EP1175215A2 - L'osanetant dans le traitement des troubles de l'humeur - Google Patents
L'osanetant dans le traitement des troubles de l'humeurInfo
- Publication number
- EP1175215A2 EP1175215A2 EP00918941A EP00918941A EP1175215A2 EP 1175215 A2 EP1175215 A2 EP 1175215A2 EP 00918941 A EP00918941 A EP 00918941A EP 00918941 A EP00918941 A EP 00918941A EP 1175215 A2 EP1175215 A2 EP 1175215A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- osanetant
- treatment
- disorders
- mood disorders
- production
- 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.)
- Withdrawn
Links
- 208000019022 Mood disease Diseases 0.000 title claims abstract description 7
- 239000003814 drug Substances 0.000 title claims abstract description 5
- DZOJBGLFWINFBF-UMSFTDKQSA-N osanetant Chemical compound C([C@](C1)(CCCN2CCC(CC2)(N(C(C)=O)C)C=2C=CC=CC=2)C=2C=C(Cl)C(Cl)=CC=2)CCN1C(=O)C1=CC=CC=C1 DZOJBGLFWINFBF-UMSFTDKQSA-N 0.000 title abstract description 11
- 229950009875 osanetant Drugs 0.000 title abstract description 11
- 150000003839 salts Chemical class 0.000 claims abstract description 7
- 208000020401 Depressive disease Diseases 0.000 claims description 11
- 208000024714 major depressive disease Diseases 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- 230000036506 anxiety Effects 0.000 claims description 2
- 208000024732 dysthymic disease Diseases 0.000 claims description 2
- 239000002775 capsule Substances 0.000 description 5
- 150000001875 compounds Chemical class 0.000 description 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- 229920003081 Povidone K 30 Polymers 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 239000002050 international nonproprietary name Substances 0.000 description 2
- 238000007918 intramuscular administration Methods 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 229960001021 lactose monohydrate Drugs 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 238000005550 wet granulation Methods 0.000 description 2
- -1 3- (1-benzoyl-3- (3,4-dichlorophenyl) piperidin-3-yl) propyl Chemical group 0.000 description 1
- 101001125071 Homo sapiens Neuromedin-K receptor Proteins 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 description 1
- 229940123445 Tricyclic antidepressant Drugs 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000001430 anti-depressive effect Effects 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 239000012059 conventional drug carrier Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000003291 dopaminomimetic effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 229910003002 lithium salt Inorganic materials 0.000 description 1
- 159000000002 lithium salts Chemical class 0.000 description 1
- 239000002899 monoamine oxidase inhibitor Substances 0.000 description 1
- 230000002474 noradrenergic effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000000697 serotonin reuptake Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
Classifications
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
Definitions
- the subject of the present invention is a new use of the osanetant.
- the osanetant is the International Nonproprietary Name (INN) of (R) - (+) - N - [(3- (1-benzoyl-3- (3,4-dichlorophenyl) piperidin-3-yl) propyl) -4 - phenylpiperidin-4-yl] -N-methyl acetamide of formula:
- ososetant and its pharmaceutically acceptable salts are useful in the treatment of mood disorders, in particular in the treatment of depression.
- depression is meant in particular major depressive disorders minor depressive disorders, dysthymic disorders, depressive disorders associated with anxiety as well as depressive disorders associated with bipolar disorders.
- ososetant The effect of ososetant on major depressive disorders is studied in patients aged 18 to 65 years. Patients receive osmetanant (200 mg / day) for a period of approximately 6 weeks. The improvement in depressive syndromes is measured by a significant decrease in scores on the Hamilton scale (J. Neurol. Neurosurg. Psychiat., 1960, 23, 56-62) as well as by the collection of impressions from the clinician and overall patient impressions.
- the subject of the present invention is the use of the osanetant and its pharmaceutically acceptable salts for the preparation of drugs useful in the treatment of mood disorders, particularly in the treatment of depression.
- Ososetant and its pharmaceutically acceptable salts are prepared according to European patent application EP 673 928, likewise the pharmaceutical compositions can be prepared according to the description of this same patent application.
- compositions of the present invention for oral, sublingual, subcutaneous, intramuscular, intravenous, transdermal, local or rectal administration
- the active ingredient alone or in combination with another active ingredient can be administered in unit form of administration, in admixture with conventional pharmaceutical carriers, to animals and humans.
- Suitable unit administration forms include oral forms such as tablets, capsules, powders, granules and oral solutions or suspensions, sublingual and oral administration forms, aerosols, implants, forms subcutaneous, transdermal, intramuscular, intravenous, intranasal and rectal administration forms.
- the daily dosage of the compound according to the invention is from 0.05 to 5 mg / kg, advantageously from 1 to 2.5 mg / kg, preferably from 2 to 2.5 mg / kg, to be administered in one or more times.
- the compounds are generally formulated in dosage unit containing from 2.5 to 500 mg, advantageously from 50 to 250 mg, preferably from 100 to 250 mg, of active principle per dosage unit, to be administered once, twice or more times , as required.
- these dosages are examples of average situations, there may be special cases where higher or lower dosages are appropriate, such dosages also belong to the invention.
- the appropriate dosage for each patient is determined by the doctor according to the mode of administration, the age, the weight and the response of said patient.
- oral forms of administration are preferred.
- the compounds according to the invention can be administered in combination with another active principle, in particular another antidepressant such as a lithium salt, a tricyclic antidepressant, a monoamine oxidase inhibitor or a serotonin reuptake reuptake inhibitor, by example.
- another antidepressant such as a lithium salt, a tricyclic antidepressant, a monoamine oxidase inhibitor or a serotonin reuptake reuptake inhibitor, by example.
- the invention also relates to a method of treatment of mood disorders, more particularly, to a method of treatment of depression, by administration to the patient of an appropriate dose of osanetant or of a pharmaceutically salt thereof. acceptable.
- EXAMPLE 1 Capsule with 250 mg of osanetant. osanetant 250 mg lactose monohydrate (200 mesh) 40.80 mg corn starch 40.80 mg povidone K-30 8.40 mg purified water * 90.00 mg magnesium stearate 3.40 mg for an opaque white capsule of size 0 , filled to 343.4 mg
- EXAMPLE 2 Capsule with 100 mg of osanetant. osanetant 100 mg lactose monohydrate (200 mesh) 115.80 mg corn starch 115.80 mg povidone K-30 8.40 mg purified water * 90.00 mg magnesium stearate 3.40 mg for an opaque white capsule of size 0 , filled to 343.4 mg
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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9904699 | 1999-04-13 | ||
| FR9904699A FR2792199B3 (fr) | 1999-04-13 | 1999-04-13 | Utilisation de l'osanetant pour la preparation de medicaments utiles dans le traitement des troubles de l'humeur |
| PCT/FR2000/000924 WO2000061125A2 (fr) | 1999-04-13 | 2000-04-11 | L'osanetant dans le traitement des troubles de l'humeur |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EP1175215A2 true EP1175215A2 (fr) | 2002-01-30 |
Family
ID=9544412
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP00918941A Withdrawn EP1175215A2 (fr) | 1999-04-13 | 2000-04-11 | L'osanetant dans le traitement des troubles de l'humeur |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US6420388B1 (id) |
| EP (1) | EP1175215A2 (id) |
| JP (1) | JP2002541190A (id) |
| KR (1) | KR20010105418A (id) |
| CN (1) | CN1354662A (id) |
| AR (1) | AR023452A1 (id) |
| AU (1) | AU3971600A (id) |
| BG (1) | BG105984A (id) |
| BR (1) | BR0009704A (id) |
| CA (1) | CA2369638A1 (id) |
| CZ (1) | CZ20013645A3 (id) |
| EE (1) | EE200100527A (id) |
| FR (1) | FR2792199B3 (id) |
| HR (1) | HRP20010741A2 (id) |
| HU (1) | HUP0200655A3 (id) |
| ID (1) | ID30458A (id) |
| IS (1) | IS6098A (id) |
| MX (1) | MXPA01010340A (id) |
| NO (1) | NO20014953L (id) |
| PE (1) | PE20010032A1 (id) |
| PL (1) | PL351554A1 (id) |
| SK (1) | SK14552001A3 (id) |
| TR (1) | TR200102930T2 (id) |
| WO (1) | WO2000061125A2 (id) |
| ZA (1) | ZA200108289B (id) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001095904A1 (en) * | 2000-06-12 | 2001-12-20 | University Of Rochester | Method of treating symptoms of hormonal variation, including hot flashes, using tachykinin receptor antagonist |
| CA2549956C (en) * | 2003-12-22 | 2016-04-12 | Glaxo Group Limited | Immunoglobulins |
| WO2005094801A1 (en) * | 2004-03-25 | 2005-10-13 | Smithkline Beecham Corporation | Use of an nk3 antagonist for the treatment of bipolar disorders |
| US8193146B2 (en) * | 2005-03-15 | 2012-06-05 | Sumitomo Chemical Company, Limited | Method of ameliorating symptom caused by mood disturbance |
| JP2006320201A (ja) * | 2005-05-17 | 2006-11-30 | Sumitomo Chemical Co Ltd | 気分障害又は関連障害による疾患症状を改善させる方法 |
| GB0525662D0 (en) | 2005-12-16 | 2006-01-25 | Glaxo Group Ltd | Immunoglobulins |
| WO2015200594A2 (en) * | 2014-06-25 | 2015-12-30 | Emory University | Methods of managing conditioned fear with neurokinin receptor antagonists |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2719311B1 (fr) | 1994-03-18 | 1998-06-26 | Sanofi Sa | Composés antagonistes sélectifs du récepteur NK3 humain et leur utilisation comme médicaments et outils de diagnostic. |
| FR2729954B1 (fr) * | 1995-01-30 | 1997-08-01 | Sanofi Sa | Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant |
| FR2738819B1 (fr) | 1995-09-14 | 1997-12-05 | Sanofi Sa | Nouveaux composes antagonistes selectifs du recepteur nk3 humain, procede pour leur obtention et compositions pharmaceutiques les contenant |
| AU4176997A (en) | 1996-09-16 | 1998-04-02 | Warner-Lambert Company | 3-alkyl-3-phenyl-piperidines |
-
1999
- 1999-04-13 FR FR9904699A patent/FR2792199B3/fr not_active Expired - Fee Related
-
2000
- 2000-04-11 HU HU0200655A patent/HUP0200655A3/hu unknown
- 2000-04-11 BR BR0009704-7A patent/BR0009704A/pt not_active Application Discontinuation
- 2000-04-11 PL PL00351554A patent/PL351554A1/xx not_active Application Discontinuation
- 2000-04-11 MX MXPA01010340A patent/MXPA01010340A/es not_active Application Discontinuation
- 2000-04-11 US US09/958,266 patent/US6420388B1/en not_active Expired - Fee Related
- 2000-04-11 HR HR20010741A patent/HRP20010741A2/hr not_active Application Discontinuation
- 2000-04-11 TR TR2001/02930T patent/TR200102930T2/xx unknown
- 2000-04-11 CZ CZ20013645A patent/CZ20013645A3/cs unknown
- 2000-04-11 AU AU39716/00A patent/AU3971600A/en not_active Abandoned
- 2000-04-11 EE EEP200100527A patent/EE200100527A/xx unknown
- 2000-04-11 SK SK1455-2001A patent/SK14552001A3/sk unknown
- 2000-04-11 EP EP00918941A patent/EP1175215A2/fr not_active Withdrawn
- 2000-04-11 JP JP2000610458A patent/JP2002541190A/ja not_active Withdrawn
- 2000-04-11 KR KR1020017012990A patent/KR20010105418A/ko not_active Withdrawn
- 2000-04-11 WO PCT/FR2000/000924 patent/WO2000061125A2/fr not_active Ceased
- 2000-04-11 ID IDW00200102144A patent/ID30458A/id unknown
- 2000-04-11 CN CN00806091A patent/CN1354662A/zh active Pending
- 2000-04-11 CA CA002369638A patent/CA2369638A1/en not_active Abandoned
- 2000-04-12 AR ARP000101670A patent/AR023452A1/es unknown
- 2000-04-13 PE PE2000000343A patent/PE20010032A1/es not_active Application Discontinuation
-
2001
- 2001-09-28 IS IS6098A patent/IS6098A/is unknown
- 2001-10-05 BG BG105984A patent/BG105984A/bg unknown
- 2001-10-09 ZA ZA200108289A patent/ZA200108289B/xx unknown
- 2001-10-11 NO NO20014953A patent/NO20014953L/no not_active Application Discontinuation
Non-Patent Citations (1)
| Title |
|---|
| See references of WO0061125A2 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU3971600A (en) | 2000-11-14 |
| CA2369638A1 (en) | 2000-10-19 |
| MXPA01010340A (es) | 2002-05-06 |
| CZ20013645A3 (cs) | 2002-01-16 |
| HRP20010741A2 (en) | 2002-10-31 |
| WO2000061125A2 (fr) | 2000-10-19 |
| FR2792199B3 (fr) | 2001-05-18 |
| US6420388B1 (en) | 2002-07-16 |
| KR20010105418A (ko) | 2001-11-28 |
| TR200102930T2 (tr) | 2002-04-22 |
| AR023452A1 (es) | 2002-09-04 |
| NO20014953D0 (no) | 2001-10-11 |
| JP2002541190A (ja) | 2002-12-03 |
| IS6098A (is) | 2001-09-28 |
| FR2792199A1 (fr) | 2000-10-20 |
| EE200100527A (et) | 2002-12-16 |
| ZA200108289B (en) | 2002-12-24 |
| WO2000061125A3 (fr) | 2001-04-19 |
| CN1354662A (zh) | 2002-06-19 |
| SK14552001A3 (sk) | 2002-02-05 |
| HUP0200655A2 (hu) | 2002-07-29 |
| NO20014953L (no) | 2001-12-11 |
| BG105984A (bg) | 2002-04-30 |
| BR0009704A (pt) | 2002-01-08 |
| PL351554A1 (en) | 2003-05-05 |
| ID30458A (id) | 2001-12-06 |
| PE20010032A1 (es) | 2001-04-11 |
| HUP0200655A3 (en) | 2002-11-28 |
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