PE20211447A1 - Indazol-3-carboxamidas sustituidas con 5-heteroarilo y preparacion y uso de las mismas - Google Patents
Indazol-3-carboxamidas sustituidas con 5-heteroarilo y preparacion y uso de las mismasInfo
- Publication number
- PE20211447A1 PE20211447A1 PE2020001271A PE2020001271A PE20211447A1 PE 20211447 A1 PE20211447 A1 PE 20211447A1 PE 2020001271 A PE2020001271 A PE 2020001271A PE 2020001271 A PE2020001271 A PE 2020001271A PE 20211447 A1 PE20211447 A1 PE 20211447A1
- Authority
- PE
- Peru
- Prior art keywords
- unsubstituted
- compounds
- preparation
- heteroaryl
- indazol
- Prior art date
Links
Classifications
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
-
- 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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
-
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- 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
- C07D417/14—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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Referido a un compuesto, o una sal farmaceuticamente aceptable del mismo, de Formula I; donde R1, R2, y R4 se seleccionan independientemente del grupo que consiste en H y haluro; R3 es un anillo de heteroarilo de 5 miembros opcionalmente sustituido con 1-4 R42; R5 se selecciona del grupo que consiste en -(alquilo C1-9) sin sustituir, -(alquenilo C2-9) sin sustituir, -(alquinilo C2-9) sin sustituir, entre otros. Estos compuestos son Indazol-3-carboxamidas sustituidas con 5-heteroarilo. Estos compuestos son inhibidores de una o mas proteinas en la ruta Wnt. Tambien se refiere a metodos de preparacion de dichos compuestos, y su uso en el en tratamiento de trastornos caracterizados por la activacion de la senalizacion de la ruta Wnt, tales como tendinopatia, dermatitis, psoriasis, morfea; asi como afecciones, trastornos, o enfermedades neurologicas relacionadas con la sobreexpresion de DYRK1A.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862634656P | 2018-02-23 | 2018-02-23 | |
PCT/US2019/019129 WO2019165192A1 (en) | 2018-02-23 | 2019-02-22 | 5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20211447A1 true PE20211447A1 (es) | 2021-08-05 |
Family
ID=65812386
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2020001271A PE20211447A1 (es) | 2018-02-23 | 2019-02-22 | Indazol-3-carboxamidas sustituidas con 5-heteroarilo y preparacion y uso de las mismas |
Country Status (18)
Country | Link |
---|---|
US (2) | US10934297B2 (es) |
EP (1) | EP3755696B1 (es) |
JP (1) | JP7369132B2 (es) |
KR (1) | KR20200126393A (es) |
CN (1) | CN112020501A (es) |
AU (1) | AU2019224075A1 (es) |
BR (1) | BR112020017087A2 (es) |
CA (1) | CA3091913A1 (es) |
CL (1) | CL2020002177A1 (es) |
EA (1) | EA202092002A1 (es) |
ES (1) | ES2945558T3 (es) |
IL (1) | IL276814A (es) |
MA (1) | MA51908A (es) |
MX (1) | MX2020008852A (es) |
PE (1) | PE20211447A1 (es) |
PH (1) | PH12020551300A1 (es) |
SG (1) | SG11202008029UA (es) |
WO (1) | WO2019165192A1 (es) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MX2020008852A (es) | 2018-02-23 | 2020-10-14 | Samumed Llc | Indazol-3-carboxamidas sustituidas con 5-heteroarilo y preparacion y uso de las mismas. |
PL3790873T3 (pl) * | 2018-05-07 | 2022-06-27 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Związki 1h-indazolo-3-karboksyamidowe jako inhibitory kinazy syntazy glikogenu 3 beta |
JP7444458B2 (ja) * | 2018-09-21 | 2024-03-06 | 学校法人福岡大学 | プリオン病治療薬 |
CN114867718A (zh) * | 2019-12-16 | 2022-08-05 | 韩国化学研究院 | 新型吲唑衍生物及其用途 |
WO2021120890A1 (en) * | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
Family Cites Families (27)
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US4164559A (en) | 1977-09-21 | 1979-08-14 | Cornell Research Foundation, Inc. | Collagen drug delivery device |
US4474752A (en) | 1983-05-16 | 1984-10-02 | Merck & Co., Inc. | Drug delivery system utilizing thermosetting gels |
US4783443A (en) | 1986-03-03 | 1988-11-08 | The University Of Chicago | Amino acyl cephalosporin derivatives |
US6440102B1 (en) | 1998-07-23 | 2002-08-27 | Durect Corporation | Fluid transfer and diagnostic system for treating the inner ear |
DE19853299C2 (de) | 1998-11-19 | 2003-04-03 | Thomas Lenarz | Katheter zur Applikation von Medikamenten in Flüssigkeitsräumen des menschlichen Innenohrs |
US6120484A (en) | 1999-02-17 | 2000-09-19 | Silverstein; Herbert | Otological implant for delivery of medicament and method of using same |
US6967023B1 (en) | 2000-01-10 | 2005-11-22 | Foamix, Ltd. | Pharmaceutical and cosmetic carrier or composition for topical application |
YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
US6648873B2 (en) | 2001-09-21 | 2003-11-18 | Durect Corp. | Aural catheter system including anchor balloon and balloon inflation device |
GB0218625D0 (en) * | 2002-08-10 | 2002-09-18 | Astex Technology Ltd | Pharmaceutical compounds |
WO2004029050A1 (en) | 2002-09-25 | 2004-04-08 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, and benzoisothiazoles, and preparation and uses thereof |
FR2845382A1 (fr) | 2002-10-02 | 2004-04-09 | Sanofi Synthelabo | Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique |
US7008953B2 (en) | 2003-07-30 | 2006-03-07 | Agouron Pharmaceuticals, Inc. | 3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
FR2867778B1 (fr) * | 2004-03-16 | 2006-06-09 | Sanofi Synthelabo | Utilisation de derives d'indazolecarboxamides pour la preparation d'un medicament destine au traitement et a la prevention du paludisme |
CN101001856A (zh) * | 2004-03-25 | 2007-07-18 | 记忆药物公司 | 吲唑、苯并噻唑、苯并异噻唑、苯并异噁唑及其制备和用途 |
CA2560741C (en) * | 2004-03-25 | 2013-08-06 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof |
WO2011050245A1 (en) * | 2009-10-23 | 2011-04-28 | Yangbo Feng | Bicyclic heteroaryls as kinase inhibitors |
CN103889976A (zh) * | 2011-08-12 | 2014-06-25 | 弗·哈夫曼-拉罗切有限公司 | 吲唑化合物、组合物及使用方法 |
CN103929963A (zh) | 2011-09-14 | 2014-07-16 | 萨穆梅德有限公司 | 吲唑-3-羧酰胺及其作为WNT/β-CATENIN信号传导通路抑制剂的用途 |
KR20140130124A (ko) * | 2012-02-21 | 2014-11-07 | 아지엔드 키미쉐 리유나이트 안젤리니 프란체스코 에이.씨.알.에이.에프. 에스.피.에이 | 글리코겐 합성효소 키나아제 3 베타 억제제로서 1h-인다졸-3-카복사미드 화합물 |
PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
SG10201914111XA (en) * | 2014-03-20 | 2020-03-30 | Samumed Llc | 5-substituted indazole-3-carboxamides and preparation and use thereof |
WO2016040182A1 (en) * | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
EP3370721A4 (en) | 2015-11-06 | 2019-05-22 | Samumed, LLC | TREATMENT OF OSTEOARTHRITIS |
HUE060797T2 (hu) | 2016-06-01 | 2023-04-28 | Biosplice Therapeutics Inc | Eljárás N-(5-(3-(7-(3-fluorfenil)-3H-imidazo[4,5-c]piridin-2-il)-1H-indazol-5-il)- piridin-3-il)-3-metilbutánamid elõállítására |
EP3528808B1 (en) * | 2016-10-21 | 2021-10-06 | BioSplice Therapeutics, Inc. | Methods of using indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors |
MX2020008852A (es) | 2018-02-23 | 2020-10-14 | Samumed Llc | Indazol-3-carboxamidas sustituidas con 5-heteroarilo y preparacion y uso de las mismas. |
-
2019
- 2019-02-22 MX MX2020008852A patent/MX2020008852A/es unknown
- 2019-02-22 US US16/283,366 patent/US10934297B2/en active Active
- 2019-02-22 CA CA3091913A patent/CA3091913A1/en active Pending
- 2019-02-22 CN CN201980027314.1A patent/CN112020501A/zh active Pending
- 2019-02-22 PE PE2020001271A patent/PE20211447A1/es unknown
- 2019-02-22 MA MA051908A patent/MA51908A/fr unknown
- 2019-02-22 WO PCT/US2019/019129 patent/WO2019165192A1/en unknown
- 2019-02-22 BR BR112020017087-9A patent/BR112020017087A2/pt not_active IP Right Cessation
- 2019-02-22 EA EA202092002A patent/EA202092002A1/ru unknown
- 2019-02-22 SG SG11202008029UA patent/SG11202008029UA/en unknown
- 2019-02-22 ES ES19711736T patent/ES2945558T3/es active Active
- 2019-02-22 AU AU2019224075A patent/AU2019224075A1/en not_active Abandoned
- 2019-02-22 EP EP19711736.9A patent/EP3755696B1/en active Active
- 2019-02-22 JP JP2020544501A patent/JP7369132B2/ja active Active
- 2019-02-22 KR KR1020207027174A patent/KR20200126393A/ko not_active Application Discontinuation
-
2020
- 2020-08-19 IL IL276814A patent/IL276814A/en unknown
- 2020-08-20 PH PH12020551300A patent/PH12020551300A1/en unknown
- 2020-08-24 CL CL2020002177A patent/CL2020002177A1/es unknown
- 2020-12-30 US US17/138,098 patent/US11713320B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
EA202092002A1 (ru) | 2021-01-21 |
SG11202008029UA (en) | 2020-09-29 |
WO2019165192A1 (en) | 2019-08-29 |
MX2020008852A (es) | 2020-10-14 |
CL2020002177A1 (es) | 2021-01-08 |
US10934297B2 (en) | 2021-03-02 |
KR20200126393A (ko) | 2020-11-06 |
US20220402921A1 (en) | 2022-12-22 |
EP3755696B1 (en) | 2023-04-05 |
JP2021516674A (ja) | 2021-07-08 |
BR112020017087A2 (pt) | 2020-12-22 |
EP3755696A1 (en) | 2020-12-30 |
US20190263821A1 (en) | 2019-08-29 |
CA3091913A1 (en) | 2019-08-29 |
MA51908A (fr) | 2021-06-02 |
PH12020551300A1 (en) | 2021-10-25 |
JP7369132B2 (ja) | 2023-10-25 |
CN112020501A (zh) | 2020-12-01 |
ES2945558T3 (es) | 2023-07-04 |
IL276814A (en) | 2020-10-29 |
AU2019224075A1 (en) | 2020-09-10 |
US11713320B2 (en) | 2023-08-01 |
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