Nothing Special   »   [go: up one dir, main page]

AR076694A1 - Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion - Google Patents

Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion

Info

Publication number
AR076694A1
AR076694A1 ARP100101771A ARP100101771A AR076694A1 AR 076694 A1 AR076694 A1 AR 076694A1 AR P100101771 A ARP100101771 A AR P100101771A AR P100101771 A ARP100101771 A AR P100101771A AR 076694 A1 AR076694 A1 AR 076694A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
hydroxyalkyl
haloalkyl
independently
Prior art date
Application number
ARP100101771A
Other languages
English (en)
Inventor
Tsze H Tsang
Charles M Blazey
Cristina A Zaharia
Owen Joseph Bowles
Amy L Tsuhako
Joerg Bussenius
Chris Allen Buhr
Jason R Harris
Angie Inyoung Kim
Anagha Joshi
Stephanie Ng
Csaba J Peto
Neel Kumar Anand
Kenneth D Rice
Steven Charles Defina
Larisa Dubenko
Sunghoon Ma
Jeffry Kimo Curtis
Eileen Jackson-Ugueto
Jean-Claire Limun Manalo
Original Assignee
Exelixis Inc
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 Exelixis Inc filed Critical Exelixis Inc
Publication of AR076694A1 publication Critical patent/AR076694A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se preveen composiciones farmacéuticas que comprenden métodos para preparar y uso de los compuestos en el tratamiento del cáncer. Reivindicacion 1: Un compuesto de la formula 1: o uno de sus estereoisomeros individuales o una mezcla de estereoisomeros y además, opcionalmente como una de sus sales farmacéuticamente aceptables, en donde R1es fenilo opcionalmente sustituido con uno, dos o tres grupos R6 o R1 es heteroarilo opcionalmente sustituido con uno, dos o tres R7 R2 es heteroarilo sustituido con R3, R3a, R3b, R3c y R3d; R3, R3a, R3b, R3c y R3d son, de modo independiente, hidrogeno, ciano, alquilo, alquenilo, halo, haloalquilo, hidroxialquilo, alcoxialquilo, cianoalquilo, -SR12, -S(O) 2R20, -C(O)OR4, halocarbonilo, -NR11R11a, -OR11a fenilo opcionalmente sustituido, fenilalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido o alquilo sustituido con uno o dos R16 o dos de R3, R3a, R3b, R3c y R3d cuando se unen con el mismo carbono, forman un cicloalquilo opcionalmente sustituido o un heterocicloalquilo opcionalmente sustituido; y el otro de R3, R3a, R3b, R3c y R3d son, de modo independiente, hidrogeno, ciano, alquilo, alquenilo, halo, haloalquilo, hidroxialquilo, alcoxialquilo, cianoalquilo, -SR12, -S(O)2R20, -C(O)OR4, halocarbonilo, -NR11R11a, -OR11a, fenilo opcionalmente sustituido, fenilalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, heteroarilo opcionalmente, heteroarilalquilo opcionalmente sustituido o alquilo sustituido con uno o dos R16 R4 es alquilo, alquenilo, alquinilo, hidroxialquilo, alcoxialquilo, haloalquilo, bencilo o heterocicloalquilalquilo opcionalmente sustituido; R5a y R5c son, de modo independiente, hidrogeno o alquilo; R5h es hidrogeno o halo; R5b es hidrogeno, amino o halo; R5d, R5e, R5f y R5g son hidrogeno; cada R6, cuando R6 está presente, es, de modo independiente, nitro; ciano; halo; alquilo; alquenilo; alquinilo; haloalquilo; -OR8a; -NR8R8a; -C(O)NR8R8a; - S(O)2R8, -NR8C(O)OR9, -NR8C(O)R9, -NR8S(O)2R8a;. -NR8C(O)NR8aR9 carboxi, -C(O)OR9 halocarbonilo; alquilcarbonilo; alquilo sustituido con uno o dos -C(O)NR8R8a; heteroarilo opcionalmente sustituido con 1, 2 o 3 R14; o heterocicloalquilo opcionalmente sustituido; cada R7, cuando R7 está presente, es, de modo independiente, oxo; nitro; ciano; alquilo; alquenilo; alquinilo; halo; haloalquilo; hidroxialquilo; alcoxialquilo; -OR8a; -SR13 -S(O)R13a, -S(O)2R13a; -NR8R8a; -C(O)NR8R8a, -NR8C(O)OR9, -NR8C(O)R9; -NR8S(O)2R8a; -NR8C(O)NR8aR9, -C(O)OR9 halocarbonilo; alquilcarbonilo; -S(O)2NR8R9 alquilsulfonilalquilo; alquilo sustituido con uno o dos -NR8R8a; alquilo sustituido con uno o dos -NR8C(O)R8a; alquilo sustituido, con uno o dos -NR8C(O)OR9 alquilo sustituido con uno o dos -S(O)2R13a; cicloalquilo opcionalmente sustituido; cicloalquilalquilo opcionalmente sustituido; heterocicloalquilo opcionalmente sustituido; heterocicloalquilalquilo opcionalmente sustituido; fenilo opcionalmente sustituido; fenilalquilo opcionalmente sustituido; heteroarilo opcionalmente sustituido; o heteroarilalquilo opcionalmente sustituido; cada R8, R11, R15, R17 y R18 es, de modo independiente, hidrogeno, alquilo, alquenilo, alquinilo, hidroxialquilo, alcoxialquilo o haloalquilo; cada R8a, R11a , R15a es, de modo independiente, hidrogeno, alquilo, alquenilo, alquinilo, haloalquilo, hidroxialquilo, cianoalquilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, alcoxialquilo, carboxialquilo, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, fenilo opcionalmente sustituido, fenilalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heteroarilalquilo opcionalmente sustituido; R9 es hidrogeno; alquilo; alquenilo; alquinilo; hidroxialquilo; alcoxialquilo; aminoalquilo; alquilaminoalquilo; dialquilaminoalquilo; haloalquilo; hidroxialquilo sustituido con uno, dos o tres grupos que son, de modo independiente, halo, amino, alquilamino o dialquilamino; alquilo sustituido con uno o dos aminocarbonilo; fenilo opcionalmente sustituido; fenilalquilo opcionalmente sustituido; cicloalquilo opcionalmente sustituido; cicloalquilalquilo opcionalmente sustituido; heteroarilo opcionalmente sustituido; heteroarilalquilo opcionalmente sustituido; heterocicloalquilo opcionalmente sustituido; o heterocicloalquilalquilo opcionalmente sustituido; R12 es alquilo o fenilalquilo opcionalmente sustituido; R13 es alquilo, hidroxialquilo o haloalquilo; y R13a es hidroxi, alquilo, haloalquilo, hidroxialquilo o heterocicloalquilo opcionalmente sustituido con uno o dos grupos que son, de modo independiente, halo, amino, alquilamino, dialquilamino, hidroxi, alquilo o hidroxialquilo; cada R14, cuando R14 está presente, es, de modo independiente, amino, alquilamino, dialquilamino, acilamino, halo, hidroxi, alquilo, haloalquilo, hidroxialquilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, alcoxicarbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo o fenilo opcionalmente sustituido; cada R16 es, de modo independiente, -NR11R12a, -NR15S(O)R15a, -OC(O)R17 u -OR18 y R20 es alquilo, haloalquilo, hidroxialquilo, amino, alquilamino, dialquilamino o heterocicloalquilo.
ARP100101771A 2009-05-22 2010-05-21 Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion AR076694A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US21698009P 2009-05-22 2009-05-22

