AR080151A1 - Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia - Google Patents
Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagiaInfo
- Publication number
- AR080151A1 AR080151A1 ARP110100408A ARP110100408A AR080151A1 AR 080151 A1 AR080151 A1 AR 080151A1 AR P110100408 A ARP110100408 A AR P110100408A AR P110100408 A ARP110100408 A AR P110100408A AR 080151 A1 AR080151 A1 AR 080151A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- cancer
- alkyl
- optionally
- heteroaryl
- Prior art date
Links
Classifications
-
- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicacion 1: Método para tratar el cáncer, comprendiendo dicho método administrar a un paciente una cantidad terapéuticamente eficaz de un Compuesto de Formula 1: o un isomero sencillo del mismo en el que el compuesto está opcionalmente en forma de una sal farmacéuticamente aceptable y además opcionalmente en forma de un hidrato y además opcionalmente en forma de un solvato del mismo; o administrar una composicion farmacéutica que comprende una cantidad terapéuticamente eficaz de un Compuesto de Formula 1 y un vehículo, excipiente o diluyente farmacéuticamente aceptable junto con uno o más inhibidores autofágicos, en los que en el Compuesto de Formula 1: R1 es hidrogeno, alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, arilo opcionalmente sustituido, arilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heteroarilalquilo opcionalmente sustituido; R2 es hidrogeno o alquilo, en el que el alquilo está opcionalmente sustituido con 1,2,3,465 grupos R8 X es -NR3-; 25 R3 hidrogeno; R4 es alquilo opcionalmente sustituido; R5 es hidrogeno; y R6 es fenilo, acilo o heteroarilo en los que el fenilo y el heteroarilo están opcionalmente sustituidos con 1, 2, 3, 4 o 5 grupos R9 cada R8, cuando está presente, es independientemente hidroxi, halo, alcoxi, haloalcoxi, amino, alquilamino, dialquilaminoalquilo o alcoxialquilamino; y cada R9, cuando está presente, es independientemente halo, alquilo, haloalquilo, alcoxi, haloalcoxi, ciano, amino, alquilamino, dialquilamino, alcoxialquilo, carboxialquilo, alcoxicarbonilo, aminoalquilo, cicloalquilo, arilo, arilalquilo, ariloxi, heterocicloalquilo o heteroarilo y en el que cada cicloalquilo, arilo, heterocicloalquilo y heteroarilo, solos o como parte de otro grupo dentro de R9, están independientemente sustituidos opcionalmente con 1, 2, 3 6 4 grupos seleccionados entre halo, alquilo, haloalquilo, hidroxi, alcoxi, haloalcoxi, amino, alquilamino y dialquilamino. Reivindicacion 2: El método de la reivindicacion 1, en el que el cáncer se selecciona entre cáncer de mama, cáncer de colon, cáncer rectal, cáncer endometrial, carcinoma gástrico, glioblastoma, carcinoma hepatocelular, cáncer de pulmon de células pequenas, cáncer de pulmon de células no pequenas, melanoma, cáncer ovárico, cáncer cervical, cáncer pancreático, carcinoma prostático, leucemia mielogenosa aguda (AML), leucemia mielogenosa cronica (CML) y carcinoma tiroideo. . Reivindicacion 4: El método de la reivindicacion 1, 2 6 3, en el que el inhibidor autofágico es cloroquina.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30289710P | 2010-02-09 | 2010-02-09 | |
| US36750510P | 2010-07-26 | 2010-07-26 | |
| US36751210P | 2010-07-26 | 2010-07-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080151A1 true AR080151A1 (es) | 2012-03-14 |
Family
ID=43804402
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100408A AR080151A1 (es) | 2010-02-09 | 2011-02-09 | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8901137B2 (es) |
| AR (1) | AR080151A1 (es) |
| TW (1) | TW201139436A (es) |
| UY (1) | UY33221A (es) |
| WO (1) | WO2011100319A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007044813A1 (en) * | 2005-10-07 | 2007-04-19 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα |
| JP5270353B2 (ja) * | 2005-10-07 | 2013-08-21 | エクセリクシス， インク． | ホスファチジルイノシトール３−キナーゼインヒビターとその使用方法 |
| US20100075947A1 (en) | 2006-08-16 | 2010-03-25 | Exelixis, Inc. | Methods of Using PI3K and MEK Modulators |
| UY33221A (es) | 2010-02-09 | 2011-09-30 | Univ California | MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA |
| CA2812089C (en) | 2010-09-14 | 2020-02-18 | Exelixis Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| AR086209A1 (es) * | 2011-04-29 | 2013-11-27 | Exelixis Inc | METODO DE TRATAMIENTO CONTRA EL LINFOMA CON INHIBIDORES DE PIRIDOPIRIMIDINONA DE PI3K/mTOR, COMPUESTO, COMPOSICION FARMACEUTICA |
| CA2854159A1 (en) | 2011-11-01 | 2013-05-10 | Sanofi | N- (3-{[(3-{[2-chloro-5-(methoxy)phenyl] amino} quinoxalin- 2 -yl) amino] sulfonyl} phe nyl) - 2 -methylalaninamide as phosphatidylinositol 3- kinase inhibitor for the treatment of lymphoproliferative malignancies |
