AR080987A1 - Formas cristalinas polimorficas a y d de la sal mesilato de 7-metil-5(3-piperazin-1-ilmetil-[1,2,4]oxadiazol-5-il)-2-(4-trifluorometoxibencil)2,3-dihidroisoindol-1-ona,metodo para prepararlas, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento del dolor y la ansied - Google Patents
Formas cristalinas polimorficas a y d de la sal mesilato de 7-metil-5(3-piperazin-1-ilmetil-[1,2,4]oxadiazol-5-il)-2-(4-trifluorometoxibencil)2,3-dihidroisoindol-1-ona,metodo para prepararlas, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento del dolor y la ansiedInfo
- Publication number
- AR080987A1 AR080987A1 ARP110101484A ARP110101484A AR080987A1 AR 080987 A1 AR080987 A1 AR 080987A1 AR P110101484 A ARP110101484 A AR P110101484A AR P110101484 A ARP110101484 A AR P110101484A AR 080987 A1 AR080987 A1 AR 080987A1
- Authority
- AR
- Argentina
- Prior art keywords
- oxadiazol
- piperazin
- methyl
- salt
- trifluorometoxibencil
- Prior art date
Links
- AFVFQIVMOAPDHO-UHFFFAOYSA-M Methanesulfonate Chemical compound CS([O-])(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-M 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- 229950002475 mesilate Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 4
- -1 oxadiazol-5-yl Chemical group 0.000 abstract 4
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 4
- CTENDTMNSNDLCP-UHFFFAOYSA-N 2-[[4-(trifluoromethoxy)phenyl]methyl]-3h-isoindol-1-one Chemical compound C1=CC(OC(F)(F)F)=CC=C1CN1C(=O)C2=CC=CC=C2C1 CTENDTMNSNDLCP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000173 4-trifluoromethoxy benzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC(F)(F)F)C([H])([H])* 0.000 abstract 1
Classifications
-
- 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
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- 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
- 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
- A61P25/22—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)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Reivindicacion 2: La sal mesilato de 7-metil-5-(3-piperazin-1-ilmetil-[1,2,4]oxadiazol-5-il)-2-(4-trifluormetoxibencil)-2,3-dihidroisoindoI-1-ona, Polimorfo A, donde los valores d, 2-theta y los recuentos medidos por XRPD son: segun el cuadro (1) : 2-theta/s valor d recuentos (gamma = 1,5418L) 8,0, 11,1, 250; 17,8, 4,98,1932; 18,4, 4,81, 841; 19, 4,55,1471; 21,0, 4,22, 1841. Reivindicacion 3: La sal mesilato de 7-metil-5-(3-piperazin-1-ilmetil-[1,2,4]oxadiazol-5-il)-2(4-trifluormetoxibencil)-2,3-dihidroisoindol-1-ona, Polimorfo A, de acuerdo con la reivindicacion 2, donde los valores d, 2-theta y recuentos adicionales, medidos por XRPD, son como en cuadro (2): 2-theta/s valor d recuentos ( gamma = 1,5418L) 11,8, 7,5, 264; 15,6, 5,7, 465; 17,1, 5,2, 469; 20,4 4,35, 758; 21,3, 4,2 ,471. Reivindicacion 10: La sal mesilato de 7-metil-5-(3-piperazin-1-ilmetil-[1,2,4]oxadiazol-5-il)-2-(4-trifluormetoxibencil)-2,3-dihidroisoindol-1-ona, Polimorfo D, donde los valores d, 2-theta y los recuentos, medidos por XRPD, son: 2-theta/°, valor d, recuentos (gamma = 1,5418L) 10,9, 8,1 977; 15,8, 5,6, 766; 17,7, 5,0, 1003; 18,0, 4,93, 1056; 20,2, 4,39, 913. Reivindicacion 11: La sal mesilato de 7-metil-5-(3-piperazin-1-ilmetil-[1,2,4]oxadiazol-5-il)-2-(4-trifluormetoxibencil)-2,3-dihidroisoindol-1-ona, Polimorfo D, de acuerdo con la reivindicacion 2, donde los valores d, 2-theta y recuentos adicionales, medidos por XRPD, son: 2-theta/° valor d, recuentos (gamma = 1,5418L) 16,9, 5,2, 637; 11,8, 7,5, 1668; 14,3, 6,2, 1171.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32966210P | 2010-04-30 | 2010-04-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080987A1 true AR080987A1 (es) | 2012-05-23 |
Family
ID=44861775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101484A AR080987A1 (es) | 2010-04-30 | 2011-04-28 | Formas cristalinas polimorficas a y d de la sal mesilato de 7-metil-5(3-piperazin-1-ilmetil-[1,2,4]oxadiazol-5-il)-2-(4-trifluorometoxibencil)2,3-dihidroisoindol-1-ona,metodo para prepararlas, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento del dolor y la ansied |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20130237548A1 (es) |
| EP (1) | EP2563782A4 (es) |
| JP (1) | JP2013525427A (es) |
| KR (1) | KR20130094179A (es) |
| CN (1) | CN102858766A (es) |
| AR (1) | AR080987A1 (es) |
| AU (1) | AU2011245737A1 (es) |
| BR (1) | BR112012027628A2 (es) |
| CA (1) | CA2795218A1 (es) |
| IL (1) | IL222601A0 (es) |
| MX (1) | MX2012012447A (es) |
| RU (1) | RU2012144778A (es) |
| SG (1) | SG184449A1 (es) |
| TW (1) | TW201206913A (es) |
