AR100645A1 - Derivados de pirazolo-pirimidina - Google Patents
Derivados de pirazolo-pirimidinaInfo
- Publication number
- AR100645A1 AR100645A1 ARP150101686A ARP150101686A AR100645A1 AR 100645 A1 AR100645 A1 AR 100645A1 AR P150101686 A ARP150101686 A AR P150101686A AR P150101686 A ARP150101686 A AR P150101686A AR 100645 A1 AR100645 A1 AR 100645A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- ring
- amino
- alkoxy
- Prior art date
Links
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
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
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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
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- 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]
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- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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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
-
- 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
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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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
- A61P37/08—Antiallergic agents
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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
- A61P9/00—Drugs for disorders of the cardiovascular system
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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
- A61P9/08—Vasodilators for multiple indications
Abstract
La presente describe derivados de pirazolo-pirimidina, los cuales están generalmente interactuando con la actividad proteolítica y auto-proteolítica de MALT1, y en particular que pueden inhibir esa actividad. La presente describe además la síntesis de estos derivados de pirazolo-pirimidina, su uso como un medicamento, en especial mediante su interacción con la actividad proteolítica y auto-proteolítica de MALT1. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: R¹ es halógeno, ciano, o alquilo C₁₋₃ opcionalmente sustituido por halógeno; R² es alquilo C₁₋₆ opcionalmente sustituido una o más veces por alquilo C₁₋₆, alquenilo C₂₋₆, hidroxilo, N,N-dialquilo C₁₋₆-amino, N-mono-alquilo C₁₋₆-amino, O-Rᵍ, Rᵍ, fenilo, o por alcoxilo C₁₋₆, en donde el alcoxilo nuevamente puede estar opcionalmente sustituido por alcoxilo C₁₋₆, N,N-dialquilo C₁₋₆-amino, Rᵍ o fenilo; cicloalquilo C₃₋₆ opcionalmente sustituido por alquilo C₁₋₆, N,N-dialquilo C₁₋₆-amino, o alcoxilo C₁₋₆-alquilo C₁₋₆, y/o dos de los sustituyentes opcionales junto con los átomos con los que están enlazados, pueden formar un anillo heterocíclico saturado de 4 a 6 miembros anulado o espirocíclico que comprende de 1 a 2 átomos de oxígeno (O); fenilo opcionalmente sustituido por alcoxilo C₁₋₆; un anillo de heteroarilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados a partir de N y O, estando este anillo opcionalmente sustituido por alquilo C₁₋₆ que puede estar opcionalmente sustituido por amino, o hidroxilo; Rᵍ; o N,N-dialquilo C₁₋₆-amino-carbonilo; en donde: Rᵍ es un anillo heterocíclico de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados a partir de N y O, estando este anillo opcionalmente sustituido por alquilo C₁₋₆, alcoxilo C₁₋₆-alquilo C₁₋₆, alcoxilo C₁₋₆-carbonilo; R es fenilo independientemente sustituido dos o más veces por Rᵃ, 2-piridilo independientemente sustituido una o más veces por Rᵇ, 3-piridilo independientemente sustituido una o más veces por Rᶜ, o 4-piridilo independientemente sustituido una o más veces por Rᵈ; en donde: Rᵃ independientemente uno del otro es halógeno; ciano; -COO-alquilo C₁₋₆; alcoxilo C₁₋₆; alquilo C₁₋₆ opcionalmente sustituido por halógeno o un anillo heterocíclico de 5 a 6 miembros que tiene de 1 a 2 heteroátomos seleccionados a partir de N y O, cuyo anillo está opcionalmente sustituido por alquilo C₁₋₆; un anillo de heteroarilo de 5 a 6 miembros que tiene de 1 a 3 heteroátomos seleccionados a partir de N y O, estando este anillo opcionalmente sustituido por amino, alquilo C₁₋₆ opcionalmente sustituido por amino, o hidroxilo, o por N-mono- o N,N-dialquilo C₁₋₆-amino-carbonilo; y/o dos Rᵃ junto con los átomos en el anillo con los que están enlazados, pueden formar un anillo heterocíclico o heteroaromático de 5 a 6 miembros que tiene de 1 a 2 átomos de nitrógeno (N), estando este anillo opcionalmente sustituido por alquilo C₁₋₆ u oxo; Rᵇ, Rᶜ y Rᵈ, independientemente unos de otros, son halógeno; oxo; hidroxilo; ciano; alcoxilo C₁₋₆ opcionalmente sustituido por halógeno; alcoxilo C₁₋₆-carbonilo; fenilo; N,N-dialquilo C₁₋₆-amino; alquilo C₁₋₆ opcionalmente sustituido por halógeno o fenilo; un anillo de heteroarilo de 5 a 6 miembros que tiene de 1 a 3 átomos de nitrógeno (N), estando este anillo opcionalmente sustituido por alquilo C₁₋₆ opcionalmente sustituido por amino, o hidroxilo, o por mono- o di-N-alquilo C₁₋₆-amino-carbonilo; O-Rʰ; o Rʰ; en donde: Rʰ es un anillo heterocíclico de 5 a 6 miembros que tiene de 1 a 4 heteroátomos seleccionados a partir de N, O y S, estando este anillo opcionalmente sustituido por alquilo C₁₋₆, hidroxilo u oxo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14170408 | 2014-05-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR100645A1 true AR100645A1 (es) | 2016-10-19 |
Family
ID=50828759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150101686A AR100645A1 (es) | 2014-05-28 | 2015-05-28 | Derivados de pirazolo-pirimidina |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US9815842B2 (es) |
| EP (1) | EP3149001B1 (es) |
| JP (1) | JP6545197B2 (es) |
| KR (1) | KR20170007311A (es) |
| CN (1) | CN106170489B (es) |
| AP (1) | AP2016009487A0 (es) |
| AR (1) | AR100645A1 (es) |
| AU (1) | AU2015265478B2 (es) |
| BR (1) | BR112016024545A2 (es) |
| CA (1) | CA2945077A1 (es) |
| CL (1) | CL2016002942A1 (es) |
| CR (1) | CR20160548A (es) |
| CU (1) | CU24393B1 (es) |
| CY (1) | CY1121946T1 (es) |
| DK (1) | DK3149001T3 (es) |
| EA (1) | EA032050B1 (es) |
| ES (1) | ES2738695T3 (es) |
| GT (1) | GT201600249A (es) |
| HR (1) | HRP20191261T1 (es) |
| HU (1) | HUE044351T2 (es) |
| IL (1) | IL247949A0 (es) |
| LT (1) | LT3149001T (es) |
| MX (1) | MX2016015544A (es) |
| MY (1) | MY182487A (es) |
| PE (1) | PE20170189A1 (es) |
| PH (1) | PH12016501862A1 (es) |
| PL (1) | PL3149001T3 (es) |
| PT (1) | PT3149001T (es) |
| RS (1) | RS59039B1 (es) |
| SG (1) | SG11201607895PA (es) |
| SI (1) | SI3149001T1 (es) |
| SV (1) | SV2016005328A (es) |
| TR (1) | TR201910730T4 (es) |
| TW (1) | TWI709561B (es) |
| UY (1) | UY36143A (es) |
| WO (1) | WO2015181747A1 (es) |
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| CN103739550B (zh) * | 2014-01-02 | 2016-06-01 | 中国药科大学 | 2,3-二甲基-6-脲-2h-吲唑类化合物及其制备方法与应用 |
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