AR074558A1 - 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
- AR074558A1 AR074558A1 ARP090104760A ARP090104760A AR074558A1 AR 074558 A1 AR074558 A1 AR 074558A1 AR P090104760 A ARP090104760 A AR P090104760A AR P090104760 A ARP090104760 A AR P090104760A AR 074558 A1 AR074558 A1 AR 074558A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compounds
- synthesis
- compound
- useful
- 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 11
- 230000015572 biosynthetic process Effects 0.000 abstract 4
- 238000003786 synthesis reaction Methods 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 229940127291 Calcium channel antagonist Drugs 0.000 abstract 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- -1 Spiro azepan oxazolidinones Chemical class 0.000 abstract 1
- 210000001744 T-lymphocyte Anatomy 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 239000000480 calcium channel blocker Substances 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 229910052805 deuterium Inorganic materials 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 230000007823 neuropathy Effects 0.000 abstract 1
- 201000001119 neuropathy Diseases 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
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Child & Adolescent Psychology (AREA)
- Biomedical Technology (AREA)
- Emergency Medicine (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Espiro azepan oxazolidinonas como bloqueadores del canal de calcio Kv1.3 voltaje dependiente, a composiciones farmacéuticas que contienen estos compuestos, a métodos para preparar los compuestos, a compuestos intermedios útiles para su síntesis. Usos de tales compuestos y composiciones, particularmente a su uso para administrarlos a pacientes para lograr un efecto terapéutico en diabetes y neuropatías inflamatorias, incluyendo enfermedades autoinmunes en las cuales las células T actúan como mediador, tales como artritis reumatoide y esclerosis múltiple. Reivindicación 1: Un compuesto de fórmula (1), o un tautómero, estereoisómero, o una sal farmacológicamente aceptable de cualquiera de los precedentes, caracterizado por la fórmula (1) donde R1 y R2 son independientemente hidrógeno, deuterio, flúor, CF3 o alquilo C1-3, no substituido o substituido con uno o más átomos de flúor; n es 0, 1 ó 2; R3 se selecciona entre halógeno, alquilo C1-3, CF3, CN, NH2, NHAc, OH, OCH3, u OCF3; m es 0 (cero), 1, 2 ó 3; R4 se selecciona entre halógeno, alquilo C1-3, CF3, CN, NH2, NHAc, OH, OCH3, u OCF3, o (R4)m y el anillo fenilo al cual está unido forman un grupo naftilo. Reivindicación 7: Un compuesto de fórmula (2), útil en la síntesis de los compuestos de fórmula (1), donde R1, R2, n y R3 tienen los significados dados en la reivindicación 1. Reivindicación 8: Un compuesto de fórmula (3), útil en la síntesis de los compuestos de fórmula (1), donde R1, R2, n y R3 tienen los significados dados en la reivindicación 1. Reivindicación 9: Un compuesto de fórmula (4), útil en la síntesis de los compuestos de fórmula (1), donde R1, R2, n y R3 tienen los significados dados en la reivindicación 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08171421 | 2008-12-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074558A1 true AR074558A1 (es) | 2011-01-26 |
Family
ID=40513443
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104760A AR074558A1 (es) | 2008-12-12 | 2009-12-09 | 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 (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HK1201048A1 (en) | 2011-10-03 | 2015-08-21 | The Regents Of The University Of California | Treatment of obesity and obesity-related disorders by pharmacological targeting of kv1.3 potassium channels |
| KR20150075091A (ko) * | 2012-10-29 | 2015-07-02 | 에프. 호프만-라 로슈 아게 | 3,4-이치환된 옥사졸리디논 유도체 및 칼슘 활성화 칼륨 채널의 억제제로서 이의 용도 |
| 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 |
| 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 |
| 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 |
| KR20220079575A (ko) * | 2019-10-07 | 2022-06-13 | 디.이. 쇼우 리서치, 엘엘씨 | Kv1.3 칼륨 셰이커 채널 차단제로서의 아릴 헤테로비시클릭 화합물 |
| WO2021071812A1 (en) * | 2019-10-07 | 2021-04-15 | D.E Shaw Research, Llc | Arylmethylene heterocyclic compounds as kv1.3 potassium shaker channel blockers |
| JP7780440B2 (ja) * | 2019-10-07 | 2025-12-04 | ディー．イー．ショウ リサーチ，エルエルシー | Ｋｖ１．３カリウムシェーカーチャネル遮断薬としてのアリール複素二環式化合物 |
| 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 |
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 TW TW098142079A patent/TW201026708A/zh unknown
- 2009-12-09 AR ARP090104760A patent/AR074558A1/es unknown
- 2009-12-10 BR BRPI0922714A patent/BRPI0922714A2/pt not_active IP Right Cessation
- 2009-12-10 EA EA201170801A patent/EA201170801A1/ru unknown
- 2009-12-10 CA CA2743557A patent/CA2743557A1/en not_active Abandoned
- 2009-12-10 KR KR1020117016047A patent/KR20110110165A/ko not_active Withdrawn
- 2009-12-10 US US13/133,042 patent/US8575148B2/en not_active Expired - Fee Related
- 2009-12-10 JP JP2011540106A patent/JP2012511546A/ja active Pending
- 2009-12-10 EP EP09765127A patent/EP2376501A1/en not_active Withdrawn
- 2009-12-10 WO PCT/EP2009/066836 patent/WO2010066840A1/en not_active Ceased
- 2009-12-10 AU AU2009324358A patent/AU2009324358A1/en not_active Abandoned
- 2009-12-10 PE PE2011001198A patent/PE20110772A1/es not_active Application Discontinuation
- 2009-12-10 MX MX2011006221A patent/MX2011006221A/es not_active Application Discontinuation
- 2009-12-10 CN CN2009801494792A patent/CN102333782A/zh active Pending
-
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 |
|---|---|
| US20110237569A1 (en) | 2011-09-29 |
| EA201170801A1 (ru) | 2011-12-30 |
| US8575148B2 (en) | 2013-11-05 |
| ZA201104041B (en) | 2012-11-28 |
| TW201026708A (en) | 2010-07-16 |
| CO6390036A2 (es) | 2012-02-29 |
| EP2376501A1 (en) | 2011-10-19 |
| KR20110110165A (ko) | 2011-10-06 |
| PE20110772A1 (es) | 2011-10-19 |
| WO2010066840A1 (en) | 2010-06-17 |
| MX2011006221A (es) | 2011-06-28 |
| DOP2011000164A (es) | 2011-06-30 |
| BRPI0922714A2 (pt) | 2016-01-05 |
| AU2009324358A1 (en) | 2011-06-23 |
| CR20110302A (es) | 2011-10-27 |
| ECSP11011118A (es) | 2011-07-29 |
| IL212948A0 (en) | 2011-07-31 |
| CN102333782A (zh) | 2012-01-25 |
| CA2743557A1 (en) | 2010-06-17 |
| JP2012511546A (ja) | 2012-05-24 |
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| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |