RU2396957C2 - S-миртазапин для лечения приливов - Google Patents
S-миртазапин для лечения приливов Download PDFInfo
- Publication number
- RU2396957C2 RU2396957C2 RU2007122391/14A RU2007122391A RU2396957C2 RU 2396957 C2 RU2396957 C2 RU 2396957C2 RU 2007122391/14 A RU2007122391/14 A RU 2007122391/14A RU 2007122391 A RU2007122391 A RU 2007122391A RU 2396957 C2 RU2396957 C2 RU 2396957C2
- Authority
- RU
- Russia
- Prior art keywords
- mirtazapine
- treatment
- rats
- vasomotor symptoms
- hot flashes
- Prior art date
Links
- RONZAEMNMFQXRA-MRXNPFEDSA-N esmirtazapine Chemical compound C1C2=CC=CN=C2N2CCN(C)C[C@@H]2C2=CC=CC=C21 RONZAEMNMFQXRA-MRXNPFEDSA-N 0.000 title claims abstract description 39
- 206010060800 Hot flush Diseases 0.000 title claims abstract description 38
- 208000033830 Hot Flashes Diseases 0.000 title claims abstract description 36
- 239000003814 drug Substances 0.000 claims abstract description 20
- 229960001785 mirtazapine Drugs 0.000 claims abstract description 20
- RONZAEMNMFQXRA-UHFFFAOYSA-N mirtazapine Chemical compound C1C2=CC=CN=C2N2CCN(C)CC2C2=CC=CC=C21 RONZAEMNMFQXRA-UHFFFAOYSA-N 0.000 claims abstract description 19
- 229940079593 drug Drugs 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 9
- 239000004480 active ingredient Substances 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 230000000694 effects Effects 0.000 abstract description 28
- 239000000126 substance Substances 0.000 abstract 1
- 241000700159 Rattus Species 0.000 description 45
- 208000024891 symptom Diseases 0.000 description 44
- 230000001457 vasomotor Effects 0.000 description 40
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 17
- 230000037023 motor activity Effects 0.000 description 13
- 210000001672 ovary Anatomy 0.000 description 10
- 238000002474 experimental method Methods 0.000 description 8
- 229940088597 hormone Drugs 0.000 description 8
- 239000000902 placebo Substances 0.000 description 8
- 229940068196 placebo Drugs 0.000 description 8
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 8
- 239000005556 hormone Substances 0.000 description 7
- 241001465754 Metazoa Species 0.000 description 5
- 229940011871 estrogen Drugs 0.000 description 5
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- 230000009245 menopause Effects 0.000 description 5
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- 102000012673 Follicle Stimulating Hormone Human genes 0.000 description 4
- 108010079345 Follicle Stimulating Hormone Proteins 0.000 description 4
- 239000002585 base Substances 0.000 description 4
- 239000002775 capsule Substances 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 229940028334 follicle stimulating hormone Drugs 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 206010016334 Feeling hot Diseases 0.000 description 3
- PIWKPBJCKXDKJR-UHFFFAOYSA-N Isoflurane Chemical compound FC(F)OC(Cl)C(F)(F)F PIWKPBJCKXDKJR-UHFFFAOYSA-N 0.000 description 3
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- 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 description 2
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 description 2
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 2
- 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 2
- 201000000736 Amenorrhea Diseases 0.000 description 2
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- 208000019901 Anxiety disease Diseases 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
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- 208000037490 Medically Unexplained Symptoms Diseases 0.000 description 2
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
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- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 description 2
- 229930182833 estradiol Natural products 0.000 description 2
- 229960002464 fluoxetine Drugs 0.000 description 2
- 239000012458 free base Substances 0.000 description 2
- 239000007943 implant Substances 0.000 description 2
- 238000002513 implantation Methods 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
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- 230000006742 locomotor activity Effects 0.000 description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
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- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 229940124531 pharmaceutical excipient Drugs 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 230000035807 sensation Effects 0.000 description 2
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- 208000019116 sleep disease Diseases 0.000 description 2
- 230000002269 spontaneous effect Effects 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 238000012546 transfer Methods 0.000 description 2
- 230000007704 transition Effects 0.000 description 2
- 230000004614 tumor growth Effects 0.000 description 2
- 210000004291 uterus Anatomy 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- 229940082496 Adrenoreceptor antagonist Drugs 0.000 description 1
- 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 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 206010012374 Depressed mood Diseases 0.000 description 1
- 206010016275 Fear Diseases 0.000 description 1
- SXRSQZLOMIGNAQ-UHFFFAOYSA-N Glutaraldehyde Chemical compound O=CCCCC=O SXRSQZLOMIGNAQ-UHFFFAOYSA-N 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 229940123486 Hormone receptor agonist Drugs 0.000 description 1
- RONZAEMNMFQXRA-INIZCTEOSA-N LSM-5894 Chemical compound C1C2=CC=CN=C2N2CCN(C)C[C@H]2C2=CC=CC=C21 RONZAEMNMFQXRA-INIZCTEOSA-N 0.000 description 1
- 229920004011 Macrolon® Polymers 0.000 description 1
- BQCADISMDOOEFD-UHFFFAOYSA-N Silver Chemical compound [Ag] BQCADISMDOOEFD-UHFFFAOYSA-N 0.000 description 1
- 206010072170 Skin wound Diseases 0.000 description 1
- BLGXFZZNTVWLAY-CCZXDCJGSA-N Yohimbine Natural products C1=CC=C2C(CCN3C[C@@H]4CC[C@@H](O)[C@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-CCZXDCJGSA-N 0.000 description 1
- 210000003489 abdominal muscle Anatomy 0.000 description 1
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- 239000003098 androgen Substances 0.000 description 1
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- 238000010171 animal model Methods 0.000 description 1
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- 239000000935 antidepressant agent Substances 0.000 description 1
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- 238000013459 approach Methods 0.000 description 1
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- BLGXFZZNTVWLAY-UHFFFAOYSA-N beta-Yohimbin Natural products C1=CC=C2C(CCN3CC4CCC(O)C(C4CC33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-UHFFFAOYSA-N 0.000 description 1
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- 230000005540 biological transmission Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 229960001736 buprenorphine Drugs 0.000 description 1
- 229960002798 cetrimide Drugs 0.000 description 1
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- 229960003333 chlorhexidine gluconate Drugs 0.000 description 1
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- 230000004064 dysfunction Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 230000001135 feminizing effect Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 235000012907 honey Nutrition 0.000 description 1
- 239000000698 hormone receptor stimulating agent Substances 0.000 description 1
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- 230000036565 night sweats Effects 0.000 description 1
- 206010029410 night sweats Diseases 0.000 description 1
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 description 1
- 238000009806 oophorectomy Methods 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000027758 ovulation cycle Effects 0.000 description 1
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- -1 trifluorophenyl-difluoromethyl ether Chemical compound 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 230000005186 women's health Effects 0.000 description 1
- BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 description 1
- 229960000317 yohimbine Drugs 0.000 description 1
- AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 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
- A61K31/55—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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04105778.7 | 2004-11-15 | ||
| EP04105778 | 2004-11-15 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2007122391A RU2007122391A (ru) | 2008-12-20 |
| RU2396957C2 true RU2396957C2 (ru) | 2010-08-20 |
Family
ID=34929859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007122391/14A RU2396957C2 (ru) | 2004-11-15 | 2005-11-14 | S-миртазапин для лечения приливов |
Country Status (30)
| Country | Link |
|---|---|
| US (4) | US20070265245A1 (enExample) |
| EP (1) | EP1814555B1 (enExample) |
| JP (1) | JP2008519810A (enExample) |
| KR (1) | KR20070085470A (enExample) |
| CN (2) | CN102772414A (enExample) |
| AR (1) | AR053780A1 (enExample) |
| AT (1) | ATE439843T1 (enExample) |
| AU (1) | AU2005303778B2 (enExample) |
| BR (1) | BRPI0517818A2 (enExample) |
| CA (1) | CA2587283C (enExample) |
| CY (1) | CY1110538T1 (enExample) |
| DE (1) | DE602005016141D1 (enExample) |
| DK (1) | DK1814555T3 (enExample) |
| ES (1) | ES2329815T3 (enExample) |
| HR (1) | HRP20090513T1 (enExample) |
| IL (1) | IL182767A (enExample) |
| MX (1) | MX2007005827A (enExample) |
| MY (1) | MY144089A (enExample) |
| NO (1) | NO20072285L (enExample) |
| NZ (1) | NZ554858A (enExample) |
| PE (1) | PE20061051A1 (enExample) |
| PL (1) | PL1814555T3 (enExample) |
| PT (1) | PT1814555E (enExample) |
| RS (1) | RS51138B (enExample) |
| RU (1) | RU2396957C2 (enExample) |
| SI (1) | SI1814555T1 (enExample) |
| TW (1) | TW200631584A (enExample) |
| UA (1) | UA88655C2 (enExample) |
| WO (1) | WO2006051111A1 (enExample) |
| ZA (1) | ZA200703884B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007002174A2 (en) * | 2005-06-27 | 2007-01-04 | N.V. Organon. | A method of treatment of hormone depletion induced vasomotor symptoms |
| US20070129611A1 (en) * | 2005-12-06 | 2007-06-07 | University Of North Texas Health Science Center At Fort Worth | System, Method and Apparatus for Assessing Menopausal or Post-Hysterectomy Symptoms |
| CA2644985A1 (en) * | 2006-03-06 | 2007-09-13 | N.V. Organon | An improved method of weaning from hormonal treatment of hormone depletion induced vasomotor symptoms |
| US20100129425A1 (en) * | 2006-11-22 | 2010-05-27 | N.V. Organon | Vaginal delivery system for mirtazapine |
| US7645750B2 (en) * | 2006-12-13 | 2010-01-12 | Yung Shin Pharmaceutical Ind. Co., Ltd. | Method of treating symptoms of hormonal variations |
| JP2009018992A (ja) | 2007-07-10 | 2009-01-29 | Sumitomo Chemical Co Ltd | 光学活性ミルタザピンの製造方法 |
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