AR039983A1 - DERIVATIVES OF HETROXI TETRAHIDRO-NAFTALENILUREA - Google Patents
DERIVATIVES OF HETROXI TETRAHIDRO-NAFTALENILUREAInfo
- Publication number
- AR039983A1 AR039983A1 ARP030101614A ARP030101614A AR039983A1 AR 039983 A1 AR039983 A1 AR 039983A1 AR P030101614 A ARP030101614 A AR P030101614A AR P030101614 A ARP030101614 A AR P030101614A AR 039983 A1 AR039983 A1 AR 039983A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- amino
- optionally substituted
- tri
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C275/32—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C275/40—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
Abstract
Se refiere a derivados de tetrahidronaftaleno y a sales de los mismos que son útiles como ingredientes activos de preparaciones farmacéuticas. Los derivados de tetrahidro-naftaleno de la presente tienen una excelente actividad como antagonistas de VR1 y son útiles para la profilaxis y tratamiento de enfermedades asociadas con la actividad de VR1, en particular para el tratamiento de la imperiosidad urinaria, vejiga superactiva, dolor crónico, dolor neuropático, dolor postoperatorio, dolor de artritis reumatoide, neuralgia, neuropatías, algesia, lesión de nervios, isquemia, neurodegeneración, apoplejía, incontinencia, trastornos inflamatorios tales como asma y COPD. Reivindicación 1: Un derivado de hidroxi-tetrahidro-naftalenilurea de fórmula (1), sus formas tautomérica y estereoisomérica y las sales del mismo en la que: X representa alquilo C1-6, o un grupo de fórmula (2); donde: Y representa un enlace directo, o un grupo de fórmula (3), R1, R2 y R3 representan independientemente hidrógeno, halógeno, hidroxi, nitro, carboxi, amino, alquil(C1-6)-amino di(alquil)amino, cicloalquil(C3-8)-amino, alcoxi(C1-6)-carbonilo, fenilo, bencilo, sulfonamida, alcanoilo C1-6, -amino, carbamoilo, alquil(C1-6)-carbamoilo, ciano, alquilo C1-6 opcionalmente sustituido con ciano, alcoxi(C1-6)carbonilo mono-, di- o tri-halógeno, alcoxi C1-6 opcionalmente sustituido con mono-, di- o tri-halógeno, fenoxi opcionalmente sustituido con halógeno o alquilo C1-6, o alquiltio C1-6 opcionalmente sustituido con mono-, di- o tri-halógeno; R4, R5, R5, R6 y R7 representan independientemente hidrógeno, alquilo C1-6 o fenilo; Z1 representa hidrógeno o alquilo C1-6; y Z2 representa hidrógeno, halógeno o alquilo C1-6.It refers to tetrahydronaphthalene derivatives and salts thereof that are useful as active ingredients in pharmaceutical preparations. The tetrahydro-naphthalene derivatives herein have excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with the activity of VR1, in particular for the treatment of urinary empire, superactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritis pain, neuralgia, neuropathies, algesia, nerve injury, ischemia, neurodegeneration, stroke, incontinence, inflammatory disorders such as asthma and COPD. Claim 1: A hydroxy-tetrahydro-naphthalenylurea derivative of formula (1), its tautomeric and stereoisomeric forms and salts thereof wherein: X represents C1-6 alkyl, or a group of formula (2); where: Y represents a direct bond, or a group of formula (3), R1, R2 and R3 independently represent hydrogen, halogen, hydroxy, nitro, carboxy, amino, (C1-6) alkyl-amino di (alkyl) amino, C3-8 cycloalkyl-amino, (C 1-6) alkoxycarbonyl, phenyl, benzyl, sulfonamide, C 1-6 alkanoyl, -amino, carbamoyl, (C 1-6) alkylcarbamoyl, cyano, C 1-6 alkyl optionally substituted with cyano, (C1-6) alkoxy mono-, di- or tri-halogen, C1-6 alkoxy optionally substituted with mono-, di- or tri-halogen, phenoxy optionally substituted with halogen or C1-6 alkyl, or C1-6 alkylthio optionally substituted with mono-, di- or tri-halogen; R4, R5, R5, R6 and R7 independently represent hydrogen, C1-6 alkyl or phenyl; Z1 represents hydrogen or C1-6 alkyl; and Z2 represents hydrogen, halogen or C1-6 alkyl.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0210512.0A GB0210512D0 (en) | 2002-05-08 | 2002-05-08 | Tetrahydro-napthalene derivatives |
GBGB0227262.3A GB0227262D0 (en) | 2002-05-08 | 2002-11-21 | Tetrahydro-naphthalene derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
AR039983A1 true AR039983A1 (en) | 2005-03-09 |
Family
ID=9936269
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030101614A AR039983A1 (en) | 2002-05-08 | 2003-05-08 | DERIVATIVES OF HETROXI TETRAHIDRO-NAFTALENILUREA |
Country Status (13)
Country | Link |
---|---|
KR (1) | KR101000688B1 (en) |
AR (1) | AR039983A1 (en) |
CU (1) | CU23422B7 (en) |
DO (1) | DOP2003000642A (en) |
EC (1) | ECSP045413A (en) |
GB (2) | GB0210512D0 (en) |
GT (1) | GT200300102A (en) |
MA (1) | MA30728B1 (en) |
MY (1) | MY155011A (en) |
PE (1) | PE20040363A1 (en) |
PT (1) | PT1506167E (en) |
UA (1) | UA77301C2 (en) |
ZA (1) | ZA200408993B (en) |
-
2002
- 2002-05-08 GB GBGB0210512.0A patent/GB0210512D0/en not_active Ceased
- 2002-11-21 GB GBGB0227262.3A patent/GB0227262D0/en not_active Ceased
-
2003
- 2003-04-28 KR KR1020047017969A patent/KR101000688B1/en not_active IP Right Cessation
- 2003-04-28 UA UA20041210079A patent/UA77301C2/en unknown
- 2003-04-28 PT PT03722554T patent/PT1506167E/en unknown
- 2003-05-05 GT GT200300102A patent/GT200300102A/en unknown
- 2003-05-06 MY MYPI20031696A patent/MY155011A/en unknown
- 2003-05-07 PE PE2003000445A patent/PE20040363A1/en not_active Application Discontinuation
- 2003-05-07 DO DO2003000642A patent/DOP2003000642A/en unknown
- 2003-05-08 AR ARP030101614A patent/AR039983A1/en active IP Right Grant
-
2004
- 2004-11-04 CU CU20040254A patent/CU23422B7/en unknown
- 2004-11-05 MA MA27935A patent/MA30728B1/en unknown
- 2004-11-05 ZA ZA2004/08993A patent/ZA200408993B/en unknown
- 2004-11-08 EC EC2004005413A patent/ECSP045413A/en unknown
Also Published As
Publication number | Publication date |
---|---|
KR20040108784A (en) | 2004-12-24 |
PE20040363A1 (en) | 2004-07-03 |
ECSP045413A (en) | 2005-01-03 |
DOP2003000642A (en) | 2003-11-15 |
KR101000688B1 (en) | 2010-12-10 |
PT1506167E (en) | 2007-12-10 |
GB0227262D0 (en) | 2002-12-31 |
MA30728B1 (en) | 2009-10-01 |
GT200300102A (en) | 2004-03-17 |
MY155011A (en) | 2015-08-28 |
UA77301C2 (en) | 2006-11-15 |
GB0210512D0 (en) | 2002-06-19 |
ZA200408993B (en) | 2006-01-25 |
CU23422B7 (en) | 2009-09-08 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant, registration |