AR040350A1 - Inhibidores de caspasa y usos de los mismos - Google Patents
Inhibidores de caspasa y usos de los mismosInfo
- Publication number
- AR040350A1 AR040350A1 ARP030102352A ARP030102352A AR040350A1 AR 040350 A1 AR040350 A1 AR 040350A1 AR P030102352 A ARP030102352 A AR P030102352A AR P030102352 A ARP030102352 A AR P030102352A AR 040350 A1 AR040350 A1 AR 040350A1
- Authority
- AR
- Argentina
- Prior art keywords
- disease
- halo
- straight
- ocf3
- branched
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
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- 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
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- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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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
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- A61P25/16—Anti-Parkinson drugs
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- 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
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
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- Virology (AREA)
- Communicable Diseases (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Tropical Medicine & Parasitology (AREA)
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Abstract
Reivindicación 1: Un compuesto de fórmula (1), en donde: X es un CH o N; Y es halo, trifluorfenoxi o tetrafluorfenoxi; R2 es alquilo C1-6 de cadena recta o ramificada; R3 es hidrógeno, halo, OCF3, CN o CF3; y R4 es hidrógeno, halo, OCF3, SR, CN, CF3, Ar o T-Ar; en donde: T es O ó S; R es un alquilo C1-6 de cadena recta o ramificada; Ar es un anillo fenilo opcionalmente sustituido con 1 a 3 grupos seleccionados entre halo, CH3, CF3, CN, OMe, OCF3 y NR5R6; y R5 y R6 son, cada uno en forma independiente, H o alquilo C1-6 de cadena recta o ramificada, o R5 y R6, tomados juntos, forman un anillo de 5 a 7 miembros que opcionalmente contiene hasta 3 heteroátomos seleccionados entre O, S, NH y N(alquilo C1-6 de cadena recta o ramificada); siempre que Y sea halo, entonces R3 y R4 no son simultáneamente hidrógeno. Reivindicación 21: Una composición farmacéutica que comprende: a) un compuesto conforme a cualquiera de las reivindicaciones 1 a 20; b) un portador, adyuvante o vehículo farmacéuticamente aceptable. Reivindicación 22: Un método para tratar una enfermedad en un paciente, en donde dicha enfermedad se selecciona entre una enfermedad regulada por IL-1,una enfermedad regulada por apoptosis, una enfermedad inflamatoria, una enfermedad autoinmune, un trastorno óseo destructivo, un trastorno proliferativo, una enfermedad infecciosa, una enfermedad degenerativa, una enfermedad asociada con la muerte celular, una enfermedad por ingestión de exceso de alcohol dietario, una enfermedad regulada viral, trastornos de la retina, uveítis, peritonitis inflamatoria, osteoartritis, pancreatitis, asma, síndrome de insuficiencia respiratoria del adulto, glomerulonefritis, artritis reumatoidea, lupus eritematoso sistémico, esclerodermia, tiroiditis crónica, enfermedad de Grave, gastritis autoinmune, diabetes, anemia hemolítica autoinmune, neutropenia autoinmune, trombocitopenia, hepatitis activa crónica, miastenia grave, enfermedad intestinal inflamatoria, enfermedad de Crohn, psoriasis, dermatitis atópica, cicatrización patológica, enfermedad de injerto contra huésped, rechazo de transplante de órganos, apoptosis de órganos luego de danos por