NZ503171A - A combination of a 5-HT reuptake inhibitor and a h5-HT1B antagonist or partial agonist - Google Patents
A combination of a 5-HT reuptake inhibitor and a h5-HT1B antagonist or partial agonistInfo
- Publication number
- NZ503171A NZ503171A NZ503171A NZ50317198A NZ503171A NZ 503171 A NZ503171 A NZ 503171A NZ 503171 A NZ503171 A NZ 503171A NZ 50317198 A NZ50317198 A NZ 50317198A NZ 503171 A NZ503171 A NZ 503171A
- Authority
- NZ
- New Zealand
- Prior art keywords
- tetrahydro
- methylpiperazin
- mmol
- affective
- methoxy
- Prior art date
Links
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 title claims abstract description 61
- 239000003112 inhibitor Substances 0.000 title claims abstract description 20
- 239000005557 antagonist Substances 0.000 title claims abstract description 16
- 239000004031 partial agonist Substances 0.000 title claims abstract description 11
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 29
- 230000009471 action Effects 0.000 claims abstract description 21
- 150000003839 salts Chemical class 0.000 claims abstract description 17
- 229910052736 halogen Inorganic materials 0.000 claims abstract description 11
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 10
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims abstract description 10
- 150000002367 halogens Chemical class 0.000 claims abstract description 10
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims abstract description 7
- 239000012453 solvate Substances 0.000 claims abstract description 6
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims abstract description 4
- 150000001875 compounds Chemical class 0.000 claims description 145
- 238000002360 preparation method Methods 0.000 claims description 61
- 229910052739 hydrogen Inorganic materials 0.000 claims description 25
- 239000001257 hydrogen Substances 0.000 claims description 24
- 150000002431 hydrogen Chemical group 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 230000008569 process Effects 0.000 claims description 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 208000019022 Mood disease Diseases 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- WSEQXVZVJXJVFP-HXUWFJFHSA-N (R)-citalopram Chemical compound C1([C@@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WSEQXVZVJXJVFP-HXUWFJFHSA-N 0.000 claims description 5
- 229960001653 citalopram Drugs 0.000 claims description 5
- 125000001246 bromo group Chemical group Br* 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- AHOUBRCZNHFOSL-YOEHRIQHSA-N (+)-Casbol Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-YOEHRIQHSA-N 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 3
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 claims description 3
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- HHAZUISNXJLXHR-UHFFFAOYSA-N 2-morpholin-4-ylbenzamide Chemical compound NC(=O)C1=CC=CC=C1N1CCOCC1 HHAZUISNXJLXHR-UHFFFAOYSA-N 0.000 claims description 2
- GDLIGKIOYRNHDA-UHFFFAOYSA-N Clomipramine Chemical compound C1CC2=CC=C(Cl)C=C2N(CCCN(C)C)C2=CC=CC=C21 GDLIGKIOYRNHDA-UHFFFAOYSA-N 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 229960004606 clomipramine Drugs 0.000 claims description 2
- 229960002464 fluoxetine Drugs 0.000 claims description 2
- 229960002073 sertraline Drugs 0.000 claims description 2
- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 claims description 2
- 208000020401 Depressive disease Diseases 0.000 claims 2
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- 239000004000 serotonin 1B antagonist Substances 0.000 claims 2
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- XCSBGPAPGUIEFO-OAQYLSRUSA-N n-[(2r)-5-methoxy-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-yl]-4-morpholin-4-ylbenzamide Chemical compound C([C@H](CC=12)NC(=O)C=3C=CC(=CC=3)N3CCOCC3)CC=1C(OC)=CC=C2N1CCN(C)CC1 XCSBGPAPGUIEFO-OAQYLSRUSA-N 0.000 claims 1
- HWSWMVFTXFBDRW-JOCHJYFZSA-N n-[(2r)-8-(4-methylpiperazin-1-yl)-1,2,3,4-tetrahydronaphthalen-2-yl]-4-morpholin-4-ylbenzamide Chemical compound C1CN(C)CCN1C1=CC=CC2=C1C[C@H](NC(=O)C=1C=CC(=CC=1)N1CCOCC1)CC2 HWSWMVFTXFBDRW-JOCHJYFZSA-N 0.000 claims 1
- AWSYYXWVLMMNAP-UHFFFAOYSA-N n-benzoylmorpholine-4-carboxamide Chemical compound C1COCCN1C(=O)NC(=O)C1=CC=CC=C1 AWSYYXWVLMMNAP-UHFFFAOYSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract description 53
- -1 -C(O)-morpholino Chemical group 0.000 abstract description 29
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- 239000012458 free base Substances 0.000 abstract description 4
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- 239000011541 reaction mixture Substances 0.000 description 38
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- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 36
- 239000000741 silica gel Substances 0.000 description 34
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- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 25
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 24
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Classifications
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- A—HUMAN NECESSITIES
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- 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
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- 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
- A61K31/535—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
-
- 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
-
- 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
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- 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
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Replacement Of Web Rolls (AREA)
- Winding, Rewinding, Material Storage Devices (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE9703375A SE9703375D0 (sv) | 1997-09-18 | 1997-09-18 | A new combination |
| PCT/SE1998/001601 WO1999013877A1 (en) | 1997-09-18 | 1998-09-09 | A COMBINATION OF A 5-HT REUPTAKE INHIBITOR AND A h5-HT1B ANTAGONIST OR PARTIAL AGONIST |
Publications (1)
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|---|---|
| NZ503171A true NZ503171A (en) | 2002-02-01 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ503171A NZ503171A (en) | 1997-09-18 | 1998-09-09 | A combination of a 5-HT reuptake inhibitor and a h5-HT1B antagonist or partial agonist |
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| EP (1) | EP1014985B1 (enExample) |
| JP (1) | JP2001516718A (enExample) |
| KR (1) | KR20010024076A (enExample) |
| CN (1) | CN1195519C (enExample) |
| AR (1) | AR015448A1 (enExample) |
| AT (1) | ATE240733T1 (enExample) |
| AU (1) | AU752722B2 (enExample) |
| BR (1) | BR9812088A (enExample) |
| CA (1) | CA2302382A1 (enExample) |
| DE (1) | DE69814882T2 (enExample) |
| DK (1) | DK1014985T3 (enExample) |
| EE (1) | EE04141B1 (enExample) |
| ES (1) | ES2200370T3 (enExample) |
| HU (1) | HUP0200602A3 (enExample) |
| IL (1) | IL134776A0 (enExample) |
| IS (1) | IS5406A (enExample) |
| MY (1) | MY116280A (enExample) |
| NO (1) | NO20001399L (enExample) |
| NZ (1) | NZ503171A (enExample) |
| PL (1) | PL339371A1 (enExample) |
| PT (1) | PT1014985E (enExample) |
| RU (1) | RU2214824C2 (enExample) |
| SE (1) | SE9703375D0 (enExample) |
| SK (1) | SK2852000A3 (enExample) |
| TR (1) | TR200000727T2 (enExample) |
| TW (1) | TW589183B (enExample) |
| WO (1) | WO1999013877A1 (enExample) |
| ZA (1) | ZA987817B (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9601110D0 (sv) | 1996-03-22 | 1996-03-22 | Astra Ab | Substituted 1,2,3,4-tetrahydronaphthalene derivatives |
| AR021155A1 (es) * | 1999-07-08 | 2002-06-12 | Lundbeck & Co As H | Tratamiento de desordenes neuroticos |
| UA77650C2 (en) | 1999-12-06 | 2007-01-15 | Lundbeck & Co As H | Use of serotonin reuptake inhibitor in combination with deramcyclane |
| WO2002066454A1 (fr) * | 2001-02-21 | 2002-08-29 | Sankyo Company, Limited | Derives de chromene |
| US20040198809A1 (en) * | 2001-05-01 | 2004-10-07 | Connie Sanchez | Use of enantiomeric pure escitalopram |
| ES2323451T7 (es) * | 2001-07-20 | 2011-08-01 | Psychogenics Inc. | Tratamiento para el trastorno de hiperactividad con deficit de atencion. |
| UA78974C2 (en) | 2001-10-20 | 2007-05-10 | Boehringer Ingelheim Pharma | Use of flibanserin for treating disorders of sexual desire |
| US10675280B2 (en) | 2001-10-20 | 2020-06-09 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
| SE0203778D0 (sv) * | 2002-12-09 | 2002-12-09 | Astrazeneca Ab | A new oral immediated release dosage form |
| AR047553A1 (es) | 2003-07-04 | 2006-01-25 | Lundbeck & Co As H | La combinacion de un inhibidor de reabsorcion de serotonina y agomelatina |
| KR100511288B1 (ko) * | 2003-11-14 | 2005-08-31 | 엘지전자 주식회사 | 4대의 압축기를 구비한 공기조화기의 실외기 |
| WO2006091725A1 (en) * | 2005-02-23 | 2006-08-31 | The Silvan S. Tomkins Institute | Treatment of anhedonia |
| EP1912650B8 (en) | 2005-08-03 | 2017-10-18 | Sprout Pharmaceuticals, Inc. | Use of flibanserin in the treatment of obesity |
| FR2890862B1 (fr) * | 2005-09-19 | 2008-01-25 | Sanofi Aventis Sa | Association d'agoniste aux recepteurs beta 3 et d'inhibiteur de la recapture de monoamnies, compostion pharmaceutique la contenant et son utilisation en therapeutique. |
| JP2009513604A (ja) | 2005-10-29 | 2009-04-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 月経前障害及び他の女性の性的障害治療用のベンゾイミダゾロン誘導体 |
| US8748419B2 (en) | 2006-06-16 | 2014-06-10 | Theracos, Inc. | Treating obesity with muscarinic receptor M1 antagonists |
| US7893053B2 (en) | 2006-06-16 | 2011-02-22 | Theracos, Inc. | Treating psychological conditions using muscarinic receptor M1 antagonists |
| RU2455981C2 (ru) * | 2006-06-16 | 2012-07-20 | Теракос, Инк. | Лечение ожирения антагонистами мускаринового рецептора м1 |
| ATE456369T1 (de) | 2006-06-30 | 2010-02-15 | Boehringer Ingelheim Int | Flibanserin zur behandlung von harninkontinenz und assoziierten erkrankungen |
| CL2007002214A1 (es) | 2006-08-14 | 2008-03-07 | Boehringer Ingelheim Int | Composicion farmaceutica en la forma de comprimido, donde al menos la longitud del comprimido en el estado anterior de la aplicacion es al menos 7/12 del diametro pilorico del paciente y despues de ingerirlo en estado alimentado, la longitud del comp |
| EA200900264A1 (ru) | 2006-08-14 | 2009-08-28 | Бёрингер Ингельхайм Интернациональ Гмбх | Композиции флибансерина и способ их приготовления |
| JP5220746B2 (ja) | 2006-08-25 | 2013-06-26 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 制御放出システム及びその製造方法 |
| CL2008002693A1 (es) | 2007-09-12 | 2009-10-16 | Boehringer Ingelheim Int | Uso de flibanserina para el tratamiento de sintomas vasomotores seleccionados de sofocos, sudores nocturnos, cambios de estado de animo e irritabilidad |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9119932D0 (en) * | 1991-09-18 | 1991-10-30 | Glaxo Group Ltd | Chemical compounds |
| DE69232003T2 (de) * | 1991-09-18 | 2002-04-25 | Glaxo Group Ltd., Greenford | Benzanilidderivate als 5-HT1D-Antagonisten |
| SE9601110D0 (sv) * | 1996-03-22 | 1996-03-22 | Astra Ab | Substituted 1,2,3,4-tetrahydronaphthalene derivatives |
| SE9703374D0 (sv) * | 1997-09-18 | 1997-09-18 | Astra Ab | A new combination |
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1997
- 1997-09-18 SE SE9703375A patent/SE9703375D0/xx unknown
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1998
- 1998-08-27 ZA ZA987817A patent/ZA987817B/xx unknown
- 1998-08-29 TW TW087114344A patent/TW589183B/zh not_active IP Right Cessation
- 1998-09-09 PL PL98339371A patent/PL339371A1/xx unknown
- 1998-09-09 NZ NZ503171A patent/NZ503171A/en unknown
- 1998-09-09 WO PCT/SE1998/001601 patent/WO1999013877A1/en not_active Ceased
- 1998-09-09 KR KR1020007002822A patent/KR20010024076A/ko not_active Ceased
- 1998-09-09 AT AT98944375T patent/ATE240733T1/de not_active IP Right Cessation
- 1998-09-09 CN CNB98811206XA patent/CN1195519C/zh not_active Expired - Fee Related
- 1998-09-09 ES ES98944375T patent/ES2200370T3/es not_active Expired - Lifetime
- 1998-09-09 IL IL13477698A patent/IL134776A0/xx unknown
- 1998-09-09 BR BR9812088-3A patent/BR9812088A/pt not_active IP Right Cessation
- 1998-09-09 US US09/171,580 patent/US6159971A/en not_active Expired - Fee Related
- 1998-09-09 TR TR2000/00727T patent/TR200000727T2/xx unknown
- 1998-09-09 HU HU0200602A patent/HUP0200602A3/hu unknown
- 1998-09-09 RU RU2000109563/14A patent/RU2214824C2/ru not_active IP Right Cessation
- 1998-09-09 EP EP98944375A patent/EP1014985B1/en not_active Expired - Lifetime
- 1998-09-09 DE DE69814882T patent/DE69814882T2/de not_active Expired - Fee Related
- 1998-09-09 EE EEP200000141A patent/EE04141B1/xx not_active IP Right Cessation
- 1998-09-09 CA CA002302382A patent/CA2302382A1/en not_active Abandoned
- 1998-09-09 PT PT98944375T patent/PT1014985E/pt unknown
- 1998-09-09 SK SK285-2000A patent/SK2852000A3/sk unknown
- 1998-09-09 JP JP2000511499A patent/JP2001516718A/ja active Pending
- 1998-09-09 AU AU91930/98A patent/AU752722B2/en not_active Ceased
- 1998-09-09 DK DK98944375T patent/DK1014985T3/da active
- 1998-09-16 MY MYPI98004225A patent/MY116280A/en unknown
- 1998-09-17 AR ARP980104634A patent/AR015448A1/es unknown
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2000
- 2000-03-15 IS IS5406A patent/IS5406A/is unknown
- 2000-03-17 NO NO20001399A patent/NO20001399L/no not_active Application Discontinuation
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