AR047537A1 - Piridazinonaureas como antagonistas de integrinas - Google Patents
Piridazinonaureas como antagonistas de integrinasInfo
- Publication number
- AR047537A1 AR047537A1 ARP050100450A ARP050100450A AR047537A1 AR 047537 A1 AR047537 A1 AR 047537A1 AR P050100450 A ARP050100450 A AR P050100450A AR P050100450 A ARP050100450 A AR P050100450A AR 047537 A1 AR047537 A1 AR 047537A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- heteroaryl
- independently selected
- hydroxy
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
- C07D237/14—Oxygen atoms
- C07D237/16—Two oxygen atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- 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
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- 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
- A61P9/10—Drugs 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Toxicology (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Métodos para la preparacion de estos compuestos, composiciones, intermediarios y derivados de los mismos. Reivindicacion 1: Un compuesto de formula (1), en el cual: R1 se selecciona independientemente del grupo que consiste en hidrogeno, alquilo C1- 6, alcoxi C1-6, arilo, heteroarilo, heterociclilo, heterociclilo fusionado con un benzo, cicloalquilo fusionado con un benzo, heterociclilo fusionado con un heteroarilo, cicloalquilo fusionado con un heteroarilo, ariloxi, heteroariloxi, heterocicliloxi, cicloalquiloxi, -NR10R20, halogeno, hidroxi, y -Salquilo(C1-6); en el cual el alcoxi C1-6 se sustituye opcionalmente con uno a cuatro sustituyentes independientemente seleccionados de Ra; donde Ra se selecciona independientemente del grupo que consiste en arilo, heteroarilo, heterociclilo, cicloalquilo, alcoxi(C1-6)carbonilo, carboxi, amino, alquilamino, dialquilamino, hidroxialcoxi(C1-6), uno a tres átomos de halogeno e hidroxi; donde R10 y R20 se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo C1-6, alilo, alquilo(C1-6)halogenado, hidroxi, hidroxialquilo(C1-4), arilalquilo (C1-4), arilo y cicloalquilo; además, R10 y R20 se toman opcionalmente junto con los átomos a los que están unidos para formar un anillo monocíclico de cinco a siete miembros; donde los sustituyentes arilo y ariloxi de R1 se sustituyen opcionalmente con un sustituyente seleccionado independientemente del grupo que consiste en uno a tres sustituyentes alquilo C1-6, hidroxialquilo (C1-6), arilalquilo (C1-6), alcoxi C1-6, arilo, heteroarilo, alcoxi(C1-6)carbonilo, arilalcoxi(C1-6)carbonilo, alquil(C1-6)carbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, hidroxi, ciano, nitro, -SO2alquilo(C1-3), -SO2arilo, -SO2heteroarilo, trifluorometilo, trifluorometoxi y de uno a tres átomos de halogeno; y donde los sustituyentes heteroarilo y heterociclilo de R1 se sustituyen opcionalmente con uno a tres sustituyentes seleccionados independientemente del grupo que consiste en alquilo C1-6, alcoxi C1-6, arilo, heteroarilo, halogeno e hidroxi; además, R1 y R2 opcionalmente se toman conjuntamente con los átomos a los que están unidos para formar un anillo heterocíclico o carbocíclico de cinco a siete miembros; R2 se selecciona independientemente del grupo que consiste en hidrogeno, alquilo C1-6, alqueniloxi C2-6, hidroxi, amino, alquilamino, dialquilamino y halogeno; donde R1 y R2 se toman opcionalmente junto con los átomos a los que están unidos para formar un anillo carbocíclico o heterocíclico de cinco a siete miembros; R3 se selecciona independientemente del grupo que consiste en hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, heterociclilo y cicloalquilo; donde el alquilo, alquenilo, y alquinilo se sustituyen opcionalmente con un sustituyente seleccionado independientemente del grupo que consiste en aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, arilo, heteroarilo, heterociclilo, cicloalquilo, carboxi, uno a tres átomos de halogeno, hidroxi y -C(=O)C1-6alquilo; R4 se selecciona independientemente del grupo que consiste en hidrogeno, fluor, cloro y metilo; R5 es hidrogeno o alquilo C1-3, siempre que R5 sea alquilo C1-3 solo cuando se lo toma con Y y los átomos a los que se unen R5 e Y se unan para formar un heterociclo de cinco a siete miembros; Y se selecciona del grupo que consiste en hidroximetilo, - C(=O)NH2, -C(=O)NH(OH), -C(=O)NH(alquilo C1-6), -C(=O)NH(hidroxialquilo (C1-6)), -C(=O)N(alquilo C1-6)2, -C(=O)NHSO2alquilo(C1-4), carboxi, tetrazolilo y -C(=O)alcoxi C1-6; donde dicho alcoxi se sustituye opcionalmente con uno a dos sustituyentes seleccionados independientemente del grupo que consiste en hidroxi, -NR30R40, heterociclilo, heteroarilo, halogeno y -OCH2CH2OCH3; donde R30 y R40 se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo C1-6, hidroxi e hidroxialquilo (C1-4), donde dichos R30 y R40 opcionalmente se toman conjuntamente con los átomos a los que están unidos para formar un anillo monocíclico de cinco a diez