AR073396A1 - Derivados de 3-amino-indazol o de 3-amino-4, 5, 6, 7-tetrahidro-indazol - Google Patents

Derivados de 3-amino-indazol o de 3-amino-4, 5, 6, 7-tetrahidro-indazol

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Publication number
AR073396A1
AR073396A1 ARP090103663A ARP090103663A AR073396A1 AR 073396 A1 AR073396 A1 AR 073396A1 AR P090103663 A ARP090103663 A AR P090103663A AR P090103663 A ARP090103663 A AR P090103663A AR 073396 A1 AR073396 A1 AR 073396A1
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AR
Argentina
Prior art keywords
group
substituted
cycloalkyl
alkoxy
hydroxy
Prior art date
Application number
ARP090103663A
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English (en)
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Hoffmann La Roche
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Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR073396A1 publication Critical patent/AR073396A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P19/08—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos compuestos son moduladores del FXR y pueden utilizarse como medicamentos utiles para disminuir la absorcion de colesterol, se disminuye el colesterol LDL y los triglicéridos y se reduce la ateroesclerosis inflamatoria. Reivindicacion 1: Compuestos de la formula (1) en la que R1 es un anillo elegido entre el grupo formado por fenilo, naftilo y heteroarilo, dicho anillo está sin sustituir o sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior y ciano; R2, R3, R4 y R5 se eligen con independencia entre si entre el grupo formado por hidrogeno, halogeno y alquilo inferior; R2' y R3' juntos así como R4' y R5' juntos se reemplazan por un doble enlace, o R2', R3', R4' y R5' son hidrogeno; R6 se elige entre el grupo formado por alquilo inferior, cicloalquilo, alcoxialquilo inferior, fenilo sin sustituir o fenilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, (alcoxi inferior)-carbonilo, alcoxicarbonilalquilo inferior, carboxilalcoxi inferior, alcoxicarbonilalcoxi inferior y ciano, fenilalquilo inferior, cuyo fenilo está sin sustituir o sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior y ciano, heterociclilo y heteroarilo sin sustituir o heteroarilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior y ciano; R7 se elige entre el grupo formado por hidrogeno, -C(O)-NH-R8, -C(O)-R9, -S(O)2-R10 y -C(O)-OR11; R8 se elige entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilo inferior, cicloalquilo sustituido por hidroxi, carboxilo, tetrazolilo o carboxilalquilo inferior, heterociclilo, fenilo sin sustituir y fenilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, tetrazolilo, (alcoxi inferior)-carbonilo, alcoxicarbonilalquilo inferior, carboxilalquilo inferior, carboxilalcoxi inferior, alcoxicarbonilalcoxi inferior, ciano y cicloalquiloxi, cuyo resto cicloalquilo está sustituido por carboxilo; R9 se elige entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilo inferior y fenilalquilo inferior, cuyo fenilo está sin sustituir o sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, tetrazolilo, (alcoxi inferior)-carbonilo, alcoxicarbonilalquilo inferior, carboxilalquilo inferior, carboxilalcoxi inferior, alcoxicarbonilalcoxi inferior, ciano y cicloalquiloxi, cuyo resto cicloalquilo está sustituido por carboxilo; R10 se elige entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilo inferior y fenilalquilo inferior, cuyo fenilo está sin sustituir o sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, tetrazolilo, (alcoxi inferior)-carbonilo, alcoxicarbonilalquilo inferior, carboxilalquilo inferior, carboxilalcoxi inferior, alcoxicarbonilalcoxi inferior, ciano y cicloalquiloxi cuyo resto cicloalquilo está sustituido por carboxilo; y R11 se elige entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilo inferior, cicloalquilo sustituido por hidroxi, carboxilo, tetrazolilo o carboxilalquilo inferior, heterociclilo, fenilo sin sustituir y fenilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, tetrazolilo, (alcoxi inferior)-carbonilo, alcoxicarbonilalquilo inferior, carboxilalquilo inferior, carboxilalcoxi inferior, alcoxicarbonilalcoxi inferior, ciano y cicloalquiloxi, cuyo resto cicloalquilo está sustituido por carboxilo; o las sales farmacéuticamente aceptables de los mismos.
ARP090103663A 2008-09-25 2009-09-23 Derivados de 3-amino-indazol o de 3-amino-4, 5, 6, 7-tetrahidro-indazol AR073396A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08165137 2008-09-25

Publications (1)

Publication Number Publication Date
AR073396A1 true AR073396A1 (es) 2010-11-03

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ID=41382044

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ARP090103663A AR073396A1 (es) 2008-09-25 2009-09-23 Derivados de 3-amino-indazol o de 3-amino-4, 5, 6, 7-tetrahidro-indazol

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US (1) US8153663B2 (es)
EP (1) EP2346834B1 (es)
JP (1) JP5450632B2 (es)
KR (1) KR101444988B1 (es)
CN (1) CN102164900B (es)
AR (1) AR073396A1 (es)
AU (1) AU2009295967A1 (es)
BR (1) BRPI0919248A2 (es)
CA (1) CA2736434A1 (es)
ES (1) ES2443947T3 (es)
IL (1) IL211674A0 (es)
MX (1) MX2011002793A (es)
TW (1) TW201020234A (es)
WO (1) WO2010034657A1 (es)

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US9012497B2 (en) 2010-05-25 2015-04-21 Symrise Ag Cyclohexyl carbamate compounds as active anti-cellulite ingredients
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
WO2013037482A1 (en) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Farnesoid x receptor agonists for cancer treatment and prevention
JP6366721B2 (ja) 2013-09-11 2018-08-01 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Ｂ型肝炎ウイルス感染症を処置するための方法及び医薬組成物
MX2018015443A (es) 2016-06-13 2019-04-11 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4).
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WO2018153933A1 (en) 2017-02-21 2018-08-30 Genfit Combination of a ppar agonist with a fxr agonist
JP6906626B2 (ja) 2017-03-28 2021-07-21 ギリアード サイエンシーズ， インコーポレイテッド 肝疾患を処置するための治療的組み合わせ
JP2020515564A (ja) 2017-03-30 2020-05-28 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物
BR112021011762A2 (pt) 2019-01-15 2021-11-03 Gilead Sciences Inc Compostos para modulação de fxr (nr1h4)
AU2020225225B2 (en) 2019-02-19 2022-12-22 Gilead Sciences, Inc. Solid forms of FXR agonists
JP2022540699A (ja) 2019-07-18 2022-09-16 ウエヌイグレックオ・ファーマ インターフェロンの有害作用を減少させる方法
JP2023510274A (ja) 2020-01-15 2023-03-13 アンセルム（アンスティチュート・ナシオナル・ドゥ・ラ・サンテ・エ・ドゥ・ラ・ルシェルシュ・メディカル） Ｄ型肝炎ウイルスによる感染を処置するためのｆｘｒアゴニストの使用
MX2023008365A (es) 2021-01-14 2023-10-04 Enyo Pharma Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv.
CA3213217A1 (en) 2021-04-28 2022-11-03 Raphael Darteil Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
CN113372276B (zh) * 2021-05-25 2022-04-22 三峡大学 吲唑类衍生物及其应用

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Also Published As

Publication number Publication date
KR101444988B1 (ko) 2014-09-26
JP2012503618A (ja) 2012-02-09
BRPI0919248A2 (pt) 2019-09-24
EP2346834A1 (en) 2011-07-27
JP5450632B2 (ja) 2014-03-26
US8153663B2 (en) 2012-04-10
WO2010034657A1 (en) 2010-04-01
TW201020234A (en) 2010-06-01
MX2011002793A (es) 2011-04-05
ES2443947T3 (es) 2014-02-21
US20100076026A1 (en) 2010-03-25
CA2736434A1 (en) 2010-04-01
EP2346834B1 (en) 2013-11-20
IL211674A0 (en) 2011-06-30
AU2009295967A1 (en) 2010-04-01
CN102164900B (zh) 2014-04-16
CN102164900A (zh) 2011-08-24
KR20110059890A (ko) 2011-06-07

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