ES2570183T3 - Combinaciones de agentes terapéuticos para uso en el tratamiento de enfermedades neurodegenerativas - Google Patents
Combinaciones de agentes terapéuticos para uso en el tratamiento de enfermedades neurodegenerativasInfo
- Publication number
- ES2570183T3 ES2570183T3 ES12705457T ES12705457T ES2570183T3 ES 2570183 T3 ES2570183 T3 ES 2570183T3 ES 12705457 T ES12705457 T ES 12705457T ES 12705457 T ES12705457 T ES 12705457T ES 2570183 T3 ES2570183 T3 ES 2570183T3
- Authority
- ES
- Spain
- Prior art keywords
- disease
- mtor
- methyl
- formula
- treatment
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 230000004770 neurodegeneration Effects 0.000 title abstract 2
- 208000015122 neurodegenerative disease Diseases 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- 229940124597 therapeutic agent Drugs 0.000 title 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 abstract 4
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 abstract 4
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical group O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 abstract 3
- 239000000126 substance Substances 0.000 abstract 3
- -1 2-hydroxyethoxy Chemical group 0.000 abstract 2
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical group C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 abstract 2
- 229940125528 allosteric inhibitor Drugs 0.000 abstract 2
- 230000003197 catalytic effect Effects 0.000 abstract 2
- 229950006418 dactolisib Drugs 0.000 abstract 2
- 229960005167 everolimus Drugs 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- 208000002569 Machado-Joseph Disease Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000036834 Spinocerebellar ataxia type 3 Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- AKWHREAVLKZDDE-UHFFFAOYSA-N hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone Chemical compound CCCCCCCC=CC=CC=CCCCC(=O)CCC=CCC(=O)CCCC(=O)CCCCCCC(=O)C(C)=O AKWHREAVLKZDDE-UHFFFAOYSA-N 0.000 abstract 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Substances OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 abstract 1
- 230000001537 neural effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/4353—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
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Una combinación de un inhibidor alostérico de mTOR y un inhibidor catalítico de mTOR para uso en el tratamiento o prevención de una enfermedad neurodegenerativa seleccionada de enfermedad de Huntington, enfermedad de Parkinson, ataxia espinocerebelar tipo 3, enfermedad de Alzheimer y enfermedad neuronal motora en donde el inhibidor alostérico de mTOR es RAD001 y el inhibidor catalítico de mTOR es BEZ235 o CCG168; en donde RAD001 tiene el siguiente nombre y estructura química: (1R,9S,12S,15R, 16E, 18R, 19R, 21R, 23S, 24E, 26E, 28E, 30S, 32S, 35R)-1,18-dihidroxi-12-{(1R)-2-[(1S,3R,4R)-4- (2-hidroxietoxi)-3-metoxiciclohexil]-1-metiletil}-19,30-dimetoxi-15,17,21,23,29,35-hexametil-11,36-dioxa-4-azatriciclo[ 30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-2,3,10,14,20-pentaona**Fórmula** BEZ235 tiene el siguiente nombre químico y estructura: 2-metil-2-[4-(3-metil-2-oxo-8-quinolin-3-il-2,3- dihidroimidazo[4,5-c]quinolin-1-il)-fenil]-propionitrilo**Fórmula** y CCG168 tiene el siguiente nombre químico y estructura: {5-[2,4-bis-((S)-3-metil-morfolin-4-il)-pirido[2,3d]pirimidin-7- il]-2-metoxi-fenil}-metanol**Fórmula**