quemaduras, osteoporosis, leucemias y trastornos relacionados, síndrome mielodisplásico, trastorno óseo relacionado con mieloma múltiple, leucemia mielógena aguda, leucemia mielógena crónica, melanoma metastático, sarcoma de Kaposi, mieloma múltiple, choque hemorrágico, sepsis, choque séptico, quemaduras, siguelosis, mal de Alzheimer, enfermedad de Parkinson, enfermedad de Huntington, enfermedad de Kennedy, enfermedad priónica, isquemia cerebral, epilepsia, isquemia de miocardio, enfermedad cardiaca aguda y crónica, infarto de miocardio, insuficiencia cardiaca congestiva, aterosclerosis, derivación aortocoronaria (bypass), atrofia muscular espinal, esclerosis lateral amiotrófica, esclerosis múltiple, encefalitis relacionada con HIV, envejecimiento, alopecia, dano neurológico debido a apoplejía, colitis ulcerativa, dano cerebral traumático, dano de la medula espinal, hepatitis B, hepatitis C, hepatitis G, fiebre amarilla, fiebre del dengue, o encefalitis japonesa, varias formas de enfermedad hepática, enfermedad renal, enfermedad del rinón poliquística, enfermedad ulcerosa duodenal y gástrica asociada con H. Pylori, infección de HIV, tuberculosis, meningitis, insuficiencia de órganos, tratamiento de complicaciones asociadas con derivaciones aortocoronarias (bypass), y una inmunoterapia para el tratamiento de varias formas de cáncer; en donde dicho método comprende la etapa de administrar a dicho paciente una composición farmacéutica conforme a la reivindicación 21. Reivindicación 31: Un método de preparación de un compuesto de fórmula (1), en donde dicho método comprende: hacer reaccionar un ácido o derivado ácido de fórmula (2), con un amino alcohol de fórmula (4), para proporcionar un compuestos de fórmula (3); convertir el intermediario (3) en compuesto (1), en donde: X es CH o N; Y es halo, trifluorfenoxi o tetrafluorfenoxi; R2 es alquilo C1-6 de cadena recta o ramificada; R3 es hidrógeno, halo, OCF3, CN o CF3; y R4 es hidrógeno, halo, OCF3, SR, CN, CF3, Ar o T-Ar; en donde: T es O ó S; R es un alquilo C1-6 de cadena recta o ramificada; Ar es un anillo fenilo opcionalmente sustituido con 1 a 3 grupos seleccionados entre halo, CH3, CF3,CN, OMe, OCF3 y NR5R6; R5 y R6 son, cada uno en forma independiente, H o alquilo C1-6 de cadena recta o ramificada, o R5 y R6, tomados juntos, forman un anillo de 5 a 7 miembros que opcionalmente contiene hasta 3 heteroátomos seleccionados entre O, S, NH y N(alquilo C1-6 de cadena recta o ramificada); y R7 es un grupo protector adecuado; siempre que cuando Y es halo, entonces R3 y R4 no son simultáneamente hidrógeno. Reivindicación 32: Un compuesto de fórmula (5), en donde: X es CH o N; R2 es alquilo C1-6 de cadena recta o ramificada; R3 es hidrógeno, halo, OCF3, CN o CF3; y R4 es hidrógeno, halo, OCF3, SR, CN, CF3, Ar o T-Ar; en donde: T es O ó S; R es un alquilo C1-6 de cadena recta o ramificada; Ar es un anillo fenilo opcionalmente sustituido con 1 a 3 grupos seleccionados entre halo, CH3, CF3, CN, OMe, OCF3 y NR5R6; y R5 y R6 son, cada uno en forma independiente, H o alquilo C1-6 de cadena recta o ramificada, o R5 y R6, tomados juntos, forman un anillo de 5 a 7 miembros que opcionalmente contiene hasta 3 heteroátomos seleccionados entre O, S, NH y N(alquilo C1-6 de cadena recta o ramificada).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US39259202P | 2002-06-28 | 2002-06-28 | |
US43507302P | 2002-12-20 | 2002-12-20 |
Publications (1)
Publication Number | Publication Date |
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AR040350A1 true AR040350A1 (es) | 2005-03-30 |
