NZ537023A - Pharmaceutical salts of reboxetine - Google Patents
Pharmaceutical salts of reboxetineInfo
- Publication number
- NZ537023A NZ537023A NZ537023A NZ53702303A NZ537023A NZ 537023 A NZ537023 A NZ 537023A NZ 537023 A NZ537023 A NZ 537023A NZ 53702303 A NZ53702303 A NZ 53702303A NZ 537023 A NZ537023 A NZ 537023A
- Authority
- NZ
- New Zealand
- Prior art keywords
- salt
- reboxetine
- succinate
- fumarate
- phenoxy
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title claims abstract description 26
- 229960003770 reboxetine Drugs 0.000 title abstract description 46
- CBQGYUDMJHNJBX-RTBURBONSA-N reboxetine Chemical class CCOC1=CC=CC=C1O[C@H](C=1C=CC=CC=1)[C@@H]1OCCNC1 CBQGYUDMJHNJBX-RTBURBONSA-N 0.000 title abstract description 18
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims abstract description 35
- 150000003890 succinate salts Chemical class 0.000 claims abstract description 21
- 238000000034 method Methods 0.000 claims abstract description 16
- 239000003814 drug Substances 0.000 claims abstract description 10
- 238000004519 manufacturing process Methods 0.000 claims abstract description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 239000012458 free base Substances 0.000 claims description 16
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 10
- 241000124008 Mammalia Species 0.000 claims description 9
- 238000002425 crystallisation Methods 0.000 claims description 8
- 230000008025 crystallization Effects 0.000 claims description 8
- 230000005764 inhibitory process Effects 0.000 claims description 8
- IWYDHOAUDWTVEP-UHFFFAOYSA-M mandelate Chemical compound [O-]C(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-M 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 7
- 230000000966 norepinephrine reuptake Effects 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 230000008569 process Effects 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 5
- 239000002253 acid Substances 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- IWYDHOAUDWTVEP-ZETCQYMHSA-N (S)-mandelic acid Chemical compound OC(=O)[C@@H](O)C1=CC=CC=C1 IWYDHOAUDWTVEP-ZETCQYMHSA-N 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 claims description 3
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract description 16
- CBQGYUDMJHNJBX-UHFFFAOYSA-N 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine Chemical compound CCOC1=CC=CC=C1OC(C=1C=CC=CC=1)C1OCCNC1 CBQGYUDMJHNJBX-UHFFFAOYSA-N 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 20
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 18
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- 239000007787 solid Substances 0.000 description 16
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 15
- CBQGYUDMJHNJBX-OALUTQOASA-N (2S)-2-[(S)-(2-ethoxyphenoxy)-phenylmethyl]morpholine Chemical class CCOC1=CC=CC=C1O[C@@H](C=1C=CC=CC=1)[C@H]1OCCNC1 CBQGYUDMJHNJBX-OALUTQOASA-N 0.000 description 13
- 208000035475 disorder Diseases 0.000 description 11
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 11
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 9
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- 239000000126 substance Substances 0.000 description 7
- 238000004458 analytical method Methods 0.000 description 6
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- 230000000694 effects Effects 0.000 description 6
- 229960003269 reboxetine mesylate Drugs 0.000 description 6
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- CGTZMJIMMUNLQD-STYNFMPRSA-N (2r)-2-[(r)-(2-ethoxyphenoxy)-phenylmethyl]morpholine;methanesulfonic acid Chemical class CS(O)(=O)=O.CCOC1=CC=CC=C1O[C@H](C=1C=CC=CC=1)[C@@H]1OCCNC1 CGTZMJIMMUNLQD-STYNFMPRSA-N 0.000 description 4
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- 241000282412 Homo Species 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
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- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 description 1
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 1
- TWHNMSJGYKMTRB-KXYUELECSA-N (2r,3r)-2,3-dihydroxybutanedioic acid;2-[(1r)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1([C@@H](CCN(C(C)C)C(C)C)C=2C(=CC=C(C)C=2)O)=CC=CC=C1 TWHNMSJGYKMTRB-KXYUELECSA-N 0.000 description 1
- STGNLGBPLOVYMA-MAZDBSFSSA-N (E)-but-2-enedioic acid Chemical compound OC(=O)\C=C\C(O)=O.OC(=O)\C=C\C(O)=O STGNLGBPLOVYMA-MAZDBSFSSA-N 0.000 description 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- 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]
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- 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
- A61P3/02—Nutrients, e.g. vitamins, minerals
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- 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
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Nutrition Science (AREA)
- Toxicology (AREA)
- Physical Education & Sports Medicine (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Anesthesiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02077366 | 2002-06-17 | ||
| PCT/EP2003/005261 WO2003106441A1 (en) | 2002-06-17 | 2003-06-04 | Pharmaceutical salts of reboxetine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ537023A true NZ537023A (en) | 2006-09-29 |
Family
ID=29724495
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ537023A NZ537023A (en) | 2002-06-17 | 2003-06-04 | Pharmaceutical salts of reboxetine |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US20070010517A1 (https=) |
| EP (1) | EP1515959B1 (https=) |
| JP (1) | JP4563172B2 (https=) |
| KR (1) | KR100779786B1 (https=) |
| CN (2) | CN1662511B (https=) |
| AR (1) | AR040222A1 (https=) |
| AT (1) | ATE439354T1 (https=) |
| AU (1) | AU2003227755B2 (https=) |
| BR (1) | BR0311878A (https=) |
| CA (1) | CA2489763C (https=) |
| DE (1) | DE60328787D1 (https=) |
| DK (1) | DK1515959T3 (https=) |
| ES (1) | ES2328472T3 (https=) |
| MX (1) | MXPA04011916A (https=) |
| MY (1) | MY131231A (https=) |
| NO (1) | NO329346B1 (https=) |
| NZ (1) | NZ537023A (https=) |
| PE (1) | PE20040565A1 (https=) |
| PL (1) | PL375211A1 (https=) |
| RU (1) | RU2286341C2 (https=) |
| TW (1) | TWI267510B (https=) |
| WO (1) | WO2003106441A1 (https=) |
| ZA (1) | ZA200409624B (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0319793D0 (en) | 2003-08-22 | 2003-09-24 | Lilly Co Eli | Pyridinylmorpholine derivatives |
| WO2005082869A1 (en) * | 2004-02-20 | 2005-09-09 | Pharmacia & Upjohn Company Llc | Method for the preparation of aryl ethers |
| US8580776B2 (en) * | 2007-07-10 | 2013-11-12 | The Board Of Trustees Of The University Of Illinois | Compositions and methods for treating neurodegenerating diseases |
| US20100069389A1 (en) * | 2008-09-06 | 2010-03-18 | Bionevia Pharmaceuticals, Inc. | Novel forms of reboxetine |
| US20190185438A1 (en) * | 2016-12-06 | 2019-06-20 | Tonix Pharmaceuticals Holding Corp. | Salts and polymorphs of esreboxetine |
| US12565478B1 (en) | 2025-01-21 | 2026-03-03 | Axsome Therapeutics, Inc. | (S)-2-((S)-(2-ethoxyphenoxy)(phenyl)methyl)-4-nitrosomorpholine |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2167407B (en) * | 1984-11-22 | 1988-05-11 | Erba Farmitalia | Enantiomers of phenoxy derivatives of benzyl morpholine and salts thereof |
| AU9214498A (en) * | 1997-09-23 | 1999-04-12 | Eli Lilly And Company | Treatment of attention-deficit/hyperactivity disorder |
| UA57107C2 (uk) * | 1997-09-23 | 2003-06-16 | Елі Ліллі Енд Компані | Спосіб лікування розладу поведінки |
| UA56257C2 (uk) * | 1997-09-23 | 2003-05-15 | Елі Ліллі Енд Компані | Спосіб лікування неадекватної визивної поведінки |
| IT1305322B1 (it) * | 1998-04-23 | 2001-05-04 | Pharmacia & Upjohn Spa | Uso di reboxetina per il trattamento di disturbi nervosi |
| US6465458B1 (en) * | 1999-07-01 | 2002-10-15 | Pharmacia & Upjohn Company | Method of treating or preventing chronic pain with a highly selective norepinephrine reuptake inhibitor |
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2003
- 2003-06-04 CN CN038139839A patent/CN1662511B/zh not_active Expired - Fee Related
- 2003-06-04 CA CA002489763A patent/CA2489763C/en not_active Expired - Fee Related
- 2003-06-04 MX MXPA04011916A patent/MXPA04011916A/es active IP Right Grant
- 2003-06-04 PL PL03375211A patent/PL375211A1/xx not_active Application Discontinuation
- 2003-06-04 ES ES03725195T patent/ES2328472T3/es not_active Expired - Lifetime
- 2003-06-04 RU RU2005100846/04A patent/RU2286341C2/ru not_active IP Right Cessation
- 2003-06-04 DE DE60328787T patent/DE60328787D1/de not_active Expired - Lifetime
- 2003-06-04 CN CNA200810093308XA patent/CN101298440A/zh active Pending
- 2003-06-04 DK DK03725195T patent/DK1515959T3/da active
- 2003-06-04 AU AU2003227755A patent/AU2003227755B2/en not_active Ceased
- 2003-06-04 NZ NZ537023A patent/NZ537023A/en unknown
- 2003-06-04 WO PCT/EP2003/005261 patent/WO2003106441A1/en not_active Ceased
- 2003-06-04 AT AT03725195T patent/ATE439354T1/de not_active IP Right Cessation
- 2003-06-04 KR KR1020047020412A patent/KR100779786B1/ko not_active Expired - Fee Related
- 2003-06-04 EP EP03725195A patent/EP1515959B1/en not_active Expired - Lifetime
- 2003-06-04 US US10/588,808 patent/US20070010517A1/en not_active Abandoned
- 2003-06-04 BR BR0311878-9A patent/BR0311878A/pt not_active IP Right Cessation
- 2003-06-04 JP JP2004513273A patent/JP4563172B2/ja not_active Expired - Fee Related
- 2003-06-11 TW TW092115889A patent/TWI267510B/zh not_active IP Right Cessation
- 2003-06-11 MY MYPI20032183A patent/MY131231A/en unknown
- 2003-06-13 AR ARP030102115A patent/AR040222A1/es unknown
- 2003-06-17 PE PE2003000594A patent/PE20040565A1/es not_active Application Discontinuation
-
2004
- 2004-11-29 ZA ZA200409624A patent/ZA200409624B/xx unknown
-
2005
- 2005-01-12 NO NO20050183A patent/NO329346B1/no not_active IP Right Cessation
-
2009
- 2009-05-21 US US12/469,780 patent/US20090291953A1/en not_active Abandoned
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| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) | ||
| ASS | Change of ownership |
Owner name: PFIZER ITALIA S.R.L., IT Free format text: OLD OWNER(S): PHARMACIA ITALIA S.P.A. |