AR062011A1 - Derivados de diazol y sus composiciones como inhibidores de itpkb - Google Patents

Derivados de diazol y sus composiciones como inhibidores de itpkb

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Publication number
AR062011A1
AR062011A1 ARP070103248A ARP070103248A AR062011A1 AR 062011 A1 AR062011 A1 AR 062011A1 AR P070103248 A ARP070103248 A AR P070103248A AR P070103248 A ARP070103248 A AR P070103248A AR 062011 A1 AR062011 A1 AR 062011A1
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AR
Argentina
Prior art keywords
alkyl
substituted
halogen
hydrogen
independently selected
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ARP070103248A
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English (en)
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Irm Llc
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Publication of AR062011A1 publication Critical patent/AR062011A1/es

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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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Composiciones farmacéuticas que comprenden estos compuestos, y métodos para utilizar tales compuestos con el fin de tratar o prevenir las enfermedades o trastornos asociados con actividades de células B anormales o mal reguladas, en particular enfermedades o trastornos que involucren una activación al errante de la 3-cinasa B de 1,4,5-trifosfato de inositol (ITPKb). Reivindicación 1: Un compuesto de la fórmula (1) en donde: n se selecciona a partir de 0, 1, 2 y 3; m se selecciona a partir de 0, 1, 2 y 3; A puede tener hasta 3 grupos seleccionados a partir de -CR¹=, -CR²=, -CR³=, -CR⁴= y -CR⁵= reemplazados con N; R¹, R², R³, R⁴ y R⁵ se seleccionan independientemente a partir de hidrógeno, hidroxilo, halógeno, ciano, alquilo C₁₋₆, alquilo C₁₋₆ sustituido por halógeno, alquilo C₁₋₆ sustituido por hidroxilo, alquilo C₁₋₆ sustituido por ciano, heterocicloalquilo C₃₋₈-alquilo C₀₋₄, heteroarilo C₁₋₁₀-alquilo C₀₋₄, -XSO₂R¹¹, -XSO₂NR¹¹R¹², -XSO₂NR¹¹C(O)R¹², -XC(NR¹¹)NR¹¹OR¹², -XCR¹¹=NOR¹², -XC(O)R¹¹, -XC(O)OR¹¹, -XNR¹¹R¹², -XC(O)NR¹¹R¹², -XOC(O)NR¹¹R¹², -XNR¹¹C(O)NR¹¹R¹², -XNR¹¹XOR¹², XN(XOR¹²)₂, -XNR¹¹XC(O)OR¹², -XNR¹¹XNR¹¹C(O)R¹², -XNR¹¹XNR¹¹R¹², -XNR¹¹C(O)R¹²; en donde cada X se selecciona independientemente a partir de un enlace y alquileno C₁₋₄; cada R¹¹ se selecciona a partir de hidrógeno y alquilo C₁₋₆; y R¹² se selecciona a partir de hidrógeno, alquilo C₁₋₆, y arilo C₆₋₁₀; o R¹¹ y R¹² junto con el átomo de nitrógeno con el que R¹¹ y R¹² están unidos, forman un heterocicloalquilo C₃₋₈; en donde el heteroarilo o heterocicloalquilo de R¹, R², R³, R⁴ o R⁵ está opcionalmente sustituido con 1 a 3 radicales independientemente seleccionados a partir de halógeno, hidroxilo, ciano, alquilo C₁₋₆, alquilo C₁₋₆ sustituido por halógeno, alquilo C₁₋₆ sustituido por hidroxilo, alquilo C₁₋₆ sustituido por ciano, y carboxilo; R⁶ y R⁷ se seleccionan independientemente a partir de hidrógeno y alquilo C₁₋₃; o R⁶ y R⁷, junto con el átomo de carbono con el que están ambos unidos, forman cicloalquilo C₃₋₇; R⁸ se selecciona a partir de alquilo C₁₋₆, alquilo C₁₋₃ sustituido por halógeno, alcoxilo C₁₋₆, -CH₂OR⁸ᵃ, -COOR⁸ᵃ, y alquenilo C₂₋₆; o dos grupos R⁸ unidos a diferentes átomos de carbono pueden combinarse para formar un puente de alquilo; o dos grupos R⁸ unidos al mismo átomo de carbono pueden formar un grupo cicloalquilo C₃₋₈ o un grupo carbonilo; en donde R⁸ᵃ se selecciona a partir de hidrógeno y alquilo C₁₋₆; R⁹ se selecciona a partir de arilo C₆₋₁₀, y heteroarilo C₁₋₁₀; en donde este arilo o heteroarilo de R⁹ está opcionalmente sustituido con 1 a 3 radicales independientemente seleccionados a partir de halógeno, ciano, hidroxilo, alquilo C₁₋₃, alquilo C₁₋₃ sustituido por halógeno, alquilo C₁₋₃ sustituido por ciano, alquilo C₁₋₃ sustituido por hidroxilo, -C(O)R¹³, -C(O)NR¹³R¹⁴; en donde cada R¹³ y R¹⁴ se seleccionan independientemente a partir de hidrógeno y alquilo C₁₋₆; R¹⁰ se selecciona a partir de hidrógeno, alquilo C₁₋₆, -NR¹⁵R¹⁶, -NR¹⁵C(O)R¹⁶ y -C(O)NR¹⁵R¹⁶; en donde cada R¹⁵ y R¹⁶ se seleccionan independientemente a partir de hidrógeno, alquilo C₁₋₆, arilo C₆₋₁₀, heteroarilo C₁₋₁₀, cicloalquilo C₃₋₁₂, y heterocicloalquilo C₃₋₈; en donde dichos arilo, heteroarilo, cicloalquilo, y heterocicloalquilo pueden estar opcionalmente sustituidos con 1 a 3 radicales independientemente seleccionados a partir de halógeno, hidroxilo, ciano, alquilo C₁₋₆, alquilo C₁₋₆ sustituido por halógeno, alcoxilo C₁₋₆, y alcoxilo C₁₋₆ sustituido por halógeno; Y y Z se seleccionan independientemente a partir de CR²⁰ y N; en donde R²⁰ se selecciona a partir de hidrógeno y alquilo C₁₋₄; y las sales farmacéuticamente aceptables de los mismos; con la condición de que los compuestos de la fórmula (1) no incluyen a los compuestos de la fórmula (2).
ARP070103248A 2006-07-21 2007-07-20 Derivados de diazol y sus composiciones como inhibidores de itpkb AR062011A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83268106P 2006-07-21 2006-07-21
US89387407P 2007-03-08 2007-03-08

