AR055133A1 - Inhibidores de la p38- map - quinasa para el uso de los mismos - Google Patents

Inhibidores de la p38- map - quinasa para el uso de los mismos

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Publication number
AR055133A1
AR055133A1 ARP060103656A ARP060103656A AR055133A1 AR 055133 A1 AR055133 A1 AR 055133A1 AR P060103656 A ARP060103656 A AR P060103656A AR P060103656 A ARP060103656 A AR P060103656A AR 055133 A1 AR055133 A1 AR 055133A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
heteroalkyl
heteroaryl
aryl
Prior art date
Application number
ARP060103656A
Other languages
English (en)
Inventor
Nolan James Dewdney
Tobias Gabriel
Kristen Lynn Mccaleb
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR055133A1 publication Critical patent/AR055133A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P11/16—Central respiratory analeptics
    • 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
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P19/08—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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
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    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Ophthalmology & Optometry (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
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  • Pain & Pain Management (AREA)
  • Hematology (AREA)
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  • Vascular Medicine (AREA)
  • Biotechnology (AREA)

Abstract

Se describen también métodos para la obtencion de los compuestos de interés y métodos para el uso de los compuestos en el tratamiento de las enfermedades mediadas por la p38-MAP-quinasa. Reivindicacion 1: Un compuesto de la formula (1a) (1b), (1c), (1d), (1e), (1f), (1g) o (1h) o una sal farmacéuticamente aceptable del mismo, en las que: R1 esa arilo, heteroarilo, aralquilo o cicloalquilo; R2 es arilo, heteroarilo, cicloalquilo, alquilo ramificado, heterociclilo, hidroxialquilo, cicloalquenilo o hidroxicicloalquilo; R3 es H o alquilo; R4 es H, alquilo, hidroxi, amino, heteroalquilo, heterociclilo, heterociclilalquilo, hidroxicicloalquilo, cicloalquilalquilo, alquilsulfonilo, alquilsulfonamido, arilo, heteroarilo, aralquilo, heteroaralquilo, -(CHRa)r-C(=O)-Rb, -(CHRa) r-O-C(=O)-Rb, -(CHRa)r-NH-C(=O)-Rb o -SO2-Rb, en los que Ra es H, alquilo o heteroalquilo; Rb es alquilo, hidroxi, amino, heteroalquilo, arilo, aralquilo, heteroarilo, o heterociclilo; r es un numero de 0 a 4; R5 es H, -C(=O)-Rc, -(O=)P(ORd)2, -S(=O)2ORd o un mono-, di- o tri-péptido; R6 es -C(=O)-Rc o -(O=)P(ORd)2-, -S(=O)2ORd o un mono-, di- o tri-péptido; en los que Rc es alquilo, alcoxi, amino, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquiloxi, cicloalquilalquiloxi, ariloxi, arilalquiloxi, heteroariloxi, heteroarilalquiloxi, heterociclilo, heterocicliloxi, -(CH2)p-C(=O)-Re, -(CH=CH)-C(=O)-Re, o -CH(NH2)-Rf; en los que Re es H, hidroxi, alcoxi o amino; p es 2 o 3; Rf es H, alquilo, hidroxialquilo, aminoalquilo, fenilo opcionalmente sustituido, bencilo, guanidinilalquilo, carboxialquilo, amidoalquilo, tioalquilo o imidazolalquilo; Rd es H, alquilo, un ion de metal alcalino o un ion de metal alcalinotérreo; X e Y son N, o uno de X e Y es N y el otro es CRg; en el que Rg es H, alquilo, hidroxi, alcoxi, amino, haloalquilo, ciano, halogeno, heteroalquilo, C(=O)-Rh o -SO2-Rh, en los que Rh es H o alquilo; D es -(CR7R8)n-; en el que n es un numero de 1 a 3; R7 y R8 con independencia entre sí son H o alquilo; W es un enlace, O, S(O)q, CH2 o NRi; E es O, S(O)q, CH2 o NRi; en los que q es un numero de 0 a 2; Ri es H, alquilo, heteroalquilo, heterociclilo, hidroxicicloalquilo, -C(=O)- Rj o -SO2-Rj, en los que Rj es alquilo, arilo, aralquilo, heteroarilo, heteroalquilo o heterociclilo; o R4 y Ri junto con los átomos a los que están unidos pueden formar un anillo heterocíclico; A es O, CH2, S(O)s, C(=O), NRk, o CH(ORk), en los que s es un numero de 0 a 2; Rk es H o alquilo; k es el numero 0 o 1; B es O, S(O)j, -(CHRm)t, -NRmSO2-, NRm, NRmC(=O) o C(=O), en los que j es el numero 0, 1 o 2; t es un numero de 1 a 3, y Rm es H o alquilo.
ARP060103656A 2005-08-25 2006-08-23 Inhibidores de la p38- map - quinasa para el uso de los mismos AR055133A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US71200705P 2005-08-25 2005-08-25

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AR055133A1 true AR055133A1 (es) 2007-08-08

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Family Applications (1)

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ARP060103656A AR055133A1 (es) 2005-08-25 2006-08-23 Inhibidores de la p38- map - quinasa para el uso de los mismos

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US (1) US7608603B2 (es)
EP (1) EP1919914A2 (es)
JP (1) JP2009506009A (es)
KR (1) KR20080039438A (es)
CN (1) CN101248077B (es)
AR (1) AR055133A1 (es)
AU (1) AU2006283945A1 (es)
BR (1) BRPI0615272A2 (es)
CA (1) CA2620106A1 (es)
IL (1) IL189382A0 (es)
MX (1) MX2008002590A (es)
TW (1) TW200740816A (es)
WO (1) WO2007023115A2 (es)

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GB2467670B (en) 2007-10-04 2012-08-01 Intellikine Inc Chemical entities and therapeutic uses thereof
JP5547099B2 (ja) 2008-03-14 2014-07-09 インテリカイン， エルエルシー キナーゼ阻害剤および使用方法
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
AU2009268611B2 (en) 2008-07-08 2015-04-09 Intellikine, Llc Kinase inhibitors and methods of use
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
CA2771532C (en) 2009-08-17 2021-03-23 Intellikine, Inc. Heterocyclic compounds and uses thereof
CN106619647A (zh) 2011-02-23 2017-05-10 因特利凯有限责任公司 激酶抑制剂的组合及其用途
JP6360881B2 (ja) 2013-03-22 2018-07-18 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． 触媒的ｍｔｏｒｃ１／２阻害薬及びオーロラａキナーゼの選択的阻害薬の組合せ
CA2965558A1 (en) * 2014-10-30 2016-05-06 Sandoz Ag Synthesis of substituted 1h-pyrazolo[3,4-d]pyrimidines
CN114732910A (zh) 2017-10-05 2022-07-12 弗尔康医疗公司 P38激酶抑制剂降低dux4和下游基因表达以用于治疗fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
JP7431435B2 (ja) 2019-11-14 2024-02-15 国立大学法人大阪大学 新規リゾホスファチジン酸誘導体

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DK1140938T3 (da) * 1999-01-11 2003-12-22 Univ Princeton Højaffinitetsinhibitorer for målvalidering og anvendelser heraf
KR200294211Y1 (ko) 2002-07-26 2002-11-07 김관호 사각지대가 없는 자동차용 사이드 미러
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
KR100843526B1 (ko) * 2004-02-27 2008-07-03 에프. 호프만-라 로슈 아게 피라졸의 접합 유도체
EP1926734A1 (en) * 2005-08-22 2008-06-04 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators

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CA2620106A1 (en) 2007-03-01
AU2006283945A1 (en) 2007-03-01
US7608603B2 (en) 2009-10-27
WO2007023115A3 (en) 2007-04-12
KR20080039438A (ko) 2008-05-07
MX2008002590A (es) 2008-03-18
TW200740816A (en) 2007-11-01
US20070049597A1 (en) 2007-03-01
JP2009506009A (ja) 2009-02-12
BRPI0615272A2 (pt) 2009-08-04
EP1919914A2 (en) 2008-05-14
CN101248077A (zh) 2008-08-20
CN101248077B (zh) 2011-07-20
IL189382A0 (en) 2008-06-05
WO2007023115A2 (en) 2007-03-01

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