CA2966753A1 - Onapristone extended-release compositions and methods - Google Patents
Onapristone extended-release compositions and methods Download PDFInfo
- Publication number
- CA2966753A1 CA2966753A1 CA2966753A CA2966753A CA2966753A1 CA 2966753 A1 CA2966753 A1 CA 2966753A1 CA 2966753 A CA2966753 A CA 2966753A CA 2966753 A CA2966753 A CA 2966753A CA 2966753 A1 CA2966753 A1 CA 2966753A1
- Authority
- CA
- Canada
- Prior art keywords
- onapristone
- extended release
- pharmaceutical composition
- per day
- extended
- 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.)
- Pending
Links
- IEXUMDBQLIVNHZ-YOUGDJEHSA-N (8s,11r,13r,14s,17s)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(3-hydroxypropyl)-13-methyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one Chemical compound C1=CC(N(C)C)=CC=C1[C@@H]1C2=C3CCC(=O)C=C3CC[C@H]2[C@H](CC[C@]2(O)CCCO)[C@@]2(C)C1 IEXUMDBQLIVNHZ-YOUGDJEHSA-N 0.000 title claims abstract description 172
- 229950011093 onapristone Drugs 0.000 title claims abstract description 172
- 239000000203 mixture Substances 0.000 title claims abstract description 84
- 238000013265 extended release Methods 0.000 title claims abstract description 53
- 238000000034 method Methods 0.000 title claims abstract description 25
- 238000009472 formulation Methods 0.000 claims abstract description 73
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 30
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 8
- 239000002775 capsule Substances 0.000 claims abstract description 4
- 239000002552 dosage form Substances 0.000 claims abstract description 4
- 102000003998 progesterone receptors Human genes 0.000 claims description 33
- 108090000468 progesterone receptors Proteins 0.000 claims description 33
- 238000011282 treatment Methods 0.000 claims description 22
- 206010028980 Neoplasm Diseases 0.000 claims description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 15
- 201000011510 cancer Diseases 0.000 claims description 13
- 230000036470 plasma concentration Effects 0.000 claims description 8
- 210000000481 breast Anatomy 0.000 claims description 7
- 230000002611 ovarian Effects 0.000 claims description 6
- 210000002307 prostate Anatomy 0.000 claims description 3
- 239000012729 immediate-release (IR) formulation Substances 0.000 abstract description 26
- 239000004480 active ingredient Substances 0.000 abstract description 10
- 230000000694 effects Effects 0.000 abstract description 5
- 230000002411 adverse Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 239000003826 tablet Substances 0.000 description 14
- 206010006187 Breast cancer Diseases 0.000 description 10
- 208000026310 Breast neoplasm Diseases 0.000 description 9
- 229940079593 drug Drugs 0.000 description 9
- 239000003814 drug Substances 0.000 description 9
- 230000008901 benefit Effects 0.000 description 8
- 201000010099 disease Diseases 0.000 description 7
- 230000000708 anti-progestin effect Effects 0.000 description 6
- 239000003418 antiprogestin Substances 0.000 description 6
- 108020004414 DNA Proteins 0.000 description 5
- 206010014759 Endometrial neoplasm Diseases 0.000 description 5
- 208000035475 disorder Diseases 0.000 description 5
- 230000002357 endometrial effect Effects 0.000 description 5
- 238000007449 liver function test Methods 0.000 description 5
- 230000004044 response Effects 0.000 description 5
- 206010014733 Endometrial cancer Diseases 0.000 description 4
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 4
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 4
- 230000005856 abnormality Effects 0.000 description 4
- 238000009825 accumulation Methods 0.000 description 4
- 238000003364 immunohistochemistry Methods 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 210000001519 tissue Anatomy 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 3
- 229920000881 Modified starch Polymers 0.000 description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 3
- 102000001708 Protein Isoforms Human genes 0.000 description 3
- 108010029485 Protein Isoforms Proteins 0.000 description 3
- 230000001093 anti-cancer Effects 0.000 description 3
- 238000013461 design Methods 0.000 description 3
- 238000011156 evaluation Methods 0.000 description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 3
- 229960001021 lactose monohydrate Drugs 0.000 description 3
- 239000003446 ligand Substances 0.000 description 3
- 210000004185 liver Anatomy 0.000 description 3
- 230000001404 mediated effect Effects 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 230000002265 prevention Effects 0.000 description 3
- 229910001220 stainless steel Inorganic materials 0.000 description 3
