AR102827A1 - Indazoles sustituidos, procedimientos para su preparación y preparaciones farmacéuticas que los contienen - Google Patents
Indazoles sustituidos, procedimientos para su preparación y preparaciones farmacéuticas que los contienenInfo
- Publication number
- AR102827A1 AR102827A1 ARP150103876A ARP150103876A AR102827A1 AR 102827 A1 AR102827 A1 AR 102827A1 AR P150103876 A ARP150103876 A AR P150103876A AR P150103876 A ARP150103876 A AR P150103876A AR 102827 A1 AR102827 A1 AR 102827A1
- Authority
- AR
- Argentina
- Prior art keywords
- mono
- halogen
- alkyl
- polysubstituted
- hydroxy
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 title 1
- -1 radical alkyl radical Chemical class 0.000 abstract 13
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 4
- 239000012453 solvate Substances 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 201000009273 Endometriosis Diseases 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 230000006806 disease prevention Effects 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 abstract 2
- 239000002207 metabolite Substances 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 150000003254 radicals Chemical class 0.000 abstract 2
- 201000005671 spondyloarthropathy Diseases 0.000 abstract 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 abstract 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 abstract 1
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 abstract 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 208000005171 Dysmenorrhea Diseases 0.000 abstract 1
- 206010013935 Dysmenorrhoea Diseases 0.000 abstract 1
- 208000004483 Dyspareunia Diseases 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 201000005569 Gout Diseases 0.000 abstract 1
- 102000004877 Insulin Human genes 0.000 abstract 1
- 108090001061 Insulin Proteins 0.000 abstract 1
- 206010025323 Lymphomas Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 206010013990 dysuria Diseases 0.000 abstract 1
- 208000010706 fatty liver disease Diseases 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 150000002473 indoazoles Chemical class 0.000 abstract 1
- 229940125396 insulin Drugs 0.000 abstract 1
- 206010025135 lupus erythematosus Diseases 0.000 abstract 1
- 208000002780 macular degeneration Diseases 0.000 abstract 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 230000036407 pain Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000001185 psoriatic effect Effects 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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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
- C07D401/12—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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente solicitud se refiere a indazoles sustituidos, procedimientos para su preparación, su uso solos o en combinaciones para el tratamiento y/o prevención de enfermedades, así como su uso para la preparación de medicamentos para el tratamiento y/o prevención de enfermedades, en especial para el tratamiento y/o la prevención de endometriosis, así como dolores asociados con endometriosis y otros síntomas asociados con endometriosis como dismenorrea, dispareunia, disuria y disquecia, de linfomas, artritis reumatoidea, espondiloartritis (en especial espondiloartritis psoriásica y enfermedad de Bechterew), lupus eritematoso, esclerosis múltiple, degeneración macular, EPOC, gota, enfermedades de hígado graso, insuficiencia insulínica, enfermedades tumorales y psoriasis. Reivindicación 1: Compuestos la fórmula general (1) en donde: R¹ representa alquilo C₁₋₆, en donde el radical alquilo C₁₋₆ no está sustituido o está mono- o polisustituido, igual o diferente con halógeno, hidroxi, un cicloalquilo C₃₋₆ no sustituido o mono- o polisustituido con halógeno, un radical R⁶, R⁷SO₂, R⁷SO o R⁸O o representa un compuesto seleccionado del grupo de fórmulas (2) en donde * representa un sitio de unión del grupo con el radical de la molécula; R² y R³ siempre tienen el mismo significado y al mismo tiempo representan hidrógeno o alquilo C₁₋₆; R⁴ representa halógeno, ciano, alquilo C₁₋₆ no sustituido o mono- o polisustituido, igual o diferente entre sí o cicloalquilo C₃₋₆ no sustituido o mono- o polisustituido, igual o diferente entre sí, y los sustituyentes se seleccionan del grupo de halógeno e hidroxi; R⁵ representa hidrógeno, halógeno o un alquilo C₁₋₆ no sustituido o mono- o polisustituido con halógeno; R⁶ representa un heterociclo saturado monocíclico no sustituido o mono- o disustituido con metilo con 4 a 6 átomos del anillo, que contiene un heteroátomo o un heterogrupo de la serie O, S, SO y SO₂; R⁷ representa alquilo C₁₋₆, en donde el radical alquilo C₁₋₆ no está sustituido o está mono- o polisustituido, igual o diferente con halógeno, hidroxi o