AR083905A1 - Forma cristalina de un inhibidor de la interaccion de mdm2/4 y p53 - Google Patents
Forma cristalina de un inhibidor de la interaccion de mdm2/4 y p53Info
- Publication number
- AR083905A1 AR083905A1 ARP110104289A ARP110104289A AR083905A1 AR 083905 A1 AR083905 A1 AR 083905A1 AR P110104289 A ARP110104289 A AR P110104289A AR P110104289 A ARP110104289 A AR P110104289A AR 083905 A1 AR083905 A1 AR 083905A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- phenyl
- mdm2
- isoquinolin
- piperazin
- Prior art date
Links
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 title abstract 2
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 title abstract 2
- 230000003993 interaction Effects 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical class OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 abstract 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 abstract 2
- 150000003467 sulfuric acid derivatives Chemical class 0.000 abstract 2
- CLRSLRWKONPSRQ-CPOWQTMSSA-N (1s)-1-(4-chlorophenyl)-6-methoxy-2-[4-[methyl-[[4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl]methyl]amino]phenyl]-7-propan-2-yloxy-1,4-dihydroisoquinolin-3-one Chemical compound C1([C@@H]2N(C(=O)CC=3C=C(C(=CC=32)OC(C)C)OC)C=2C=CC(=CC=2)N(C)CC2CCC(CC2)N2CC(=O)N(C)CC2)=CC=C(Cl)C=C1 CLRSLRWKONPSRQ-CPOWQTMSSA-N 0.000 abstract 1
- 229910002483 Cu Ka Inorganic materials 0.000 abstract 1
- 102000017274 MDM4 Human genes 0.000 abstract 1
- 108050005300 MDM4 Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Una forma cristalina de la (S)-1-(4-cloro-fenil)-7-isopropoxi-6-metoxi-2-(4-{metil-[4-(4-metil-3-oxo-piperazin-1-il)-trans-ciclohexil-metil]-amino}-fenil)-1,4-dihidro-2H-isoquinolin-3-ona, la cual es útil en el tratamiento de una enfermedad o de un trastorno asociado con la interacción entre p53, o variantes de la misma, y MDM2 y/o MDM4, o variantes de las mismas, respectivamente y su composición farmacéutica.Reivindicación 2: Una forma cristalina de la sal de sulfato de la (S)-1-(4-cloro-fenil)-7-isopropoxi-6-metoxi-2-(4-{metil-[4-(4-metil-3-oxo-piperazin-1-il)-trans-ciclohexil-metil]-amino}-fenil)-1,4-dihidro-2H-isoquinolin-3-ona como se reclama en la reivindicación 1, en donde la sal de sulfato es la sal de bisulfato. Reivindicación 3: Una forma cristalina de la sal de bisulfato de la (S)-1-(4-cloro-fenil)-7-isopropoxi-6-metoxi-2-(4-{metil-[4-(4-metil-3-oxo-piperazin-1-il)-trans-ciclohexil-metil]-amino}-fenil)-1,4-dihidro-2H-isoquinolin-3-ona, como se describe en la reivindicación 1 o en la reivindicación 2, la cual tiene un patrón de difracción en polvo de rayos-X, utilizando radiación de Cu Ka, que incluye los picos: 18.8, 21.3 y 22.7 ángulo 2-q º, con un error de ± 0.2º.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010078927 | 2010-11-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083905A1 true AR083905A1 (es) | 2013-04-10 |
Family
ID=45093718
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110104289A AR083905A1 (es) | 2010-11-19 | 2011-11-17 | Forma cristalina de un inhibidor de la interaccion de mdm2/4 y p53 |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US8969351B2 (es) |
| EP (1) | EP2640467B1 (es) |
| JP (1) | JP5667308B2 (es) |
| KR (1) | KR101561750B1 (es) |
| AR (1) | AR083905A1 (es) |
| AU (1) | AU2011331095B2 (es) |
| BR (1) | BR112013011966A2 (es) |
| CA (1) | CA2816810A1 (es) |
| CO (1) | CO6801719A2 (es) |
| CU (1) | CU24130B1 (es) |
| CY (1) | CY1116002T1 (es) |
| DK (1) | DK2640467T3 (es) |
| EC (1) | ECSP13012628A (es) |
| ES (1) | ES2528376T3 (es) |
| GT (1) | GT201300132A (es) |
| HR (1) | HRP20150231T1 (es) |
| IL (1) | IL226182A0 (es) |
| MA (1) | MA34666B1 (es) |
| ME (1) | ME02099B (es) |
| MX (1) | MX336634B (es) |
| MY (1) | MY160880A (es) |
| NZ (1) | NZ610296A (es) |
| PE (1) | PE20140420A1 (es) |
| PH (1) | PH12013500979A1 (es) |
| PL (1) | PL2640467T3 (es) |
| PT (1) | PT2640467E (es) |
| RS (1) | RS53770B1 (es) |
| RU (1) | RU2013127661A (es) |
| SG (1) | SG190186A1 (es) |
| SI (1) | SI2640467T1 (es) |
