MD4651B1 - Derivaţi de imidazopiridazine ca modulatori ai receptorului pentru GABAA - Google Patents
Derivaţi de imidazopiridazine ca modulatori ai receptorului pentru GABAA Download PDFInfo
- Publication number
- MD4651B1 MD4651B1 MDA20150051A MD20150051A MD4651B1 MD 4651 B1 MD4651 B1 MD 4651B1 MD A20150051 A MDA20150051 A MD A20150051A MD 20150051 A MD20150051 A MD 20150051A MD 4651 B1 MD4651 B1 MD 4651B1
- Authority
- MD
- Moldova
- Prior art keywords
- gabaa receptor
- receptor modulators
- derivatives
- imidazopyridazine derivatives
- imidazopyridazine
- Prior art date
Links
- 150000005233 imidazopyridazines Chemical class 0.000 title abstract 3
- 102000027484 GABAA receptors Human genes 0.000 title abstract 2
- 108091008681 GABAA receptors Proteins 0.000 title abstract 2
- DYPBSSSLPCNNAT-UHFFFAOYSA-N 4-(3-phenylphenyl)-5h-imidazo[4,5-c]pyridazine Chemical class C1=NN=C2NC=NC2=C1C(C=1)=CC=CC=1C1=CC=CC=C1 DYPBSSSLPCNNAT-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Cosmetics (AREA)
Abstract
Prezenta invenţie se referă la derivaţi de imidazopiridazine. În particular, aceasta se referă la derivaţi ai 4-(bifenil-3-il)-7H-imidazo[4,5-c]piridazinei cu formula (I):şi la sărurile farmaceutic acceptabile ale acestora, în care R1, R2, R3, R4 şi R5 au semnificaţiile definite în descriere.Derivaţii imidazopiridazinei, conform prezentei invenţii, modulează activitatea receptorului pentru GABAA. Ei sunt utili în tratamentul diferitor stări, inclusiv a durerii.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261737157P | 2012-12-14 | 2012-12-14 | |
| PCT/IB2013/060631 WO2014091368A1 (en) | 2012-12-14 | 2013-12-04 | Imidazopyridazine derivatives as gabaa receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MD20150051A2 MD20150051A2 (ro) | 2015-09-30 |
| MD4651B1 true MD4651B1 (ro) | 2019-09-30 |
Family
ID=49880883
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20150051A MD4651B1 (ro) | 2012-12-14 | 2013-12-04 | Derivaţi de imidazopiridazine ca modulatori ai receptorului pentru GABAA |
Country Status (43)
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3154979B1 (en) * | 2014-06-12 | 2018-03-07 | Pfizer Limited | Imidazopyridazine derivatives as modulators of the gabaa receptor activity. |
| PL3174858T3 (pl) | 2014-07-31 | 2019-10-31 | Basf Se | Sposób wytwarzania pirazoli |
| PE20180327A1 (es) | 2015-05-11 | 2018-02-13 | Basf Se | Proceso para preparar 4-amino-piridazinas |
| EP3386983A1 (en) * | 2015-12-10 | 2018-10-17 | Pfizer Limited | 4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain |
| JOP20190053A1 (ar) * | 2016-09-23 | 2019-03-21 | Novartis Ag | مركبات أزا إندازول للاستخدام في إصابات الأوتار و/ أو الرباط |
| PT3515894T (pt) * | 2016-09-23 | 2021-07-13 | Novartis Ag | Compostos indazolo para utilização em lesões de tendões e/ou ligamentos |
| WO2018082964A1 (en) | 2016-11-04 | 2018-05-11 | Basf Se | Process for the production of pyridazinyl-amides in a one-pot synthesis |
| WO2018202494A1 (de) | 2017-05-02 | 2018-11-08 | Bayer Aktiengesellschaft | 2-(het)aryl-substituierte kondensierte heterocyclen-derivate als schädlingsbekämpfungsmittel |
| KR20250099259A (ko) | 2017-06-06 | 2025-07-01 | 유로반트 사이언시즈 게엠베하 | 과민성 방광의 치료를 위한 비베그론의 용도 |
| EP3796907A4 (en) * | 2018-05-22 | 2021-11-03 | Neurocycle Therapeutics, Inc. | GABAA POSITIVE ALLOSTERIC MODULATING COMPOUNDS FOR THE TREATMENT OF PRURITUS AND / OR DERMATITIS |
| TWI752400B (zh) * | 2019-01-07 | 2022-01-11 | 美商美國禮來大藥廠 | Il-17a抑制劑 |
| CN116693555B (zh) * | 2022-02-25 | 2025-07-04 | 上海赛默罗生物科技有限公司 | 咪唑并哒嗪类衍生物、其制备方法、药物组合物和用途 |
| CN117069725A (zh) * | 2022-05-10 | 2023-11-17 | 上海赛默罗生物科技有限公司 | 咪唑并哒嗪取代苯环类衍生物、制备方法、药物组合物及用途 |
| CN116655475B (zh) * | 2023-05-19 | 2024-12-31 | 山东轩鸿生物医药有限公司 | 一种盐酸氟西汀的制备方法 |
| WO2025137437A1 (en) | 2023-12-21 | 2025-06-26 | Pfizer Inc. | Solid forms of a gabaa receptor modulator and methods of its use |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| WO2000035296A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Improved release of medicament active agents from a chewing gum coating |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| US6365589B1 (en) * | 1998-07-02 | 2002-04-02 | Bristol-Myers Squibb Pharma Company | Imidazo-pyridines, -pyridazines, and -triazines as corticotropin releasing factor antagonists |
