AR052769A1 - BICYCLONONENE DERIVATIVES, PHARMACEUTICAL COMPOSITION BASED ON THE SAME AND USE OF THE COMPOUND IN THE PREPARATION OF MEDICINES - Google Patents
BICYCLONONENE DERIVATIVES, PHARMACEUTICAL COMPOSITION BASED ON THE SAME AND USE OF THE COMPOUND IN THE PREPARATION OF MEDICINESInfo
- Publication number
- AR052769A1 AR052769A1 ARP050103560A ARP050103560A AR052769A1 AR 052769 A1 AR052769 A1 AR 052769A1 AR P050103560 A ARP050103560 A AR P050103560A AR P050103560 A ARP050103560 A AR P050103560A AR 052769 A1 AR052769 A1 AR 052769A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituents
- independently selected
- halogen
- mono
- Prior art date
Links
Classifications
-
- 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
- C07D471/08—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente se refiere a derivados de biciclononeno y su uso como ingredientes activos en la preparacion de composiciones farmacéuticas. La presente también trata de aspectos relacionados que incluyen los procesos de preparacion de los compuestos, composiciones farmacéuticas que contienen uno o más de esos compuestos y en especial su uso como inhibidores de la renina. Estos compuestos son inhibidores de la renina, utiles en la regulacion de la presion sanguínea, mejorando funciones locales fisiopatologicamente alteradas, tales como la renal, cardíaca y vascular. Reivindicacion 1: Un compuesto seleccionado del grupo que consiste en compuestos de biciclononeno de formula (1), donde: X representa -NH-, -N(L)-, -CH2-, -CH(L)-, -O- o -S-; W representa 1,4-fenilo; V representa un grupo de formula -E1-Z-E2-; E1 representa un enlace o metileno; E2 representa oxígeno o -CH2-O-; Z representa una pirrolidina o anillo de azetidina; U representa arilo no sustituido; arilo mono-, di-, tri- o tetra-sustituido, en el que los sustituyentes se seleccionan en forma independiente del grupo que consiste en halogeno, -CF3, -OCF3, hidroxialquilo C1-7, R1COO-alquiloC1-7 y alquilo C1-7; o heteroarilo de cinco miembros que contiene dos heteroátomos seleccionados independientemente de nitrogeno, oxígeno y azufre (con preferencia pirazolilo o isoxazolilo), donde dicho radical heteroarilo está opcionalmente mono-, di- o tri-sustituido, en el que los sustituyentes se seleccionan independientemente de alquilo C1-7, alcoxi C1-7, -CF3, -OCF3 y halogeno; T representa -CONR1-; Q representa metileno; M representa fenilo; fenilo mono- o di-sustituido, donde los sustituyentes se seleccionan independientemente del grupo que consiste en alquilo C1-7-, alcoxi C1-7, -OCF3, -CF3, hidroxialquilo C1-7, halogeno, alquilC1-7-O-(CH2)0-4-CH2-, alquilC1-7-O(CH2)2-4-O-, y R42N-(CH2)0-4-CH2-; o piridinilo mono- o di-sustituido, donde los sustituyentes se seleccionan independientemente del grupo que consiste en halogeno, alquilo C1-7, -OCF3, -CF3, y alcoxi C1-7; con la salvedad de que los sustituyentes halogenos no estén en la posicion 2 o 6 del anillo piridinilo; L representa -R3, -COR3, -COOR3, -CONR2R3, -SO2R3, o -SO2NR2R3; R1 y R1' en forma independiente representan alquilo C1-7 o cicloalquilo; R2 y R2' en forma independiente representan alquilo C1-7, alquenilo C2-7, cicloalquilo o cicloalquilalquilo C1-7; R3 representa alquilo C1-7, cicloalquilo, o cicloalquilalquilo C1-7, en el que estos grupos pueden estar no sustituidos o mono-, di-, o tri-sustituido, donde los sustituyentes se seleccionan independientemente de hidroxi, -NH2, -OCOR2, -COOR2, -SO3H, -SO2CH3, alcoxi C1-7, ciano, -CONR2R2', -NH(NH)NH2, -NR1R1', tetrazolilo y alquilo C1-7, con la salvedad de que un átomo de carbono esté unido a lo sumo a un heteroátomo en caso de que este átomo de carbono esté hibridizado sp3; y R4 representa hidrogeno, alquilo C1-7, ciclopropilo o -C(=O)-R', donde R' es alquilo C1-4, - CF3, -CH2-CF3 o ciclopropilo; y enantiomeros opticamente puros, mezclas de enantiomeros tales como racematos, diastereomeros, mezclas de diastereomeros, racematos diastereoméricos, mezclas de racematos diastereoméricos, y formas meso, como así también complejos de sales y solventes de tales compuestos y formas morfologicas.This refers to biciclononene derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The present also deals with related aspects that include the processes of preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as renin inhibitors. These compounds are renin inhibitors, useful in the regulation of blood pressure, improving local pathophysiologically altered functions, such as renal, cardiac and vascular. Claim 1: A compound selected from the group