RU2003126176A - Кислотно-аддитивные соли тербинафина и яблочной кислоты - Google Patents
Кислотно-аддитивные соли тербинафина и яблочной кислоты Download PDFInfo
- Publication number
- RU2003126176A RU2003126176A RU2003126176/04A RU2003126176A RU2003126176A RU 2003126176 A RU2003126176 A RU 2003126176A RU 2003126176/04 A RU2003126176/04 A RU 2003126176/04A RU 2003126176 A RU2003126176 A RU 2003126176A RU 2003126176 A RU2003126176 A RU 2003126176A
- Authority
- RU
- Russia
- Prior art keywords
- compound according
- compound
- salt
- formula
- malic acid
- Prior art date
Links
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical class OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 title claims abstract 6
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Chemical class OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 title claims abstract 6
- 239000001630 malic acid Chemical class 0.000 title claims abstract 6
- 235000011090 malic acid Nutrition 0.000 title claims abstract 6
- 239000000654 additive Substances 0.000 title 1
- DOMXUEMWDBAQBQ-WEVVVXLNSA-N terbinafine Chemical class C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 DOMXUEMWDBAQBQ-WEVVVXLNSA-N 0.000 title 1
- 229960002722 terbinafine Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 15
- 150000003839 salts Chemical class 0.000 claims abstract 8
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 3
- 239000012458 free base Substances 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- KYARBIJYVGJZLB-UHFFFAOYSA-N 7-amino-4-hydroxy-2-naphthalenesulfonic acid Chemical compound OC1=CC(S(O)(=O)=O)=CC2=CC(N)=CC=C21 KYARBIJYVGJZLB-UHFFFAOYSA-N 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 208000010195 Onychomycosis Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002538 fungal effect Effects 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 201000005882 tinea unguium Diseases 0.000 claims 1
- 230000001857 anti-mycotic effect Effects 0.000 abstract 1
- 239000002543 antimycotic Substances 0.000 abstract 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
- C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
- C07C211/30—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system formed by two rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Emergency Medicine (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Surgery (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Seasonings (AREA)
Claims (10)
1. Соль соединения формулы I
и яблочной кислоты.
2. Соединение по п.1 в форме L-(-)-бималата.
3. Способ получения соединение по п.1, отличающийся тем, что соединение формулы I в форме свободного основания подвергают взаимодействию с соответствующей формой яблочной кислоты и выделяют образовавшуюся соль из реакционной смеси.
4. Фармацевтическая композиция, содержащая соединение по п.1, в сочетании по меньшей мере с одним фармацевтически приемлемым носителем или разбавителем.
5. Фармацевтическая композиция, содержащая соединение формулы I в форме свободного основания или форме фармацевтически приемлемой соли, отличной от формы кислотно-аддитивной соли яблочной кислоты, в случае, когда она получена на основе соединения по п.1.
6. Соединение по п.1, предназначенное для применения в качестве фармацевтического средства.
7. Соединение по п.1, предназначенное для приготовления лекарственного средства.
8. Соединение формулы I в форме свободного основания или в форме соли, отличной от формы кислотно-аддитивной соли яблочной кислоты, в случае, когда она получена из соединения по п.1.
9. Применение соединения по п.1 для приготовления лекарственного средства, предназначенного для лечения заболеваний, поддающихся лечению соединением формулы I в форме свободного основания или в форме соли.
10. Способ профилактики или терапевтического лечения грибковых заболеваний, таких как грибковый синусит или онихомикоз, заключающийся в том, что пациенту, нуждающемуся в таком лечении, вводят терапевтически эффективное количество соединения по п.1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0103046.9A GB0103046D0 (en) | 2001-02-07 | 2001-02-07 | Organic Compounds |
| GB0103046.9 | 2001-02-07 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2003126176A true RU2003126176A (ru) | 2005-03-10 |
| RU2289570C2 RU2289570C2 (ru) | 2006-12-20 |
Family
ID=9908301
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2003126176/04A RU2289570C2 (ru) | 2001-02-07 | 2002-02-06 | Кислотно-аддитивные соли тербинафина и яблочной кислоты, способ их получения и фармацевтическая композиция для лечения грибковой инфекции |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US20040147603A1 (ru) |
| EP (1) | EP1370513B1 (ru) |
| JP (1) | JP4078206B2 (ru) |
| KR (2) | KR100859609B1 (ru) |
| CN (1) | CN1216034C (ru) |
| AT (1) | ATE294154T1 (ru) |
| AU (1) | AU2002238534C1 (ru) |
| BR (1) | BR0207077A (ru) |
| CA (1) | CA2437592A1 (ru) |
| CZ (1) | CZ20032132A3 (ru) |
| DE (1) | DE60203890T2 (ru) |
| DK (1) | DK1370513T3 (ru) |
| EC (1) | ECSP034713A (ru) |
| ES (1) | ES2240698T3 (ru) |
| GB (1) | GB0103046D0 (ru) |
| HU (1) | HUP0303174A3 (ru) |
| IL (2) | IL157241A0 (ru) |
| MX (1) | MXPA03007072A (ru) |
| NO (1) | NO20033473L (ru) |
| NZ (1) | NZ527300A (ru) |
| PL (1) | PL204812B1 (ru) |
| PT (1) | PT1370513E (ru) |
| RU (1) | RU2289570C2 (ru) |
| SI (1) | SI1370513T1 (ru) |
| SK (1) | SK9992003A3 (ru) |
| WO (1) | WO2002070455A1 (ru) |
| ZA (1) | ZA200306029B (ru) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003244633A1 (en) * | 2002-07-02 | 2004-01-23 | Novartis Ag | Methods for the treatment of sinusitis |
| GB0503942D0 (en) * | 2005-02-25 | 2005-04-06 | Novartis Ag | Purification process |
| RU2286144C2 (ru) * | 2004-12-02 | 2006-10-27 | Государственное научное учреждение Институт экспериментальной ветеринарии Сибири и Дальнего Востока Сибирского отделения Россельхозакадемии (ГНУ ИЭВСиДВ СО РАСХН) | Способ лечения микроспории кошек |
| WO2007104474A1 (en) * | 2006-03-10 | 2007-09-20 | Novartis Ag | Antifungal compositions comprising (1) a salt of terbinafine with malic acid and (2) malic acid |
| AU2007260739A1 (en) * | 2006-06-14 | 2007-12-21 | Dr. Reddy's Laboratories Limited | Topical compositions |
| RU2350343C1 (ru) * | 2007-08-13 | 2009-03-27 | Государственное научное учреждение Институт экспериментальной ветеринарии Сибири и Дальнего Востока Сибирского отделения Россельхозакадемии (ГНУ ИЭВС и ДВ СО Россельхозакадемии) | Способ лечения микроспории кошек |
| DK2387563T4 (da) | 2009-01-16 | 2022-07-18 | Exelixis Inc | Malatsalt af n-(4-{ [ 6, 7-bis(methyloxy)quinolin-4-yl]oxy}phenyl-n'-(4-fluorphenyl)cyclopropan-1,1-dicarboxamid, og krystallinske former deraf til behandling af cancer |
| CN106106449A (zh) * | 2016-06-21 | 2016-11-16 | 广西中烟工业有限责任公司 | 特比萘芬制剂及其在提高烟叶角鲨烯含量中的应用 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3507755A (en) * | 1967-10-17 | 1970-04-21 | Bayer Ag | Process for the purification of acrylonitrile by distillation with side stream withdrawal and decantation |
| US4276125A (en) | 1979-02-02 | 1981-06-30 | Asahi Kasei Kogyo Kabushiki Kaisha | Process for purification of crude olefinically unsaturated nitrile and condenser useful for same process |
| US4269667A (en) | 1979-08-02 | 1981-05-26 | Standard Oil Company | Acrylonitrile purification by extractive distillation |
| CY1410A (en) * | 1979-08-22 | 1988-04-22 | Sandoz Ag | Propenylamines, processes for their production, pharmaceutical compositions containing them and their use as pharmaceuticals |
| KR850001603B1 (ko) | 1980-12-03 | 1985-10-24 | 아사히 가세이 고오교오 가부시기가이샤 | 불포화 니트릴의 제조법 |
| GB8608335D0 (en) | 1986-04-04 | 1986-05-08 | Pfizer Ltd | Pharmaceutically acceptable salts |
| NZ227042A (en) * | 1987-11-27 | 1991-05-28 | Banyu Pharma Co Ltd | Substituted alkylamine derivatives and pharmaceutical compositions |
| HU223343B1 (hu) * | 1991-05-20 | 2004-06-28 | Novartis Ag. | Allil-amin-származékot tartalmazó gyógyászati készítmények és eljárás azok előállítására |
| US6005001A (en) * | 1991-05-20 | 1999-12-21 | Novartis Ag (Formerly Sandoz Ag) | Pharmaceutical composition |
| HU219480B (hu) | 1991-05-23 | 2001-04-28 | Novartis Ag. | Eljárás gombás körömmegbetegségek ellen helyileg alkalmazható, allil-amin-származékot tartalmazó gyógyászati készítmények előállítására |
| US5461068A (en) * | 1993-09-29 | 1995-10-24 | Corwood Laboratories, Inc. | Imidazole derivative tincture and method of manufacture |
| DE4400770C1 (de) * | 1994-01-13 | 1995-02-02 | Lohmann Therapie Syst Lts | Wirkstoffhaltiges Pflaster zur Abgabe von Estradiol mit mindestens einem Penetrationsverstärker, Verfahren zu seiner Herstellung und seine Verwendung |
| NZ280065A (en) * | 1995-09-20 | 1998-04-27 | Apotex Inc | Preparation of n-alkyl-n-(1-naphthylmethyl)alk-2-en-4-ynylamine derivatives |
| JP2001518879A (ja) * | 1997-03-31 | 2001-10-16 | ジョンソン・アンド・ジョンソン・コンシューマー・カンパニーズ・インコーポレイテッド | 薬剤化合物の向上した浸透性のための溶媒システム |
| AU3212099A (en) | 1998-03-31 | 1999-10-18 | Johnson & Johnson Consumer Companies, Inc. | Method for increasing the permeability of horny human tissue |
| US6231875B1 (en) | 1998-03-31 | 2001-05-15 | Johnson & Johnson Consumer Companies, Inc. | Acidified composition for topical treatment of nail and skin conditions |
| ATE292956T1 (de) * | 1998-07-24 | 2005-04-15 | Seo Hong Yoo | Klare wässrige lösungen enthaltend gallensäuren |
| JP2000053681A (ja) | 1998-08-10 | 2000-02-22 | Sankyo Co Ltd | 三環性複素環化合物を含有する抗菌剤 |
| DK1222160T3 (da) | 1999-10-22 | 2003-11-17 | Richter Gedeon Vegyeszet | Fremgangsmåde til fremstilling af substituerede allylaminderivater og salte deraf |
| GB0014448D0 (en) | 2000-06-13 | 2000-08-09 | Novartis Ag | Organic compounds |
| JP4899139B2 (ja) | 2000-08-10 | 2012-03-21 | 株式会社ポーラファルマ | 抗真菌医薬組成物 |
| JP4803511B2 (ja) | 2000-08-25 | 2011-10-26 | 株式会社ポーラファルマ | 抗真菌医薬組成物 |
| JP2002068975A (ja) | 2000-08-25 | 2002-03-08 | Pola Chem Ind Inc | 抗真菌医薬組成物 |
-
2001
- 2001-02-07 GB GBGB0103046.9A patent/GB0103046D0/en not_active Ceased
-
2002
- 2002-02-06 SI SI200230146T patent/SI1370513T1/xx unknown
- 2002-02-06 AU AU2002238534A patent/AU2002238534C1/en not_active Ceased
- 2002-02-06 NZ NZ527300A patent/NZ527300A/en unknown
- 2002-02-06 PL PL362554A patent/PL204812B1/pl not_active IP Right Cessation
- 2002-02-06 MX MXPA03007072A patent/MXPA03007072A/es active IP Right Grant
- 2002-02-06 AT AT02704689T patent/ATE294154T1/de not_active IP Right Cessation
- 2002-02-06 IL IL15724102A patent/IL157241A0/xx unknown
- 2002-02-06 CZ CZ20032132A patent/CZ20032132A3/cs unknown
- 2002-02-06 WO PCT/EP2002/001249 patent/WO2002070455A1/en not_active Ceased
- 2002-02-06 HU HU0303174A patent/HUP0303174A3/hu unknown
- 2002-02-06 BR BR0207077-4A patent/BR0207077A/pt not_active IP Right Cessation
- 2002-02-06 RU RU2003126176/04A patent/RU2289570C2/ru not_active IP Right Cessation
- 2002-02-06 JP JP2002569776A patent/JP4078206B2/ja not_active Expired - Fee Related
- 2002-02-06 ES ES02704689T patent/ES2240698T3/es not_active Expired - Lifetime
- 2002-02-06 SK SK999-2003A patent/SK9992003A3/sk not_active Application Discontinuation
- 2002-02-06 PT PT02704689T patent/PT1370513E/pt unknown
- 2002-02-06 EP EP02704689A patent/EP1370513B1/en not_active Expired - Lifetime
- 2002-02-06 US US10/470,885 patent/US20040147603A1/en not_active Abandoned
- 2002-02-06 CA CA002437592A patent/CA2437592A1/en not_active Abandoned
- 2002-02-06 DK DK02704689T patent/DK1370513T3/da active
- 2002-02-06 CN CN028046080A patent/CN1216034C/zh not_active Expired - Fee Related
- 2002-02-06 KR KR1020037010291A patent/KR100859609B1/ko not_active Expired - Fee Related
- 2002-02-06 DE DE60203890T patent/DE60203890T2/de not_active Expired - Lifetime
- 2002-02-06 KR KR1020087010521A patent/KR20080041756A/ko not_active Withdrawn
-
2003
- 2003-08-04 IL IL157241A patent/IL157241A/en not_active IP Right Cessation
- 2003-08-05 ZA ZA200306029A patent/ZA200306029B/en unknown
- 2003-08-05 NO NO20033473A patent/NO20033473L/no not_active Application Discontinuation
- 2003-08-06 EC EC2003004713A patent/ECSP034713A/es unknown
-
2006
- 2006-11-29 US US11/606,268 patent/US7488759B2/en not_active Expired - Fee Related
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20110207 |