WO2010007073A1 - Piperazine derivatives used as cav2.2 calcium channel modulators - Google Patents
Piperazine derivatives used as cav2.2 calcium channel modulators Download PDFInfo
- Publication number
- WO2010007073A1 WO2010007073A1 PCT/EP2009/059012 EP2009059012W WO2010007073A1 WO 2010007073 A1 WO2010007073 A1 WO 2010007073A1 EP 2009059012 W EP2009059012 W EP 2009059012W WO 2010007073 A1 WO2010007073 A1 WO 2010007073A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- methyl
- sulfonyl
- mmol
- piperazine
- trifluoromethyl
- 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.)
- Ceased
Links
- XVWVKPWBVLXMKA-AWEZNQCLSA-N C[C@@H](CN(CC1)C(c2ccc(C)nc2)=O)N1S(c1ccc(C(F)(F)F)cc1/[O]=C\O)(=O)=O Chemical compound C[C@@H](CN(CC1)C(c2ccc(C)nc2)=O)N1S(c1ccc(C(F)(F)F)cc1/[O]=C\O)(=O)=O XVWVKPWBVLXMKA-AWEZNQCLSA-N 0.000 description 1
- KHYHJQWOCKZSQP-AWEZNQCLSA-N C[C@@H](CN(CC1)C(c2cnc(C)cc2)=O)N1S(c(cc1)ccc1Cl)(=O)=O Chemical compound C[C@@H](CN(CC1)C(c2cnc(C)cc2)=O)N1S(c(cc1)ccc1Cl)(=O)=O KHYHJQWOCKZSQP-AWEZNQCLSA-N 0.000 description 1
- KUZVKEBKUWSQFD-NSHDSACASA-N C[C@@H](CN(CC1)S(c(cc(C(F)(F)F)cc2)c2Br)(=O)=O)N1C(OC(C)(C)C)=O Chemical compound C[C@@H](CN(CC1)S(c(cc(C(F)(F)F)cc2)c2Br)(=O)=O)N1C(OC(C)(C)C)=O KUZVKEBKUWSQFD-NSHDSACASA-N 0.000 description 1
- CZEPKYCKQNSXFC-INIZCTEOSA-N C[C@@H](CN(CC1)S(c2ccc(C(F)(F)F)cc2)(=O)=O)N1C(c(cc1)c(C)nc1N1CCOCC1)=O Chemical compound C[C@@H](CN(CC1)S(c2ccc(C(F)(F)F)cc2)(=O)=O)N1C(c(cc1)c(C)nc1N1CCOCC1)=O CZEPKYCKQNSXFC-INIZCTEOSA-N 0.000 description 1
- IADCODPTDZZHPZ-ZDUSSCGKSA-N C[C@@H](CN(CC1)S(c2ccc(C(F)(F)F)cc2)(=O)=O)N1C(c(cc1)cnc1NC)=O Chemical compound C[C@@H](CN(CC1)S(c2ccc(C(F)(F)F)cc2)(=O)=O)N1C(c(cc1)cnc1NC)=O IADCODPTDZZHPZ-ZDUSSCGKSA-N 0.000 description 1
Classifications
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- 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
- 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
- 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
-
- 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
Definitions
- Ca v 2.2 calcium channels have been shown to be important for normal neuronal function (Winquist et al. (2005) Biochemical Pharmacology, 70: 489-499). Therefore, the aim is to identify novel molecules that preferentially block Ca v 2.2 under conditions of increased neuronal excitability, so-called use-dependent blockers, as is the case in chronic pain syndromes.
- Process (c) may be performed using conventional interconversion procedures such as epimerisation, oxidation, reduction, alkylation, nucleophilic or electrophilic aromatic substitution.
- interconversion may be interconversion of a compound as defined in the first to fourth aspect wherein R 3 represents bromine to a compound as defined in the first to fourth aspect wherein R 3 represents cyano.
- Such interconversion may be carried out by treating the bromine compound with a cyanide salt (for example copper (I) cyanide) in a suitable solvent (such as N, N- dimethylformamide) at elevated temperatures (such as 200°C using microwave irradiation).
- a cyanide salt for example copper (I) cyanide
- suitable solvent such as N, N- dimethylformamide
- the compound as defined in the first to fourth aspect or a pharmaceutically acceptable salt thereof may be used in combination with other medicaments indicated to be useful as either disease modifying or symptomatic treatments of Alzheimer's disease.
- the above method has a flow rate of 1 ml/min.
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Priority Applications (12)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EA201170209A EA018621B1 (ru) | 2008-07-17 | 2009-07-15 | ПРОИЗВОДНЫЕ ПИПЕРАЗИНА, ПРИМЕНЯЕМЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ КАЛЬЦИЕВОГО КАНАЛА Ca2.2 |
| CA2730471A CA2730471C (en) | 2008-07-17 | 2009-07-15 | Piperazine derivatives used as cav2.2 calcium channel modulators |
| BRPI0916622-0A BRPI0916622A2 (pt) | 2008-07-17 | 2009-07-15 | derivados de piperazina usados como moduladores de canal de cálcio cav2,2 |
| JP2011517911A JP5543966B2 (ja) | 2008-07-17 | 2009-07-15 | Ｃａｖ２．２カルシウムチャネルモジュレーターとして使用されるピペラジン誘導体 |
| AU2009272762A AU2009272762B2 (en) | 2008-07-17 | 2009-07-15 | Piperazine derivatives used as Cav2.2 calcium channel modulators |
| MX2011000600A MX2011000600A (es) | 2008-07-17 | 2009-07-15 | Derivados de piperazina usados como moduladores del canal de calcio cav2.2. |
| ES09780587T ES2396962T3 (es) | 2008-07-17 | 2009-07-15 | Derivados de piperazina utilizados como moduladores de los canales de calcio Cav2.2 |
| PL09780587T PL2300432T3 (pl) | 2008-07-17 | 2009-07-15 | Pochodne piperazyny stosowane jako modulatory kanałów wapniowych CAV2.2 |
| CN200980127788XA CN102099337B (zh) | 2008-07-17 | 2009-07-15 | 用作cav2.2钙通道调节剂的哌嗪衍生物 |
| EP09780587A EP2300432B1 (en) | 2008-07-17 | 2009-07-15 | Piperazine derivatives used as cav2.2 calcium channel modulators |
| IL210446A IL210446A (en) | 2008-07-17 | 2011-01-03 | History of fibrin and medicinal preparations containing them |
| ZA2011/00014A ZA201100014B (en) | 2008-07-17 | 2011-01-03 | Piperazine derivatives used as cav2.2 calcium channel modulators |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0813142.7A GB0813142D0 (en) | 2008-07-17 | 2008-07-17 | Novel compounds |
| GB0813142.7 | 2008-07-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2010007073A1 true WO2010007073A1 (en) | 2010-01-21 |
Family
ID=39737239
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2009/059012 Ceased WO2010007073A1 (en) | 2008-07-17 | 2009-07-15 | Piperazine derivatives used as cav2.2 calcium channel modulators |
| PCT/EP2009/059011 Ceased WO2010007072A1 (en) | 2008-07-17 | 2009-07-15 | Piperazine derivatives used as cav2.2 calcium channel modulators |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2009/059011 Ceased WO2010007072A1 (en) | 2008-07-17 | 2009-07-15 | Piperazine derivatives used as cav2.2 calcium channel modulators |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8530478B2 (https=) |
| EP (2) | EP2300432B1 (https=) |
| JP (2) | JP5543966B2 (https=) |
| KR (1) | KR101599087B1 (https=) |
| CN (1) | CN102099337B (https=) |
| AR (1) | AR072809A1 (https=) |
| AU (1) | AU2009272762B2 (https=) |
| BR (1) | BRPI0916622A2 (https=) |
| CA (1) | CA2730471C (https=) |
| EA (1) | EA018621B1 (https=) |
| ES (2) | ES2396960T3 (https=) |
| GB (1) | GB0813142D0 (https=) |
| IL (1) | IL210446A (https=) |
| MX (1) | MX2011000600A (https=) |
| PL (1) | PL2300432T3 (https=) |
| TW (1) | TW201016677A (https=) |
| UY (1) | UY31990A (https=) |
| WO (2) | WO2010007073A1 (https=) |
| ZA (1) | ZA201100014B (https=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013000651A1 (en) | 2011-06-27 | 2013-01-03 | Newron Pharmaceuticals S.P.A. | Fluorinated arylalkylaminocarboxamide derivatives |
| JP2014502993A (ja) * | 2011-01-19 | 2014-02-06 | クオンベルゲンセ プハルマセウトイカルス リミテッド | ＣａＶ２．２カルシウムチャンネルブロッカーとしてのピペラジン誘導体 |
| WO2017046581A1 (en) * | 2015-09-14 | 2017-03-23 | Calchan Limited | Composition comprising cav2.2 calcium channel blocker and opioid |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0813142D0 (en) * | 2008-07-17 | 2008-08-27 | Glaxo Group Ltd | Novel compounds |
| GB201000685D0 (en) * | 2010-01-15 | 2010-03-03 | Glaxo Group Ltd | Novel compounds |
| CA2945529A1 (en) | 2014-04-14 | 2015-10-22 | Grunenthal Gmbh | Aryl substituted heterocyclyl sulfones |
| AR100073A1 (es) | 2014-04-14 | 2016-09-07 | Gruenenthal Gmbh | Sulfonas heterocíclicas sustituidas con heteroarilos |
| TW201718557A (zh) | 2015-10-08 | 2017-06-01 | 歌林達有限公司 | 經吡唑基取代之四氫吡喃基碸 |
| TW201726128A (zh) | 2015-10-08 | 2017-08-01 | 歌林達有限公司 | 經吡唑基取代之四氫哌喃基碸 |
| JP7321097B2 (ja) * | 2017-04-26 | 2023-08-04 | カビオン・インコーポレイテッド | 記憶および認知を改善する、ならびに記憶および認知障害を処置するための方法 |
| CN118085389B (zh) * | 2024-03-11 | 2024-11-05 | 伟建实业(苏州)有限公司 | 一种环保型抗菌海绵及其制备方法 |
Citations (2)
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| WO2007111921A1 (en) * | 2006-03-23 | 2007-10-04 | Amgen Inc. | 1-phenylsulfonyl-diaza heterocyclic amide compounds and their uses as modulators of hydroxsteroid dehydrogenases |
| WO2008024284A2 (en) * | 2006-08-21 | 2008-02-28 | Merck & Co., Inc. | Sulfonylated piperazines as cannabinoid-1 receptor modulators |
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