AR092045A1 - Combinaciones farmaceuticas - Google Patents
Combinaciones farmaceuticasInfo
- Publication number
- AR092045A1 AR092045A1 ARP130102776A ARP130102776A AR092045A1 AR 092045 A1 AR092045 A1 AR 092045A1 AR P130102776 A ARP130102776 A AR P130102776A AR P130102776 A ARP130102776 A AR P130102776A AR 092045 A1 AR092045 A1 AR 092045A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- substituents
- deuterium
- fluorine
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Una combinación farmacéutica, la cual comprende: (a) un inhibidor de BRaf, (b) un inhibidor del receptor del factor de crecimiento epidérmico (EGFR) y, opcionalmente, (c) un inhibidor de PI3K; los usos de esta combinación en el tratamiento de enfermedades proliferativas; y los métodos para el tratamiento de un sujeto que padezca de una enfermedad proliferativa, los cuales comprenden administrar una cantidad terapéuticamente efectiva de esta combinación. Reivindicación 1: Una combinación farmacéutica, la cual comprende: (a) un inhibidor de B-Raf de la fórmula (3) o una sal farmacéuticamente aceptable del mismo, (b) un inhibidor del receptor del factor de crecimiento epidérmico (EGFR) y, opcionalmente, (c) un inhibidor de PI3Ka, para su administración simultánea, separada o en secuencia. Reivindicación 5: Una combinación de la reivindicación 1, en donde el inhibidor de PI3K es un compuesto de la fórmula (1) en donde: A representa un heteroarilo seleccionado a partir del grupo que consiste en el grupo de fórmulas (2); R¹ representa uno de los siguientes sustituyentes: (i) alquilo C₁₋₇ insustituido o sustituido, de preferencia sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a nueve de las siguientes fracciones: deuterio, flúor, o de una a dos de las siguientes fracciones: cicloalquilo C₃₋₅; (ii) cicloalquilo C₃₋₅ opcionalmente sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a cuatro de las siguientes fracciones: deuterio, alquilo de 1 a 4 átomos de carbono (de preferencia metilo), flúor, ciano, amino-carbonilo; (iii) fenilo opcionalmente sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a dos de las siguientes fracciones: deuterio, halógeno, ciano, alquilo C₁₋₇, alquilo C₁₋₇-amino, di-(alquilo C₁₋₇)-amino, alquilo C₁₋₇-amino-carbonilo, di-(alquilo C₁₋₇)-amino-carbonilo, alcoxilo C₁₋₇; (iv) amina opcionalmente mono- o di-sustituida; en donde los sustituyentes se seleccionan independientemente a partir de las siguientes fracciones: deuterio, alquilo C₁₋₇ (que está insustituido o sustituido por uno o más sustituyentes seleccionados a partir del grupo de deuterio, flúor, cloro, hidroxilo), fenil-sulfonilo (que está insustituido o sustituido por uno o más, de preferencia un alquilo C₁₋₇, alcoxilo C₁₋₇, di-(alquilo C₁₋₇)-amino-alcoxilo C₁₋₇); (v) sulfonilo sustituido; en donde este sustituyente se selecciona a partir de las siguientes fracciones: alquilo C₁₋₇ (que está insustituido o sustituido por uno o más sustituyentes seleccionados a partir del grupo de deuterio, flúor), pirrolidino (que está insustituido o sustituido por uno o más sustituyentes seleccionados a partir del grupo de deuterio, hidroxilo, oxo; en