Family
ID=30003264
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030102352A AR040350A1 (es) | 2002-06-28 | 2003-06-27 | Inhibidores de caspasa y usos de los mismos |
Country Status (19)
Country | Link |
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US (2) | US7553852B2 (es) |
EP (1) | EP1539701A1 (es) |
JP (2) | JP4616643B2 (es) |
KR (1) | KR20050013260A (es) |
CN (1) | CN100503572C (es) |
AR (1) | AR040350A1 (es) |
AU (1) | AU2003248758A1 (es) |
BR (1) | BR0312232A (es) |
CA (1) | CA2493646A1 (es) |
IL (1) | IL165986A0 (es) |
MX (1) | MXPA05000069A (es) |
NO (1) | NO20050851L (es) |
NZ (1) | NZ537807A (es) |
PE (1) | PE20040728A1 (es) |
PL (1) | PL374598A1 (es) |
RU (1) | RU2005102094A (es) |
TW (1) | TW200404783A (es) |
UY (1) | UY27872A1 (es) |
WO (1) | WO2004002961A1 (es) |
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2003
- 2003-06-27 CN CNB038187930A patent/CN100503572C/zh not_active Expired - Fee Related
- 2003-06-27 KR KR10-2004-7021300A patent/KR20050013260A/ko not_active Application Discontinuation
- 2003-06-27 AU AU2003248758A patent/AU2003248758A1/en not_active Abandoned
- 2003-06-27 WO PCT/US2003/020557 patent/WO2004002961A1/en active Application Filing
- 2003-06-27 PL PL03374598A patent/PL374598A1/xx not_active Application Discontinuation
- 2003-06-27 CA CA002493646A patent/CA2493646A1/en not_active Abandoned
- 2003-06-27 AR ARP030102352A patent/AR040350A1/es unknown
- 2003-06-27 TW TW092117681A patent/TW200404783A/zh unknown
- 2003-06-27 MX MXPA05000069A patent/MXPA05000069A/es unknown
- 2003-06-27 JP JP2004518103A patent/JP4616643B2/ja not_active Expired - Fee Related
- 2003-06-27 IL IL16598603A patent/IL165986A0/xx unknown
- 2003-06-27 EP EP03762231A patent/EP1539701A1/en not_active Withdrawn
- 2003-06-27 BR BR0312232-8A patent/BR0312232A/pt not_active IP Right Cessation
- 2003-06-27 RU RU2005102094/04A patent/RU2005102094A/ru unknown
- 2003-06-27 PE PE2003000653A patent/PE20040728A1/es not_active Application Discontinuation
- 2003-06-27 NZ NZ537807A patent/NZ537807A/en unknown
- 2003-06-27 US US10/609,147 patent/US7553852B2/en not_active Expired - Fee Related
- 2003-06-30 UY UY27872A patent/UY27872A1/es unknown
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2005
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2009
- 2009-05-12 US US12/464,380 patent/US8129381B2/en not_active Expired - Fee Related
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2010
- 2010-02-04 JP JP2010023632A patent/JP2010143942A/ja active Pending
Also Published As
Publication number | Publication date |
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CN1675184A (zh) | 2005-09-28 |
MXPA05000069A (es) | 2005-04-11 |
PE20040728A1 (es) | 2004-10-23 |
JP4616643B2 (ja) | 2011-01-19 |
UY27872A1 (es) | 2003-12-31 |
WO2004002961A1 (en) | 2004-01-08 |
CN100503572C (zh) | 2009-06-24 |
RU2005102094A (ru) | 2006-02-27 |
US20040072850A1 (en) | 2004-04-15 |
AU2003248758A1 (en) | 2004-01-19 |
CA2493646A1 (en) | 2004-01-08 |
PL374598A1 (en) | 2005-10-31 |
EP1539701A1 (en) | 2005-06-15 |
IL165986A0 (en) | 2006-01-15 |
US20090281128A1 (en) | 2009-11-12 |
US7553852B2 (en) | 2009-06-30 |
KR20050013260A (ko) | 2005-02-03 |
BR0312232A (pt) | 2005-05-10 |
NO20050851L (no) | 2005-03-29 |
TW200404783A (en) | 2004-04-01 |
US8129381B2 (en) | 2012-03-06 |
JP2005533825A (ja) | 2005-11-10 |
JP2010143942A (ja) | 2010-07-01 |
NZ537807A (en) | 2007-05-31 |
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