cicloalquilo C₃₋₆; o R⁷ representa cicloalquilo C₃₋₆; R⁸ representa alquilo C₁₋₆, en donde el radical alquilo C₁₋₆ no está sustituido o está mono- o polisustituido, igual o diferente, con halógeno; y sus diastereómeros, enantiómeros, sus metabolitos, sus sales, sus solvatos o los solvatos de sus sales. Reivindicación 22: Compuestos de la fórmula general (3), en donde R¹ representa 4,4,4-trifluorobutilo, 3-hidroxi-3-metilbutilo, 3-metoxipropilo, 3-hidroxipropilo, 3-hidroxibutilo, 3-hidroxi-2-metilpropilo, 3-hidroxi-2,2-dimetilpropilo, 3-trifluorometoxipropilo, 2-metoxietilo, 2-hidroxietilo, 2-(metilsulfonil)etilo, 3-(metilsulfonil)propilo o 2-(1-hidroxiciclopropil)etilo; R⁴ representa difluorometilo, trifluorometilo o metilo; y R⁵ representan hidrógeno o flúor; así como sus diastereómeros, enantiómeros, sus metabolitos, sus sales, sus solvatos o los solvatos de sus sales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14195032 | 2014-11-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR102827A1 true AR102827A1 (es) | 2017-03-29 |
Family
ID=51982455
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150103876A AR102827A1 (es) | 2014-11-26 | 2015-11-26 | Indazoles sustituidos, procedimientos para su preparación y preparaciones farmacéuticas que los contienen |
Country Status (42)
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017505337A (ja) | 2014-01-10 | 2017-02-16 | アウリジーン ディスカバリー テクノロジーズ リミテッド | Ｉｒａｋ４阻害剤としてのインダゾール化合物 |
| AU2015205374B2 (en) | 2014-01-13 | 2018-08-23 | Aurigene Oncology Limited | Bicyclic heterocyclyl derivatives as IRAK4 inhibitors |
| JO3705B1 (ar) * | 2014-11-26 | 2021-01-31 | Bayer Pharma AG | إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية |
| TW201701879A (zh) * | 2015-04-30 | 2017-01-16 | 拜耳製藥公司 | Ｉｒａｋ４抑制劑組合 |
| EP3195865A1 (de) * | 2016-01-25 | 2017-07-26 | Bayer Pharma Aktiengesellschaft | Kombinationen von irak4 inhibitoren und btk inhibitoren |
| JP6871919B2 (ja) | 2015-06-16 | 2021-05-19 | ナノファギックス エルエルシー | 薬物送達及びイメージング化学コンジュゲート、製剤及びその使用方法 |
| JP6947743B2 (ja) | 2016-03-03 | 2021-10-13 | バイエル・ファルマ・アクティエンゲゼルシャフト | 新規な２−置換インダゾール、その製造方法、それを含有する医薬製剤、および薬物を製造するためのその使用 |
| EP3219329A1 (en) * | 2016-03-17 | 2017-09-20 | Bayer Pharma Aktiengesellschaft | Combinations of copanlisib |
| EP3448848B1 (en) * | 2016-04-29 | 2023-09-27 | Bayer Pharma Aktiengesellschaft | Polymorphic form of n-{6-(2-hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2h-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide |
| EA035867B1 (ru) * | 2016-04-29 | 2020-08-24 | Байер Фарма Акциенгезельшафт | Синтез индазолов |
| PT3448849T (pt) * | 2016-04-29 | 2020-06-30 | Bayer Pharma AG | Síntese de indazóis |
| TN2018000409A1 (en) * | 2016-06-01 | 2020-06-15 | Bayer Pharma AG | Use of 2-substituted indazoles for the treatment and prophylaxis of autoimmune diseases |
| ES2898771T3 (es) * | 2016-06-01 | 2022-03-08 | Bayer Animal Health Gmbh | Indazoles sustituidos útiles para el tratamiento y la prevención de enfermedades alérgicas y/o inflamatorias en animales |
| US20180072718A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine compounds and uses thereof |
| TW201811799A (zh) | 2016-09-09 | 2018-04-01 | 美商英塞特公司 | 吡唑并嘧啶化合物及其用途 |
| MA46191A (fr) | 2016-09-09 | 2021-04-21 | Incyte Corp | Dérivés de pyrazolopyridine comme modulateurs de hpk1 et leurs utilisations pour le traitement du cancer |
| WO2018060072A1 (de) | 2016-09-29 | 2018-04-05 | Bayer Pharma Aktiengesellschaft | Neue substituierte benzimidazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
| WO2018152220A1 (en) | 2017-02-15 | 2018-08-23 | Incyte Corporation | Pyrazolopyridine compounds and uses thereof |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| RS64411B1 (sr) | 2017-03-31 | 2023-09-29 | Aurigene Oncology Ltd | Jedinjenja i kompozicije za lečenje hematoloških poremećaja |
| US11957931B2 (en) | 2017-04-26 | 2024-04-16 | Yale University | Compositions and methods for treating vitiligo |
| PE20200756A1 (es) | 2017-08-16 | 2020-07-27 | Univ Vanderbilt | Compuestos de indazol como potenciadores alostericos mglur4, composiciones y metodos de tratamiento de la disfuncion neurologica |
| US10722495B2 (en) | 2017-09-08 | 2020-07-28 | Incyte Corporation | Cyanoindazole compounds and uses thereof |
| PE20211305A1 (es) | 2018-01-05 | 2021-07-20 | Cybrexa 1 Inc | Compuestos, composiciones y metodos para tratar enfermedades que involucren tejidos con enfermedades acidas o hipoxicas |
| US10745388B2 (en) | 2018-02-20 | 2020-08-18 | Incyte Corporation | Indazole compounds and uses thereof |
| LT3755703T (lt) | 2018-02-20 | 2022-10-10 | Incyte Corporation | N-(fenil)-2-(fenil)pirimidin-4-karboksamido dariniai ir susiję junginiai, kaip hpk1 inhibitoriai, skirti vėžio gydymui |
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