particular un oxo); (vi) flúor, cloro; R² representa hidrógeno; R³ representa: (i) hidrógeno, (ii) flúor, cloro, (iii) metilo opcionalmente sustituido, en donde los sustituyentes se seleccionan independientemente a partir de una o más, de preferencia de una a tres de las siguientes fracciones: deuterio, flúor, cloro, o dimetilamino; con la excepción de la 1-({5-[2-(terbutil)-pirimidin-4-il]-4-metil-tiazol-2-il}-amida) de 2-amida del ácido (S)-pirrolidin-1,2-dicarboxílico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261680473P | 2012-08-07 | 2012-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092045A1 true AR092045A1 (es) | 2015-03-18 |
Family
ID=48980368
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130102776A AR092045A1 (es) | 2012-08-07 | 2013-08-05 | Combinaciones farmaceuticas |
Country Status (39)
| Country | Link |
|---|---|
| US (1) | US9474754B2 (es) |
| EP (2) | EP3574904A1 (es) |
| JP (3) | JP6342396B2 (es) |
| KR (1) | KR102112885B1 (es) |
| CN (1) | CN104519887B (es) |
| AR (1) | AR092045A1 (es) |
| AU (1) | AU2013299841B8 (es) |
| CA (1) | CA2879548C (es) |
| CL (1) | CL2015000294A1 (es) |
| CO (1) | CO7200273A2 (es) |
| CY (1) | CY1122143T1 (es) |
| DK (1) | DK2882440T3 (es) |
| EA (1) | EA028420B1 (es) |
| EC (1) | ECSP15008695A (es) |
| ES (1) | ES2717911T3 (es) |
| GT (1) | GT201500025A (es) |
| HK (1) | HK1211831A1 (es) |
| HR (1) | HRP20190537T1 (es) |
| HU (1) | HUE042877T2 (es) |
| IL (1) | IL236934B (es) |
| IN (1) | IN2015DN00450A (es) |
| JO (1) | JOP20130236B1 (es) |
| LT (1) | LT2882440T (es) |
| MA (1) | MA37829A1 (es) |
| MX (1) | MX359403B (es) |
| MY (1) | MY176031A (es) |
| NZ (1) | NZ703940A (es) |
| PE (2) | PE20191655A1 (es) |
| PH (1) | PH12015500246A1 (es) |
| PL (1) | PL2882440T3 (es) |
| PT (1) | PT2882440T (es) |
| RS (1) | RS58734B1 (es) |
| SG (1) | SG11201500321YA (es) |
| SI (1) | SI2882440T1 (es) |
| TN (1) | TN2015000027A1 (es) |
| TR (1) | TR201904980T4 (es) |
| TW (1) | TWI607754B (es) |
| UA (1) | UA115786C2 (es) |
| WO (1) | WO2014025688A1 (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201500321YA (en) * | 2012-08-07 | 2015-04-29 | Novartis Ag | Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor |
| EP2976106B1 (en) | 2013-03-21 | 2021-04-14 | Array BioPharma Inc. | Combination therapy comprising a b-raf inhibitor and a second inhibitor |
| WO2015145388A2 (en) * | 2014-03-27 | 2015-10-01 | Novartis Ag | Methods of treating colorectal cancers harboring upstream wnt pathway mutations |
| EA201790019A1 (ru) * | 2014-06-16 | 2017-06-30 | Уорлдуайд Иновейтив Нетуорк | Способ выбора персонализированной трехкомпонентной терапии для лечения рака |
| WO2016193955A1 (en) * | 2015-06-04 | 2016-12-08 | Giorgio Stassi | Combinations of kinase inhibitors for treating colorectal cancer |
| CN107921026A (zh) * | 2015-08-28 | 2018-04-17 | 诺华股份有限公司 | 药物组合物包含(a)α‑同种型特异性PI3K抑制剂alpelisib(BYL719)和(b)AKT抑制剂,优选MK‑2206,afuresertib或uprosertib及其在治疗/预防癌症中的应用 |
| EP3355886A1 (en) * | 2015-08-28 | 2018-08-08 | Novartis AG | Pharmaceutical combination comprising the pi3k inhibitor alpelisib and the b-raf inhibitor dabrafenib; the use of such combination in the treatment or prevention of cancer |
