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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Mycology (AREA)
- Immunology (AREA)
- Microbiology (AREA)
- Biomedical Technology (AREA)
- Hematology (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 (2) | HK1204976A1 (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 (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA115786C2 (uk) * | 2012-08-07 | 2017-12-26 | Новартіс Аг | ФАРМАЦЕВТИЧНА КОМБІНАЦІЯ, ЩО МІСТИТЬ ІНГІБІТОР B-Raf, ІНГІБІТОР EGFR ТА, НЕОБОВ'ЯЗКОВО, ІНГІБІТОР РІ3K-? |
| MX2015013466A (es) | 2013-03-21 | 2016-06-21 | Novartis Ag | Terapia de combinacion que comprende un inhibidor deb-raf y un segundo inhibidor. |
| WO2015145388A2 (en) * | 2014-03-27 | 2015-10-01 | Novartis Ag | Methods of treating colorectal cancers harboring upstream wnt pathway mutations |
| DK3155126T3 (en) * | 2014-06-16 | 2018-09-03 | Worldwide Innovative Network | METHOD OF CHOOSING PERSONAL TRIAL TREATMENT FOR CANCER TREATMENT |
| WO2016193955A1 (en) * | 2015-06-04 | 2016-12-08 | Giorgio Stassi | Combinations of kinase inhibitors for treating colorectal cancer |
| EP3380097A2 (en) * | 2015-08-28 | 2018-10-03 | Novartis AG | Pharmaceutical combination comprising (a) the alpha-isoform specific pi3k inhibitor alpelisib (byl719) and (b) an akt inhibitor, preferably mk-2206, afuresertib or uprosertib, and the use thereof in the treatment/prevention of cancer |
| 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 |
| CR20190002A (es) | 2016-06-03 | 2019-06-10 | Zhu Alexander Cao | Combinaciones farmacéuticas |
| JP7114575B2 (ja) | 2016-09-19 | 2022-08-08 | ノバルティス アーゲー | Ｒａｆ阻害剤及びｅｒｋ阻害剤を含む治療用組合せ |
| KR102641827B1 (ko) | 2017-05-02 | 2024-03-04 | 노파르티스 아게 | 병용 요법 |
| SG11201913249SA (en) * | 2017-08-03 | 2020-02-27 | Novartis Ag | Therapeutic combination of a third-generation egfr tyrosine kinase inhibitor and a raf inhibitor |
| PL3860998T3 (pl) | 2018-10-05 | 2024-06-17 | Annapurna Bio Inc. | Związki i kompozycje do leczenia schorzeń związanych z aktywnością receptora apj |
| 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 |
| GB2629956A (en) * | 2022-01-27 | 2024-11-13 | Univ Tohoku | 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 |
| WO2024073364A1 (en) * | 2022-09-26 | 2024-04-04 | Beigene, Ltd. | Combinations of a b-raf inhibitor, and an anti-egfr antibody for the treatment of cancer |
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 |
| MY150697A (en) | 2007-04-10 | 2014-02-28 | Exelixis Inc | Methods of treating cancer using pyridopyrimdinone inhibitors of p13k alpha |
| UA104147C2 (uk) | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| BR112012003926A2 (pt) * | 2009-08-24 | 2020-08-11 | Genentech Inc | método para identificar um paciente não responsivo ao tratamento com um inibidor de b-raf, método para determinar se um tumor irá responder ao tratamento com um inibidor de b-raf, método para predizer se um paciente será não responsivo ao tratamento com um inibidor de braf específico, kit, método para classificar um tumor de mama, pulmão, cólon, ovário, tiroide, melanoma, ou pancreático e método para identificar um tumor não responsivo ao tratamento com um inibidor de b-raf |
| AR077975A1 (es) * | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| EP2488184A4 (en) * | 2009-10-12 | 2013-04-24 | Glaxosmithkline Llc | COMBINATION |
| US20120045433A1 (en) | 2010-08-17 | 2012-02-23 | Kapil Dhingra | Combination therapy |