- 239000010935 stainless steel Substances 0.000 description 3
- 238000013518 transcription Methods 0.000 description 3
- 230000035897 transcription Effects 0.000 description 3
- 102000013138 Drug Receptors Human genes 0.000 description 2
- 108010065556 Drug Receptors Proteins 0.000 description 2
- 102000012673 Follicle Stimulating Hormone Human genes 0.000 description 2
- 108010079345 Follicle Stimulating Hormone Proteins 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 description 2
- 229940123788 Progesterone receptor antagonist Drugs 0.000 description 2
- 206010060862 Prostate cancer Diseases 0.000 description 2
- 206010051259 Therapy naive Diseases 0.000 description 2
- 239000008186 active pharmaceutical agent Substances 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 239000003433 contraceptive agent Substances 0.000 description 2
- 230000002254 contraceptive effect Effects 0.000 description 2
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 231100000371 dose-limiting toxicity Toxicity 0.000 description 2
- 239000013583 drug formulation Substances 0.000 description 2
- 229940088679 drug related substance Drugs 0.000 description 2
- 239000000945 filler Substances 0.000 description 2
- 229940028334 follicle stimulating hormone Drugs 0.000 description 2
- 238000001794 hormone therapy Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000003204 osmotic effect Effects 0.000 description 2
- 230000026731 phosphorylation Effects 0.000 description 2
- 238000006366 phosphorylation reaction Methods 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000000044 progesterone antagonist Substances 0.000 description 2
- 239000000583 progesterone congener Substances 0.000 description 2
- 208000037821 progressive disease Diseases 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
- 229960001603 tamoxifen Drugs 0.000 description 2
- 208000037965 uterine sarcoma Diseases 0.000 description 2
- 102000002260 Alkaline Phosphatase Human genes 0.000 description 1
- 108020004774 Alkaline Phosphatase Proteins 0.000 description 1
- 208000003174 Brain Neoplasms Diseases 0.000 description 1
- 241000276583 Cottus Species 0.000 description 1
- 102000004328 Cytochrome P-450 CYP3A Human genes 0.000 description 1
- 108010081668 Cytochrome P-450 CYP3A Proteins 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- -1 Hydroxypropyl Chemical group 0.000 description 1
- 102000009151 Luteinizing Hormone Human genes 0.000 description 1
- 108010073521 Luteinizing Hormone Proteins 0.000 description 1
- 206010027452 Metastases to bone Diseases 0.000 description 1
- 206010059282 Metastases to central nervous system Diseases 0.000 description 1
- 206010027457 Metastases to liver Diseases 0.000 description 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical compound [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 description 1
- 102220497176 Small vasohibin-binding protein_T47D_mutation Human genes 0.000 description 1
- 238000008050 Total Bilirubin Reagent Methods 0.000 description 1
- 238000010811 Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry Methods 0.000 description 1
- 208000002495 Uterine Neoplasms Diseases 0.000 description 1
- 206010046798 Uterine leiomyoma Diseases 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 229940041181 antineoplastic drug Drugs 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000000090 biomarker Substances 0.000 description 1
- 238000001574 biopsy Methods 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000000679 carrageenan Substances 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 229940113118 carrageenan Drugs 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 229940109239 creatinine Drugs 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 238000002405 diagnostic procedure Methods 0.000 description 1
- 230000000447 dimerizing effect Effects 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 238000009261 endocrine therapy Methods 0.000 description 1
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 description 1
- 210000004696 endometrium Anatomy 0.000 description 1
- 210000002919 epithelial cell Anatomy 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 230000007717 exclusion Effects 0.000 description 1
- 239000007941 film coated tablet Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 238000011223 gene expression profiling Methods 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 238000002657 hormone replacement therapy Methods 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 208000019016 inability to swallow Diseases 0.000 description 1