Publications (1)

Publication Number Publication Date
AR076694A1 true AR076694A1 (es) 2011-06-29

Family

ID=42556812

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101771A AR076694A1 (es) 2009-05-22 2010-05-21 Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion

Country Status (13)

Country Link
US (1) US8648066B2 (es)
EP (1) EP2432779A1 (es)
JP (1) JP2012527474A (es)
KR (1) KR20120034666A (es)
CN (1) CN102459249A (es)
AR (1) AR076694A1 (es)
AU (1) AU2010249790A1 (es)
BR (1) BRPI1010974A2 (es)
CA (1) CA2763099A1 (es)
IL (1) IL216472A0 (es)
MX (1) MX2011012345A (es)
TW (1) TW201111371A (es)
WO (1) WO2010135524A1 (es)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
NZ717410A (en) 2008-01-04 2017-07-28 Intellikine Llc Heterocyclic containing entities, compositions and methods
US8637499B2 (en) 2009-05-26 2014-01-28 Exelixis, Inc. Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture
US8765940B2 (en) * 2009-06-25 2014-07-01 Amgen Inc. Heterocyclic compounds and their uses
ES2693257T3 (es) 2010-09-14 2018-12-10 Exelixis, Inc. Inhibidores de PI3K-delta y métodos para su uso y fabricación
ME02663B (me) 2010-10-06 2017-06-20 Glaxosmithkline Llc Derivati benzimidazola kao inhibitori pi3 kinaze
DE102010049595A1 (de) * 2010-10-26 2012-04-26 Merck Patent Gmbh Chinazolinderivate
US20140066431A1 (en) * 2010-11-15 2014-03-06 Exelixis, Inc. Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
WO2012068096A2 (en) * 2010-11-15 2012-05-24 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
MX2013005826A (es) * 2010-11-24 2013-08-27 Exelixis Inc Benzoxazepinas como inhibidores de fosfatidilinositol 3-cinasa/objetivo de rapamicina en mamiferos (p13k/mtor) y metodos de uso y fabricacion.
JP2013544826A (ja) * 2010-11-24 2013-12-19 エクセリクシス, インク. PI3K/mTORの阻害剤としてのベンゾオキサゼピン類ならびにそれらの使用法および製造法
US20140005172A1 (en) * 2010-11-24 2014-01-02 Elelixis, Inc. Benzoxazepines as Inhibitors of PI3K/M TOR and Methods of Their Use and Manufacture
CN103328485A (zh) * 2010-11-24 2013-09-25 埃克塞里艾克西斯公司 作为mTOR抑制剂的苯并氧氮杂卓及其使用和生产方法
AR084824A1 (es) 2011-01-10 2013-06-26 Intellikine Inc Procesos para preparar isoquinolinonas y formas solidas de isoquinolinonas
KR20140032383A (ko) * 2011-03-21 2014-03-14 에프. 호프만-라 로슈 아게 Pi3k p110 델타에 대하여 선택적인 벤즈옥사제핀 화합물 및 이의 사용 방법
JP6240063B2 (ja) * 2011-04-28 2017-11-29 ザ ブロード インスティテュート, インコーポレイテッド ヒストンデアセチラーゼ阻害剤
CN103732588B (zh) * 2011-07-27 2016-10-12 南京奥昭生物科技有限公司 螺环分子作为蛋白激酶抑制剂
EA201490905A1 (ru) 2011-11-01 2014-11-28 Экселиксис, Инк. N-(3-{[(3-{[2-хлор-5-(метокси)фенил]амино}хиноксалин-2-ил)амино]сульфонил}фенил)-2-метилаланинамид как ингибитор фосфатидилинозитол-3-киназы для лечения лимфопролиферативных злокачественных заболеваний
JP5949070B2 (ja) * 2012-04-03 2016-07-06 Jsr株式会社 液晶配向剤、液晶配向膜及び液晶表示素子
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
NZ702334A (en) * 2012-06-13 2016-11-25 Hoffmann La Roche New diazaspirocycloalkane and azaspirocycloalkane
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
CA2880117C (en) 2012-07-27 2021-04-06 The Broad Institute, Inc. Inhibitors of histone deacetylase
UA116547C2 (uk) 2012-09-25 2018-04-10 Ф. Хоффманн-Ля Рош Аг Біциклічні похідні
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
PL3074400T3 (pl) 2013-11-26 2018-03-30 F.Hoffmann-La Roche Ag Pochodne oktahydrocyklobuta[1,2-c;3,4-c']dipirolu jako inhibitory autotaksyny