Publications (1)

Publication Number Publication Date
AR062011A1 true AR062011A1 (es) 2008-08-10

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ARP070103248A AR062011A1 (es) 2006-07-21 2007-07-20 Derivados de diazol y sus composiciones como inhibidores de itpkb

Country Status (14)

Country Link
US (1) US20090306039A1 (es)
EP (1) EP2057124A2 (es)
JP (1) JP2009544626A (es)
KR (1) KR20090029274A (es)
AR (1) AR062011A1 (es)
AU (1) AU2007275049B2 (es)
BR (1) BRPI0714440A2 (es)
CA (1) CA2656715A1 (es)
CL (1) CL2007002123A1 (es)
MX (1) MX2009000771A (es)
PE (1) PE20080405A1 (es)
RU (1) RU2425826C2 (es)
TW (1) TW200817375A (es)
WO (1) WO2008011611A2 (es)

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WO2008157210A1 (en) 2007-06-15 2008-12-24 Irm Llc Compounds and compositions as itpkb inhibitors
KR20100137557A (ko) * 2008-04-04 2010-12-30 아이알엠 엘엘씨 Ｉｔｐｋｂ 억제제로서의 화합물 및 조성물
BRPI0921496A2 (pt) * 2008-11-04 2016-01-19 Chemocentryx Inc composto, composição farmacêutica, e, métodos para tratar doença ou distúrbio, para inibir ligação de quimiocinas a um receptor, para formar imagem de um dito tumor, orgão ou tecido, e para detectar níveis elevados de cxcr7 em uma amostra
US8853202B2 (en) 2008-11-04 2014-10-07 Chemocentryx, Inc. Modulators of CXCR7
BR102012024778A2 (pt) 2012-09-28 2014-08-19 Cristalia Prod Quimicos Farm Compostos heteroaromáticos; processo para preparar os compostos, composições farmacêuticas, usos e método de tratamento para as dores aguda e crônica
BR112015012366A8 (pt) 2012-11-29 2019-10-01 Chemocentryx Inc antagonistas de cxcr7, uso dos mesmos, composição farmacêutica, bem como métodos para detectar níveis elevados de cxcr7 em uma amostra e para imagear um tumor, órgão, ou tecido
WO2014089364A1 (en) 2012-12-06 2014-06-12 Quanticel Pharmaceuticals, Inc Histone demethylase inhibitors
EP2948447B1 (en) 2013-01-23 2016-09-21 Astrazeneca AB Chemical compounds
MX2016008130A (es) 2013-12-20 2016-10-13 Esteve Labor Dr Derivados de piperidina con actividad multimodal contra el dolor.
DK3186242T3 (da) 2014-08-29 2021-12-20 Tes Pharma S R L Alfa-amino-beta-carboxymuconsyre-semialdehyd-decarboxylasehæmmere
SI3319959T1 (sl) 2015-07-06 2022-02-28 Alkermes, Inc. Hetero-halo inhibitorji histonske deacetilaze
WO2017007755A1 (en) 2015-07-06 2017-01-12 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
KR102526032B1 (ko) 2017-01-11 2023-04-25 로딘 테라퓨틱스, 인크. 히스톤 데아세틸라제의 바이시클릭 억제제
US11225475B2 (en) 2017-08-07 2022-01-18 Alkermes, Inc. Substituted pyridines as inhibitors of histone deacetylase
CN113194956A (zh) 2018-12-12 2021-07-30 凯莫森特里克斯股份有限公司 用于癌症治疗的cxcr7抑制剂

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AU6517196A (en) * 1995-07-13 1997-02-10 Knoll Aktiengesellschaft Piperazine derivatives as therapeutic agents
US6727264B1 (en) * 2001-07-05 2004-04-27 Synaptic Pharmaceutical Corporation Substituted anilinic piperidines as MCH selective antagonists
GB0228417D0 (en) * 2002-12-05 2003-01-08 Cancer Rec Tech Ltd Pyrazole compounds
WO2005019182A1 (en) * 2003-08-20 2005-03-03 Bayer Healthcare Ag Pyrazolylmethylbenzamide derivatives as p2xt-receptor antagonists

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EP2057124A2 (en) 2009-05-13
RU2009105829A (ru) 2010-08-27
CL2007002123A1 (es) 2008-06-13
PE20080405A1 (es) 2008-06-18
WO2008011611A3 (en) 2008-05-02
KR20090029274A (ko) 2009-03-20
JP2009544626A (ja) 2009-12-17
WO2008011611A2 (en) 2008-01-24
US20090306039A1 (en) 2009-12-10
MX2009000771A (es) 2009-01-30
BRPI0714440A2 (pt) 2013-04-24
AU2007275049B2 (en) 2011-03-03
TW200817375A (en) 2008-04-16
CA2656715A1 (en) 2008-01-24
RU2425826C2 (ru) 2011-08-10
AU2007275049A1 (en) 2008-01-24

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