AR086481A1 - COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTOR - Google Patents
COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTORInfo
- Publication number
- AR086481A1 AR086481A1 ARP120101389A ARP120101389A AR086481A1 AR 086481 A1 AR086481 A1 AR 086481A1 AR P120101389 A ARP120101389 A AR P120101389A AR P120101389 A ARP120101389 A AR P120101389A AR 086481 A1 AR086481 A1 AR 086481A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- substituents
- deuterium
- fluorine
- Prior art date
Links
- 108091007960 PI3Ks Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 229940124302 mTOR inhibitor Drugs 0.000 title abstract 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 title abstract 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 10
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 229910052805 deuterium Inorganic materials 0.000 abstract 8
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 7
- 229910052731 fluorine Inorganic materials 0.000 abstract 7
- 239000011737 fluorine Substances 0.000 abstract 7
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 4
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 abstract 4
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 abstract 4
- 229910052801 chlorine Inorganic materials 0.000 abstract 4
- 239000000460 chlorine Substances 0.000 abstract 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 102000038030 PI3Ks Human genes 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric Acid Chemical compound [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 239000004202 carbamide Substances 0.000 abstract 1
- -1 cyano , aminocarbonyl Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
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
- A61K31/435—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
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
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- 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
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- Health & Medical Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
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- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Virology (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Gastroenterology & Hepatology (AREA)
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Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161478572P | 2011-04-25 | 2011-04-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086481A1 true AR086481A1 (es) | 2013-12-18 |
Family
ID=46018130
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101389A AR086481A1 (es) | 2011-04-25 | 2012-04-23 | COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTOR |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US20140066474A1 (enExample) |
| EP (1) | EP2701703A1 (enExample) |
| JP (2) | JP6086902B2 (enExample) |
| KR (1) | KR101925656B1 (enExample) |
| CN (1) | CN103491955B (enExample) |
| AR (1) | AR086481A1 (enExample) |
| AU (2) | AU2012250010A1 (enExample) |
| BR (1) | BR112013027486A2 (enExample) |
| CA (1) | CA2833962A1 (enExample) |
| CL (1) | CL2013003078A1 (enExample) |
| CO (1) | CO6801759A2 (enExample) |
| EA (1) | EA025948B1 (enExample) |
| EC (1) | ECSP13012994A (enExample) |
| GT (1) | GT201300263A (enExample) |
| IL (1) | IL229008A (enExample) |
| MA (1) | MA35038B1 (enExample) |
| MX (1) | MX2013012385A (enExample) |
| NZ (1) | NZ615593A (enExample) |
| PE (1) | PE20140601A1 (enExample) |
| PH (1) | PH12013502077A1 (enExample) |
| SG (1) | SG193919A1 (enExample) |
| TN (1) | TN2013000392A1 (enExample) |
| TW (1) | TWI602567B (enExample) |
| UA (1) | UA110961C2 (enExample) |
| WO (1) | WO2012148846A1 (enExample) |
| ZA (1) | ZA201306973B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2014005414A (es) * | 2011-11-02 | 2014-09-22 | Novartis Ag | Derivados de 2-carboxamida-cicloamino-urea para su uso en el tratamiento de las enfermedades dependientes del factor de crecimiento endotelial vascular (vegf). |
| HK1219421A1 (zh) * | 2013-03-15 | 2017-04-07 | 因特利凯有限责任公司 | 激酶抑制剂的组合及其用途 |
| EA201690987A1 (ru) * | 2013-11-13 | 2016-10-31 | Новартис Аг | Низкодозовые иммуностимулирующие ингибиторы mtor и их применения |
| AU2015216590A1 (en) * | 2014-02-11 | 2016-06-30 | Novartis Ag | Pharmaceutical combinations comprising a PI3K inhibitor for the treatment of cancer |
| WO2015148626A1 (en) * | 2014-03-26 | 2015-10-01 | Millennium Pharmaceuticals, Inc. | Treatment of fibrotic disorders |
| EP3200772B1 (en) * | 2014-10-03 | 2022-08-03 | Novartis AG | Pharmaceutical compositions comprising alpelisib |
| US20160339030A1 (en) * | 2015-05-19 | 2016-11-24 | University Of Maryland, Baltimore | Treatment agents for inhibiting hiv and cancer in hiv infected patients |
| JP6691337B2 (ja) * | 2016-02-29 | 2020-04-28 | 学校法人北里研究所 | 膀胱癌患者の予後を予測するための方法 |
| GB202010627D0 (en) * | 2020-07-10 | 2020-08-26 | Qbd (Qs-Ip) Ltd | Blocking method |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT98990A (pt) | 1990-09-19 | 1992-08-31 | American Home Prod | Processo para a preparacao de esteres de acidos carboxilicos de rapamicina |
| US5120842A (en) | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5100883A (en) | 1991-04-08 | 1992-03-31 | American Home Products Corporation | Fluorinated esters of rapamycin |
| US5118678A (en) | 1991-04-17 | 1992-06-02 | American Home Products Corporation | Carbamates of rapamycin |
| US5118677A (en) | 1991-05-20 | 1992-06-02 | American Home Products Corporation | Amide esters of rapamycin |
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| BR9408323A (pt) | 1993-12-17 | 1997-08-19 | Sandoz Ag | Derivados de rapamicina |
| DE69624921T2 (de) | 1995-06-09 | 2003-09-11 | Novartis Ag, Basel | Rapamycinderivate |
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| AR044519A1 (es) * | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| AU2006315512B2 (en) * | 2005-11-14 | 2012-11-01 | Ariad Pharmaceuticals, Inc. | Administration of an mTOR inhibitor to treat patients with cancer |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| CA2736361C (en) * | 2008-10-31 | 2017-10-10 | Novartis Ag | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor |
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2012
- 2012-04-23 WO PCT/US2012/034647 patent/WO2012148846A1/en not_active Ceased
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- 2012-04-23 UA UAA201311138A patent/UA110961C2/uk unknown
- 2012-04-23 PE PE2013002391A patent/PE20140601A1/es not_active Application Discontinuation
- 2012-04-23 KR KR1020137027718A patent/KR101925656B1/ko not_active Expired - Fee Related
- 2012-04-23 US US14/113,316 patent/US20140066474A1/en not_active Abandoned
- 2012-04-23 JP JP2014508463A patent/JP6086902B2/ja not_active Expired - Fee Related
- 2012-04-23 SG SG2013070461A patent/SG193919A1/en unknown
- 2012-04-23 CA CA2833962A patent/CA2833962A1/en not_active Abandoned
- 2012-04-23 CN CN201280020528.4A patent/CN103491955B/zh not_active Expired - Fee Related
- 2012-04-23 PH PH1/2013/502077A patent/PH12013502077A1/en unknown
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- 2012-04-23 EA EA201391565A patent/EA025948B1/ru not_active IP Right Cessation
- 2012-04-23 AU AU2012250010A patent/AU2012250010A1/en not_active Abandoned
- 2012-04-23 EP EP12717568.5A patent/EP2701703A1/en not_active Withdrawn
- 2012-04-23 BR BR112013027486A patent/BR112013027486A2/pt not_active Application Discontinuation
- 2012-04-24 TW TW101114591A patent/TWI602567B/zh not_active IP Right Cessation
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2013
- 2013-09-17 ZA ZA2013/06973A patent/ZA201306973B/en unknown
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- 2016-10-27 US US15/335,957 patent/US20170095463A1/en not_active Abandoned
- 2016-11-18 JP JP2016224893A patent/JP2017061527A/ja active Pending
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2017
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