| WO (1) | WO2011136723A1 (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI417095B (zh) | 2006-03-15 | 2013-12-01 | Janssen Pharmaceuticals Inc | １，４-二取代之３-氰基-吡啶酮衍生物及其作為ｍＧｌｕＲ２-受體之正向異位性調節劑之用途 |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| CA2696948C (en) | 2007-09-14 | 2013-04-30 | Jose Maria Cid-Nunez | 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones |
| KR20100080597A (ko) | 2007-09-14 | 2010-07-09 | 오르토-맥닐-얀센 파마슈티칼스 인코포레이티드 | １,３-이치환된-４-페닐-1ｈ-피리딘-2-온 |
| CA2735764C (en) | 2008-09-02 | 2016-06-14 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors |
| AU2009304293B2 (en) | 2008-10-16 | 2012-04-26 | Addex Pharma S.A. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
| BRPI0921333A2 (pt) | 2008-11-28 | 2015-12-29 | Addex Pharmaceuticals Sa | derivados de indol e benzoxazina como moduladores de receptores de glutamato metabotrópicos |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| NZ596078A (en) | 2009-05-12 | 2013-06-28 | Janssen Pharmaceuticals Inc | 1,2,4-TRIAZOLO [4,3-a] PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS |
| EA020671B1 (ru) | 2009-05-12 | 2014-12-30 | Янссен Фармасьютикалз, Инк. | ПРОИЗВОДНЫЕ 1,2,4-ТРИАЗОЛО[4,3-a]ПИРИДИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПОЛОЖИТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2 |
| CN103298810B (zh) | 2010-11-08 | 2016-03-16 | 杨森制药公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途 |
| EP2643320B1 (en) | 2010-11-08 | 2015-03-04 | Janssen Pharmaceuticals, Inc. | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| CA2815002C (en) | 2010-11-08 | 2019-10-22 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| JO3367B1 (ar) | 2013-09-06 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2 |
| LT3431106T (lt) | 2014-01-21 | 2021-02-10 | Janssen Pharmaceutica Nv | Deriniai, apimantys 2 potipio metabotropinio glutamaterginio receptoriaus teigiamus alosterinius moduliatorius arba ortosterinius agonistus, ir jų panaudojimas |
| KR102414246B1 (ko) | 2014-01-21 | 2022-06-27 | 얀센 파마슈티카 엔.브이. | 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도 |
| KR200482429Y1 (ko) | 2016-02-16 | 2017-01-23 | 이순호 | 막힘 해소장치를 갖는 양변기 |
| GB2621323A (en) * | 2022-08-03 | 2024-02-14 | Sirgartan Holdings Ltd | Treatments for obsessive compulsive disorder |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070185095A1 (en) * | 2004-02-18 | 2007-08-09 | Astrazeneca Ab | Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists |
| TWI417100B (zh) * | 2007-06-07 | 2013-12-01 | Astrazeneca Ab | 二唑衍生物及其作為代謝型麩胺酸受體增效劑-８４２之用途 |
| SG181958A1 (en) * | 2010-01-07 | 2012-07-30 | Astrazeneca Ab | Process for making a metabotropic glutamate receptor positive allosteric modulator - 874 |
-
2011
- 2011-04-21 CA CA2795218A patent/CA2795218A1/en not_active Abandoned
- 2011-04-21 RU RU2012144778/04A patent/RU2012144778A/ru not_active Application Discontinuation
- 2011-04-21 CN CN2011800218010A patent/CN102858766A/zh active Pending
- 2011-04-21 BR BR112012027628A patent/BR112012027628A2/pt not_active IP Right Cessation
- 2011-04-21 EP EP11775372.3A patent/EP2563782A4/en not_active Withdrawn
- 2011-04-21 KR KR1020127028219A patent/KR20130094179A/ko not_active Withdrawn
- 2011-04-21 AU AU2011245737A patent/AU2011245737A1/en not_active Abandoned
- 2011-04-21 US US13/695,140 patent/US20130237548A1/en not_active Abandoned
- 2011-04-21 JP JP2013507916A patent/JP2013525427A/ja not_active Withdrawn
- 2011-04-21 WO PCT/SE2011/050489 patent/WO2011136723A1/en not_active Ceased
- 2011-04-21 SG SG2012073912A patent/SG184449A1/en unknown
- 2011-04-21 MX MX2012012447A patent/MX2012012447A/es not_active Application Discontinuation
- 2011-04-28 AR ARP110101484A patent/AR080987A1/es unknown
- 2011-04-28 TW TW100114940A patent/TW201206913A/zh unknown
-
2012
- 2012-10-22 IL IL222601A patent/IL222601A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011136723A1 (en) | 2011-11-03 |
| EP2563782A4 (en) | 2013-09-04 |
| KR20130094179A (ko) | 2013-08-23 |
| AU2011245737A1 (en) | 2012-12-20 |
| TW201206913A (en) | 2012-02-16 |
| MX2012012447A (es) | 2012-11-21 |
| SG184449A1 (en) | 2012-11-29 |
| EP2563782A1 (en) | 2013-03-06 |
| CA2795218A1 (en) | 2011-11-03 |
| US20130237548A1 (en) | 2013-09-12 |
| IL222601A0 (en) | 2012-12-31 |
| JP2013525427A (ja) | 2013-06-20 |
| RU2012144778A (ru) | 2014-06-10 |
| BR112012027628A2 (pt) | 2016-08-09 |
| CN102858766A (zh) | 2013-01-02 |
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Legal Events
| Date | Code | Title | Description |
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| FB | Suspension of granting procedure |