| AR090151A1 (es) | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| WO2015068142A2 (en) * | 2013-11-11 | 2015-05-14 | Cellworks Group, Inc. | Compositions, process of preparation of said compositions, uses and method of management of myeloproliferative disorder |
| US11364237B2 (en) * | 2017-02-07 | 2022-06-21 | Oncocross Co., Ltd. | Composition for inhibiting cancer metastasis and treating cancer |
| KR102341010B1 (ko) * | 2018-02-06 | 2021-12-20 | 주식회사 온코크로스 | 암의 전이 억제 및 치료용 조성물 |
| EP3589634A4 (en) * | 2017-03-03 | 2020-08-12 | Auckland Uniservices Limited | FGFR KINASE INHIBITORS AND PHARMACEUTICAL USES |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| IL117923A (en) | 1995-05-03 | 2000-06-01 | Warner Lambert Co | Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds |
| EP0964864B1 (en) | 1997-02-05 | 2008-04-09 | Warner-Lambert Company LLC | Pyrido 2,3-d pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation |
| JP2003523358A (ja) | 2000-01-27 | 2003-08-05 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | 神経変性疾患の治療のためのピリドピリミジノン誘導体 |
| NZ520962A (en) | 2000-03-06 | 2003-09-26 | Warner Lambert Co | 5-alkylpyrido[2,3-d]pyrimidines cyclin-dependent tyrosine kinase inhibitors |
| CA2407593C (en) | 2000-04-27 | 2011-01-11 | Yamanouchi Pharmaceutical Co. Ltd. | Fused heteroaryl derivatives |
| AU2002233706C1 (en) | 2001-02-26 | 2005-12-22 | Tanabe Seiyaku Co., Ltd. | Pyridopyrimidine or naphthyridine derivative |
| US7019002B2 (en) | 2001-12-11 | 2006-03-28 | Pharmacia & Upjohn, S.P.A. | Pyridopyrimidinones derivatives as telomerase inhibitors |
| AU2003225072A1 (en) | 2002-04-19 | 2003-11-03 | Smithkline Beecham Corporation | Novel compounds |
| CA2484921A1 (en) | 2002-05-06 | 2003-11-13 | Genelabs Technologies, Inc. | Nucleoside derivatives for treating hepatitis c virus infection |
| JP2004083587A (ja) | 2002-08-06 | 2004-03-18 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| WO2004063195A1 (en) | 2003-01-03 | 2004-07-29 | Sloan-Kettering Institute For Cancer Research | Pyridopyrimidine kinase inhibitors |
| WO2004089930A1 (en) | 2003-04-02 | 2004-10-21 | Imclone Systems Incorporated | 4-fluoroquinolone derivatives and their use as kinase inhibitors |
| JP2007504283A (ja) | 2003-05-20 | 2007-03-01 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | β−アミロイド斑に作用物質を結合させる方法 |
| WO2005082903A1 (en) | 2004-02-18 | 2005-09-09 | Warner-Lambert Company Llc | 2-(pyridin-3-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
| WO2005105097A2 (en) | 2004-04-28 | 2005-11-10 | Gpc Biotech Ag | Pyridopyrimidines for treating inflammatory and other diseases |
| WO2005105801A1 (en) | 2004-05-04 | 2005-11-10 | Warner-Lambert Company Llc | Pyrrolyl substituted pyrido[2,3-d]pyrimidin-7-ones and derivatives thereof as therapeutic agents |
| CA2590294A1 (en) | 2004-12-13 | 2006-06-22 | Sunesis Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
| WO2007044813A1 (en) | 2005-10-07 | 2007-04-19 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα |
| EA201200669A1 (ru) | 2005-10-07 | 2012-11-30 | Экселиксис, Инк. | ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα |
| JP5270353B2 (ja) | 2005-10-07 | 2013-08-21 | エクセリクシス， インク． | ホスファチジルイノシトール３−キナーゼインヒビターとその使用方法 |
| US20100075947A1 (en) * | 2006-08-16 | 2010-03-25 | Exelixis, Inc. | Methods of Using PI3K and MEK Modulators |
| AU2007316417B2 (en) | 2006-11-06 | 2013-08-22 | Tolero Pharmaceuticals, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| EA020022B1 (ru) | 2007-04-10 | 2014-08-29 | Экселиксис, Инк. | Способы лечения с применением пиридопиримидиноновых ингибиторов pi3k-альфа |
| JP2010523677A (ja) | 2007-04-11 | 2010-07-15 | エクセリクシス， インク． | 癌の治療のためのＰＩ３Ｋα阻害剤としてのピリド［２，３−Ｄ］ピリミジン−７−オン |
| EA019064B1 (ru) | 2007-04-11 | 2013-12-30 | Экселиксис, Инк. | Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа |
| NZ579945A (en) | 2007-04-11 | 2012-05-25 | Exelixis Inc | Pyrido [2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
| JP2012504628A (ja) * | 2008-09-30 | 2012-02-23 | エグゼリクシス， インコーポレイテッド | ＰＩ３ＫαおよびｍＴＯＲのピリドピリミジノン阻害剤 |
| UY33221A (es) | 2010-02-09 | 2011-09-30 | Univ California | MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA |
-
2011
- 2011-02-09 UY UY0001033221A patent/UY33221A/es not_active Application Discontinuation
- 2011-02-09 TW TW100104323A patent/TW201139436A/zh unknown
- 2011-02-09 WO PCT/US2011/024187 patent/WO2011100319A1/en active Application Filing
- 2011-02-09 AR ARP110100408A patent/AR080151A1/es unknown
- 2011-02-09 US US13/578,058 patent/US8901137B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US8901137B2 (en) | 2014-12-02 |
| US20130172371A1 (en) | 2013-07-04 |
| UY33221A (es) | 2011-09-30 |
| TW201139436A (en) | 2011-11-16 |
| WO2011100319A1 (en) | 2011-08-18 |
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| FB | Suspension of granting procedure |