| WO2017066664A1 (en) * | 2015-10-16 | 2017-04-20 | Millennium Pharmaceuticals, Inc. | Combination therapy including a raf inhibitor for the treatment of colorectal cancer |
| BR112018074941A2 (pt) | 2016-06-03 | 2019-03-12 | Caponigro Giordano | combinações farmacêuticas |
| KR102341660B1 (ko) * | 2016-09-19 | 2021-12-23 | 노파르티스 아게 | Raf 억제제 및 erk 억제제를 포함하는 치료적 조합 |
| CN110494166B (zh) | 2017-05-02 | 2022-11-08 | 诺华股份有限公司 | 组合疗法 |
| JOP20200014A1 (ar) * | 2017-08-03 | 2022-10-30 | Novartis Ag | توليفة علاجية لمثبط كيناز تيروزين egfr من الجيل الثالث ومثبط raf |
| TWI833819B (zh) | 2018-10-05 | 2024-03-01 | 美商安尼波那生物公司 | 用於治療與apj受體活性相關的病狀的化合物及組成物 |
| TWI849043B (zh) * | 2019-01-25 | 2024-07-21 | 英屬開曼群島商百濟神州有限公司 | B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 |
| WO2020164997A1 (en) * | 2019-02-12 | 2020-08-20 | Bayer Aktiengesellschaft | Combination of pi3k-inhibitors |
| BR112021022335A2 (pt) | 2019-05-13 | 2021-12-28 | Novartis Ag | Formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinopiridin-4-il)-4-metilfenil)-2 (trifluorome-til)isonicotinamida como inibidores raf para o tratamento de câncer |
| US20250108051A1 (en) * | 2022-01-27 | 2025-04-03 | Tohoku University | Therapeutic agent for cancer |
| WO2023230554A1 (en) | 2022-05-25 | 2023-11-30 | Pfizer Inc. | Combination of a braf inhibitor, an egfr inhibitor, and a pd-1 antagonist for the treatment of braf v600e-mutant, msi-h/dmmr colorectal cancer |
| TW202421133A (zh) * | 2022-09-26 | 2024-06-01 | 美商馬布可爾公司 | 用於治療癌症的ｂ－ｒａｆ抑制劑和抗ｅｇｆｒ抗體之組合 |
| WO2025003956A1 (en) | 2023-06-30 | 2025-01-02 | Pfizer Inc. | High drug loading formulations of encorafenib |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU4128089A (en) | 1988-09-15 | 1990-03-22 | Rorer International (Overseas) Inc. | Monoclonal antibodies specific to human epidermal growth factor receptor and therapeutic methods employing same |
| US6235883B1 (en) | 1997-05-05 | 2001-05-22 | Abgenix, Inc. | Human monoclonal antibodies to epidermal growth factor receptor |
| KR101626435B1 (ko) | 2007-04-10 | 2016-06-01 | 엑셀리시스, 인코포레이티드 | Ｐｉ３ｋ 알파의 피리도피리미디논 억제제를 이용한 암 치료 방법 |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| AU2010289794B2 (en) | 2009-08-24 | 2014-10-02 | Genentech, Inc. | Determining sensitivity of cells to B-Raf inhibitor treatment by detecting Kras mutation and RTK expression levels |
| AR077975A1 (es) | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| US20120202822A1 (en) * | 2009-10-12 | 2012-08-09 | Kurtis Earl Bachman | Combination |
| US20120045433A1 (en) | 2010-08-17 | 2012-02-23 | Kapil Dhingra | Combination therapy |
| AU2011328227B2 (en) * | 2010-11-08 | 2015-04-09 | Novartis Ag | Use of 2-carboxamide cycloamino urea derivatives in the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members |
| WO2013070998A1 (en) | 2011-11-10 | 2013-05-16 | Memorial Sloan-Kettering Cancer Center | TREATMENT OF OVARIAN CANCER WITH 2-AMINO-4H-NAPHTHO[1,2-b]PYRAN-3-CARBONITRILES |
| BR112014011223A8 (pt) * | 2011-11-11 | 2023-01-31 | Novartis Ag | Método de tratar uma doença proliferativa |
