxígeno, en el que ## es el sitio de unión al anillo de fenilo; m es el número 0, 1 ó 2; R⁴ es halógeno, difluorometilo, trifluorometilo, alquilo C₁₋₄, difluorometoxi, trifluorometoxi o alcoxi C₁₋₄; R⁵A es hidrógeno o deuterio; R⁵B es hidrógeno, deuterio o alquilo C₁₋₄; R⁶ es hidrógeno o flúor; R⁷ es hidrógeno o flúor; R⁸ es halógeno, difluorometilo, trifluorometilo, alquilo C₁₋₄ o nitro; R⁹ es hidrógeno, halógeno, difluorometilo, trifluorometilo, alquilo C₁₋₄, nitro o alquil C₁₋₄-tio; R³ es un grupo de la fórmula (5) en la que # es el sitio de unión al átomo de nitrógeno del uracilo; el anillo Q es heterociclo de 5 a 7 miembros o heteroarilo de 5 ó 6 miembros, en el que el heterociclo de 5 a 7 miembros o el heteroarilo de 5 ó 6 miembros puede estar sustituido con 1 a 4 sustituyentes seleccionados independientemente del grupo de halógeno, difluorometilo, trifluorometilo, trideuterometilo, alquilo C₁₋₆, cicloalquilo C₃₋₇, oxo, hidroxilo, alquil C₁₋₄-carbonilo, alcoxi C₁₋₄-carbonilo, aminocarbonilo y alquil C₁₋₄-sulfonilo, en el que el alquilo C₁₋₆ y el cicloalquilo C₃₋₇, ₐ ₛᵘ ᵛₑᶻ, ₚᵘₑᵈₑₙ ₑₛₜₐʳ ₛᵘₛₜⁱₜᵘⁱᵈₒₛ ᶜₒₙ ₁ ₐ ₃ ₛᵘₛₜⁱₜᵘʸₑₙₜₑₛ ₛₑₗₑᶜᶜⁱₒₙₐᵈₒₛ ⁱₙᵈₑₚₑₙᵈⁱₑₙₜₑₘₑₙₜₑ ᵈₑₗ ᵍʳᵘₚₒ ᵈₑ ₕₐₗóᵍₑₙₒ, ᶜⁱₐₙₒ, ₜʳⁱᶠₗᵘₒʳₒₘₑₜⁱₗₒ, ᶜⁱᶜₗₒₐₗqᵘⁱₗₒ C₃₋₇, hidroxilo, alcoxi C₁₋₄ y heterociclo de 4 a 7 miembros, y en el que dos radicales alquilo C₁₋₆ unidos a un átomo de carbono del heterociclo de 5 a 7 miembros y el heteroarilo de 5 ó 6 miembros, junto con el átomo de carbono al que están unidos, pueden formar un carbociclo de 3 a 6 miembros; R²⁴ es halógeno, alquilo C₁₋₄ o alcoxi C₁₋₄; n es el número 0, 1, 2 ó 3; y las sales, solvatos y solvatos de las sales del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12167231 | 2012-05-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR090994A1 true AR090994A1 (es) | 2014-12-30 |
Family
ID=48289199
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130101600A AR090994A1 (es) | 2012-05-09 | 2013-05-08 | Uracilos sustituidos biciclicamente y uso de los mismos |
Country Status (44)
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA112897C2 (uk) * | 2012-05-09 | 2016-11-10 | Байєр Фарма Акцієнгезелльшафт | Біциклічно заміщені урацили та їх застосування для лікування і/або профілактики захворювань |
| JP2016535769A (ja) * | 2013-11-08 | 2016-11-17 | バイエル ファーマ アクチエンゲゼルシャフト | キマーゼ阻害薬としての置換されているウラシル類 |
| US9926305B2 (en) * | 2013-11-08 | 2018-03-27 | Bayer Pharma Aktiengesellschaft | Salts |
| CN105899500A (zh) * | 2013-11-08 | 2016-08-24 | 拜耳医药股份有限公司 | 取代的1，2，4-三嗪-3，5-二酮及其作为类糜蛋白酶抑制剂的用途 |
| WO2015067630A1 (de) * | 2013-11-08 | 2015-05-14 | Bayer Pharma Aktiengesellschaft | Substituierte uracile und ihre verwendung |
| WO2017162661A1 (en) | 2016-03-22 | 2017-09-28 | Bayer Pharma Aktiengesellschaft | 1h-benzo[de]isoquinoline-1,3(2h)-diones |
| EP3338780A1 (de) * | 2016-12-20 | 2018-06-27 | Bayer Pharma Aktiengesellschaft | Verwendung von chymaseinhibitoren zur behandlung von endometriose, post-operativer fibrose und erkrankungen die durch fibrosebildung gekennzeichnet sind |
| EP3615031A1 (en) | 2017-04-27 | 2020-03-04 | Bayer Aktiengesellschaft | Selective adrenoreceptor alpha2c receptor antagonists alone, or in combination with chymase inhibitors for use in the treatment and/or prophylaxis of peripheral artery diseases (pad) |
| EA202092680A1 (ru) | 2018-05-15 | 2021-04-13 | Байер Акциенгезельшафт | 1,3-тиазол-2-ил-замещенные бензамиды для лечения заболеваний, ассоциированных с сенситизацией нервных волокон |
| CN110229067A (zh) * | 2019-06-05 | 2019-09-13 | 南京焕然生物科技有限公司 | 一种2-氨基茚制备方法 |
| WO2021000933A1 (zh) * | 2019-07-03 | 2021-01-07 | 南京明德新药研发有限公司 | 作为糜酶抑制剂的嘧啶酮类化合物及其应用 |
| CN111440141A (zh) * | 2020-05-20 | 2020-07-24 | 安徽泽升科技有限公司 | 一种羟甲基取代芳杂环类化合物的制备方法 |
| CN114671856B (zh) * | 2020-12-25 | 2023-10-20 | 广东东阳光药业股份有限公司 | 多取代的尿嘧啶衍生物及其用途 |
| CN114671878B (zh) * | 2020-12-25 | 2023-08-04 | 广东东阳光药业有限公司 | 取代的含氮双环化合物及其用途 |
| CN114685472B (zh) * | 2020-12-25 | 2024-04-26 | 广东东阳光药业股份有限公司 | 多取代的尿嘧啶衍生物及其用途 |
| WO2023107470A1 (en) * | 2021-12-06 | 2023-06-15 | Pretzel Therapeutics, Inc. | Lonp1 inhibitors, uses and methods |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| TW202404601A (zh) * | 2022-04-05 | 2024-02-01 | 加拿大商索科普拉健康與人類科學兩合公司 | 用於選擇性消退血栓性或血栓栓塞性疾病中血栓的凝乳酶抑制劑 |
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| JP2010523700A (ja) | 2007-04-13 | 2010-07-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | キナーゼインヒビターとして有用なアミノピリミジン |
| WO2009049112A1 (en) | 2007-10-10 | 2009-04-16 | Smithkline Beecham Corporation | Prolyl hydroxylase inhibitors |
| WO2009050242A2 (de) | 2007-10-19 | 2009-04-23 | Boehringer Ingelheim International Gmbh | Heterocyclus-substituierte piperazino-dihydrothienopyrimidine |
| WO2009135299A1 (en) * | 2008-05-05 | 2009-11-12 | Merck Frosst Canada Ltd. | 3, 4 - substituted piperidine derivatives as renin inhibitors |
| DE102008030091B4 (de) * | 2008-06-25 | 2011-03-03 | Resprotect Gmbh | Uracilderivate und deren Verwendung |
| CA2727340A1 (en) | 2008-06-25 | 2009-12-30 | Daiichi Sankyo Company, Limited | Carboxylic acid compound |
| UA112897C2 (uk) * | 2012-05-09 | 2016-11-10 | Байєр Фарма Акцієнгезелльшафт | Біциклічно заміщені урацили та їх застосування для лікування і/або профілактики захворювань |
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