- 239000000411 inducer Substances 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 201000010260 leiomyoma Diseases 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229940040129 luteinizing hormone Drugs 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 239000013563 matrix tablet Substances 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 230000001394 metastastic effect Effects 0.000 description 1
- 206010061289 metastatic neoplasm Diseases 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 102000006255 nuclear receptors Human genes 0.000 description 1
- 108020004017 nuclear receptors Proteins 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 101150038105 pr gene Proteins 0.000 description 1
- 239000000186 progesterone Substances 0.000 description 1
- 229960003387 progesterone Drugs 0.000 description 1
- 239000002379 progesterone receptor modulator Substances 0.000 description 1
- 150000003146 progesterones Chemical class 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 229940095745 sex hormone and modulator of the genital system progesterone receptor modulator Drugs 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 238000004885 tandem mass spectrometry Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000002103 transcriptional effect Effects 0.000 description 1
- 238000004704 ultra performance liquid chromatography Methods 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 206010046766 uterine cancer Diseases 0.000 description 1
- 201000007954 uterine fibroid Diseases 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462080868P | 2014-11-17 | 2014-11-17 | |
| US62/080,868 | 2014-11-17 | ||
| PCT/US2015/060940 WO2016081383A1 (en) | 2014-11-17 | 2015-11-16 | Onapristone extended-release compositions and methods |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2966753A1 true CA2966753A1 (en) | 2016-05-26 |
Family
ID=56014429
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2966753A Pending CA2966753A1 (en) | 2014-11-17 | 2015-11-16 | Onapristone extended-release compositions and methods |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US10786461B2 (OSRAM) |
| EP (1) | EP3247362A4 (OSRAM) |
| JP (1) | JP6655075B2 (OSRAM) |
| KR (1) | KR20170084086A (OSRAM) |
| CN (2) | CN106999501B (OSRAM) |
| AU (2) | AU2015350241B2 (OSRAM) |
| CA (1) | CA2966753A1 (OSRAM) |
| HK (1) | HK1246653A1 (OSRAM) |
| MX (1) | MX391191B (OSRAM) |
| RU (1) | RU2017112748A (OSRAM) |
| WO (1) | WO2016081383A1 (OSRAM) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US20180148471A1 (en) | 2016-11-30 | 2018-05-31 | Arno Therapeutics, Inc. | Methods for onapristone synthesis dehydration and deprotection |
Family Cites Families (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4780461A (en) | 1983-06-15 | 1988-10-25 | Schering Aktiengesellschaft | 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same |
| DE3321826A1 (de) | 1983-06-15 | 1984-12-20 | Schering AG, 1000 Berlin und 4709 Bergkamen | 13(alpha)-alkylgonane, deren herstellung und diese enthaltende pharmazeutische praeparate |
| ES8502612A1 (es) | 1983-06-15 | 1985-02-01 | Schering Ag | Procedimiento para la preparacion de 13a-alquilgonanos |
| US4742000A (en) | 1986-05-02 | 1988-05-03 | University Of Chicago | Antibody to human progesterone receptor and diagnostic materials and methods |
| DE3630030A1 (de) | 1986-09-01 | 1988-03-03 | Schering Ag | 13(alpha)-alkylgonan-(delta)(pfeil hoch)9(pfeil hoch)(pfeil hoch)((pfeil hoch)(pfeil hoch)1(pfeil hoch)1(pfeil hoch))(pfeil hoch)-5,10-epoxide |
| US4774236A (en) | 1986-09-17 | 1988-09-27 | Research Triangle Institute | 17α-(substituted-methyl)-17β-hydroxy/esterified hydroxy steroids and pharmaceutical compositions containing them |
| IE60780B1 (en) | 1987-01-23 | 1994-08-10 | Akzo Nv | New 11-aryl steroid derivatives |
| DE3822770A1 (de) | 1988-07-01 | 1990-01-04 | Schering Ag | 13-alkyl-11ss-phenylgonane |
| US5283190A (en) | 1989-07-31 | 1994-02-01 | Traish Adbulmaged M | Specific monoclonal antibodies against a defined epitope of progesterone receptor and methods for their use |
| DE4008584A1 (de) | 1990-03-15 | 1991-09-26 | Schering Ag | Verfahren zur herstellung von zwischenprodukten fuer die antigestagensynthese (onapristonsynthese) |
| US5141961A (en) | 1991-06-27 | 1992-08-25 | Richrdson-Vicks Inc. | Process for solubilizing difficulty soluble pharmaceutical actives |
| MX9301121A (es) | 1992-03-02 | 1993-09-01 | Schering Ag | Metodo y equipo para la contracepcion oral y regulacion de la menstruacion con estrogeno/progestina/aniprogestina. |
| CN1053450C (zh) | 1992-11-19 | 2000-06-14 | 北京第三制药厂 | 17位取代11β－取代芳香基－4,9－雌甾二烯类化合物的全合成法 |
