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AR055041A1 - Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas. - Google Patents

Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas.

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Publication number
AR055041A1
AR055041A1 ARP060100953A ARP060100953A AR055041A1 AR 055041 A1 AR055041 A1 AR 055041A1 AR P060100953 A ARP060100953 A AR P060100953A AR P060100953 A ARP060100953 A AR P060100953A AR 055041 A1 AR055041 A1 AR 055041A1
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AR
Argentina
Prior art keywords
alkyl
group
atoms
substituted
membered aromatic
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Application number
ARP060100953A
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Merck Frosst Canada Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37023348&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR055041(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Frosst Canada Ltd filed Critical Merck Frosst Canada Ltd
Publication of AR055041A1 publication Critical patent/AR055041A1/es

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
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    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Epidemiology (AREA)
  • Dermatology (AREA)
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  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
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  • Hematology (AREA)
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  • Pregnancy & Childbirth (AREA)
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Abstract

Composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de formula estructural (1) y las sales, ésteres y solvatos farmacéuticamente aceptables de la misma, en los que: -------- se selecciona de un enlace simple y un enlace doble; ôAö se selecciona a partir de un grupo que consta de (a) un anillo aromático de 5 miembros que contiene (i) uno o más átomos de C, (ii) un heteroátomo seleccionado a partir de O y S, y (iii) 0, 1, 2 o 3 átomos de N; (b) un anillo aromático de 5 miembros que contiene uno o más átomos de C y de uno a cuatro átomos de N, (c) un anillo aromático de 6 miembros que contiene átomos de C y 1, 2 o 3 átomos de N; (d) un sistema anillo bicíclico seleccionado de benzotienilo, indolilo, quinolinilo y naftalenilo; (e) fenilo, y (f) -CH2-fenil; y en los que A está opcionalmente mono- o di-sustituida con un sustituyente independientemente seleccionado en cada aparicion del grupo consistente en (i) -F, (ii) -Cl, (iii) -alquilo C1-3 opcionalmente sustituido con uno o más grupos halo, (iv) -Oalquil C1-3 opcionalmente sustituido con uno o más grupos halo, (v) -Ocicloalquil C3-6, (vi) -CH2OH, (vii) -COOR1, (viii) -CN y (ix) -NR10R11; X se selecciona de -O- y -S-; Y se selecciona de (a) -NR6- CHR7 y -NR8-C(O)- en los que el N en Y está unido al resto heterocíclico de 5 miembros de formula (1) y el C en Y está unido al resto heterocíclico bicíclico de formula (1), (b) -S- y (c) -O-; R1 se selecciona del grupo consistente en - H, alquil C1- 6 y -cicloalquil C3-6; R2 se selecciona del grupo consistente en -H, -OH, -F, -alquil C1-3, -Oalquil C1-3 y -OC(O)-alquil C1-3; R3 se selecciona del grupo consistente en -H, -alquil C1-6, -alquil C1-6 sustituido con uno o más grupos fluoro, -alquil C1-6 sustituido con R9, -alquenil C2-6, -cicloalquil C3-6, -cicloalquenil C5-7 y -Z; R4 se selecciona del grupo consistente en -H, -alquil C1-6, -alquil C1-6 sustituido con uno o más grupos fluoro, -alquil C1-6 sustituido con R9, -alquenil C2-6, - cicloalquil C3-6, -cicloalquenil C5-7 y -Z; o R3 y R4 representan conjuntamente oxo; o R3 y R4 se articulan conjuntamente con el C al cual están unidos para formar un anillo seleccionado del grupo consistente en un anillo - cicloalquil C3-6 y un anillo -cicloalquenil C5-7, dado que cuando R3 y R4 se articulan conjuntamente con el C al cual están unidos para formar un anillo -cicloalquenil C5-7, no hay doble enlace en la posicion C-1 en el anillo; o R2, R3 y R4 se articulan conjuntamente con el C al cual están unidos para formar un anillo cicloalquenilo seleccionado de las formulas (2), R5 está ausente o es un sustituyente seleccionado a partir del grupo consistente en -alquil C1-6, cicloalquil C3-6 y halo; R6 se selecciona del grupo consistente en (a) -H, (b) -alquil C1-4, (c) -C(O)alquil C1-4 y (d) -C(O)fenil opcionalmente sustituido con -alquil C1-4; R7 se selecciona del grupo consistente en (a) -h, (b) alquilo C1-4, (c) -cicloalquil C3-6 y (d) fenilo opcionalmente mono- o di- sustituido con un sustituyente independientemente seleccionado en cada aparicion del grupo consistente en -alquil C1-4, -F y -Cl, y (e) un anillo aromático de 5 miembros que contiene (i) uno o más átomos de C, (ii) un heteroátomo seleccionado a partir de O y S; y (iii) 0, 1, 2 o 3 átomos de N; R8 se selecciona del grupo consistente en -H y -alquil C1-4; R9 se selecciona del grupo consistente en -COOR1, -C(O)H, -CN, -CR1R1OH, -OR1, -S-alquil C1-6 y -S-cicloalquil C3-6; R10 se selecciona del grupo consistente en -H, - alquil C1-6, -cicloalquil C3-6 y -COOR1; R11 se selecciona del grupo consistente en -H, -alquil C1-6 y -cicloalquil C3-6; y Z se selecciona del grupo consistente en (a) un anillo aromático de 5 miembros que contiene (i) uno o más átomos de C, (ii) un heteroátomo seleccionado a partir de O y S, y (iii) 0, 1, 2 o 3 átomos de N; (b) un anillo aromático de 5 miembros que contiene uno o más átomos de C y de uno a cuatro átomos de N, (c) un anillo aromático de 6 miembros que contiene átomos de C y 1, 2 o 3 átomos de N; (d) fenilo, y (e) -CH2-fenil y -CH2-dioxolanil, y en el que Z está opcionalmente mono- o di-sustituida con un sustituyente independientemente seleccionado en cada aparicion del grupo consistente en (i) - F, (ii) -Cl, (iii) -alquil C1-3 opcionalmente sustituido con uno o más grupos halo que incluye por ejemplo -CF3, (iv) -Oalquil C1-3 opcionalmente sustituido con uno o más grupos halo, (v) -Ocicloalquil C3-6, (vi) -CH2OH, (vii) -COOR1, (viii) -CN y (ix) -NR10R11.
ARP060100953A 2005-03-23 2006-03-13 Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas. AR055041A1 (es)

