ES427480A1 - Corticoid-containing inhalant preparations - Google Patents
Corticoid-containing inhalant preparationsInfo
- Publication number
- ES427480A1 ES427480A1 ES427480A ES427480A ES427480A1 ES 427480 A1 ES427480 A1 ES 427480A1 ES 427480 A ES427480 A ES 427480A ES 427480 A ES427480 A ES 427480A ES 427480 A1 ES427480 A1 ES 427480A1
- Authority
- ES
- Spain
- Prior art keywords
- general formula
- group
- oxidizing
- formula
- compounds
- 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.)
- Expired
Links
- 238000002360 preparation method Methods 0.000 title abstract 3
- 239000003470 adrenal cortex hormone Substances 0.000 title abstract 2
- RKHQGWMMUURILY-UHRZLXHJSA-N cortivazol Chemical compound C([C@H]1[C@@H]2C[C@H]([C@]([C@@]2(C)C[C@H](O)[C@@H]1[C@@]1(C)C2)(O)C(=O)COC(C)=O)C)=C(C)C1=CC1=C2C=NN1C1=CC=CC=C1 RKHQGWMMUURILY-UHRZLXHJSA-N 0.000 title abstract 2
- 230000001590 oxidative effect Effects 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 239000002253 acid Substances 0.000 abstract 3
- 150000007513 acids Chemical class 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 230000001131 transforming effect Effects 0.000 abstract 3
- 239000003246 corticosteroid Substances 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- -1 fluoromethylene group Chemical group 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 239000004215 Carbon black (E152) Substances 0.000 abstract 1
- XFXPMWWXUTWYJX-UHFFFAOYSA-N Cyanide Chemical compound N#[C-] XFXPMWWXUTWYJX-UHFFFAOYSA-N 0.000 abstract 1
- 150000001241 acetals Chemical class 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 150000001298 alcohols Chemical class 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 229960001334 corticosteroids Drugs 0.000 abstract 1
- 229910001385 heavy metal Inorganic materials 0.000 abstract 1
- 150000002373 hemiacetals Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 229930195733 hydrocarbon Natural products 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (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)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Otolaryngology (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Procedure for the preparation of an inhalation agent containing corticosteroids, characterized in that a corticoid of the general formula I is prepared as an active substance **(See formula)** where -BA- means the -CH2-CH2-, -CH = CH- or -CCl = CH- groupings, X means a hydrogen atom, a fluorine atom or a methyl group, Y means a hydrogen atom, a fluorine atom or a chlorine atom, Z means a methylene group, a hydroxymethylan group, a fluoromethylene group, a cloxaroethylene group or a corbonyl group, R1 means a hydrogen atom or a methyl group, and R2 means a hydrogen atom or R1 and R2 together signify an isopropylidenedioxy group; and R3 signifies a hydrocarbon radical with 1 to 12 carbon atoms, a) oxidizing the 20-hydroxy group of compounds of the general formula II **(See formula)** where -AB-, X, Y, Z, R'1, R2 and R2 have the same meanings as in formula I, if desired by oxidizing a free hydroxy group present at position 11, and if desired by saponifying or transesterifying the 21-esters of the general formula I, and transforming into their salts or esterifying the free acids of the general formula I; or b) oxidizing the steroid-aldehydes of the general formula III **(See formula)** where -AB, X, Y, Z, R1 and R2 have the aforementioned meanings or the hydrates, hemiacetals or acetals of these compounds in the presence of alcohols and cyanide ions, with oxides of heavy metals with oxidizing action, if desired oxidizing a free hydroxy group present at position 11, saponifying or transesterifying, if desired, the 21-esters of the general formula I, and transforming into their salts or esterifying the free acids of the general formula I; or c) for the preparation of compounds of the general formula I in which -A-B- has the meaning of a group -CH = CH-, dehydrogenating the compounds of the general formula IV, **(See formula)** where X, Y, Z, R1, R2 and R3 have the aforementioned meanings, if desired by oxidizing a free hydroxy group present in position 11, saponifying or transesterifying eventually the 21-esters of the general formula I, and transforming into their salts or esterifying the free acids of the general formula I; and bringing the corticosteroid of the general formula I thus obtained into a form suitable for inhalation. (Machine-translation by Google Translate, not legally binding)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE2332663A DE2332663C2 (en) | 1973-06-23 | 1973-06-23 | Use of corticosteroid active ingredients for inhalation therapy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES427480A1 true ES427480A1 (en) | 1976-07-16 |
Family
ID=5885228
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES427480A Expired ES427480A1 (en) | 1973-06-23 | 1974-06-20 | Corticoid-containing inhalant preparations |
Country Status (13)
| Country | Link |
|---|---|
| JP (1) | JPS6245846B2 (en) |
| BE (1) | BE816709A (en) |
| DD (1) | DD112437A5 (en) |
| DE (1) | DE2332663C2 (en) |
| DK (1) | DK337574A (en) |
| ES (1) | ES427480A1 (en) |
| FR (1) | FR2233987B1 (en) |
| GB (1) | GB1479488A (en) |
| IE (1) | IE39516B1 (en) |
| IL (1) | IL45087A (en) |
| NL (1) | NL184724C (en) |
| SE (1) | SE7408091L (en) |
| ZA (1) | ZA744022B (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX3864E (en) | 1975-05-27 | 1981-08-26 | Syntex Corp | A PROCESS TO PREPARE THE CRYSTALLINE COMPOUND 6-FLUIRO-11B 21-DIHIROXI-16 17-ISOPROPILIDENDIOXIPREGNA-1 4-DIEN-3 20-DIONA |
| DE2829953A1 (en) * | 1978-07-03 | 1980-01-24 | Schering Ag | PHARMACEUTICAL PREPARATION FOR TREATING THE KOLITIS ULCEROSA AND KOLITIS GRANULOMATOSA |
| US5215979A (en) * | 1985-12-19 | 1993-06-01 | Aktiebolaget Draco | 16,17-acetalsubstituted pregnane 21-oic acid derivatives |
| EP1806148A4 (en) * | 2004-10-22 | 2009-12-02 | Ono Pharmaceutical Co | Medicinal composition for inhalation |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB799902A (en) * | 1954-08-11 | 1958-08-13 | Merck & Co Inc | Therapeutic preparations |
| US3320125A (en) * | 1964-04-28 | 1967-05-16 | Merck & Co Inc | Inhalation aerosol composition |
| GB1242211A (en) * | 1967-08-08 | 1971-08-11 | Fisons Pharmaceuticals Ltd | Pharmaceutical composition |
| GB1381872A (en) * | 1971-06-22 | 1975-01-29 | Fisons Ltd | Pharmaceutical compositions for inhalation |
| BE787100A (en) * | 1971-08-06 | 1973-02-02 | Beecham Group Ltd | COMPOSITION FOR THE TREATMENT OF ASTHMA |
| GB1387911A (en) * | 1971-10-04 | 1975-03-19 | Schering Ag | Pregnane acid derivatives |
| DE2150268C3 (en) * | 1971-10-04 | 1980-11-06 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | Pregnanic acid derivatives, processes for their preparation and pharmaceuticals containing them |
| DE2264003C2 (en) * | 1972-12-22 | 1982-11-04 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | New pregnanic acid derivatives, processes for their production and pharmaceutical preparations containing them |
| DE2319479C2 (en) * | 1973-04-14 | 1982-10-28 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | Pregnanic acid derivatives, processes for their production and pharmaceutical preparations containing them |
-
1973
- 1973-06-23 DE DE2332663A patent/DE2332663C2/en not_active Expired
-
1974
- 1974-06-19 SE SE7408091A patent/SE7408091L/ not_active Application Discontinuation
- 1974-06-20 ES ES427480A patent/ES427480A1/en not_active Expired
- 1974-06-20 IE IE1292/74A patent/IE39516B1/en unknown
- 1974-06-21 IL IL45087A patent/IL45087A/en unknown
- 1974-06-21 NL NLAANVRAGE7408421,A patent/NL184724C/en not_active IP Right Cessation
- 1974-06-21 ZA ZA00744022A patent/ZA744022B/en unknown
- 1974-06-21 BE BE145751A patent/BE816709A/en not_active IP Right Cessation
- 1974-06-24 GB GB27902/74A patent/GB1479488A/en not_active Expired
- 1974-06-24 FR FR7421859A patent/FR2233987B1/fr not_active Expired
- 1974-06-24 DK DK337574A patent/DK337574A/da unknown
- 1974-06-24 JP JP49072169A patent/JPS6245846B2/ja not_active Expired
- 1974-06-24 DD DD179417A patent/DD112437A5/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| GB1479488A (en) | 1977-07-13 |
| FR2233987A1 (en) | 1975-01-17 |
| FR2233987B1 (en) | 1977-07-08 |
| NL184724C (en) | 1989-10-16 |
| NL184724B (en) | 1989-05-16 |
| DE2332663A1 (en) | 1975-01-16 |
| NL7408421A (en) | 1974-12-30 |
| ZA744022B (en) | 1975-06-25 |
| IL45087A0 (en) | 1974-09-10 |
| BE816709A (en) | 1974-12-23 |
| AU7042174A (en) | 1976-01-08 |
| JPS5047967A (en) | 1975-04-28 |
| DE2332663C2 (en) | 1986-07-31 |
| JPS6245846B2 (en) | 1987-09-29 |
| IE39516L (en) | 1974-12-23 |
| IE39516B1 (en) | 1978-10-25 |
| DK337574A (en) | 1975-03-17 |
| DD112437A5 (en) | 1975-04-12 |
| SE7408091L (en) | 1974-12-23 |
| IL45087A (en) | 1978-04-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD1A | Patent lapsed |
Effective date: 19930210 |