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)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Microbiology (AREA)
- Mycology (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 |
|---|---|---|---|---|
| DK2882440T3 (da) * | 2012-08-07 | 2019-05-06 | Novartis Ag | Farmaceutiske kombinationer, der omfatter en b-raf-inhibitor, en egfr-inhibitor og eventuelt en pi3k-alfa-inhibitor |
| CN105209073A (zh) | 2013-03-21 | 2015-12-30 | 诺华股份有限公司 | 包含B-Raf抑制剂和第二抑制剂的组合疗法 |
| WO2015145388A2 (en) * | 2014-03-27 | 2015-10-01 | Novartis Ag | Methods of treating colorectal cancers harboring upstream wnt pathway mutations |
| JP6704861B2 (ja) * | 2014-06-16 | 2020-06-03 | ワールドワイド・イノベイティブ・ネットワークＷｏｒｌｄｗｉｄｅ Ｉｎｎｏｖａｔｉｖｅ Ｎｅｔｗｏｒｋ | 癌処置のための個別化三剤治療を選択するための方法 |
| WO2016193955A1 (en) * | 2015-06-04 | 2016-12-08 | Giorgio Stassi | Combinations of kinase inhibitors for treating colorectal cancer |
| US10328065B2 (en) | 2015-08-28 | 2019-06-25 | 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 |
| WO2017037578A2 (en) * | 2015-08-28 | 2017-03-09 | Novartis Ag | Combination therapy |
| WO2017066664A1 (en) * | 2015-10-16 | 2017-04-20 | Millennium Pharmaceuticals, Inc. | Combination therapy including a raf inhibitor for the treatment of colorectal cancer |
| HUE060653T2 (hu) * | 2016-06-03 | 2023-04-28 | Array Biopharma Inc | Gyógyászati kombinációk |
| CN109715163B (zh) * | 2016-09-19 | 2022-11-22 | 诺华股份有限公司 | 包含raf抑制剂和erk抑制剂的治疗组合 |
| ES2952265T3 (es) | 2017-05-02 | 2023-10-30 | Novartis Ag | Terapia combinada que comprende un inhibidor de Raf y trametinib |
| WO2019026007A1 (en) * | 2017-08-03 | 2019-02-07 | Novartis Ag | THERAPEUTIC ASSOCIATION OF THIRD GENERATION TYFRSINE KINASE INHIBITOR AND RAF INHIBITOR |
| JP2022508648A (ja) | 2018-10-05 | 2022-01-19 | アンナプルナ バイオ インコーポレイテッド | Ａｐｊ受容体活性に関連する状態を処置するための化合物および組成物 |
| KR20210120039A (ko) * | 2019-01-25 | 2021-10-06 | 베이진 엘티디 | B-raf 키나제 이합체 억제제의 안정적인 고체 분산액, 이의 제조 방법 및 용도 |
| WO2020164997A1 (en) * | 2019-02-12 | 2020-08-20 | Bayer Aktiengesellschaft | Combination of pi3k-inhibitors |
| WO2023145530A1 (ja) * | 2022-01-27 | 2023-08-03 | 国立大学法人東北大学 | 癌治療剤 |
| 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 |
| JP2010523670A (ja) | 2007-04-10 | 2010-07-15 | エクセリクシス， インク． | Ｐｉ３ｋアルファのピリドピリミジノン阻害剤を使用した治療方法 |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| US20120214828A1 (en) * | 2009-08-24 | 2012-08-23 | Georgia Hatzivassiliou | Determining sensitivity of cells to b-raf inhibitor treatment by detecting kras mutation and rtk expression levels |
| JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| WO2011046894A1 (en) | 2009-10-12 | 2011-04-21 | Glaxosmithkline Llc | Combination |
| US20120045433A1 (en) | 2010-08-17 | 2012-02-23 | Kapil Dhingra | Combination therapy |
| EP2637661B1 (en) * | 2010-11-08 | 2017-12-20 | Novartis AG | Use of (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)- pyridin-4-yl]-thiazol-2-yl}-amide) in the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members |
| AU2012335665A1 (en) | 2011-11-10 | 2014-07-03 | Memorial Sloan-Kettering Cancer Center | Treatment of ovarian cancer with 2-amino-4H-naphtho[1,2-B]pyran-3-carbonitriles |
| CN103917236A (zh) * | 2011-11-11 | 2014-07-09 | 诺华股份有限公司 | 治疗增生性疾病的方法 |
| DK2882440T3 (da) * | 2012-08-07 | 2019-05-06 | Novartis Ag | Farmaceutiske kombinationer, der omfatter en b-raf-inhibitor, en egfr-inhibitor og eventuelt en pi3k-alfa-inhibitor |
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2013
- 2013-08-05 DK DK13748243.6T patent/DK2882440T3/da active
- 2013-08-05 CA CA2879548A patent/CA2879548C/en active Active
- 2013-08-05 NZ NZ703940A patent/NZ703940A/en unknown
- 2013-08-05 SG SG11201500321YA patent/SG11201500321YA/en unknown
- 2013-08-05 JP JP2015526606A patent/JP6342396B2/ja active Active
- 2013-08-05 PL PL13748243T patent/PL2882440T3/pl unknown
- 2013-08-05 SI SI201331387T patent/SI2882440T1/sl unknown
- 2013-08-05 KR KR1020157002982A patent/KR102112885B1/ko active IP Right Grant
- 2013-08-05 CN CN201380042229.5A patent/CN104519887B/zh active Active
- 2013-08-05 AU AU2013299841A patent/AU2013299841B8/en active Active
- 2013-08-05 IN IN450DEN2015 patent/IN2015DN00450A/en unknown
- 2013-08-05 LT LTEP13748243.6T patent/LT2882440T/lt unknown
- 2013-08-05 AR ARP130102776A patent/AR092045A1/es not_active Application Discontinuation
- 2013-08-05 EA EA201590332A patent/EA028420B1/ru not_active IP Right Cessation
- 2013-08-05 ES ES13748243T patent/ES2717911T3/es active Active
- 2013-08-05 PE PE2019001539A patent/PE20191655A1/es unknown
- 2013-08-05 EP EP19159506.5A patent/EP3574904A1/en active Pending
- 2013-08-05 US US14/419,256 patent/US9474754B2/en active Active
- 2013-08-05 UA UAA201500424A patent/UA115786C2/uk unknown
- 2013-08-05 RS RS20190351A patent/RS58734B1/sr unknown
- 2013-08-05 WO PCT/US2013/053619 patent/WO2014025688A1/en active Application Filing
- 2013-08-05 MX MX2015001732A patent/MX359403B/es active IP Right Grant
- 2013-08-05 TR TR2019/04980T patent/TR201904980T4/tr unknown
- 2013-08-05 MY MYPI2015000102A patent/MY176031A/en unknown
- 2013-08-05 HU HUE13748243A patent/HUE042877T2/hu unknown
- 2013-08-05 PT PT13748243T patent/PT2882440T/pt unknown
- 2013-08-05 EP EP13748243.6A patent/EP2882440B1/en active Active
- 2013-08-05 PE PE2015000130A patent/PE20150673A1/es not_active Application Discontinuation
- 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 CO CO15024921A patent/CO7200273A2/es unknown
- 2015-02-06 CL CL2015000294A patent/CL2015000294A1/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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