DOP2013000305A - 1-piperazino-3-fenil-indanos deuterados para el tratamiento de esquizofrenia - Google Patents
1-piperazino-3-fenil-indanos deuterados para el tratamiento de esquizofreniaInfo
- Publication number
- DOP2013000305A DOP2013000305A DO2013000305A DO2013000305A DOP2013000305A DO P2013000305 A DOP2013000305 A DO P2013000305A DO 2013000305 A DO2013000305 A DO 2013000305A DO 2013000305 A DO2013000305 A DO 2013000305A DO P2013000305 A DOP2013000305 A DO P2013000305A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- treatment
- piperazino
- deuterated
- phenyl
- indanos
- Prior art date
Links
- 201000000980 schizophrenia Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 210000003169 central nervous system Anatomy 0.000 abstract 2
- QPABODDHXQJCDN-UHFFFAOYSA-N 1-(3-phenyl-2,3-dihydro-1h-inden-1-yl)piperazine Chemical class C12=CC=CC=C2C(C=2C=CC=CC=2)CC1N1CCNCC1 QPABODDHXQJCDN-UHFFFAOYSA-N 0.000 abstract 1
- 102000056834 5-HT2 Serotonin Receptors Human genes 0.000 abstract 1
- 108091005479 5-HT2 receptors Proteins 0.000 abstract 1
- 101150049660 DRD2 gene Proteins 0.000 abstract 1
- 108090000511 Dopamine D1 Receptors Proteins 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000000034 method Methods 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
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
-
- 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
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
- C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
- C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente invención se refiere a 1piperazino3fenilindanos deuterados y sus sales con actividad en receptores dopamínicos D1 y D2, así como los receptores de 5HT2 en el sistema nervioso central, a medicamentos que comprenden tales compuestos como ingredientes activos, al uso de tales compuestos en el tratamiento de enfermedades en el sistema nervioso central y a métodos de tratamiento que comprenden la administración de tales compuestos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161498651P | 2011-06-20 | 2011-06-20 | |
US201161537103P | 2011-09-21 | 2011-09-21 |
Publications (1)
Publication Number | Publication Date |
---|---|
DOP2013000305A true DOP2013000305A (es) | 2014-02-28 |
Family
ID=46682855
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DO2013000305A DOP2013000305A (es) | 2011-06-20 | 2013-12-16 | 1-piperazino-3-fenil-indanos deuterados para el tratamiento de esquizofrenia |
Country Status (40)
Country | Link |
---|---|
US (8) | US8575174B2 (es) |
EP (4) | EP2720989B1 (es) |
JP (1) | JP5668177B2 (es) |
KR (2) | KR101939546B1 (es) |
CN (1) | CN103649019B (es) |
AP (1) | AP3310A (es) |
AR (1) | AR086987A1 (es) |
AU (1) | AU2012273657B2 (es) |
BR (1) | BR112013031702B1 (es) |
CA (1) | CA2837820C (es) |
CL (1) | CL2013003646A1 (es) |
CO (1) | CO6821965A2 (es) |
CR (1) | CR20130654A (es) |
CY (2) | CY1118158T1 (es) |
DK (2) | DK2720989T3 (es) |
DO (1) | DOP2013000305A (es) |
EA (1) | EA024651B1 (es) |
EC (1) | ECSP14013155A (es) |
ES (3) | ES2939477T3 (es) |
GE (1) | GEP201706655B (es) |
GT (1) | GT201300304A (es) |
HR (2) | HRP20161348T1 (es) |
HU (2) | HUE030883T2 (es) |
IL (1) | IL229640B (es) |
JO (1) | JO3128B1 (es) |
LT (2) | LT3135656T (es) |
MA (1) | MA35268B1 (es) |
MD (1) | MD4538C1 (es) |
ME (2) | ME03375B (es) |
MX (1) | MX339552B (es) |
MY (1) | MY196998A (es) |
PE (2) | PE20141113A1 (es) |
PH (1) | PH12013502598A1 (es) |
PL (2) | PL2720989T3 (es) |
PT (2) | PT3135656T (es) |
RS (2) | RS58546B1 (es) |
SI (2) | SI2720989T1 (es) |
SM (2) | SMT201900179T1 (es) |
TW (3) | TWI627956B (es) |
WO (1) | WO2012176066A1 (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8575174B2 (en) | 2011-06-20 | 2013-11-05 | H. Lundbeck A/S | Deuterated 1-piperazino-3-phenyl-indanes for treatment of schizophrenia |
AR094054A1 (es) * | 2012-12-19 | 2015-07-08 | H Lundbeck As | 6-cloro-3-(fenil-d₅)-inden-1-ona y uso de la misma |
PT3679018T (pt) | 2017-09-07 | 2022-04-05 | Otsuka Pharma Co Ltd | Processo industrial de monoalquilação de um nitrogénio de piperidina em derivados de piperidina com alquilo deuterado |
WO2020089147A1 (en) * | 2018-10-29 | 2020-05-07 | H. Lundbeck A/S | Amorphous compounds of formula (i) and amorphous compounds of formula (i) salts |
US11535600B2 (en) | 2018-12-03 | 2022-12-27 | H. Lundbeck A/S | Prodrugs of 4-((1R,3S)-6-chloro-3-phenyl-2,3-dihydro-1H-inden-1-yl)-1,2,2-trimethylpiperazine and 4-((1R,3S)-6-chloro-3-(phenyl-d5)-2,3-dihydro-1H-inden-1-yl)-2,2-dimethyl-1-(methyl-d3)piperazine |
EA202191731A1 (ru) * | 2018-12-21 | 2021-10-28 | Консерт Фармасьютикалз, Инк. | Дейтерированные формы и производные волинансерина |
CA3132953A1 (en) * | 2019-03-13 | 2020-09-17 | Otsuka Pharmaceutical Co., Ltd. | Method for introducing deuterated lower alkyl into amine moiety of compound containing secondary amine |
Family Cites Families (48)
Publication number | Priority date | Publication date | Assignee | Title |
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NZ196284A (en) | 1980-02-29 | 1983-12-16 | Kefalas As | 1-piperazino-3-phenylindane derivatives:pharmaceutical compositions |
GB8427125D0 (en) | 1984-10-26 | 1984-12-05 | Lundbeck & Co As H | Organic compounds |
ATE60571T1 (de) | 1984-12-04 | 1991-02-15 | Sandoz Ag | Inden-analoga von mevalonolakton und ihre derivate. |
DK286990D0 (da) | 1990-12-04 | 1990-12-04 | Lundbeck & Co As H | Indanderivater |
DK55192D0 (da) | 1992-04-28 | 1992-04-28 | Lundbeck & Co As H | 1-piperazino-1,2-dihydroindenderivater |
US6221335B1 (en) | 1994-03-25 | 2001-04-24 | Isotechnika, Inc. | Method of using deuterated calcium channel blockers |
KR20040068613A (ko) | 1994-03-25 | 2004-07-31 | 이소테크니카 인코포레이티드 | 중수소화된 화합물 이를 포함하는 고혈압 치료용 조성물 |
JP2001517666A (ja) | 1997-09-23 | 2001-10-09 | 藤沢薬品工業株式会社 | チアゾール誘導体 |
US6350786B1 (en) | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
SE9904850D0 (sv) | 1999-12-30 | 1999-12-30 | Pharmacia & Upjohn Ab | Novel process and intermediates |
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MXPA06001838A (es) | 2003-08-18 | 2006-05-04 | Lundbeck & Co As H | Sales de succinato y malonato de la trans-4- ((ir, 3s)-6 -cloro-3- fenilindan -1-il)-1, 2, 2- trimetilpiperazina y su uso como medicamento. |
ATE552247T1 (de) * | 2003-08-18 | 2012-04-15 | Lundbeck & Co As H | Succinat- und malonatsalz von trans-4-(1r,3s)-6- chlor-3-phenylindan-1-yl)-1,2,2- trimethylpiperazin und die verwendung als medikament |
RU2366654C2 (ru) | 2004-06-08 | 2009-09-10 | ЭнЭсЭйБи, ФИЛИАЛ АФ НЕУРОСЕРЧ СВИДЕН АБ, СВЕРИЙЕ | Новые дизамещенные фенилпиперидины/пиперазины в качестве модуляторов допаминовой нейротрансмиссии |
WO2005121087A1 (en) | 2004-06-08 | 2005-12-22 | A. Carlsson Research Ab | New disubstituted phenylpiperidines/piperazines as modulators of dopamine neurotransmission |
AU2006215956A1 (en) * | 2005-02-16 | 2006-08-24 | H. Lundbeck A/S | Tartrate and malate salts of trans-1-((1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine |
TWI453198B (zh) | 2005-02-16 | 2014-09-21 | Lundbeck & Co As H | 製造反式-1-((1r,3s)-6-氯基-3-苯基茚滿-1-基) -3 , 3 -二甲基六氫吡與其鹽類之方法及製造4-((1r , 3s)-6 -氯基-3-苯基茚滿-1-基 )-1,2,2-三甲基六氫吡與其鹽類之方法 |
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