| SM (1) | SMT201500059B (es) |
| TW (1) | TWI520950B (es) |
| WO (1) | WO2012066095A1 (es) |
| ZA (1) | ZA201303155B (es) |
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| DK2118123T3 (en) | 2007-01-31 | 2016-01-25 | Dana Farber Cancer Inst Inc | Stabilized p53 peptides and uses thereof |
| KR101623985B1 (ko) | 2007-03-28 | 2016-05-25 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 스티칭된 폴리펩티드 |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| DK2603600T3 (da) | 2010-08-13 | 2019-03-04 | Aileron Therapeutics Inc | Peptidomimetiske makrocyklusser |
| BR112014009418A2 (pt) | 2011-10-18 | 2017-04-18 | Aileron Therapeutics Inc | macrociclos peptidomiméticos |
| US9408885B2 (en) * | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
| CN112500466B (zh) | 2012-02-15 | 2022-05-03 | 艾瑞朗医疗公司 | 拟肽大环化合物 |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| WO2013175417A1 (en) | 2012-05-24 | 2013-11-28 | Novartis Ag | Pyrrolopyrrolidinone compounds |
| WO2014071241A1 (en) | 2012-11-01 | 2014-05-08 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
| WO2014115080A1 (en) | 2013-01-22 | 2014-07-31 | Novartis Ag | Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction |
| US9403827B2 (en) | 2013-01-22 | 2016-08-02 | Novartis Ag | Substituted purinone compounds |
| BR112015029491A2 (pt) | 2013-05-27 | 2017-07-25 | Novartis Ag | derivados de imidazopirrolidinona e seu uso no tratamento de doença |
| MX2015016421A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. |
| ES2650562T3 (es) | 2013-05-28 | 2018-01-19 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona y su uso en el tratamiento de enfermedades |
| EP3071571A1 (en) | 2013-11-21 | 2016-09-28 | Novartis AG | Pyrrolopyrrolone derivatives and their use as bet inhibitors |
| BR112016012506A8 (pt) * | 2013-12-23 | 2018-01-30 | Novartis Ag | combinações farmacêuticas, seus usos, e uso de um portador de dados |
| ES2864352T3 (es) * | 2013-12-23 | 2021-10-13 | Novartis Ag | Combinaciones farmacéuticas |
| MX389354B (es) | 2014-09-24 | 2025-03-20 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y formulaciones de los mismos. |
| CA2961258A1 (en) | 2014-09-24 | 2016-03-31 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| CA2979847A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| TWI750129B (zh) | 2015-08-03 | 2021-12-21 | 瑞士商諾華公司 | 作為血液學毒性生物標記之ｇｄｆ-１５ |
| WO2017037579A1 (en) | 2015-08-28 | 2017-03-09 | Novartis Ag | Mdm2 inhibitors and combinations thereof |
| CN108348611A (zh) * | 2015-08-28 | 2018-07-31 | 诺华股份有限公司 | 使用pi3k抑制剂和mdm2抑制剂的联合疗法 |
| WO2017044633A1 (en) | 2015-09-10 | 2017-03-16 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles as modulators of mcl-1 |
| KR101838687B1 (ko) * | 2016-01-26 | 2018-03-15 | 한국생명공학연구원 | 나노포어를 이용한 단백질-단백질 상호작용 저해제 스크리닝 방법 |
| WO2017201449A1 (en) | 2016-05-20 | 2017-11-23 | Genentech, Inc. | Protac antibody conjugates and methods of use |
| SI3541387T1 (sl) | 2016-11-15 | 2021-08-31 | Novartis Ag | Odmerek in režim za zaviralce interakcije HDM2-P53 |
| WO2018092064A1 (en) | 2016-11-18 | 2018-05-24 | Novartis Ag | Combinations of mdm2 inhibitors and bcl-xl inhibitors |
| AU2017375958A1 (en) | 2016-12-12 | 2019-07-04 | Multivir Inc. | Methods and compositions comprising viral gene therapy and an immune checkpoint inhibitor for treatment and prevention of cancer and infectious diseases |
| US11413284B2 (en) | 2017-09-12 | 2022-08-16 | Novartis Ag | Protein kinase C inhibitors for treatment of uveal melanoma |
| CN111163781B (zh) | 2017-10-12 | 2023-05-16 | 诺华股份有限公司 | 用于治疗癌症的mdm2抑制剂与erk抑制剂的组合 |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
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-
2010
- 2010-12-21 CU CU2012000098A patent/CU24130B1/es active IP Right Grant
-
2011
- 2011-11-17 JP JP2013539265A patent/JP5667308B2/ja not_active Expired - Fee Related
- 2011-11-17 DK DK11790916.8T patent/DK2640467T3/en active
- 2011-11-17 BR BR112013011966A patent/BR112013011966A2/pt not_active IP Right Cessation
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