| JP4302980B2 (ja) | 2000-11-10 | 2009-07-29 | メルク シャープ エンド ドーム リミテッド | Ｇａｂａ受容体リガンドとしてのイミダゾ−トリアジン誘導体 |
| GB0117277D0 (en) * | 2001-07-16 | 2001-09-05 | Merck Sharp & Dohme | Therapeutic agents |
| EP1713784A1 (en) * | 2004-02-12 | 2006-10-25 | Neurogen Corporation | Imidazo-pyridazines, triazolo-pyridazines and related benzodiazepine receptor ligands |
| WO2006078891A2 (en) | 2005-01-21 | 2006-07-27 | Neurogen Corporation | Imidazolylmethyl and pyrazolylmethyl heteroaryl derivatives |
| EP1845098A1 (en) * | 2006-03-29 | 2007-10-17 | Ferrer Internacional, S.A. | Imidazo[1,2-b]pyridazines, their processes of preparation and their use as GABA receptor ligands |
| DE602008000809D1 (de) | 2007-03-23 | 2010-04-29 | Icagen Inc | Ionenkanal-Hemmer |
| NZ593473A (en) | 2009-01-12 | 2013-02-22 | Pfizer Ltd | Sulfonamide derivatives |
| NZ599597A (en) * | 2009-10-30 | 2013-05-31 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
| CA2803118C (en) * | 2010-07-09 | 2015-11-03 | Pfizer Limited | Sulfonamide derivatives as nav 1.7 inhibitors |
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2013
- 2013-04-12 UA UAA201504677A patent/UA112028C2/uk unknown
- 2013-12-04 HR HRP20161559TT patent/HRP20161559T1/hr unknown
- 2013-12-04 CN CN201380065006.0A patent/CN104837843B/zh active Active
- 2013-12-04 AU AU2013356894A patent/AU2013356894B2/en active Active
- 2013-12-04 ME MEP-2016-258A patent/ME02566B/me unknown
- 2013-12-04 PE PE2015000912A patent/PE20151163A1/es not_active Application Discontinuation
- 2013-12-04 CU CUP2015000058A patent/CU24338B1/es unknown
- 2013-12-04 EA EA201590761A patent/EA025635B1/ru not_active IP Right Cessation
- 2013-12-04 WO PCT/IB2013/060631 patent/WO2014091368A1/en not_active Ceased
- 2013-12-04 MA MA38112A patent/MA38112B1/fr unknown
- 2013-12-04 JP JP2015547219A patent/JP5869740B2/ja active Active
- 2013-12-04 HU HUE13812165A patent/HUE032400T2/hu unknown
- 2013-12-04 EP EP13812165.2A patent/EP2938615B1/en active Active
- 2013-12-04 PT PT138121652T patent/PT2938615T/pt unknown
- 2013-12-04 BR BR112015014097-1A patent/BR112015014097B1/pt active IP Right Grant
- 2013-12-04 SG SG11201503735YA patent/SG11201503735YA/en unknown
- 2013-12-04 RS RS20160986A patent/RS55307B1/sr unknown
- 2013-12-04 LT LTEP13812165.2T patent/LT2938615T/lt unknown
- 2013-12-04 AP AP2015008526A patent/AP2015008526A0/xx unknown
- 2013-12-04 GE GEAP201313849A patent/GEP201706710B/en unknown
- 2013-12-04 MD MDA20150051A patent/MD4651B1/ro not_active IP Right Cessation
- 2013-12-04 CA CA2892174A patent/CA2892174C/en active Active
- 2013-12-04 DK DK13812165.2T patent/DK2938615T3/da active
- 2013-12-04 SI SI201330382T patent/SI2938615T1/sl unknown
- 2013-12-04 ES ES13812165.2T patent/ES2608640T3/es active Active
- 2013-12-04 KR KR1020157017073A patent/KR101746314B1/ko active Active
- 2013-12-04 PL PL13812165T patent/PL2938615T3/pl unknown
- 2013-12-04 MX MX2015007598A patent/MX366023B/es active IP Right Grant
- 2013-12-11 TW TW102145600A patent/TWI478926B/zh active
- 2013-12-12 US US14/103,960 patent/US8952008B2/en active Active
- 2013-12-12 AR ARP130104648A patent/AR093937A1/es unknown
- 2013-12-12 UY UY35185A patent/UY35185A/es unknown
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2014
- 2014-12-19 US US14/576,796 patent/US20150105396A1/en not_active Abandoned
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2015
- 2015-05-14 CR CR20150254A patent/CR20150254A/es unknown
- 2015-05-29 US US14/725,234 patent/US20150259352A1/en not_active Abandoned
- 2015-06-04 IL IL239243A patent/IL239243A0/en active IP Right Grant
- 2015-06-05 PH PH12015501293A patent/PH12015501293B1/en unknown
- 2015-06-09 TN TNP2015000261A patent/TN2015000261A1/fr unknown
- 2015-06-11 NI NI201500081A patent/NI201500081A/es unknown
- 2015-06-11 ZA ZA2015/04226A patent/ZA201504226B/en unknown
- 2015-06-12 DO DO2015000147A patent/DOP2015000147A/es unknown
- 2015-06-12 CL CL2015001652A patent/CL2015001652A1/es unknown
- 2015-07-11 EC ECIEPI201529822A patent/ECSP15029822A/es unknown
- 2015-08-04 GT GT201500159A patent/GT201500159A/es unknown
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2016
- 2016-12-05 CY CY20161101251T patent/CY1118568T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| KA4A | Patent for invention lapsed due to non-payment of fees (with right of restoration) |