AR035494A1 - Derivados de pirazina, composiciones farmaceuticas que los comprenden, y los usos de tales compuestos y composiciones en la elaboracion de medicamento - Google Patents
Derivados de pirazina, composiciones farmaceuticas que los comprenden, y los usos de tales compuestos y composiciones en la elaboracion de medicamentoInfo
- Publication number
- AR035494A1 AR035494A1 ARP010104452A ARP010104452A AR035494A1 AR 035494 A1 AR035494 A1 AR 035494A1 AR P010104452 A ARP010104452 A AR P010104452A AR P010104452 A ARP010104452 A AR P010104452A AR 035494 A1 AR035494 A1 AR 035494A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- substituted
- hydroxyalkyl
- halo
- Prior art date
Links
Classifications
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Derivados de pirazina que inhiben la actividad de la tirosín quinasa, y que tienen la fórmula (1) o sales farmacéuticamente aceptables de los mismos, en donde: R1 es seleccionado de entre el grupo consistente en cicloalquilo, heterociclilo, biheterociclilo, arilo, biarilo, heteroarilo y biheteroarilo opcionalmente sustituidos con 1 a 5 sustituyentes entre sí seleccionados de entre el grupo consistente en alquilo, alquilo inferior, alquenilo, alquinilo, alcoxi, alcoxi inferior, heterociclilo, heterociclilalquilo, heterociclilalquenilo, heterociclil alquinilo, heterociclilalcoxi, arilo, arilalquilo, arilalquenilo, arilalquinilo, arilalcoxi, heteroarilo, heteroarilalquilo, heteroarilalquenilo, heteroarilalquinilo, heteroaril alcoxi, OH, hidroxialquilo, halógeno, ciano, nitro, amino, alquilamino, alquilaminoalquilo, alquilaminoalquilamino, aminoalquilo, aminoalquilamino, di(alquil)amino, di(alquil)aminoalquilo, di(alquil)aminoalquilamino, (hidroxialquil) amino, di(hidroxialquil)amino, carbamoílo, acilo, acilalquilo, alcoxicarbonilo, alcoxicarbonilalquilo, acilamino, alquilsulfonilo, alquilsulfonilamino, arilsulfonil amino (estando arilo sustituido con de 1 a 3 sustituyentes independientemente entre sí seleccionados de entre el grupo consistente en ciano, halógeno, hidroxi, nitro, alquilo inferior tri (halo) sustituido y alcoxi inferior tri(halo) sustituido, aminosulfonilo, aminosulfonilalquilo, alquilaminosulfonilo, alquilamino sulfonil alquilo, di(alquil)aminosulfonilo, di(alquil)aminosulfonilalquilo, carboxilo, (hidroxi alquil)carbonilo, (hidroxialcoxi)carbonilo, alquilo inferior tri-halo sustituido y alcoxi inferior tri(halo) sustituido; A es seleccionado de entre el grupo consistente en -N(R4)(CH2)x-, -O(CH2)x-, -S(CH2)x-, -SO2(CH2)x-, -SO2N(CH2)x-, -NSO2(CH2)x-, -N(R4)(CH2)1-4O(CH2)x-, -N(R4)(CH2)1-4NH(CH2)x-, y N(R4)CNNH(CH2)x-, siendo x un número entero de 0 a 4; R4 es seleccionado de entre el grupo consistente en H, alquilo inferior, alquilo, hidroxialquilo, alcoxialquilo, arilalquilo, alquenilo inferior, alquenilo, arilo y heteroarilo; siendo arilo y heteroarilo opcionalmente sustituidos con 1 a 5 sustituyentes entre sí seleccionados de entre el grupo consistente en OH, halógeno, ciano, nitro, amino, alquilamino, di(alquil)amino, (hidroxialquil) amino, di(hidroxialquil)amino, alquilo, alquilo inferior, alcoxi, alcoxi inferior, alquilo inferior tri(halo) sustituido y alcoxi inferior tri(halo) sustituido; R2 es seleccionado de entre el grupo consistente en heteroarilo y biheteroarilo opcionalmente sustituido con de 1 a 2 sustituyentes independientemente entre sí R7 y un sustituyente seleccionado entre R8; R7 es seleccionado de entre el grupo consistente en alquilo, alquilo inferior, alcoxi inferior, alquenilo, alquinilo, heterociclilo, heterociclilalquilo, heterociclilalcoxi, arilo, arilalquilo, arilalcoxi, OH, hidroxialquilo, halógeno, ciano, nitro, amino, alquilamino, di(alquilo) amino, (hidroxialquil)amino, di(hidroxialquil) amino, carbamoílo, acilo, acilalquilo, alcoxicarbonilo, alcoxicarbonilalquilo, acilamino, alquilsulfonilo, alquilsulfonilamino, arilsulfonilamino (en el cual arilo está sustituido con de 1 a 3 sustituyentes seleccionados independientemente entre sí de entre el grupo consiste en ciano, halógeno, hidroxi, nitro, alquilo inferior tri (halo) sustituido y alcoxi inferior tri(halo)sustituido, carboxilo, (hidroxialquil) carbonilo, (hidroxialcoxi)carbonilo, alquilo inferior tri(halo) sustituido y alcoxi inferior tri(halo) sustituido; R8 es seleccionado de entre el grupo consistente en alquilo, OH, hidroxi alquilo, halógeno, ciano, amino, alquil amino, di(alquil) amino, (hidroxialquil) amino, di(hidroxialquil) amino, carbamoílo, alquilcarbonilamino, alquilcarbonilo, alcoxi carbonilo, (hidroxialquil)carbonilo, (hidroxialcoxi)carbonilo, O(CH2)nR5, O(CH2)nO(CH2)R5, O(CH2)nCH[(CH2)mR5]2, O(CH2)nN[(CH2)mR5]2, OCON[(CH2)]mR5]2, NH(CH2)nR5, NH(CH2)nCH(R5)2, NH(CH2)nSO2(CH2)mR5, NH(CH2)nO(CH2)mR5, NH(CH2)nOCH[(CH2)mR5]2, NH(CH2)nO(CH2)mO(CH2)mR5, NH(CH2)nN[(CH2)mR5]2, NH(CH2)nSO2NH(CH2)mR5, NH(CH2)nCH(OH) (CH2)mR5, NH(CH2)nCH(OH) (CH2)mOR5, NH(CH2)nCH(OH) (CH2)mN[(CH2)mR5]2, NH(CH2)nCO(CH2)mN[(CH2)mR5]2, NH(CH2)nCO2(CH2)mR5, NH(CH2)nCO(CH2)mSO2NH(CH2)mR5, NHCO(CH2)nCH(R5)2, NHCO(CH2)nR5, NHCO(CH2)nO(CH2)mR5, NHCO(CH2)nO(CH2)mO(CH2)mR5, NHCO(CH2)nO(CH2)mCO(CH2)mR5, NHCO(CH2)nN[(CH2)mR5]2, CONH(CH2)nO(CH2)mR5 y CONH(CH2)nN[(CH2)mR5]2; en lo cual n es un número entero de 0 a 6 y m es un número entero de 0 a 4; con la condición de que m es por lo menos 1 cuando R5 es seleccionado de entre el grupo consistente en OH, amino, alquilamino y di(alquil) amino. R5 es seleccionado de entre el grupo consiste en H, OH, alquilo inferior, amino, alquilamino, di(alquil) amino, arilo, heteroarilo, biheteroarilo y heterociclilo; siendo arilo, heteroarilo y heterociclilo opcionalmente sustituidos con de 1 a 3 sustituyentes independientemente entre sí seleccionados de entre el grupo consistente en alquilo, alquilo inferior, acilo, carboxilo, arilo (opcionalmente sustituido con de 1 a 5 sustituyentes halógeno), OH, halógeno, ciano, amino, alquil amino, di(alquil) amino, hidroxi (alquil) amino, di(hidroxialquil) amino, alquilsulfonilo, amino sulfonilo, alquilaminosulfonilo y aminosulfonilalquilo; y, en el cual heterociclilo está además opcionalmente sustituido con de 1 a 3 sustituyentes oxo; y R3 es seleccionado de entre el grupo consistente en H, alquilo, alquilo inferior, alcoxi, alcoxi inferior, alquenilo, alquinilo, heterociclilo, heterociclilalquilo, heterocicloalcoxi, arilo, arilalquilo, arilalcoxi, OH, hidroxi alquilo, halógeno, ciano, nitro, amino, alquil amino, di(alquil) amino, (hidroxialquil) amino, carbamoílo, acilo, acilalquilo, alcoxi carbonilo, alcoxicarbonilalquilo, acilamino, alquilsulfonilo, alquilsulfinil amino, arilsulfinil amino (siendo arilo sustituido con de 1 a 3 sustituyentes seleccionados independientemente entre sí de entre el grupo consistente en ciano, halógeno, hidroxi, nitro, alquilo inferior tri(halo) sustituido y alcoxi inferior tri (halo) sustituido, carboxilo, (hidroxi alquil) carbonilo, (hidroxi alcoxi) carbonilo, alquilo inferior tri(halo) sustituido y alcoxi inferior tri(halo) sustituido. Estos derivados de pirazina son particularmente útiles como inhibidores contra el dominio quinasa (enzima tirosn-quinasa)del Receptor del Factor de Crecimiento Endotelial Vascular (VEGF-R), que inhibe la actividad del receptor VEGF in vitro e in vivo. Estos compuestos son útiles para tratar enfermedades mediadas por la actividad del VEGF-R que incluyen, pero no se limitan a, cánceres de tumor sólido, angiogénesis, retinopatía diabética, artritis reumatoide, endometriosis y psoriasis. Además, se dan a conocer composiciones farmacéuticas que los comprenden, y los usos de tales compuestos y composiciones en la elaboración de medicamentos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US23396800P | 2000-09-20 | 2000-09-20 | |
US09/955,780 US6710048B2 (en) | 2000-09-20 | 2001-09-19 | Pyrazine derivatives as modulators of tyrosine kinases |
Publications (1)
Publication Number | Publication Date |
---|---|
AR035494A1 true AR035494A1 (es) | 2004-06-02 |
Family
ID=22879359
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP010104452A AR035494A1 (es) | 2000-09-20 | 2001-09-20 | Derivados de pirazina, composiciones farmaceuticas que los comprenden, y los usos de tales compuestos y composiciones en la elaboracion de medicamento |
Country Status (14)
Country | Link |
---|---|
US (1) | US6710048B2 (es) |
EP (1) | EP1330452B1 (es) |
JP (1) | JP2004523474A (es) |
AR (1) | AR035494A1 (es) |
AT (1) | ATE415396T1 (es) |
AU (1) | AU9458401A (es) |
CA (1) | CA2423050A1 (es) |
DE (1) | DE60136731D1 (es) |
DK (1) | DK1330452T3 (es) |
ES (1) | ES2315308T3 (es) |
HK (1) | HK1054393B (es) |
PT (1) | PT1330452E (es) |
TW (1) | TWI254711B (es) |
WO (1) | WO2002024681A2 (es) |
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AU7149798A (en) | 1997-06-30 | 1999-01-19 | R.J. Reynolds Tobacco Company | 3-pyridyl-1-aza-bicyclo-alkane derivatives for prevention and treatment of cn s disorders |
AU4831899A (en) * | 1998-06-30 | 2000-01-17 | Eli Lilly And Company | 5-HT1F agonists |
HU225917B1 (en) * | 1999-09-16 | 2007-12-28 | Tanabe Seiyaku Co | Pyrimidine and pyrazine derivatives, pharmaceutical compositions containing them and their use |
BR0108363A (pt) * | 2000-02-16 | 2004-02-10 | Neurogen Corp | Composto, métodos para modular função de receptor de crf e acoplado a proteìna g, para tratar um distúrbio ou doença do snc, para localizar receptores de crf em amostras de seção de tecidos, para inibir a ligação de crf a um receptor de crf¹ e para alterar a atividade de transdução de sinal de um receptor de crf¹ e composição farmacêutica |
-
2001
- 2001-09-19 EP EP01975243A patent/EP1330452B1/en not_active Revoked
- 2001-09-19 US US09/955,780 patent/US6710048B2/en not_active Expired - Lifetime
- 2001-09-19 ES ES01975243T patent/ES2315308T3/es not_active Expired - Lifetime
- 2001-09-19 DE DE60136731T patent/DE60136731D1/de not_active Expired - Lifetime
- 2001-09-19 PT PT01975243T patent/PT1330452E/pt unknown
- 2001-09-19 CA CA002423050A patent/CA2423050A1/en not_active Abandoned
- 2001-09-19 WO PCT/US2001/029175 patent/WO2002024681A2/en active Application Filing
- 2001-09-19 AU AU9458401A patent/AU9458401A/xx active Pending
- 2001-09-19 AT AT01975243T patent/ATE415396T1/de not_active IP Right Cessation
- 2001-09-19 JP JP2002529091A patent/JP2004523474A/ja active Pending
- 2001-09-19 DK DK01975243T patent/DK1330452T3/da active
- 2001-09-20 AR ARP010104452A patent/AR035494A1/es not_active Application Discontinuation
-
2002
- 2002-09-05 TW TW091120227A patent/TWI254711B/zh not_active IP Right Cessation
-
2003
- 2003-09-19 HK HK03106746.1A patent/HK1054393B/zh not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
HK1054393B (zh) | 2009-08-28 |
PT1330452E (pt) | 2009-01-22 |
ES2315308T3 (es) | 2009-04-01 |
WO2002024681A2 (en) | 2002-03-28 |
HK1054393A1 (es) | 2003-11-28 |
DE60136731D1 (de) | 2009-01-08 |
AU9458401A (en) | 2002-04-02 |
ATE415396T1 (de) | 2008-12-15 |
US6710048B2 (en) | 2004-03-23 |
TWI254711B (en) | 2006-05-11 |
EP1330452B1 (en) | 2008-11-26 |
JP2004523474A (ja) | 2004-08-05 |
WO2002024681A3 (en) | 2002-06-20 |
CA2423050A1 (en) | 2002-03-28 |
US20030060629A1 (en) | 2003-03-27 |
DK1330452T3 (da) | 2009-03-16 |
EP1330452A2 (en) | 2003-07-30 |
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