AR080177A1 - Derivados de piperidina, un procedimiento para su preparacion, y su uso en medicamentos para el tratamiento de enfermedades mentales asociadas a la deposicion del beta-amiloide en el cerebro. - Google Patents
Derivados de piperidina, un procedimiento para su preparacion, y su uso en medicamentos para el tratamiento de enfermedades mentales asociadas a la deposicion del beta-amiloide en el cerebro.Info
- Publication number
- AR080177A1 AR080177A1 ARP110100450A ARP110100450A AR080177A1 AR 080177 A1 AR080177 A1 AR 080177A1 AR P110100450 A ARP110100450 A AR P110100450A AR P110100450 A ARP110100450 A AR P110100450A AR 080177 A1 AR080177 A1 AR 080177A1
- Authority
- AR
- Argentina
- Prior art keywords
- halogen
- lower alkyl
- substituted
- optionally substituted
- lower alkoxy
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 102000013455 Amyloid beta-Peptides Human genes 0.000 title abstract 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 title abstract 2
- 210000004556 brain Anatomy 0.000 title abstract 2
- 230000008021 deposition Effects 0.000 title abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 230000003340 mental effect Effects 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 15
- 229910052736 halogen Inorganic materials 0.000 abstract 14
- 125000005843 halogen group Chemical group 0.000 abstract 11
- 125000003545 alkoxy group Chemical group 0.000 abstract 7
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 3
- 208000024667 ABeta amyloidosis, Dutch type Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 208000005314 Multi-Infarct Dementia Diseases 0.000 abstract 1
- 201000004810 Vascular dementia Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- -1 benzo [1,3] dioxolyl Chemical group 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P25/28—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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compuestos de formula: (I) hetarilo 1 es un grupo heteroarilo de cinco o seis elementos que contiene 1 a 3 heteroátomos seleccionados de entre O, S o N, hetarilo II es un grupo heteroarilo de cinco o seis elementos que contiene 1 a 3 heteroátomos seleccionados de entre O, S o N, o es un sistema anular de dos elementos que contiene 1 a 4 heteroátomos seleccionados de entre S, O o N, en el que por lo menos un anillo es de naturaleza aromática, R1 es alquilo inferior, alcoxi inferior, alquilo inferior sustituido con halogeno, o halogeno, R2 es halogeno, alquilo inferior, alcoxi inferior, hidroxi, alquilo inferior sustituido con halogeno, alquilo inferior sustituido con hidroxi o benzo[1 ,3]dioxolilo, o es fenilo, opcionalmente sustituido con halogeno, alquilo inferior, alcoxi inferior, S(O)2- alquilo inferior, ciano, nitro, alcoxi inferior sustituido con halogeno, dimetilamino, - (CH2)-NHC(O)O-alquilo inferior, o alquilo inferior sustituido con halogeno, y R es hidrogeno, halogeno, hidroxi o alcoxi inferior, o es cicloalquenilo o cicloalquilo, opcionalmente sustituido con hidroxi o alquilo inferior sustituido con halogeno,o es un grupo heteroarilo de cinco o seis elementos, que contiene 1 a 3 heteroátomos seleccionados de entre O, S o N, que se sustituye opcionalmente con halogeno, alquilo inferior, alcoxi inferior o dimetilamino, o es Ofenilo, opcionalmente sustituido con halogeno, o es heterocicloalquilo, opcionalmente sustituido con halogeno, hidroxi, alquilo inferior sustitutido con halogeno o C(O)O-alquilo inferior, R3 es hidrogeno, alquilo inferior, ciano o fenilo, R4 es alcoxi inferior, alquilo inferior o halogeno, p: esOol, n es 0, 1 o 2; en el caso de que n sea 2, R4 puede ser igual o diferente, m es 0, 1 o 2; en el caso de que m sea 2, R1 puede ser igual o diferente, es 0, 1, 2 o 3; en el caso de que o sea 2 o 3, R2 puede ser igual o diferente, o a sales de adicion de ácido farmacéuticamente activas de los mismos. Los compuestos de formula 1 son moduladores del amiloide beta y, de esta manera, pueden resultar utiles para el tratamiento o prevencion de una enfermedad asociada a la deposicion del í3- amiloide en el cerebro, en particular la enfermedad de Alzheimer, y otras enfermedades, tales como la angiopatía amiloide cerebral, la hemorragia cerebral hereditaria con amiloidosis, tipo Dutch (HCHWAD), la demencia multiinfarto, la demencia pugilística y el síndrome de Down.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10153843 | 2010-02-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080177A1 true AR080177A1 (es) | 2012-03-21 |
Family
ID=43757885
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100450A AR080177A1 (es) | 2010-02-17 | 2011-02-15 | Derivados de piperidina, un procedimiento para su preparacion, y su uso en medicamentos para el tratamiento de enfermedades mentales asociadas a la deposicion del beta-amiloide en el cerebro. |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8486967B2 (es) |
| EP (1) | EP2536710B1 (es) |
| JP (1) | JP5559362B2 (es) |
| KR (1) | KR101472648B1 (es) |
| CN (1) | CN103025724B (es) |
| AR (1) | AR080177A1 (es) |
| BR (1) | BR112012020607A2 (es) |
| CA (1) | CA2789058A1 (es) |
| CY (1) | CY1117976T1 (es) |
| DK (1) | DK2536710T3 (es) |
| ES (1) | ES2594491T3 (es) |
| HR (1) | HRP20161232T1 (es) |
| HU (1) | HUE028178T2 (es) |
| LT (1) | LT2536710T (es) |
| MX (1) | MX2012009545A (es) |
| PL (1) | PL2536710T3 (es) |
| PT (1) | PT2536710T (es) |
| RS (1) | RS55243B1 (es) |
| RU (1) | RU2554353C2 (es) |
| SI (1) | SI2536710T1 (es) |
| TW (1) | TW201130818A (es) |
| WO (1) | WO2011101304A2 (es) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8703763B2 (en) | 2011-03-02 | 2014-04-22 | Hoffmann-La Roche Inc. | Bridged piperidine derivatives |
| EP2527344A1 (en) | 2011-05-25 | 2012-11-28 | Almirall, S.A. | Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases |
| JP6479476B2 (ja) * | 2012-02-21 | 2019-03-06 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
| EA201690523A1 (ru) * | 2013-09-05 | 2016-07-29 | Ф. Хоффманн-Ля Рош Аг | Триазолопиридины, композиции и способы их применения |
| WO2015066696A1 (en) * | 2013-11-04 | 2015-05-07 | Forum Pharmaceuticals Inc. | Fused morphlinopyrimidines and methods of use thereof |
| WO2015090224A1 (zh) * | 2013-12-20 | 2015-06-25 | 中国人民解放军军事医学科学院毒物药物研究所 | 新型哌啶氨甲酰类化合物、制备方法及其用途 |
| WO2015138689A1 (en) * | 2014-03-13 | 2015-09-17 | Forum Pharmaceuticals Inc. | Fused morpholinopyrimidines and methods of use thereof |
| CN103896875B (zh) * | 2014-04-14 | 2015-10-14 | 仪征市海帆化工有限公司 | 一种5-乙氧基-3-三氯甲基-1,2,4-噻二唑的合成方法 |
| JP6831372B2 (ja) * | 2015-09-09 | 2021-02-17 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 架橋ピペリジン誘導体 |
| JP6872550B2 (ja) * | 2015-12-10 | 2021-05-19 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 架橋されたピペリジン誘導体 |
| JP7012715B2 (ja) * | 2016-06-27 | 2022-01-28 | エフ．ホフマン－ラ ロシュ アーゲー | γ－セクレターゼモジュレーターとしてのトリアゾロピリジン |
| AR109829A1 (es) * | 2016-09-29 | 2019-01-30 | Hoffmann La Roche | Derivados de piperidina puenteados |
| EP3523304B1 (en) * | 2016-10-04 | 2021-01-27 | H. Hoffnabb-La Roche Ag | Bicyclic heteroaryl derivatives |
| JP7111704B2 (ja) * | 2016-11-01 | 2022-08-02 | エフ．ホフマン－ラ ロシュ アーゲー | 二環式ヘテロアリール誘導体 |
| WO2019141832A1 (en) * | 2018-01-22 | 2019-07-25 | F. Hoffmann-La Roche Ag | Triazolo-azepine derivatives |
| MA53541B1 (fr) * | 2018-09-03 | 2024-02-29 | Hoffmann La Roche | Dérivés hétéroaryles bicycliques |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| RS65821B1 (sr) | 2018-12-13 | 2024-09-30 | Hoffmann La Roche | Derivati 7-fenoksi-n-(3-azabiciklo[3.2.1]oktan-8-il)-6,7-dihidro-5h-pirolo[1,2-b][1,2,4]triazol-2-amina i srodna jedinjenja kao modulatori gama-sekretaze za lečenje alchajmerove bolesti |
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| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| BR112022002698A2 (pt) | 2019-08-14 | 2022-07-19 | Incyte Corp | Compostos de imidazolil pirimidinilamina como inibidores de cdk2 |
| BR112022006977A2 (pt) | 2019-10-11 | 2022-09-20 | Incyte Corp | Aminas bicíclicas como inibidores de cdk2 |
| EP4146639A1 (en) | 2020-05-06 | 2023-03-15 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| TW202241889A (zh) | 2020-12-23 | 2022-11-01 | 美商雅捷可斯治療公司 | 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
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- 2011-02-14 WO PCT/EP2011/052101 patent/WO2011101304A2/en not_active Ceased
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Also Published As
| Publication number | Publication date |
|---|---|
| SI2536710T1 (sl) | 2016-11-30 |
| RU2554353C2 (ru) | 2015-06-27 |
| CN103025724A (zh) | 2013-04-03 |
| CY1117976T1 (el) | 2017-05-17 |
| US8486967B2 (en) | 2013-07-16 |
| LT2536710T (lt) | 2016-09-26 |
| EP2536710B1 (en) | 2016-07-13 |
| KR101472648B1 (ko) | 2014-12-15 |
| BR112012020607A2 (pt) | 2016-07-19 |
| RU2012137956A (ru) | 2014-03-27 |
| JP2013519701A (ja) | 2013-05-30 |
| WO2011101304A2 (en) | 2011-08-25 |
| PT2536710T (pt) | 2016-09-27 |
| ES2594491T3 (es) | 2016-12-20 |
| CN103025724B (zh) | 2015-02-11 |
| KR20120124489A (ko) | 2012-11-13 |
| RS55243B1 (sr) | 2017-02-28 |
| TW201130818A (en) | 2011-09-16 |
| HUE028178T2 (en) | 2016-12-28 |
| PL2536710T3 (pl) | 2017-01-31 |
| WO2011101304A3 (en) | 2011-10-20 |
| JP5559362B2 (ja) | 2014-07-23 |
| EP2536710A2 (en) | 2012-12-26 |
| HK1179958A1 (en) | 2013-10-11 |
| US20110201605A1 (en) | 2011-08-18 |
| HRP20161232T1 (hr) | 2016-11-04 |
| CA2789058A1 (en) | 2011-08-25 |
| MX2012009545A (es) | 2012-09-12 |
| DK2536710T3 (en) | 2016-08-22 |
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