AR084546A1 - COMPOUNDS AS RENINA INHIBITORS - Google Patents

COMPOUNDS AS RENINA INHIBITORS

Info

Publication number
AR084546A1
AR084546A1 ARP110104889A ARP110104889A AR084546A1 AR 084546 A1 AR084546 A1 AR 084546A1 AR P110104889 A ARP110104889 A AR P110104889A AR P110104889 A ARP110104889 A AR P110104889A AR 084546 A1 AR084546 A1 AR 084546A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
nitrogen
independently selected
group
Prior art date
Application number
ARP110104889A
Other languages
Spanish (es)
Inventor
Mukul R Jain
Pravin Thombare
Jigar Desai
Original Assignee
Cadila Healthcare Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cadila Healthcare Ltd filed Critical Cadila Healthcare Ltd
Publication of AR084546A1 publication Critical patent/AR084546A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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

Abstract

La presente se refiere a inhibidores de renina de la formula general (1), intermedios involucrados en su síntesis, sus sales farmacéuticamente aceptables y composiciones farmacéuticas que las contienen. También se refiere a un proceso de preparación de compuestos de la fórmula general (1), en donde todos los símbolos son según se define en la especificación, sus formas tautoméricas, sus sales farmacéuticamente aceptables, composiciones farmacéuticas que las contienen, e intermedios involucrados en sus síntesis.Reivindicación 1: El compuesto representado por la fórmula (1), incluyendo sus estereoisómeros, tautómeros y solvatos, en donde ‘X’ se selecciona independientemente del grupo que comprende -CH2-, O, y S(O)p; p cuando aparece en cada caso se selecciona independientemente de los enteros 0, 1, 2; ‘n’ es un entero seleccionado de 1, 2; ‘M’ es nitrógeno o un átomo de carbono; R3 en cada aparición se selecciona independientemente del grupo que comprende OH, CN, halógeno, N3, NO2, COOH, OCF2H, CF3, alquilo C1-6, alquenilo C2-6, alcoxi C1-6, C(O)alquilo C1-6, C(O)O-alquilo C1-6, S(O)p-alquilo C1-6 o grupos (CH2)1-2O-alquilo; ‘q’ representa un entero de 1 - 4 y ‘p’ es como se definió antes; R1 se sustituye opcionalmente con alquilo C1-6 o grupos cicloalquilo C3-7; R2 es un anillo arilo sustituido o insustituido o un anillo heterociclilo sustituido o insustituido que contiene 1 a 3 heteroátomos seleccionados independientemente de oxígeno, azufre y nitrógeno o en una realización alternativa, R1 y R2 conjuntamente con el átomo de nitrógeno al cual se unen forman un anillo heterocíclico simple o fusionado opcionalmente sustituido saturado, insaturado o parcialmente saturado que es opcionalmente sustituido y además contiene opcionalmente uno o más heteroátomos adicionales seleccionados de nitrógeno, oxígeno o azufre o comprende un grupo -SO- o -SO2- en donde uno o más de tales átomos de nitrógeno se sustituye opcionalmente con grupos opcionalmente sustituidos seleccionados de alquilo C1-8, alcanoilo C1-8 o un grupo heterocíclico o arilo opcionalmente sustituido. Reivindicación 17: Un intermediario de la fórmula (2) y sus isómeros, en donde los símbolos R3, X, M, n, q, son como se define en la reivindicación 1.This refers to renin inhibitors of the general formula (1), intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. It also refers to a process of preparing compounds of the general formula (1), where all the symbols are as defined in the specification, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and intermediates involved in their synthesis. Claim 1: The compound represented by the formula (1), including its stereoisomers, tautomers and solvates, wherein 'X' is independently selected from the group comprising -CH2-, O, and S (O) p; p when it appears in each case is independently selected from the integers 0, 1, 2; ‘N’ is an integer selected from 1, 2; ‘M’ is nitrogen or a carbon atom; R3 at each occurrence is independently selected from the group comprising OH, CN, halogen, N3, NO2, COOH, OCF2H, CF3, C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy, C (O) C1-6 alkyl , C (O) O-C1-6 alkyl, S (O) p-C1-6 alkyl or groups (CH2) 1-2O-alkyl; ‘Q’ represents an integer of 1 - 4 and ‘p’ is as defined above; R1 is optionally substituted with C1-6 alkyl or C3-7 cycloalkyl groups; R2 is a substituted or unsubstituted aryl ring or a substituted or unsubstituted heterocyclyl ring containing 1 to 3 heteroatoms independently selected from oxygen, sulfur and nitrogen or in an alternative embodiment, R1 and R2 together with the nitrogen atom to which they are attached form a single or fused heterocyclic ring optionally substituted saturated, unsaturated or partially saturated which is optionally substituted and also optionally contains one or more additional heteroatoms selected from nitrogen, oxygen or sulfur or comprises a group -SO- or -SO2- wherein one or more of such nitrogen atoms are optionally substituted with optionally substituted groups selected from C1-8 alkyl, C1-8 alkanoyl or an optionally substituted heterocyclic or aryl group. Claim 17: An intermediate of the formula (2) and its isomers, wherein the symbols R3, X, M, n, q, are as defined in claim 1.

ARP110104889A 2010-12-22 2011-12-22 COMPOUNDS AS RENINA INHIBITORS AR084546A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IN3487MU2010 2010-12-22

Publications (1)

Publication Number Publication Date
AR084546A1 true AR084546A1 (en) 2013-05-22

Family

ID=46314551

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104889A AR084546A1 (en) 2010-12-22 2011-12-22 COMPOUNDS AS RENINA INHIBITORS

Country Status (2)

Country Link
AR (1) AR084546A1 (en)
WO (1) WO2012085935A2 (en)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2097377B1 (en) * 2006-11-17 2010-07-07 Merck Frosst Canada Ltd. Renin inhibitors
JP2010527942A (en) * 2007-05-24 2010-08-19 メルク フロスト カナダ リミテツド A new class of renin inhibitors
US20120115907A1 (en) * 2009-04-24 2012-05-10 Cadila Healthcare Limited Novel compounds as inhibitors of renin

Also Published As

Publication number Publication date
WO2012085935A2 (en) 2012-06-28
WO2012085935A3 (en) 2013-09-26

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