MX2016009135A (es) 2014-01-14 2016-10-05 Millennium Pharm Inc Heteroarilos y usos de estos.
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
DK3122750T3 (da) 2014-03-26 2019-11-04 Hoffmann La Roche Bicykliske forbindelser som autotaxin (ATX)- og lysofosfatidsyre (LPA)-produktionshæmmere
PE20161223A1 (es) 2014-03-26 2016-11-12 Hoffmann La Roche Compuestos condensados de [1,4]diazepina como inhibidores de la produccion de autotaxina (atx) y acido lisofosfatidico (lpa)
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CN104910158B (zh) * 2015-06-15 2017-04-12 河南师范大学 具有生物活性的5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶化合物及其制备方法和应用
PE20180479A1 (es) 2015-09-04 2018-03-07 Hoffmann La Roche Nuevos derivados de fenoximetilo
MX2018001890A (es) 2015-09-24 2018-06-20 Hoffmann La Roche Compuestos biciclicos como inhibidores de autotaxina (atx).
JP6846414B2 (ja) 2015-09-24 2021-03-24 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Atx阻害剤としての二環式化合物
JP6845230B2 (ja) 2015-09-24 2021-03-17 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft デュアルatx/ca阻害剤としての新規な二環式化合物
EP3353178B1 (en) 2015-09-24 2021-07-14 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
US11147818B2 (en) 2016-06-24 2021-10-19 Infinity Pharmaceuticals, Inc. Combination therapies
EP3555104B1 (en) * 2016-12-15 2021-11-24 GlaxoSmithKline Intellectual Property Development Limited Nrf2 compounds
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ.ホフマン-ラ ロシュ アーゲー Atxインヒビターとしての新規二環式化合物
CR20190423A (es) 2017-03-16 2019-11-01 Hoffmann La Roche Nuevos compuestos biciclícos como inhibidores dobles de atx/ca
RU2707751C1 (ru) 2017-03-20 2019-11-29 Форма Терапьютикс, Инк. Пирролопирроловые композиции в качестве активаторов пируваткиназы (pkr)
US12128018B2 (en) 2018-01-12 2024-10-29 KDAc Therapeutics, Inc. Combination of a selective histone deacetylase 3 (HDAC3) inhibitor and an immunotherapy agent for the treatment of cancer
CA3089566A1 (en) 2018-01-31 2019-08-08 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of gastrointestinal stromal tumors
WO2019152719A1 (en) 2018-01-31 2019-08-08 Deciphera Pharmaceuticals, Llc Combination therapy for the treatment of mastocytosis
CN113166060B (zh) 2018-09-19 2024-01-09 诺沃挪第克健康护理股份公司 用丙酮酸激酶激活化合物治疗镰状细胞病
CN113226356A (zh) 2018-09-19 2021-08-06 福马治疗股份有限公司 活化丙酮酸激酶r
WO2021030405A1 (en) 2019-08-12 2021-02-18 Deciphera Pharmaceuticals, Llc Ripretinib for treating gastrointestinal stromal tumors
AU2020329956B2 (en) 2019-08-12 2023-11-16 Deciphera Pharmaceuticals, Llc. Ripretinib for treating gastrointestinal stromal tumors
IL293864A (en) 2019-12-30 2022-08-01 Deciphera Pharmaceuticals Llc Preparations of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3- phenylurea
HRP20231699T1 (hr) 2019-12-30 2024-05-10 Deciphera Pharmaceuticals, Llc Formulacije inhibitora amorfne kinaze i postupci njihove primjene
AU2021251341A1 (en) 2020-04-07 2022-11-03 Bayer Aktiengesellschaft Substituted thiazolopyridines, salts thereof and their use as herbicidally active substances
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
TW202328151A (zh) 2021-09-07 2023-07-16 德商拜耳廠股份有限公司 經取代之2,3-二氫[1,3]噻唑并[4,5-b]吡啶、其鹽及其作為除草活性物質之用途
TW202328150A (zh) 2021-09-07 2023-07-16 德商拜耳廠股份有限公司 經取代之噻唑并吡啶、其鹽及其作為除草活性物質之用途
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors
WO2024145259A2 (en) * 2022-12-28 2024-07-04 Reservoir Neuroscience, Inc. Ep2 antagonist compounds

