DOP2011000164A - Espiro azepan oxazolidinonas como bloqueadores del canal de potasio kv1.3 - Google Patents
Espiro azepan oxazolidinonas como bloqueadores del canal de potasio kv1.3Info
- Publication number
- DOP2011000164A DOP2011000164A DO2011000164A DO2011000164A DOP2011000164A DO P2011000164 A DOP2011000164 A DO P2011000164A DO 2011000164 A DO2011000164 A DO 2011000164A DO 2011000164 A DO2011000164 A DO 2011000164A DO P2011000164 A DOP2011000164 A DO P2011000164A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- compounds
- azepan
- methods
- prepare
- blockers
- Prior art date
Links
- 102000004257 Potassium Channel Human genes 0.000 title 1
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 title 1
- 108020001213 potassium channel Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 238000000034 method Methods 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 229940127291 Calcium channel antagonist Drugs 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 210000001744 T-lymphocyte Anatomy 0.000 abstract 1
- 206010052779 Transplant rejections Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000000480 calcium channel blocker Substances 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 230000007823 neuropathy Effects 0.000 abstract 1
- 201000001119 neuropathy Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- -1 spiro azepan oxazolidinones Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- 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
- C07D498/10—Spiro-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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Child & Adolescent Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Esta invención se refiere a espiro azepan oxazolidinonas como bloqueadores del canal de calcio Kvl.3 vo1taje dependiente, a composiciones farmacéuticas que contienen estos compuestos, a métodos para preparar los compuestos, a métodos para preparar nuevos compuestos intermedios útiles para su síntesis, y a métodos para preparar composiciones. La invención también se refiere a los usos de tales compuestos y composiciones, particularmente a su uso para administrarlos a pacientes para lograr un efecto terapéutico en diabetes, psoriasis, obesidad, rechazo al trasplante y neuropatías inflamatorias, incluyendo enfermedades autoìnmunes en las cuales las células T actúan como mediador, tales como artritis reumatoide y esclerosis múltiple. Los compuestos tienen la fórmula (1) donde los símbolos tienen los significados dados en la memoria descriptiva.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12191308P | 2008-12-12 | 2008-12-12 | |
| EP08171421 | 2008-12-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DOP2011000164A true DOP2011000164A (es) | 2011-06-30 |
Family
ID=40513443
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DO2011000164A DOP2011000164A (es) | 2008-12-12 | 2011-05-31 | Espiro azepan oxazolidinonas como bloqueadores del canal de potasio kv1.3 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US8575148B2 (es) |
| EP (1) | EP2376501A1 (es) |
| JP (1) | JP2012511546A (es) |
| KR (1) | KR20110110165A (es) |
| CN (1) | CN102333782A (es) |
| AR (1) | AR074558A1 (es) |
| AU (1) | AU2009324358A1 (es) |
| BR (1) | BRPI0922714A2 (es) |
| CA (1) | CA2743557A1 (es) |
| CO (1) | CO6390036A2 (es) |
| CR (1) | CR20110302A (es) |
| DO (1) | DOP2011000164A (es) |
| EA (1) | EA201170801A1 (es) |
| EC (1) | ECSP11011118A (es) |
| IL (1) | IL212948A0 (es) |
| MX (1) | MX2011006221A (es) |
| PE (1) | PE20110772A1 (es) |
| TW (1) | TW201026708A (es) |
| WO (1) | WO2010066840A1 (es) |
| ZA (1) | ZA201104041B (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201401193XA (en) * | 2011-10-03 | 2014-05-29 | Univ California | TREATMENT OF OBESITY AND OBESITY-RELATED DISORDERS BY PHARMACOLOGICAL TARGETING OF Kv1.3 POTASSIUM CHANNELS |
| IN2015DN00961A (es) | 2012-10-29 | 2015-06-12 | Hoffmann La Roche | |
| TWI698438B (zh) | 2015-03-13 | 2020-07-11 | 德商４Ｓｃ製藥公司 | Ｋv１.３抑制劑及其醫學應用 |
| TWI701249B (zh) | 2015-03-13 | 2020-08-11 | 德商４Ｓｃ製藥公司 | Ｋv１.３抑制劑及其醫學應用 |
| CN109053751A (zh) * | 2018-08-30 | 2018-12-21 | 成都海博锐药业有限公司 | 具有螺环结构的fxr调节剂 |
| WO2020252130A1 (en) * | 2019-06-12 | 2020-12-17 | Lieber Institute, Inc. | Kv11.1-3.1 inhibiting methods and compositions |
| MX2022004145A (es) * | 2019-10-07 | 2022-06-14 | De Shaw Res Llc | Compuestos heterociclicos de arilmetileno como bloqueadores del canal de potasio tipo shaker kv1.3. |
| BR112022006292A2 (pt) * | 2019-10-07 | 2022-06-28 | De Shaw Res Llc | Compostos heterobicílicos de arila como bloqueadores de canais de agitador de potássio kv1.3 |
| AU2020363354A1 (en) * | 2019-10-07 | 2022-04-21 | D.E. Shaw Research, Llc | Aryl heterobicyclic compounds as Kv1.3 potassium shaker channel blockers |
| CN111574537B (zh) * | 2020-05-20 | 2022-11-15 | 成都药明康德新药开发有限公司 | 叔丁基-8-氧杂-3,11-二氮杂螺[5.6]十二烷-3-甲酸基酯的合成方法 |
| AU2022364718A1 (en) * | 2021-10-13 | 2024-05-16 | Vanqua Bio, Inc. | Small molecule modulators of glucocerebrosidase activity and uses thereof |
| EP4610260A4 (en) * | 2022-10-28 | 2025-11-26 | Shanghai Shenshi Wise Tech Co Ltd | Aryl heterocyclic kv1.3 inhibitor, preparation method therefor, and use thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6303637B1 (en) | 1998-10-30 | 2001-10-16 | Merck & Co., Inc. | Heterocyclic potassium channel inhibitors |
-
2009
- 2009-12-09 AR ARP090104760A patent/AR074558A1/es unknown
- 2009-12-09 TW TW098142079A patent/TW201026708A/zh unknown
- 2009-12-10 WO PCT/EP2009/066836 patent/WO2010066840A1/en not_active Ceased
- 2009-12-10 PE PE2011001198A patent/PE20110772A1/es not_active Application Discontinuation
- 2009-12-10 AU AU2009324358A patent/AU2009324358A1/en not_active Abandoned
- 2009-12-10 JP JP2011540106A patent/JP2012511546A/ja active Pending
- 2009-12-10 CA CA2743557A patent/CA2743557A1/en not_active Abandoned
- 2009-12-10 CN CN2009801494792A patent/CN102333782A/zh active Pending
- 2009-12-10 EA EA201170801A patent/EA201170801A1/ru unknown
- 2009-12-10 KR KR1020117016047A patent/KR20110110165A/ko not_active Withdrawn
- 2009-12-10 EP EP09765127A patent/EP2376501A1/en not_active Withdrawn
- 2009-12-10 MX MX2011006221A patent/MX2011006221A/es not_active Application Discontinuation
- 2009-12-10 US US13/133,042 patent/US8575148B2/en not_active Expired - Fee Related
- 2009-12-10 BR BRPI0922714A patent/BRPI0922714A2/pt not_active IP Right Cessation
-
2011
- 2011-05-17 IL IL212948A patent/IL212948A0/en unknown
- 2011-05-31 ZA ZA2011/04041A patent/ZA201104041B/en unknown
- 2011-05-31 DO DO2011000164A patent/DOP2011000164A/es unknown
- 2011-06-03 CR CR20110302A patent/CR20110302A/es not_active Application Discontinuation
- 2011-06-08 CO CO11070889A patent/CO6390036A2/es not_active Application Discontinuation
- 2011-06-09 EC EC2011011118A patent/ECSP11011118A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102333782A (zh) | 2012-01-25 |
| IL212948A0 (en) | 2011-07-31 |
| ZA201104041B (en) | 2012-11-28 |
| PE20110772A1 (es) | 2011-10-19 |
| JP2012511546A (ja) | 2012-05-24 |
| KR20110110165A (ko) | 2011-10-06 |
| WO2010066840A1 (en) | 2010-06-17 |
| AU2009324358A1 (en) | 2011-06-23 |
| CO6390036A2 (es) | 2012-02-29 |
| US8575148B2 (en) | 2013-11-05 |
| MX2011006221A (es) | 2011-06-28 |
| BRPI0922714A2 (pt) | 2016-01-05 |
| CA2743557A1 (en) | 2010-06-17 |
| US20110237569A1 (en) | 2011-09-29 |
| ECSP11011118A (es) | 2011-07-29 |
| EP2376501A1 (en) | 2011-10-19 |
| EA201170801A1 (ru) | 2011-12-30 |
| CR20110302A (es) | 2011-10-27 |
| TW201026708A (en) | 2010-07-16 |
| AR074558A1 (es) | 2011-01-26 |
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