miembros; W se selecciona independientemente del grupo que consiste en -C(=O)- y -C(=S)-; R100 y R200 se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo C1-6, alquenilo C1-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, policicloalquilo, heterociclilo, hidroxi y arilamino; donde los sustituyentes alquilo, alquenilo C2-6, alquinilo C2-6, y alcoxi de R100 y R200 se sustituyen opcionalmente con un sustituyente independientemente seleccionado del grupo que consiste en arilo, heteroarilo, heterociclilo, hidroxi, uno a tres átomos de halogeno, amino, alquilamino C1-6, hidroxialquilamino (C1-6), dialquilamino (C1-6), -C(=O)amino, y -C(=O)alcoxi C1-6; donde dichos sustituyentes arilo, heteroarilo, y heterociclilo se pueden sustituir opcionalmente con hasta cuatro sustituyentes seleccionados del grupo que consiste en alquilo C1-6, alcoxi C1-6, halogeno, arilo, amino, alquilamino, dialquilamino, hidroxi, policicloalquilo y heteroarilo; y dicho heterociclilo se sustituye opcionalmente con uno a tres sustituyentes oxo; donde dichos arilo, heteroarilo y heterociclilo de R100 y R200 se pueden sustituir opcionalmente con uno a cuatro sustituyentes seleccionados independientemente del grupo que consiste en alquilo C1-6, trifluoroalquilo, alcoxi C1-6, trifluoroalcoxi, halogeno, arilo, amino, alquilamino, dialquilamino, arilamino, hidroxi, policicloalquilo, y heteroarilo; además, dicho heterociclilo se sustituye opcionalmente con uno a tres sustituyentes oxo; y donde R100 y R200 opcionalmente se toman conjuntamente con el átomo de nitrogeno al que ambos están unidos para formar un heterociclo de cinco a diez miembros o un heterociclo fusionado con un benzo de nueve a diez miembros; en el cual el heterociclo se sustituye opcionalmente con hasta cuatro sustituyentes seleccionados independientemente del grupo que consiste en alquilo C1-6, alcoxi C1-6, halogeno, arilo, heteroarilo, amino, alquilamino, dialquilamino, hidroxi, policicloalquilo o un oxo; y un isomero optico, enantiomero, diastereomero, racemato o una sal aceptable para uso farmacéutico de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US54331504P | 2004-02-10 | 2004-02-10 |
Publications (1)
Publication Number | Publication Date |
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AR047537A1 true AR047537A1 (es) | 2006-01-25 |
Family
ID=34860402
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP050100450A AR047537A1 (es) | 2004-02-10 | 2005-02-09 | Piridazinonaureas como antagonistas de integrinas |
Country Status (13)
Country | Link |
---|---|
US (1) | US20050209232A1 (es) |
EP (1) | EP1725538B1 (es) |
JP (1) | JP2007522224A (es) |
KR (1) | KR20070001976A (es) |
CN (1) | CN1946699A (es) |
AR (1) | AR047537A1 (es) |
AT (1) | ATE371649T1 (es) |
AU (1) | AU2005212423A1 (es) |
BR (1) | BRPI0506676A (es) |
CA (1) | CA2555227A1 (es) |
DE (1) | DE602005002251D1 (es) |
MX (1) | MXPA06009099A (es) |
WO (1) | WO2005077914A1 (es) |
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JO2849B1 (en) | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
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JP5431306B2 (ja) | 2007-04-23 | 2014-03-05 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 高速解離性ドパミン2受容体アンタゴニストとしてのチア(ジア)ゾール |
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-
2005
- 2005-02-09 US US11/054,175 patent/US20050209232A1/en not_active Abandoned
- 2005-02-09 DE DE602005002251T patent/DE602005002251D1/de active Active
- 2005-02-09 EP EP05722893A patent/EP1725538B1/en active Active
- 2005-02-09 KR KR1020067017323A patent/KR20070001976A/ko not_active Application Discontinuation
- 2005-02-09 MX MXPA06009099A patent/MXPA06009099A/es not_active Application Discontinuation
- 2005-02-09 WO PCT/US2005/004181 patent/WO2005077914A1/en active IP Right Grant
- 2005-02-09 AR ARP050100450A patent/AR047537A1/es unknown
- 2005-02-09 CA CA002555227A patent/CA2555227A1/en not_active Abandoned
- 2005-02-09 AU AU2005212423A patent/AU2005212423A1/en not_active Abandoned
- 2005-02-09 JP JP2006553219A patent/JP2007522224A/ja not_active Withdrawn
- 2005-02-09 AT AT05722893T patent/ATE371649T1/de not_active IP Right Cessation
- 2005-02-09 BR BRPI0506676-0A patent/BRPI0506676A/pt not_active Application Discontinuation
- 2005-02-09 CN CNA2005800121490A patent/CN1946699A/zh active Pending
Also Published As
Publication number | Publication date |
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JP2007522224A (ja) | 2007-08-09 |
US20050209232A1 (en) | 2005-09-22 |
ATE371649T1 (de) | 2007-09-15 |
CA2555227A1 (en) | 2005-08-25 |
EP1725538B1 (en) | 2007-08-29 |
KR20070001976A (ko) | 2007-01-04 |
EP1725538A1 (en) | 2006-11-29 |
MXPA06009099A (es) | 2007-02-02 |
CN1946699A (zh) | 2007-04-11 |
DE602005002251D1 (de) | 2007-10-11 |
AU2005212423A1 (en) | 2005-08-25 |
WO2005077914A1 (en) | 2005-08-25 |
BRPI0506676A (pt) | 2007-05-15 |
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