consisting of biciclononene compounds of formula (1), wherein: X represents -NH-, -N (L) -, -CH2-, -CH (L) -, -O- or -S-; W represents 1,4-phenyl; V represents a group of formula -E1-Z-E2-; E1 represents a bond or methylene; E2 represents oxygen or -CH2-O-; Z represents a pyrrolidine or azetidine ring; U represents unsubstituted aryl; mono-, di-, tri- or tetra-substituted aryl, wherein the substituents are independently selected from the group consisting of halogen, -CF3, -OCF3, C1-7 hydroxyalkyl, R1COO-C1-7 alkyl and C1-alkyl -7; or five-membered heteroaryl containing two heteroatoms independently selected from nitrogen, oxygen and sulfur (preferably pyrazolyl or isoxazolyl), wherein said heteroaryl radical is optionally mono-, di- or tri-substituted, in which the substituents are independently selected from C1-7 alkyl, C1-7 alkoxy, -CF3, -OCF3 and halogen; T represents -CONR1-; Q represents methylene; M represents phenyl; mono- or di-substituted phenyl, where the substituents are independently selected from the group consisting of C1-7- alkyl, C1-7 alkoxy, -OCF3, -CF3, C1-7 hydroxyalkyl, halogen, C1-7-O-alkyl ( CH2) 0-4-CH2-, alkyl C1-7-O (CH2) 2-4-O-, and R42N- (CH2) 0-4-CH2-; or mono- or di-substituted pyridinyl, wherein the substituents are independently selected from the group consisting of halogen, C1-7 alkyl, -OCF3, -CF3, and C1-7 alkoxy; with the proviso that halogen substituents are not in position 2 or 6 of the pyridinyl ring; L represents -R3, -COR3, -COOR3, -CONR2R3, -SO2R3, or -SO2NR2R3; R1 and R1 'independently represent C1-7 alkyl or cycloalkyl; R2 and R2 'independently represent C1-7 alkyl, C2-7 alkenyl, cycloalkyl or C1-7 cycloalkylalkyl; R3 represents C1-7 alkyl, cycloalkyl, or C1-7 cycloalkylalkyl, in which these groups may be unsubstituted or mono-, di-, or tri-substituted, where the substituents are independently selected from hydroxy, -NH2, -OCOR2 , -COOR2, -SO3H, -SO2CH3, C1-7 alkoxy, cyano, -CONR2R2 ', -NH (NH) NH2, -NR1R1', tetrazolyl and C1-7 alkyl, with the proviso that a carbon atom is attached at most a heteroatom in case this carbon atom is hybridized sp3; and R4 represents hydrogen, C1-7 alkyl, cyclopropyl or -C (= O) -R ', where R' is C1-4 alkyl, - CF3, -CH2-CF3 or cyclopropyl; and optically pure enantiomers, mixtures of enantiomers such as racemates, diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates, and meso forms, as well as complexes of salts and solvents of such compounds and morphological forms.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP2004009476 | 2004-08-25 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR052769A1 true AR052769A1 (en) | 2007-04-04 |
Family
ID=35395835
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP050103560A AR052769A1 (en) | 2004-08-25 | 2005-08-25 | BICYCLONONENE DERIVATIVES, PHARMACEUTICAL COMPOSITION BASED ON THE SAME AND USE OF THE COMPOUND IN THE PREPARATION OF MEDICINES |
Country Status (3)
Country | Link |
---|---|
AR (1) | AR052769A1 (en) |
TW (1) | TW200628468A (en) |
WO (1) | WO2006021401A2 (en) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8129538B1 (en) | 2007-03-28 | 2012-03-06 | Takeda Pharmaceutical Company Limited | Renin inhibitors |
WO2008141462A1 (en) | 2007-05-24 | 2008-11-27 | Merck Frosst Canada Ltd. | Novel case of renin inhibitors |
EP2190811B1 (en) | 2007-08-20 | 2013-08-07 | Merck Canada Inc. | Renin inhibitors |
SG192543A1 (en) | 2008-05-05 | 2013-08-30 | Merck Canada Inc | 3, 4 - substituted piperidine derivatives as renin inhibitors |
RU2490257C2 (en) | 2008-05-30 | 2013-08-20 | Такеда Фармасьютикал Компани Лимитед | Heterocyclic compound |
AU2011313191A1 (en) | 2010-10-08 | 2013-05-02 | Mochida Pharmaceutical Co., Ltd. | Cyclic amide derivative |
WO2012147516A1 (en) | 2011-04-28 | 2012-11-01 | 持田製薬株式会社 | Cyclic amide derivative |
CN115819186B (en) * | 2023-02-14 | 2023-05-16 | 广东银珠医药科技有限公司 | Novel preparation method of 3, 5-dichlorobenzyl alcohol |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2343153C2 (en) * | 2002-04-29 | 2009-01-10 | Актелион Фармасьютиклз Лтд. | Derivatives of 7-aryl-3,9-diazabicyclo(3,3,1)non-6-ene-rhenin inhibitors |
-
2005
- 2005-08-22 WO PCT/EP2005/009048 patent/WO2006021401A2/en active Application Filing
- 2005-08-24 TW TW094128948A patent/TW200628468A/en unknown
- 2005-08-25 AR ARP050103560A patent/AR052769A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
TW200628468A (en) | 2006-08-16 |
WO2006021401A3 (en) | 2006-04-13 |
WO2006021401A2 (en) | 2006-03-02 |
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