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US (3) US7553973B2 (es)
EP (1) EP1869031B1 (es)
JP (2) JP4109316B1 (es)
KR (1) KR20070113259A (es)
CN (2) CN101146802A (es)
AR (1) AR055041A1 (es)
AU (1) AU2006227524B2 (es)
BR (1) BRPI0609687A2 (es)
CA (1) CA2600727C (es)
CR (1) CR9442A (es)
DO (1) DOP2006000069A (es)
EA (1) EA012704B1 (es)
ES (1) ES2394179T3 (es)
GT (1) GT200600117A (es)
IL (1) IL185724A0 (es)
MA (1) MA29398B1 (es)
MX (1) MX2007011638A (es)
MY (1) MY142105A (es)
NI (1) NI200700242A (es)
NO (1) NO20075384L (es)
PA (1) PA8667201A1 (es)
PE (1) PE20061328A1 (es)
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TW (1) TWI321130B (es)
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AR055041A1 (es) * 2005-03-23 2007-08-01 Merck Frosst Canada Ltd Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas.
EP1934205A4 (en) * 2005-10-05 2010-06-02 Merck Frosst Canada Ltd SUBSTITUTED QUINOLINES AS INHIBITORS OF LEUCOTRIENE BIOSYNTHESIS
AR065093A1 (es) * 2007-02-05 2009-05-13 Merck Frosst Canada Ltd Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos
AR068498A1 (es) * 2007-09-27 2009-11-18 Merck & Co Inc Compuestos de oxadiazol para inhibicion de biosintesis de leucotrienos
JP2013501064A (ja) 2009-08-04 2013-01-10 アミラ ファーマシューティカルス,インコーポレーテッド リゾホスファチジン酸受容体アンタゴニストとしての化合物
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SG191041A1 (en) 2010-12-07 2013-08-30 Amira Pharmaceuticals Inc Polycyclic lpa1 antagonist and uses thereof
PH12013501136A1 (en) 2010-12-07 2013-07-08 Amira Pharmaceuticals Inc Lysophosphatidic acid receptor antagonists and uses thereof
US8541587B2 (en) 2011-04-05 2013-09-24 Amira Pharmaceuticals, Inc. Lysophosphatidic acid receptor antagonists
EP2714680B1 (en) 2011-05-27 2015-11-25 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
WO2014031586A2 (en) * 2012-08-20 2014-02-27 Tallikut Pharmaceuticals, Inc. Methods for treating cardiovascular diseases
CN102924442B (zh) * 2012-11-15 2014-10-29 沈阳药科大学 含有噻唑环的色满类化合物及其类似物和医药用途
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