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161443493P | 2011-02-16 | 2011-02-16 | |
| PCT/IB2012/050669 WO2012110953A1 (en) | 2011-02-16 | 2012-02-14 | Combinations of therapeutic agents for use in the treatment of neurodegenerative diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2570183T3 true ES2570183T3 (es) | 2016-05-17 |
Family
ID=45755442
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12705457T Active ES2570183T3 (es) | 2011-02-16 | 2012-02-14 | Combinaciones de agentes terapéuticos para uso en el tratamiento de enfermedades neurodegenerativas |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9358236B2 (es) |
| EP (1) | EP2675450B1 (es) |
| JP (1) | JP5957469B2 (es) |
| CN (1) | CN103391780B (es) |
| ES (1) | ES2570183T3 (es) |
| WO (1) | WO2012110953A1 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016537345A (ja) * | 2013-11-13 | 2016-12-01 | ノバルティス アーゲー | 免疫応答を増強するためのｍＴＯＲ阻害剤 |
| GB2539161A (en) * | 2014-11-26 | 2016-12-14 | Neuro-Bio Ltd | Neurodegenerative disorders |
| CN107847491A (zh) * | 2015-05-20 | 2018-03-27 | 诺华公司 | 依维莫司(everolimus)与达托里昔布(dactolisib)的医药组合 |
| CN110114070A (zh) | 2016-11-23 | 2019-08-09 | 诺华公司 | 使用依维莫司(everolimus)、达托里昔布(dactolisib)或二者增强免疫反应的方法 |
| CN110869054B (zh) * | 2017-07-04 | 2022-06-07 | 比诺斯生物科技有限公司 | 大环氮杂吡啶环蕃金属复合物在治疗疾病中的用途 |
| UY37900A (es) | 2017-09-26 | 2019-04-30 | Novartis Ag | Nuevos derivados de rapamicina |
| WO2019157516A1 (en) * | 2018-02-12 | 2019-08-15 | resTORbio, Inc. | Combination therapies |
| AU2019409366B2 (en) | 2018-12-18 | 2022-10-27 | Novartis Ag | Rapamycin derivatives |
| AU2021241718B2 (en) * | 2020-03-27 | 2025-03-27 | Aeovian Pharmaceuticals, Inc. | mTORC1 modulators and uses thereof |
| TW202206093A (zh) * | 2020-08-12 | 2022-02-16 | 中國醫藥大學 | Ｓｅｍａ３ｄ拮抗劑用於預防或治療神經退化性疾病以及延長壽命之用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CN101616672A (zh) * | 2007-02-20 | 2009-12-30 | 诺瓦提斯公司 | 作为脂质激酶和mTOR双重抑制剂的咪唑并喹啉类 |
| EP2349275B1 (en) * | 2008-10-31 | 2017-03-08 | Novartis AG | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor. |
| US20100233733A1 (en) * | 2009-02-10 | 2010-09-16 | Nodality, Inc., A Delaware Corporation | Multiple mechanisms for modulation of the pi3 kinase pathway |
| EP2416792A4 (en) * | 2009-04-10 | 2012-10-24 | Haiyan Qi | NOVEL ANTI-AGING AGENTS AND METHODS OF IDENTIFICATION |
| US20120114637A1 (en) * | 2009-05-04 | 2012-05-10 | Santen Pharmaceutical Co., Ltd. | Mtor pathway inhibitors for treating ocular disorders |
| AR083267A1 (es) * | 2010-10-04 | 2013-02-13 | Novartis Ag | Combinaciones farmaceuticas |
-
2012
- 2012-02-14 US US13/985,346 patent/US9358236B2/en not_active Expired - Fee Related
- 2012-02-14 CN CN201280009288.8A patent/CN103391780B/zh not_active Expired - Fee Related
- 2012-02-14 JP JP2013554038A patent/JP5957469B2/ja not_active Expired - Fee Related
- 2012-02-14 WO PCT/IB2012/050669 patent/WO2012110953A1/en not_active Ceased
- 2012-02-14 ES ES12705457T patent/ES2570183T3/es active Active
- 2012-02-14 EP EP12705457.5A patent/EP2675450B1/en not_active Not-in-force
Also Published As
| Publication number | Publication date |
|---|---|
| US20130331388A1 (en) | 2013-12-12 |
| JP5957469B2 (ja) | 2016-07-27 |
| WO2012110953A1 (en) | 2012-08-23 |
| JP2014505722A (ja) | 2014-03-06 |
| EP2675450B1 (en) | 2016-02-10 |
| US9358236B2 (en) | 2016-06-07 |
| CN103391780A (zh) | 2013-11-13 |
| EP2675450A1 (en) | 2013-12-25 |
| CN103391780B (zh) | 2015-08-19 |
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