AR056269A1 - DERIVATIVES OF THIOAMIDS, ISOMERS OF THE SAME, OR PHARMACEUTICALLY ACCEPTABLE SALTS OF THE SAME, AS THE VANYLOID RECEIVING ANTAGONIST; AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - Google Patents
DERIVATIVES OF THIOAMIDS, ISOMERS OF THE SAME, OR PHARMACEUTICALLY ACCEPTABLE SALTS OF THE SAME, AS THE VANYLOID RECEIVING ANTAGONIST; AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAMEInfo
- Publication number
- AR056269A1 AR056269A1 ARP060100648A ARP060100648A AR056269A1 AR 056269 A1 AR056269 A1 AR 056269A1 AR P060100648 A ARP060100648 A AR P060100648A AR P060100648 A ARP060100648 A AR P060100648A AR 056269 A1 AR056269 A1 AR 056269A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- phenyl
- alkoxy
- disease
- haloc1
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C327/00—Thiocarboxylic acids
- C07C327/38—Amides of thiocarboxylic acids
- C07C327/40—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C327/44—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
Abstract
Este presente se refiere a los compuestos novedosos, isomeros de los mismos sales farmacéuticamente aceptables de los mismos como al antagonista del receptor vaniloide (receptor vaniloide 1; VR1; TRPV1); y a una composicion farmacéutica que contiene los mismos. La presente proporciona una composicion farmacéutica para prevenir o tratar una enfermedad tal como la dolencia, migrana, artralgia, neuralgia, neuropatías, danos en los nervios, enfermedad de la piel, hipersensibilidad de la vejiga urinaria, síndrome del intestino irritable, urgencia fecal, enfermedad de Crohn, un enfermedad respiratoria, irritacion de la piel, ojos o membranas mucosa, ulcera estomago-duodenal, enfermedades inflamatorias, enfermedad del oído y enfermedad cardíaca. Reivindicacion 1: Un compuesto de formula (1), un isomero de los mismos, o una sal farmacéuticamente aceptable de los mismos; en el que: X representa CHR13, en el que R13 representa hidrogeno, halogeno, o alquilo C1-5; Y representa CHR14, CHR14-CHR15, CR14=CR15, o una formula (2) o (3), en el que R14 y R15 son independientemente hidrogeno, alquilo C1-5, halogeno, o fenilo; R1 y R2 representan independientemente hidrogeno, -SO2R16, -SOR16, alquilo C1-5, alcoxi C1-5, halo-alquiloC1-5, alquenilo C2-5, alcoxicarbonilo C1-5, alquiltio C1-5, fenilo, o fenilo-alquiloC1-3, en el que, cada fenilo puede ser no sustituido o sustituido con uno o más sustituyentes seleccionados de carboxi, alquilo C1-5, halogeno, nitro, alquenilo C2-5, alcoxi C1-5, halo-alquiloC1-5, alquilcarbonilo C1-5, alquiltio C1-5, alquilsulfonilo C1-5, y alcoxicarbonilo C1-5, y R16 representa hidrogeno, amino, alquilo C1-5, alquenilo C2-5, alcoxi C1-5, halo-alquiloC1-5, trifluormetilo, fenilo, o fenilo-alquiloC1-3; R3 representa hidrogeno, hidroxi, alquilo C1-5, halo-alquiloC1-5, COOBu-t, MePhSO2-, fenilo, o fenilo-alquiloCl-3, en el que cada fenilo puede ser no sustituido o sustituido con uno o más sustituyentes seleccionados del carboxi, alquilo C1-5, halogeno, nitro, alquenilo C2-5, alcoxi C1-5, halo-alquiloC1-5, alquilcarbonilo C1-5, alquiltio C1-5, alquilsulfonilo C1-5, y alcoxicarbonilo C1-5; R4, R5, R6, y R7 independientemente representan hidrogeno, carboxi, alquilo C1- 5, halogeno, nitro, ciano, alquenilo C2-5, alquinilo C2-5, cicloalquilo C3-6, alcoxi C1-5, halo-alquiloC1-5, halo-alcoxiC1-5, alquilcarbonilo C1-5, alquilcarbonilamino C1-5, alquilsulfonilamino C1-5, fenilosulfonilamino, alquiltio C1-5, alquilsulfonilo C1-5, o alcoxicarbonilo C1-5; y R8, R9, R10, R11, y R12 independientemente representan hidrogeno, carboxi, alquilo C1-5, nitro, alquenilo C2-5, alcoxi C1-5, alquinilo C2-5, halo-alquiloC1-5, alquiltio C1-5, alquilsulfonilo C1-5, alquilcarbonilo C1-5, alcoxicarbonilo C1-5, o halogeno.This present refers to novel compounds, isomers of the same pharmaceutically acceptable salts thereof as to the vanyloid receptor antagonist (vanyloid receptor 1; VR1; TRPV1); and to a pharmaceutical composition that contains them. This provides a pharmaceutical composition to prevent or treat a disease such as ailment, migraine, arthralgia, neuralgia, neuropathies, nerve damage, skin disease, urinary bladder hypersensitivity, irritable bowel syndrome, fecal urgency, disease Crohn's disease, a respiratory disease, irritation of the skin, eyes or mucous membranes, stomach-duodenal ulcer, inflammatory diseases, ear disease and heart disease. Claim 1: A compound of formula (1), an isomer thereof, or a pharmaceutically acceptable salt thereof; wherein: X represents CHR13, in which R13 represents hydrogen, halogen, or C1-5 