AR118025A1 - BENZOTHIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS - Google Patents
BENZOTHIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORSInfo
- Publication number
- AR118025A1 AR118025A1 ARP200100328A ARP200100328A AR118025A1 AR 118025 A1 AR118025 A1 AR 118025A1 AR P200100328 A ARP200100328 A AR P200100328A AR P200100328 A ARP200100328 A AR P200100328A AR 118025 A1 AR118025 A1 AR 118025A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- bile acid
- compounds
- alkoxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/36—Seven-membered rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- 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
- 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
-
- 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
Abstract
La presente se refiere a derivados de 1,5-benzotiazepina de fórmula (1). Estos compuestos son moduladores de los ácidos biliares que tienen una actividad inhibidora en el transportador apical de ácidos biliares que dependen de sodio (ASBT) y/o en el transporte de ácidos biliares del hígado (LBAT). La presente también se refiere a composiciones farmacéuticas que comprenden estos compuestos y al uso de estos compuestos en el tratamiento de enfermedades cardiovasculares, metabolismo de ácidos grasos y trastornos de utilización de glucosa, enfermedades gastrointestinales y enfermedades hepáticas. Reivindicación 1: Un compuesto de la fórmula (1) caracterizado porque R¹ y R² cada uno de manera independiente alquilo C₁₋₄; R³ se selecciona de manera independiente del grupo que consiste en hidrógeno, halógeno, hidroxi, alquilo C₁₋₄, haloalquilo C₁₋₄, alcoxi C₁₋₄, haloalcoxi C₁₋₄, ciano, nitro, amino, N-(alquilo C₁₋₄)amino, N,N-di(alquilo C₁₋₄)amino y N-(aril-alquilo C₁₋₄)amino; n es un número entero 1, 2 ó 3; R⁴ se selecciona del grupo que consiste en hidrógeno, halógeno, hidroxi, ciano y alquilo C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄, cicloalquiloxi C₃₋₆, alquiltio C₁₋₄, cicloalquiltio C₃₋₆, amino, N-(alquilo C₁₋₄)amino y N,N-di(alquilo C₁₋₄)amino; y R⁵A, R⁵B, R⁵C y R⁵D se seleccionan independientemente del grupo que consiste en hidrógeno, halógeno, hidroxi, amino, alquilo C₁₋₄ y alcoxi C₁₋₄; o una sal farmacéuticamente aceptable de este; con la condición de que el compuesto no sea ácido 3-((7-bromo-3-butil-3-etil-1,1-dioxido-5-fenil-2,3,4,5-tetrahidro-1,5-benzotiazepina-8-il)oxi)propanoico racémico.This refers to 1,5-benzothiazepine derivatives of formula (1). These compounds are bile acid modulators that have an inhibitory activity on apical sodium-dependent bile acid transporter (ASBT) and / or liver bile acid transport (LBAT). The present also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases. Claim 1: A compound of formula (1) characterized in that R¹ and R² each independently C₁₋₄ alkyl; R³ is independently selected from the group consisting of hydrogen, halogen, hydroxy, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkoxy, cyano, nitro, amino, N- (C₁₋₄ alkyl ) amino, N, N-di (C₁₋₄ alkyl) amino and N- (aryl-C₁₋₄ alkyl) amino; n is an integer 1, 2 or 3; R⁴ is selected from the group consisting of hydrogen, halogen, hydroxy, cyano, and C₁₋₄ alkyl, C₃₋₆ cycloalkyl, C₁₋₄ alkoxy, C₃₋₆ cycloalkyloxy, C₁₋₄ alkylthio, C₃₋₆ cycloalkylthio, amino, N- (C₁₋₄ alkyl) amino and N, N-di (C₁₋₄ alkyl) amino; and R⁵A, R⁵B, R⁵C, and R⁵D are independently selected from the group consisting of hydrogen, halogen, hydroxy, amino, C₁₋₄ alkyl, and C₁₋₄ alkoxy; or a pharmaceutically acceptable salt thereof; provided that the compound is not acid 3 - ((7-bromo-3-butyl-3-ethyl-1,1-dioxide-5-phenyl-2,3,4,5-tetrahydro-1,5- benzothiazepine-8-yl) oxy) racemic propanoic.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201911004690 | 2019-02-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR118025A1 true AR118025A1 (en) | 2021-09-15 |
Family
ID=78076066
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200100329A AR118026A1 (en) | 2019-02-06 | 2020-02-06 | BENZOTIADIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS |
| ARP200100328A AR118025A1 (en) | 2019-02-06 | 2020-02-06 | BENZOTHIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200100329A AR118026A1 (en) | 2019-02-06 | 2020-02-06 | BENZOTIADIAZEPINE COMPOUNDS AND THEIR USE AS BILE ACID MODULATORS |
Country Status (2)
| Country | Link |
|---|---|
| AR (2) | AR118026A1 (en) |
| MA (1) | MA56430B1 (en) |
-
2020
- 2020-02-06 MA MA56430A patent/MA56430B1/en unknown
- 2020-02-06 AR ARP200100329A patent/AR118026A1/en unknown
- 2020-02-06 AR ARP200100328A patent/AR118025A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MA56430B1 (en) | 2023-01-31 |
| MA56430A (en) | 2022-05-11 |
| AR118026A1 (en) | 2021-09-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |