AR080692A1 - Compuestos, composiciones y metodos para la administracion no toxica de antiprogestinas - Google Patents
Compuestos, composiciones y metodos para la administracion no toxica de antiprogestinasInfo
- Publication number
- AR080692A1 AR080692A1 ARP110100899A ARP110100899A AR080692A1 AR 080692 A1 AR080692 A1 AR 080692A1 AR P110100899 A ARP110100899 A AR P110100899A AR P110100899 A ARP110100899 A AR P110100899A AR 080692 A1 AR080692 A1 AR 080692A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- acyl
- alkoxy
- hydrogen
- group
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title 1
- 231100000252 nontoxic Toxicity 0.000 title 1
- 230000003000 nontoxic effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- -1 ethoxypyrrolidinyl Chemical group 0.000 abstract 7
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 125000002252 acyl group Chemical group 0.000 abstract 3
- 125000004423 acyloxy group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 208000005171 Dysmenorrhea Diseases 0.000 abstract 1
- 206010013935 Dysmenorrhoea Diseases 0.000 abstract 1
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 abstract 1
- 206010046798 Uterine leiomyoma Diseases 0.000 abstract 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000005910 alkyl carbonate group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 125000004069 aziridinyl group Chemical group 0.000 abstract 1
- 125000004045 azirinyl group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 230000002357 endometrial effect Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229940088597 hormone Drugs 0.000 abstract 1
- 239000005556 hormone Substances 0.000 abstract 1
- 201000010260 leiomyoma Diseases 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005309 thioalkoxy group Chemical group 0.000 abstract 1
- 125000004001 thioalkyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61P5/36—Antigestagens
-
- 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
- A61K31/573—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 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
- C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
-
- 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
- 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
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- 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
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
- C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
- C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
- C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
- C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
- C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
- C07J7/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa substituted in position 16
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Reproductive Health (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pregnancy & Childbirth (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
El objeto es pertinente para el campo del tratamiento de las afecciones dependientes de hormonas. Se divulgan compuestos y métodos para tratar estas afecciones. Se divulgan métodos para tratar la endometriosis, la dismenorrea, el cáncer del seno, los fibromas uterinos y la hiperproliferacion endometrial. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula general (1) o una sal aceptable desde el punto de vista farmacéutico de este, donde R1 se selecciona del grupo que incluye: alquilo; alquenilo; cicloalquilo; cicloalquenilo; arilo; H; CH3SO; CH3SO2 acilo; alcoxi; tioalcoxi; tioalquilo, aciloxi; Si(CH3)3; el resto de formula (2) donde X e Y son acilo; aziridinilo, azirinilo, azetidinilo, pirrolidinilo, etoxipirrolidinilo, metoxipirrolidinilo, piperidinilo, etoxipiperidinilo, morfolinilo, etoximorfolinilo, oxazinilo, piperazinilo, metilpiperazinilo, etilpiperazinilo y diazinilo; R2 se selecciona del grupo que incluye: hidrogeno, halogeno, alquilo, acilo, hidroxilo, alcoxi, aciloxi, carbonato de alquilo, cipioniloxi, S-alquilo, S-CN, S-acilo y -OC(O)R6 donde R6 es alquilo, alcoxialquilo o alcoxi; R3 se selecciona del grupo que incluye: alquilo, hidroxi, alcoxi y aciloxi con la condicion de que sea distinto de acetoxi o propinilo; R4 es hidrogeno o alquilo; y X se selecciona del grupo que incluye: =O, N-OR5 donde R5 es hidrogeno o alquilo, OH, CH2, OAIk1 y OCOAlk2, donde Alk1 y Alk2 son alquilo C1-8 o aralalquilo C7-15, con la condicion de que si R1 está en la posicion para y es -OCH3, -SCH3, -NC4H8, -NC5H10, -NC4H8O, -CHO, -CH(OH)CH3, -COCH3, -O(CH2)2NC4H8 o -O(CH2)2NC5H10, X sea distinto de =O o =N-OR5, donde R5 es hidrogeno o alquilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31626310P | 2010-03-22 | 2010-03-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080692A1 true AR080692A1 (es) | 2012-05-02 |
Family
ID=44343114
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100899A AR080692A1 (es) | 2010-03-22 | 2011-03-18 | Compuestos, composiciones y metodos para la administracion no toxica de antiprogestinas |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US20130018027A1 (es) |
| EP (2) | EP3865502A1 (es) |
| JP (4) | JP5894143B2 (es) |
| KR (2) | KR20130009990A (es) |
| CN (3) | CN102906103A (es) |
| AR (1) | AR080692A1 (es) |
| AU (4) | AU2010348967C1 (es) |
| BR (2) | BR112012023281A2 (es) |
| CA (1) | CA2793712A1 (es) |
| CL (1) | CL2012002544A1 (es) |
| CO (1) | CO6602170A2 (es) |
| CR (1) | CR20120514A (es) |
| EA (1) | EA023743B1 (es) |
| EC (1) | ECSP12012226A (es) |
| IL (2) | IL221820B (es) |
| MX (1) | MX2012010327A (es) |
| MY (1) | MY164622A (es) |
| NI (2) | NI201200142A (es) |
| NZ (1) | NZ602525A (es) |
| PH (2) | PH12012501812A1 (es) |
| SG (3) | SG183924A1 (es) |
| TW (1) | TWI581797B (es) |
| UA (1) | UA110030C2 (es) |
| WO (1) | WO2011119194A1 (es) |
| ZA (1) | ZA201207688B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015256473B2 (en) * | 2014-05-05 | 2018-07-12 | Allergan pharmaceuticals International Ltd. | Formulations and methods for vaginal delivery of antiprogestins |
| HK1246653A1 (zh) | 2014-11-17 | 2018-09-14 | Context Biopharma Inc. | 奥那司酮延长释放组合物和方法 |
| AU2016326657B2 (en) | 2015-09-25 | 2019-10-24 | Context Biopharma, Inc. | Methods of making onapristone intermediates |
| CA3008422A1 (en) | 2015-12-15 | 2017-06-22 | Context Biopharma Inc. | Amorphous onapristone compositions and methods of making the same |
| US12290523B2 (en) | 2016-02-24 | 2025-05-06 | Eastern Virginia Medical School | Formulation of long-acting levonorgestrel butanoate injectable depot suspension |
| US20180148471A1 (en) | 2016-11-30 | 2018-05-31 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
Family Cites Families (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2377418A1 (fr) * | 1977-01-13 | 1978-08-11 | Roussel Uclaf | Nouveaux derives steroides 4,9-dieniques 11b-substitues, leur procede de preparation et leur application comme medicaments |
| ZA8231B (en) | 1981-01-09 | 1982-11-24 | Roussel Uclaf | New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained |
| FR2521565B1 (fr) | 1982-02-17 | 1985-07-05 | Dior Sa Parfums Christian | Melange pulverulent de constituants lipidiques et de constituants hydrophobes, procede pour le preparer, phases lamellaires lipidiques hydratees et procede de fabrication, compositions pharmaceutiques ou cosmetiques comportant des phases lamellaires lipidiques hydratees |
| FR2522328B1 (fr) * | 1982-03-01 | 1986-02-14 | Roussel Uclaf | Nouveaux produits derives de la structure 3-ceto 4,9 19-nor steroides, leur procede de preparation et leur application comme medicaments |
| FR2534487B1 (fr) | 1982-10-15 | 1988-06-10 | Dior Christian Parfums | Procede d'homogeneisation de dispersions de phases lamellaires lipidiques hydratees, et suspensions obtenues par ce procede |
| DE3461090D1 (en) | 1983-02-18 | 1986-12-04 | Schering Ag | 11-beta-aryl-estradienes, process for their preparation and pharmaceutical compositions containing them |
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| DE3347126A1 (de) | 1983-12-22 | 1985-07-11 | Schering AG, 1000 Berlin und 4709 Bergkamen | 11ss-aryl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3506785A1 (de) | 1985-02-22 | 1986-08-28 | Schering AG, Berlin und Bergkamen, 1000 Berlin | 11ss-n,n-dimethylaminophenyl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
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| CN1210079C (zh) * | 2001-04-25 | 2005-07-13 | 上海市计划生育科学研究所 | 阴道环制剂及其应用 |
| ES2360806T3 (es) * | 2004-07-09 | 2011-06-09 | The Population Council, Inc. | Composiciones de liberación prolongada que contienen moduladores de receptores de progesterona. |
| CN1846703A (zh) * | 2006-02-13 | 2006-10-18 | 程定超 | 米非司酮阴道给药制剂及其组成和制备方法 |
| PT2148681E (pt) * | 2007-04-20 | 2016-06-17 | Preglem Sa | Moduladores seletivos da progesterona no tratamento da hemorragia uterina |
| US20110208118A1 (en) * | 2007-09-20 | 2011-08-25 | Bio-Pro Medical Ltd. | Compositions and means for treating uterine leiomyomata, leiomyoma, myoma, uterine fibroids, endometriosis, adenomyosis and related disorders by mifepristone |
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