[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

    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic 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
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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
    • C07D471/14—Ortho-condensed systems
    • 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
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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 Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (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 (61)

* 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
JP5869222B2 (ja) 2008-01-04 2016-02-24 インテリカイン， エルエルシー 特定の化学的実体、組成物および方法
JP2012528165A (ja) 2009-05-26 2012-11-12 エクセリクシス， インク． ＰＩ３Ｋ／ｍＴＯＲの阻害剤としてのベンゾキサゼピンならびにそれらの使用および製造方法
US8765940B2 (en) * 2009-06-25 2014-07-01 Amgen Inc. Heterocyclic compounds and their uses
CA2812089C (en) 2010-09-14 2020-02-18 Exelixis Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
NZ608069A (en) 2010-10-06 2014-06-27 Glaxosmithkline Llc Benzimidazole derivatives as pi3 kinase inhibitors
DE102010049595A1 (de) * 2010-10-26 2012-04-26 Merck Patent Gmbh Chinazolinderivate
WO2012068096A2 (en) * 2010-11-15 2012-05-24 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
EP2640367A2 (en) * 2010-11-15 2013-09-25 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
EP2643319A1 (en) * 2010-11-24 2013-10-02 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
US20140107100A1 (en) * 2010-11-24 2014-04-17 Exelixis, Inc. Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
US20140073628A1 (en) * 2010-11-24 2014-03-13 Kenneth D. Rice Benzoxazepines asn inhibitors of p13k/m tor and methods of their use and manufacture
BR112013012961A2 (pt) * 2010-11-24 2019-09-24 Exelixis Inc benzoxazepinas como inhibidores de mtor e métodos de seu uso e fabricação
MX347708B (es) 2011-01-10 2017-05-09 Infinity Pharmaceuticals Inc Proceso para preparar isoquinolinonas y formas solidas de isoquinolinonas.
WO2012126901A1 (en) * 2011-03-21 2012-09-27 F. Hoffmann-La Roche Ag Benzoxazepin compounds selective for pi3k p110 delta and methods of use
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
US9226923B2 (en) * 2011-07-27 2016-01-05 Nanjing Allgen Pharma Co. Ltd. Spirocyclic molecules as protein kinase inhibitors
PH12014500973A1 (en) 2011-11-01 2014-06-16 Exelixis Inc Phosphatidylinositol 3-kinase inhibitors for the treatment of lymphoproliferative malignancies
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
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
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
CA2878442A1 (en) 2012-09-25 2014-04-03 F. Hoffmann-La Roche Ag Hexahydropyrrolo[3,4-c]pyrrole derivatives and related compounds as autotaxin (atx) inhibitors and as inhibitors of the lysophosphatidic acid (lpa) production for treating e.g. renal diseases
RU2702908C2 (ru) 2012-11-01 2019-10-14 Инфинити Фармасьютикалз, Инк. Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
PE20160845A1 (es) 2013-11-26 2016-09-10 Hoffmann La Roche Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo
AP2016009368A0 (en) 2014-01-14 2016-08-31 Millennium Pharm Inc Heteroaryls and uses thereof
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
HUE046820T2 (hu) 2014-03-26 2020-03-30 Hoffmann La Roche Biciklusos vegyületek autotaxin (ATX) és lizofoszfatidsav (LPA) termelésgátlókként
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
MX377277B (es) 2015-09-04 2025-03-07 Hoffmann La Roche Derivados de fenoximetilo.
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
MA42923A (fr) 2015-09-24 2021-04-28 Hoffmann La Roche Composés bicycliques comme inhibiteurs mixtes de atx/ca
BR112018006034A2 (pt) 2015-09-24 2018-10-09 Hoffmann La Roche compostos bicíclicos como inibidores de atx
RU2725138C2 (ru) 2015-09-24 2020-06-30 Ф. Хоффманн-Ля Рош Аг Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca)
MX391135B (es) 2016-06-24 2025-03-21 Infinity Pharmaceuticals Inc Terapias de combinacion.
KR20190091455A (ko) * 2016-12-15 2019-08-06 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Nrf2 화합물
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
ES2747768T3 (es) 2017-03-20 2020-03-11 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)
JP2021510733A (ja) 2018-01-12 2021-04-30 ケーディーエーシー セラピューティクス，インコーポレーテッドＫｄａｃ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ
SG11202007198WA (en) 2018-01-31 2020-08-28 Deciphera Pharmaceuticals Llc Combination therapy for the treatment of gastrointestinal stromal tumors
KR102708050B1 (ko) 2018-01-31 2024-09-24 데시페라 파마슈티칼스, 엘엘씨. 비만 세포증의 치료를 위한 병용 요법
WO2020061255A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
EP3938363A1 (en) 2019-03-11 2022-01-19 Teva Pharmaceuticals International GmbH Solid state forms of ripretinib
WO2021030405A1 (en) 2019-08-12 2021-02-18 Deciphera Pharmaceuticals, Llc Ripretinib for treating gastrointestinal stromal tumors
CN114615982A (zh) 2019-08-12 2022-06-10 德西费拉制药有限责任公司 用于治疗胃肠道间质瘤的瑞普替尼
US20220378756A1 (en) 2019-09-19 2022-12-01 Forma Therapeutics, Inc. Activating pyruvate kinase r
MX2022008103A (es) 2019-12-30 2022-09-19 Deciphera Pharmaceuticals Llc Formulaciones de inhibidores de la cinasa amorfa y metodos de estas.
CN118948772A (zh) 2019-12-30 2024-11-15 德西费拉制药有限责任公司 1-(4溴-5-(1乙基-7-(甲氨基)-2侧氧基-1,2-二氢-1,6-萘啶-3基)-2氟苯基)-3-苯基脲的组合物
CA3179378A1 (en) 2020-04-07 2021-10-14 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
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
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
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors
CN120500335A (zh) * 2022-12-28 2025-08-15 瑞瑟沃神经科学公司 Ep2拮抗剂化合物

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
CN1209063A (zh) 1995-12-29 1999-02-24 史密丝克莱恩比彻姆公司 玻连蛋白受体拮抗剂
BR9612378A (pt) 1995-12-29 1999-07-13 Smithkline Beecham Corp Antagonistas receptores de vitronectina
SE9701681D0 (sv) * 1997-05-05 1997-05-05 Astra Ab New compounds
EP1150965A4 (en) 1999-02-03 2002-05-15 Merck & Co Inc BENZAZEPINE DERIVATIVES AS ALPHA-V INTGRIN RECEPTOR ANTAGONISTS
BR0013610A (pt) 1999-08-27 2002-07-16 Procter & Gamble Componentes de formulções de ação rápida,composições e métodos para lavar roupa empregando os mesmos
BR0013608A (pt) 1999-08-27 2002-05-21 Procter & Gamble Disponibilidade controlada de componentes de formulações, composições e métodos para lavar roupa empregando os mesmos
CN1384868A (zh) 1999-08-27 2002-12-11 宝洁公司 稳定的配制组分、使用该组分的组合物和洗衣方法
MXPA02002124A (es) 1999-08-27 2002-09-18 Procter & Gamble Componentes de formulacion de incremento de estabilidad y composiciones y metodos de lavanderia que emplean los mismos.
US6677341B2 (en) 1999-09-23 2004-01-13 Pharmacia Corporation (R)-Chiral halogenated substituted heteroaryl benzyl 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
WO2003059898A2 (en) 2002-01-08 2003-07-24 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
PT2444079T (pt) 2005-05-17 2017-03-03 Sarcode Bioscience Inc Composições e métodos para tratamento de distúrbios dos olhos
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
US20080234300A1 (en) 2007-03-05 2008-09-25 Wyeth Pyrimido[5,4-c] Quinoline-2, 4-Diamine Derivatives and Methods of Use Thereof
JP5497429B2 (ja) 2007-03-07 2014-05-21 武田薬品工業株式会社 ベンゾオキサゼピン誘導体およびその用途
US20080221093A1 (en) 2007-03-07 2008-09-11 Christian Gege Metalloprotease inhibitors containing a heterocyclic moiety
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
EP2205085A1 (en) * 2007-09-25 2010-07-14 Merck Sharp & Dohme Corp. 2-aryl or heteroaryl indole derivatives
WO2009076631A1 (en) 2007-12-12 2009-06-18 Rigel Pharmaceuticals, Inc. Carboxamide, sulfonamide and amine compounds for metabolic disorders
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
JP2012528165A (ja) 2009-05-26 2012-11-12 エクセリクシス， インク． ＰＩ３Ｋ／ｍＴＯＲの阻害剤としてのベンゾキサゼピンならびにそれらの使用および製造方法

Also Published As

Publication number Publication date
BRPI1010974A2 (pt) 2019-09-24
CN102459249A (zh) 2012-05-16
US20100298290A1 (en) 2010-11-25
EP2432779A1 (en) 2012-03-28
CA2763099A1 (en) 2010-11-25
IL216472A0 (en) 2012-01-31
US8648066B2 (en) 2014-02-11
MX2011012345A (es) 2012-01-31
TW201111371A (en) 2011-04-01
JP2012527474A (ja) 2012-11-08
AU2010249790A1 (en) 2011-12-08
WO2010135524A8 (en) 2012-01-12
KR20120034666A (ko) 2012-04-12
WO2010135524A1 (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
AR108388A2 (es) Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasas
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
AR080865A1 (es) Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer.
NI201400023A (es) Derivados de pirrolopirimidina y purina
CR20140091A (es) Nuevos derivados dihidroquinolina-2-ona
AR080785A1 (es) Derivados de imidazo[1,2-a]pirimidina ,proceso para prepararlos e intermediarios de dicha sintesis, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de patologias del sistema nervioso central,tales como esquizofrenia y parkinson, entre otros.
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.
PE20142081A1 (es) Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos
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
RU2015121431A (ru) Замещенные производные индол-5-ола и их терапевтическое применение
AR079342A1 (es) Derivados de azol y metodos para producirlos, compuestos intermediarios para los derivados y metodos para producirlos, asi como tambien agentes agrohorticolas y agentes protectores de materiales industriales que contienen los derivados
AR079224A1 (es) Compuestos insecticidas basados en derivados de isoxazolina
AR060590A1 (es) Compuestos imidazo
AR069364A1 (es) Derivados heterociclicos que modulan la miosina del musculo liso y/o la miosina no muscular y composiciones farmaceuticas que los contienen
AR083200A1 (es) Compuestos de n-heteroarilo

Legal Events

Date Code Title Description
FA Abandonment or withdrawal