| JP2013542228A (ja) * | 2010-11-08 | 2013-11-21 | ノバルティス アーゲー | Ｅｇｆｒ依存性疾患またはｅｇｆｒファミリーメンバーを標的とする薬剤に対して獲得耐性を有する疾患の治療における２−カルボキサミドシクロアミノウレア誘導体の使用 |
| CA2855245A1 (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 |
| WO2013070996A1 (en) * | 2011-11-11 | 2013-05-16 | Novartis Ag | Method of treating a proliferative disease |
| UA115786C2 (uk) * | 2012-08-07 | 2017-12-26 | Новартіс Аг | ФАРМАЦЕВТИЧНА КОМБІНАЦІЯ, ЩО МІСТИТЬ ІНГІБІТОР B-Raf, ІНГІБІТОР EGFR ТА, НЕОБОВ'ЯЗКОВО, ІНГІБІТОР РІ3K-? |
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2013
- 2013-08-05 UA UAA201500424A patent/UA115786C2/uk unknown
- 2013-08-05 AR ARP130102776A patent/AR092045A1/es not_active Application Discontinuation
- 2013-08-05 TR TR2019/04980T patent/TR201904980T4/tr unknown
- 2013-08-05 EA EA201590332A patent/EA028420B1/ru not_active IP Right Cessation
- 2013-08-05 EP EP19159506.5A patent/EP3574904A1/en active Pending
- 2013-08-05 SI SI201331387T patent/SI2882440T1/sl unknown
- 2013-08-05 PE PE2019001539A patent/PE20191655A1/es unknown
- 2013-08-05 AU AU2013299841A patent/AU2013299841B8/en active Active
- 2013-08-05 NZ NZ703940A patent/NZ703940A/en unknown
- 2013-08-05 PT PT13748243T patent/PT2882440T/pt unknown
- 2013-08-05 RS RS20190351A patent/RS58734B1/sr unknown
- 2013-08-05 US US14/419,256 patent/US9474754B2/en active Active
- 2013-08-05 PE PE2015000130A patent/PE20150673A1/es not_active Application Discontinuation
- 2013-08-05 CN CN201380042229.5A patent/CN104519887B/zh active Active
- 2013-08-05 DK DK13748243.6T patent/DK2882440T3/da active
- 2013-08-05 SG SG11201500321YA patent/SG11201500321YA/en unknown
- 2013-08-05 IN IN450DEN2015 patent/IN2015DN00450A/en unknown
- 2013-08-05 CA CA2879548A patent/CA2879548C/en active Active
- 2013-08-05 WO PCT/US2013/053619 patent/WO2014025688A1/en active Application Filing
- 2013-08-05 KR KR1020157002982A patent/KR102112885B1/ko active IP Right Grant
- 2013-08-05 EP EP13748243.6A patent/EP2882440B1/en active Active
- 2013-08-05 PL PL13748243T patent/PL2882440T3/pl unknown
- 2013-08-05 JP JP2015526606A patent/JP6342396B2/ja active Active
- 2013-08-05 HU HUE13748243A patent/HUE042877T2/hu unknown
- 2013-08-05 LT LTEP13748243.6T patent/LT2882440T/lt unknown
- 2013-08-05 MY MYPI2015000102A patent/MY176031A/en unknown
- 2013-08-05 MX MX2015001732A patent/MX359403B/es active IP Right Grant
- 2013-08-05 ES ES13748243T patent/ES2717911T3/es active Active
- 2013-08-06 JO JOP/2013/0236A patent/JOP20130236B1/ar active
- 2013-08-06 TW TW102128165A patent/TWI607754B/zh 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 MA MA37829A patent/MA37829A1/fr unknown
- 2015-02-04 PH PH12015500246A patent/PH12015500246A1/en unknown
- 2015-02-06 GT GT201500025A patent/GT201500025A/es unknown
- 2015-02-06 CL CL2015000294A patent/CL2015000294A1/es unknown
- 2015-02-06 CO CO15024921A patent/CO7200273A2/es unknown
- 2015-03-06 EC ECIEPI20158695A patent/ECSP15008695A/es unknown
- 2015-06-18 HK HK15105815.5A patent/HK1204976A1/xx unknown
- 2015-11-03 HK HK15110834.2A patent/HK1211831A1/xx unknown
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2018
- 2018-02-09 JP JP2018022248A patent/JP6595024B2/ja active Active
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2019
- 2019-03-19 HR HRP20190537TT patent/HRP20190537T1/hr unknown
- 2019-04-30 CY CY20191100461T patent/CY1122143T1/el unknown
- 2019-09-25 JP JP2019174353A patent/JP6974669B2/ja active Active
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