alkyl; Y represents CHR14, CHR14-CHR15, CR14 = CR15, or a formula (2) or (3), in which R14 and R15 are independently hydrogen, C1-5 alkyl, halogen, or phenyl; R1 and R2 independently represent hydrogen, -SO2R16, -SOR16, C1-5 alkyl, C1-5 alkoxy, C1-5 halo-alkyl, C2-5 alkenyl, C1-5 alkoxycarbonyl, C1-5 alkylthio, phenyl, or phenyl-C1 alkyl -3, wherein, each phenyl may be unsubstituted or substituted with one or more substituents selected from carboxy, C1-5 alkyl, halogen, nitro, C2-5 alkenyl, C1-5 alkoxy, haloC1-5 alkyl, alkylcarbonyl C1-5, C1-5 alkylthio, C1-5 alkylsulfonyl, and C1-5 alkoxycarbonyl, and R16 represents hydrogen, amino, C1-5 alkyl, C2-5 alkenyl, C1-5 alkoxy, haloC1-5 alkyl, trifluoromethyl, phenyl, or phenylC 1-3 alkyl; R3 represents hydrogen, hydroxy, C1-5 alkyl, haloC1-5 alkyl, COOBu-t, MePhSO2-, phenyl, or phenyl-C1-alkyl, in which each phenyl can be unsubstituted or substituted with one or more substituents selected of the carboxy, C1-5 alkyl, halogen, nitro, C2-5 alkenyl, C1-5 alkoxy, C1-5 haloalkyl, C1-5 alkylcarbonyl, C1-5 alkylthio, C1-5 alkylsulfonyl, and C1-5 alkoxycarbonyl; R4, R5, R6, and R7 independently represent hydrogen, carboxy, C1-5 alkyl, halogen, nitro, cyano, C2-5 alkenyl, C2-5 alkynyl, C3-6 cycloalkyl, C1-5 alkoxy, haloC1-5 alkyl , haloC1-5 alkoxy, C1-5 alkylcarbonyl, C1-5 alkylcarbonylamino, C1-5 alkylsulfonylamino, C1-5 alkylthio, C1-5 alkylsulfonyl, or C1-5 alkoxycarbonyl; and R8, R9, R10, R11, and R12 independently represent hydrogen, carboxy, C1-5 alkyl, nitro, C2-5 alkenyl, C1-5 alkoxy, C2-5 alkynyl, haloC1-5 alkyl, C1-5 alkylthio, C1-5 alkylsulfonyl, C1-5 alkylcarbonyl, C1-5 alkoxycarbonyl, or halogen.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR20050021896 | 2005-03-16 | ||
US66234505P | 2005-03-17 | 2005-03-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR056269A1 true AR056269A1 (en) | 2007-10-03 |
Family
ID=36991887
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP060100648A AR056269A1 (en) | 2005-03-16 | 2006-02-22 | DERIVATIVES OF THIOAMIDS, ISOMERS OF THE SAME, OR PHARMACEUTICALLY ACCEPTABLE SALTS OF THE SAME, AS THE VANYLOID RECEIVING ANTAGONIST; AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME |
Country Status (2)
Country | Link |
---|---|
AR (1) | AR056269A1 (en) |
WO (1) | WO2006098554A1 (en) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AP2007004157A0 (en) | 2005-03-17 | 2007-10-31 | Pfizer | N- (N-sulfonylaminomethyl) cyclo-propanecarboxamide derivatives useful for the treatment of pain |
MX2009000925A (en) | 2006-07-27 | 2009-02-05 | Amorepacific Corp | Novel compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and pharmaceutical compositions containing the same. |
US8557872B2 (en) | 2008-01-28 | 2013-10-15 | Amorepacific Corporation | Compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and pharmaceutical compositions containing the same |
CN102137851B (en) | 2008-07-02 | 2014-08-27 | 株式会社爱茉莉太平洋 | Novel compounds, isomer thereof, or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist and pharmaceutical compositions containing the same |
US9770454B2 (en) | 2013-07-14 | 2017-09-26 | Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd. | IGF-1R signaling pathway inhibitors useful in the treatment of neurodegenerative diseases |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU763824B2 (en) * | 1999-02-22 | 2003-07-31 | Medifron Dbt Co., Ltd. | Vanilloid analogues containing resiniferatoxin pharmacophores as potent vanilloid receptor agonists and analgesics, compositions and uses thereof |
RU2003130221A (en) * | 2001-03-26 | 2005-04-10 | Новартис АГ (CH) | CONDENSED PYRIDINE DERIVATIVES INTENDED FOR USE AS AN ANAGONISTS OF A VANILLOID RECEPTOR IN TREATMENT OF PAIN |
MY138086A (en) * | 2001-09-13 | 2009-04-30 | Smithkline Beecham Plc | Novel urea derivative as vanilloid receptor-1 antagonist |
KR100707123B1 (en) * | 2003-07-02 | 2007-04-16 | 그뤼넨탈 게엠베하 | 4-methylsulfonylaminophenyl analogues as vanilloid antagonist showing excellent analgesic activity and the pharmaceutical composition containing the same |
KR20050039573A (en) * | 2003-10-23 | 2005-04-29 | 주식회사 태평양 | Thiourea derivative-containing pharmaceutical composition having improved solubility and bioavailability |
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2006
- 2006-02-21 WO PCT/KR2006/000583 patent/WO2006098554A1/en active Application Filing
- 2006-02-22 AR ARP060100648A patent/AR056269A1/en not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
WO2006098554A1 (en) | 2006-09-21 |
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