| SG11201500321YA (en) * | 2012-08-07 | 2015-04-29 | Novartis Ag | Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor |
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2013
- 2013-08-05 SG SG11201500321YA patent/SG11201500321YA/en unknown
- 2013-08-05 PE PE2019001539A patent/PE20191655A1/es unknown
- 2013-08-05 HU HUE13748243A patent/HUE042877T2/hu unknown
- 2013-08-05 PT PT13748243T patent/PT2882440T/pt unknown
- 2013-08-05 EP EP19159506.5A patent/EP3574904A1/en active Pending
- 2013-08-05 EP EP13748243.6A patent/EP2882440B1/en active Active
- 2013-08-05 US US14/419,256 patent/US9474754B2/en active Active
- 2013-08-05 JP JP2015526606A patent/JP6342396B2/ja active Active
- 2013-08-05 SI SI201331387T patent/SI2882440T1/sl unknown
- 2013-08-05 AU AU2013299841A patent/AU2013299841B8/en active Active
- 2013-08-05 DK DK13748243.6T patent/DK2882440T3/da active
- 2013-08-05 WO PCT/US2013/053619 patent/WO2014025688A1/en not_active Ceased
- 2013-08-05 UA UAA201500424A patent/UA115786C2/uk unknown
- 2013-08-05 HK HK15110834.2A patent/HK1211831A1/xx unknown
- 2013-08-05 ES ES13748243T patent/ES2717911T3/es active Active
- 2013-08-05 PE PE2015000130A patent/PE20150673A1/es not_active Application Discontinuation
- 2013-08-05 RS RS20190351A patent/RS58734B1/sr unknown
- 2013-08-05 MX MX2015001732A patent/MX359403B/es active IP Right Grant
- 2013-08-05 IN IN450DEN2015 patent/IN2015DN00450A/en unknown
- 2013-08-05 CN CN201380042229.5A patent/CN104519887B/zh active Active
- 2013-08-05 PL PL13748243T patent/PL2882440T3/pl unknown
- 2013-08-05 TR TR2019/04980T patent/TR201904980T4/tr unknown
- 2013-08-05 AR ARP130102776A patent/AR092045A1/es not_active Application Discontinuation
- 2013-08-05 MY MYPI2015000102A patent/MY176031A/en unknown
- 2013-08-05 CA CA2879548A patent/CA2879548C/en active Active
- 2013-08-05 HR HRP20190537TT patent/HRP20190537T1/hr unknown
- 2013-08-05 LT LTEP13748243.6T patent/LT2882440T/lt unknown
- 2013-08-05 KR KR1020157002982A patent/KR102112885B1/ko active Active
- 2013-08-05 NZ NZ703940A patent/NZ703940A/en unknown
- 2013-08-05 EA EA201590332A patent/EA028420B1/ru not_active IP Right Cessation
- 2013-08-06 TW TW102128165A patent/TWI607754B/zh active
- 2013-08-06 JO JOP/2013/0236A patent/JOP20130236B1/ar active
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2015
- 2015-01-19 TN TNP2015000027A patent/TN2015000027A1/fr unknown
- 2015-01-26 IL IL236934A patent/IL236934B/en active IP Right Grant
- 2015-02-04 PH PH12015500246A patent/PH12015500246A1/en unknown
- 2015-02-04 MA MA37829A patent/MA37829A1/fr unknown
- 2015-02-06 GT GT201500025A patent/GT201500025A/es unknown
- 2015-02-06 CO CO15024921A patent/CO7200273A2/es unknown
- 2015-02-06 CL CL2015000294A patent/CL2015000294A1/es unknown
- 2015-03-06 EC ECIEPI20158695A patent/ECSP15008695A/es unknown
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2018
- 2018-02-09 JP JP2018022248A patent/JP6595024B2/ja active Active
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2019
- 2019-04-30 CY CY20191100461T patent/CY1122143T1/el unknown
- 2019-09-25 JP JP2019174353A patent/JP6974669B2/ja active Active
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