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4102103A1 (de) 1991-01-25 1992-08-20 Bayer Ag Substituierte benzoxazepine und benzthiazepine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
US5272158A (en) 1991-10-29 1993-12-21 Merck & Co., Inc. Fibrinogen receptor antagonists
KR19990076876A (ko) 1995-12-29 1999-10-25 스티븐 베네티아너 비트로넥틴 수용체 길항제
CZ203898A3 (cs) 1995-12-29 1999-03-17 Smithkline Beecham Corporation Antagonista vitronektinového receptoru, farmaceutický přípravek s jeho obsahem, způsob a použití
SE9701681D0 (sv) * 1997-05-05 1997-05-05 Astra Ab New compounds
AU747503B2 (en) 1999-02-03 2002-05-16 Merck & Co., Inc. Benzazepine derivatives as alpha-V integrin receptor antagonists
JP2003508581A (ja) 1999-08-27 2003-03-04 ザ、プロクター、エンド、ギャンブル、カンパニー 処方成分の制御された有効化法、それを使用する組成物および洗濯方法
CN1384867A (zh) 1999-08-27 2002-12-11 宝洁公司 稳定性提高的配制组分、使用该组分的组合物和洗衣方法
JP2003508586A (ja) 1999-08-27 2003-03-04 ザ、プロクター、エンド、ギャンブル、カンパニー 迅速に作用する処方成分、それらの成分を使用する組成物および洗濯方法
MXPA02002128A (es) 1999-08-27 2002-09-02 Procter & Gamble Componentes para formulacion estable, composiciones y metodos para lavanderia que los emplean.
US6723752B2 (en) * 1999-09-23 2004-04-20 Pharmacia Corporation (R)-chiral halogenated substituted n-benzyl-n-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
US20030114448A1 (en) 2001-05-31 2003-06-19 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
AU2003219652A1 (en) 2002-01-08 2003-07-30 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
US7196108B2 (en) 2002-03-08 2007-03-27 Incyte San Diego Inc. Bicyclic heterocycles for the treatment of diabetes and other diseases
CL2004000409A1 (es) * 2003-03-03 2005-01-07 Vertex Pharma Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu
US7521457B2 (en) * 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
HUE031979T2 (en) 2005-05-17 2017-08-28 Sarcode Bioscience Inc Preparations and methods for treating eye disorders
CN101258136A (zh) * 2005-07-05 2008-09-03 阿斯利康(瑞典)有限公司 新化合物、其制备方法、中间体、药物组合物和其在治疗5-ht6介导的疾病例如阿尔茨海默病、认知障碍、精神分裂症相关的认知缺损、肥胖和帕金森病中的用途
WO2008109599A1 (en) * 2007-03-05 2008-09-12 Wyeth Pyrimido [5,4-c] quinoline-2, 4-diamine derivatives and methods of use thereof
CA2680312A1 (en) * 2007-03-07 2008-09-12 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors containing a heterocyclic moiety
WO2008108445A1 (ja) * 2007-03-07 2008-09-12 Takeda Pharmaceutical Company Limited ベンゾオキサゼピン誘導体およびその用途
WO2008144483A2 (en) 2007-05-18 2008-11-27 Armgo Pharma, Inc. Agents for treating disorders involving modulation of ryanodine receptors
US20110263569A1 (en) 2007-08-22 2011-10-27 President And Fellows Of Harvard College Ryanodine channel binders and uses thereof
US20100197657A1 (en) * 2007-09-25 2010-08-05 Chang Ronald K 2-aryl or heteroaryl indole derivatives
JP5650540B2 (ja) 2007-12-12 2015-01-07 ライジェル ファーマシューティカルズ, インコーポレイテッド 代謝障害のためのカルボキサミド、スルホンアミド、およびアミン化合物
CN101497612A (zh) 2009-03-03 2009-08-05 北京华禧联合科技发展有限公司 一类新喹诺酮类化合物及其制备与用途
US8637499B2 (en) * 2009-05-26 2014-01-28 Exelixis, Inc. Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture

Also Published As

Publication number Publication date
CN102459249A (zh) 2012-05-16
WO2010135524A1 (en) 2010-11-25
TW201111371A (en) 2011-04-01
WO2010135524A8 (en) 2012-01-12
US20100298290A1 (en) 2010-11-25
JP2012527474A (ja) 2012-11-08
US8648066B2 (en) 2014-02-11
KR20120034666A (ko) 2012-04-12
BRPI1010974A2 (pt) 2019-09-24
IL216472A0 (en) 2012-01-31
MX2011012345A (es) 2012-01-31
EP2432779A1 (en) 2012-03-28
AU2010249790A1 (en) 2011-12-08
CA2763099A1 (en) 2010-11-25

Similar Documents

Publication Publication Date Title
AR076694A1 (es) Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion
AR076271A1 (es) Inhibidores de mtor, composiciones farmaceuticas, metodo de fabricacion y su uso en el tratamiento de cancer
AR076922A1 (es) Benzodiazepinas como inhibidores de pi3k/mtor, una composicion farmaceutica que las comprende, metodos para su fabricacion y su uso en el tratamiento del cancer.
AR083953A1 (es) Compuestos para tratar enfermedades neurodegenerativas
AR083199A1 (es) Compuestos de n-heteroarilo con unidad de puente ciclico
AR084849A1 (es) Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
AR092108A1 (es) Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn
AR083169A1 (es) Compuestos para tratar enfermedades neurodegenerativas
NI201400023A (es) Derivados de pirrolopirimidina y purina
AR077328A1 (es) Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
CR20140091A (es) Nuevos derivados dihidroquinolina-2-ona
AR072906A1 (es) Nucleosidos modificados utiles como antivirales
AR063912A1 (es) Derivados de 1,2,4 oxadiazol. composiciones farmaceuticas.
CO6140024A2 (es) Uso de compuestos inhibidores de quinaxolina de pi3k-alfa para el tratamiento del cancer
AR067757A1 (es) Derivados de imidazo[4,5-c]piridin-2-ona, composiciones farmaceuticas que los contienen, procedimiento para su preparacion y uso de los mismos como agentes antivirales.
AR081075A1 (es) Derivados de imidazo[1,2-c]pirimidina, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias.
AR086972A1 (es) Procesos para preparar compuestos heterociclicos, que incluyen trans-7-oxo-6-(sulfooxi)-1,6-diazabiciclo[3,2,1]octano-2-carboxamida y sales de la misma
ES2531274T3 (es) Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas
RU2015121431A (ru) Замещенные производные индол-5-ола и их терапевтическое применение
AR079224A1 (es) Compuestos insecticidas basados en derivados de isoxazolina
AR066153A1 (es) Derivados de piperidina / piperazina
AR089776A1 (es) 5,8-dihidro-6h-pirazolo[3,4-h]quinazolinas como inhibidores de igf-1r/ir
AR079553A1 (es) Derivados de diaza-espiro-[5,5]-undecanos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de trastornos del snc, tales como trastornos del sueno y de la dependencia,entre otros.
AR069364A1 (es) Derivados heterociclicos que modulan la miosina del musculo liso y/o la miosina no muscular y composiciones farmaceuticas que los contienen
UY35845A (es) ?derivados de purina?.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal