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
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- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (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 |
|---|---|---|---|---|
| WO2012149308A1 (en) * | 2011-04-29 | 2012-11-01 | Exelixis, Inc. | Method of treating lymphoma using pyridopyrimidinone inhibitors of pi3k/mtor |
| KR101492795B1 (ko) * | 2005-10-07 | 2015-02-13 | 엑셀리시스, 인코포레이티드 | ＰＩ３Ｋα의 피리도피리미디논 억제제 |
| ES2513165T3 (es) * | 2005-10-07 | 2014-10-24 | Exelixis, Inc. | Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa |
| AU2007284562B2 (en) | 2006-08-16 | 2013-05-02 | Exelixis, Inc. | Using PI3K and MEK modulators in treatments of cancer |
| WO2011100319A1 (en) | 2010-02-09 | 2011-08-18 | Exelixis, Inc. | Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors |
| AR082985A1 (es) | 2010-09-14 | 2013-01-23 | Exelixis Inc | INHIBIDORES DE PI3K-d Y METODOS DE SU USO Y PREPARACION |
| JP6013498B2 (ja) | 2011-11-01 | 2016-10-25 | エクセリクシス， インク． | リンパ増殖性悪性疾患の治療のためのホスファチジルイノシトール３−キナーゼ阻害剤としてのｎ−（３−｛［（３−｛［２−クロロ−５−（メトキシ）フェニル］アミノ｝キノキサリン−２−イル）アミノ］スルホニル｝フェニル）−２−メチルアラニンアミド |
| 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 |
| JP6900067B2 (ja) * | 2017-02-07 | 2021-07-07 | オンコクロス カンパニー，リミテッド | 癌の転移抑制および治療用組成物 |
| KR102341010B1 (ko) * | 2018-02-06 | 2021-12-20 | 주식회사 온코크로스 | 암의 전이 억제 및 치료용 조성물 |
| JP7226804B2 (ja) * | 2017-03-03 | 2023-02-21 | オークランド ユニサービシズ リミテッド | Ｆｇｆｒキナーゼ阻害剤及び医薬用途 |
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 |
| EP1255755A1 (en) | 2000-01-27 | 2002-11-13 | Warner-Lambert Company | Pyridopyrimidinone derivatives for treatment of neurodegenerative disease |
| MXPA02008535A (es) | 2000-03-06 | 2002-12-13 | Warner Lambert Co | Inhibidores de 5-alquilpirido (2.3-d) pirimidinas tirosina quinasa. |
| KR100774855B1 (ko) | 2000-04-27 | 2007-11-08 | 아스텔라스세이야쿠 가부시키가이샤 | 축합 헤테로아릴 유도체 |
| MXPA03007623A (es) | 2001-02-26 | 2003-12-04 | Tanabe Seiyaku Co | Derivado de piridopirimidina o naftiridina. |
| US7019002B2 (en) | 2001-12-11 | 2006-03-28 | Pharmacia & Upjohn, S.P.A. | Pyridopyrimidinones derivatives as telomerase inhibitors |
| EP1499320B1 (en) | 2002-04-19 | 2007-08-22 | Smithkline Beecham Corporation | Novel compounds |
| US20040063658A1 (en) | 2002-05-06 | 2004-04-01 | Roberts Christopher Don | 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 |
| US20050009849A1 (en) | 2003-01-03 | 2005-01-13 | Veach Darren R. | Pyridopyrimidine kinase inhibitors |
| WO2004089930A1 (en) | 2003-04-02 | 2004-10-21 | Imclone Systems Incorporated | 4-fluoroquinolone derivatives and their use as kinase inhibitors |
| US20070053831A1 (en) | 2003-05-20 | 2007-03-08 | Barrio Jorge R | Methods for binding agents to b-amyloid plaques |
| 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 |
| ATE373659T1 (de) | 2004-05-04 | 2007-10-15 | Warner Lambert Co | Pyrrolylsubstituierte pyrido(2,3-d)pyrimidin-7- one und derivate davon als therapeutische mittel |
| CA2590294A1 (en) | 2004-12-13 | 2006-06-22 | Sunesis Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
| EP1931670B1 (en) | 2005-10-07 | 2012-09-12 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k |
| ES2513165T3 (es) | 2005-10-07 | 2014-10-24 | Exelixis, Inc. | Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa |
| KR101492795B1 (ko) | 2005-10-07 | 2015-02-13 | 엑셀리시스, 인코포레이티드 | ＰＩ３Ｋα의 피리도피리미디논 억제제 |
| AU2007284562B2 (en) | 2006-08-16 | 2013-05-02 | Exelixis, Inc. | Using PI3K and MEK modulators in treatments of cancer |
| MX2009004700A (es) | 2006-11-06 | 2009-05-15 | Supergen Inc | Derivados de imidazo[1,2-b]piridazin y pirazolo[1,5-a] pirimidina y su uso como inhibidores de proteina cinasa. |
| RS52939B (en) | 2007-04-10 | 2014-02-28 | Exelixis Inc. | PROCEDURES FOR THE CANCER TREATMENT USING PI3K ALPHA PIRIDOPYRIMIDINONE INHIBITORS |
| EA019064B1 (ru) | 2007-04-11 | 2013-12-30 | Экселиксис, Инк. | Способы лечения рака с применением хинаксолинового ингибитора pi3k-альфа |
| CN101711249A (zh) | 2007-04-11 | 2010-05-19 | 埃克塞里艾克西斯公司 | 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 |
| EP2142543B8 (en) | 2007-04-11 | 2013-07-03 | Exelixis, Inc. | Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
| EP2350070A1 (en) * | 2008-09-30 | 2011-08-03 | Exelixis, Inc. | Pyridopyrimidinone inhibitors of pi3k and mtor |
| WO2011100319A1 (en) | 2010-02-09 | 2011-08-18 | Exelixis, Inc. | Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors |
-
2011
- 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
- 2011-02-09 UY UY0001033221A patent/UY33221A/es not_active Application Discontinuation
- 2011-02-09 TW TW100104323A patent/TW201139436A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US8901137B2 (en) | 2014-12-02 |
| UY33221A (es) | 2011-09-30 |
| WO2011100319A1 (en) | 2011-08-18 |
| US20130172371A1 (en) | 2013-07-04 |
| TW201139436A (en) | 2011-11-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |