AR078770A1 - DERIVATIVES OF DIHYDROBENZO OXACINES AND THIAZINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME FOR THE TREATMENT OF INFLAMMATORY AND HYPERPROLIFERATIVE DISEASES. - Google Patents

DERIVATIVES OF DIHYDROBENZO OXACINES AND THIAZINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME FOR THE TREATMENT OF INFLAMMATORY AND HYPERPROLIFERATIVE DISEASES.

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Publication number
AR078770A1
AR078770A1 ARP100103919A ARP100103919A AR078770A1 AR 078770 A1 AR078770 A1 AR 078770A1 AR P100103919 A ARP100103919 A AR P100103919A AR P100103919 A ARP100103919 A AR P100103919A AR 078770 A1 AR078770 A1 AR 078770A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
heteroaryl
hydrogen
alk
Prior art date
Application number
ARP100103919A
Other languages
Spanish (es)
Inventor
Bernd Wendt
Lopez Arantxa Encinas
Jorge Alonso
Marcel Muelbaier
Bernd Janssen
Christoph Schultes
Original Assignee
Elara Pharmaceuticals Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Elara Pharmaceuticals Gmbh filed Critical Elara Pharmaceuticals Gmbh
Publication of AR078770A1 publication Critical patent/AR078770A1/en

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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
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • 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
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links
    • 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

Abstract

Reivindicacion 1: Compuesto de 2,3-dihidrobenzazina de la formula (1) en la que X es O o S(=O)n siendo n 0, 1 o 2; R1 es fenilo o heteroarilo monocíclico de 5 o 6 miembros unido en C, en los que el fenilo y heteroarilo de 5 o 6 miembros monocíclicos no están sustituidos o llevan 1, 2 o 3 radicales R1a que son idénticos o diferentes; R1a se selecciona del grupo constituido por halogeno, ciano, NO2, NH2, OH, SH, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-6, alquiltio C1-6, hidroxialquilo C1-6, alcoxi C1-4-alquilo C1-4, alquilo C1-2 fluorado, SF5, alcoxi C1-2 fluorado, C(O)R3, NR4R5, N(OR6)R7 y C(O)OR8, o dos radicales R1a que estén unidos a átomos de carbono adyacentes pueden formar también un resto que forme puente O-Alk-O, en el que Alk se selecciona de CH2, CH2CH2, CHF y CF2; R2 es fenilo o heteroarilo monocíclico de 5 o 6 miembros unido en C o unido en N, en los que fenilo y heteroarilo de 5 o 6 miembros monocíclico no están sustituidos o llevan 1, 2 o 3 radicales R1a que son idénticos o diferentes; R2a se selecciona del grupo constituido por halogeno, ciano, NO2, NH2, OH, SH, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-6, alquiltio C1-6, hidroxialquilo C1-6, alcoxi C1-4-alquilo C1-4, alquilo C1-2 fluorado, SF5, alcoxi C1-2 fluorado, C(O)R3, NR4R5, N(OR6)R7 y C(O)OR8, o dos radicales R2a que estén unidos a átomos de carbono adyacentes pueden formar también un resto que forme puente O-Alk-O, en el que Alk se selecciona de CH2, CH2CH2, CHF y CF2; R3 es alquilo C1-4; R4 es hidrogeno o alquilo C1-6, R5 es alquilo C1-6, hidroxialquilo C2-6, alcoxi C1-4-alquilo C2-4 o un radical C(O)Rx, en el que Rx es alquilo C1-4; o R4, R5 conjuntamente con el átomo de hidrogeno al que están unidos, forman un heterociclo de nitrogeno saturado de 5 o 6 miembros, unido en N; R6 es hidrogeno o alquilo C1-6, R7 es hidrogeno o alquilo C1-6, R8 es hidrogeno, alquilo C1-6, hidroxialquilo C2-6 o alcoxi C1-4-alquilo C2-4; sus sales farmacéuticamente aceptables, y si uno o ambos de R1 y R2 son un heteroarilo de 5 o 6 miembros que contiene nitrogeno, sus N-oxidos y las sales farmacéuticamente aceptables de dichos N-oxidos.Claim 1: Compound of 2,3-dihydrobenzazine of the formula (1) wherein X is O or S (= O) n being n 0, 1 or 2; R1 is a 5 or 6-membered C or 5-membered monocyclic phenyl or heteroaryl, in which the 5 or 6 monocyclic phenyl and heteroaryl are unsubstituted or carry 1, 2 or 3 R1a radicals that are identical or different; R1a is selected from the group consisting of halogen, cyano, NO2, NH2, OH, SH, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 hydroxyalkyl, alkoxy C1-4-C1-4 alkyl, fluorinated C1-2 alkyl, SF5, fluorinated C1-2 alkoxy, C (O) R3, NR4R5, N (OR6) R7 and C (O) OR8, or two R1a radicals that are attached adjacent carbon atoms may also form a moiety that forms an O-Alk-O bridge, in which Alk is selected from CH2, CH2CH2, CHF and CF2; R2 is 5 or 6-membered monocyclic phenyl or heteroaryl attached in C or attached in N, in which phenyl and 5 or 6 monocyclic heteroaryl are unsubstituted or carry 1, 2 or 3 R1a radicals that are identical or different; R2a is selected from the group consisting of halogen, cyano, NO2, NH2, OH, SH, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 hydroxyalkyl, alkoxy C1-4-C1-4 alkyl, fluorinated C1-2 alkyl, SF5, fluorinated C1-2 alkoxy, C (O) R3, NR4R5, N (OR6) R7 and C (O) OR8, or two R2a radicals that are attached adjacent carbon atoms may also form a moiety that forms an O-Alk-O bridge, in which Alk is selected from CH2, CH2CH2, CHF and CF2; R3 is C1-4 alkyl; R4 is hydrogen or C1-6 alkyl, R5 is C1-6 alkyl, C2-6 hydroxyalkyl, C1-4 alkoxy-C2-4 alkyl or a C (O) Rx radical, wherein Rx is C1-4 alkyl; or R4, R5 together with the hydrogen atom to which they are attached, form a 5- or 6-membered saturated nitrogen heterocycle, bonded in N; R6 is hydrogen or C1-6 alkyl, R7 is hydrogen or C1-6 alkyl, R8 is hydrogen, C1-6 alkyl, hydroxyC2-6 alkyl or C1-4 alkoxy-C2-4 alkyl; its pharmaceutically acceptable salts, and if one or both of R1 and R2 are a 5 or 6 membered heteroaryl containing nitrogen, its N-oxides and the pharmaceutically acceptable salts of said N-oxides.

ARP100103919A 2009-10-27 2010-10-25 DERIVATIVES OF DIHYDROBENZO OXACINES AND THIAZINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME FOR THE TREATMENT OF INFLAMMATORY AND HYPERPROLIFERATIVE DISEASES. AR078770A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP2009064138 2009-10-27

Publications (1)

Publication Number Publication Date
AR078770A1 true AR078770A1 (en) 2011-11-30

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ID=42044761

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103919A AR078770A1 (en) 2009-10-27 2010-10-25 DERIVATIVES OF DIHYDROBENZO OXACINES AND THIAZINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME FOR THE TREATMENT OF INFLAMMATORY AND HYPERPROLIFERATIVE DISEASES.

Country Status (3)

Country Link
AR (1) AR078770A1 (en)
TW (1) TW201120018A (en)
WO (1) WO2011057892A1 (en)

Families Citing this family (5)

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Publication number Priority date Publication date Assignee Title
JP2014533747A (en) 2011-11-30 2014-12-15 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ 3,7-Disubstituted octahydro-2H-pyrido [4,3-e] [1,3] oxazin-2-one antibiotic
CN103102329B (en) * 2013-01-24 2015-04-08 华东师范大学 Synthetic method of 2,3-dihydro-[1,4]-benzothiazine compound
KR20180025894A (en) 2015-06-11 2018-03-09 라이세라 코퍼레이션 Benzo [B] [1,4] oxazinesulfonamides and related compounds for use as agonists of RORY and the treatment of diseases
WO2020055164A1 (en) * 2018-09-12 2020-03-19 크리스탈지노믹스(주) 7-hydroxy-4h-thieno[3,2-b]pyridin-5-on derivative and use thereof
CN115557913A (en) * 2021-07-02 2023-01-03 广东东阳光药业有限公司 Benzoazaheterocyclic compounds and application thereof in medicines

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WO2011057892A1 (en) 2011-05-19

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