| DE4332283A1 (de) | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| ZA959008B (en) * | 1994-10-24 | 1996-09-16 | Schering Ag | Competitive progesterone antagonists for demand-oriented female birth control |
| US5759577A (en) | 1995-01-17 | 1998-06-02 | American Home Products Corporation | Controlled release of steroids from sugar coatings |
| US6900193B1 (en) | 1996-05-01 | 2005-05-31 | The United States Of America As Represented By The Department Of Health And Human Services | Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents |
| IL122740A (en) | 1997-01-15 | 2003-09-17 | Akzo Nobel Nv | 16-hydroxy-11-(substituted phenyl)-estra-9,4-diene derivatives, their preparation and pharmaceutical compositions containing them |
| US5962444A (en) | 1998-05-29 | 1999-10-05 | Research Triangle Institute | 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
| US6537584B1 (en) | 1999-11-12 | 2003-03-25 | Macromed, Inc. | Polymer blends that swell in an acidic environment and deswell in a basic environment |
| EP1282443B1 (en) | 2000-05-19 | 2009-09-02 | Genentech, Inc. | Gene detection assay for improving the likelihood of an effective response to an erbb antagonist cancer therapy |
| US6750015B2 (en) | 2000-06-28 | 2004-06-15 | Kathryn B. Horwitz | Progesterone receptor-regulated gene expression and methods related thereto |
| UY26966A1 (es) | 2000-10-18 | 2002-06-20 | Schering Ag | Uso de antiprogestinas para la inducción de apoptosis en una célula |
| US7381976B2 (en) | 2001-03-13 | 2008-06-03 | Triton Thalassic Technologies, Inc. | Monochromatic fluid treatment systems |
| AUPR546801A0 (en) | 2001-06-05 | 2001-06-28 | Commonwealth Scientific And Industrial Research Organisation | Recombinant antibodies |
| US7105642B2 (en) | 2001-08-03 | 2006-09-12 | Cell Signalling Technology, Inc. | Monoclonal antibodies specific for phosphorylated estrogen receptor alpha (Ser118) and uses thereof |
| US20040121304A1 (en) | 2001-12-21 | 2004-06-24 | Ulrike Fuhrmann | Method for screening for progesterone receptor isoform-specific ligands and for tissue-selective progesterone receptor ligands |
| WO2004078709A2 (en) | 2003-02-28 | 2004-09-16 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | METHOD FOR PREPARING 17 α-ACETOXY-11β-(4-N,N-DIMETHYLAMINOPHENYL)-19-NORPREGNA-4,9-DIENE-3,20-DIONE, INTERMEDIATES THEREOF, AND METHODS FOR THE PREPARATION OF SUCH INTERMEDIATES |
| US20040265371A1 (en) | 2003-06-25 | 2004-12-30 | Looney Dwayne Lee | Hemostatic devices and methods of making same |
| US7247625B2 (en) * | 2003-10-09 | 2007-07-24 | Wyeth | 6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators |
| ES2360806T3 (es) | 2004-07-09 | 2011-06-09 | The Population Council, Inc. | Composiciones de liberación prolongada que contienen moduladores de receptores de progesterona. |
| AU2005289728B2 (en) | 2004-09-22 | 2011-11-24 | Tripath Imaging, Inc. | Methods and compositions for evaluating breast cancer prognosis |
| WO2006111856A1 (en) | 2005-04-20 | 2006-10-26 | Pfizer Limited | Pyrazole derivatives as progesterone receptor antagonists |
| EP2021499A4 (en) | 2005-12-16 | 2010-02-17 | Univ Leland Stanford Junior | FUNCTIONAL ARRAYS FOR THE IDENTIFICATION OF ELEMENTS FOR GENE PRESSION REGULATION WITH HIGH THROUGHPUT |
| US20070167971A1 (en) | 2006-01-17 | 2007-07-19 | Raymond Huey | Devices and methods for promoting the formation of blood clots in esophageal varices |
| US20070166372A1 (en) | 2006-01-19 | 2007-07-19 | Mai De Ltd. | Preparation of solid coprecipitates of amorphous valsartan |
| PL1989217T4 (pl) | 2006-02-17 | 2013-02-28 | Janssen Pharmaceutica Nv | 11-fosforowe pochodne steroidowe użyteczne jako modulatory receptora progesteronu |
| DE102006054535A1 (de) | 2006-11-15 | 2008-05-21 | Bayer Schering Pharma Aktiengesellschaft | Progesteronrezeptorantagonisten |
| CN101668739A (zh) | 2007-04-24 | 2010-03-10 | 帝斯曼知识产权资产管理有限公司 | 用于制造前维生素d的光化学方法 |
| CA2596204C (en) | 2007-08-07 | 2019-02-26 | Historx, Inc. | Method and system for determining an optimal dilution of a reagent |
| WO2009025759A1 (en) | 2007-08-17 | 2009-02-26 | Progenics Pharmaceuticals (Nevada), Inc. | Tight junction proteins associated with infection and entry of hepatitis c virus (hcv), methods and uses thereof |
| AR068986A1 (es) * | 2007-10-12 | 2009-12-23 | Novartis Ag | Composiciones que comprenden moduladores del receptor de fosfato de esfingosina-1 (s1p) |
| EP2075246A1 (en) | 2007-12-27 | 2009-07-01 | M. J. Institute of Research | A process for preparation of amorphous form of atorvastatin hemi-calcium salt |
| WO2009100258A1 (en) | 2008-02-05 | 2009-08-13 | Hollis-Eden Pharmaceuticals, Inc. | Pharmaceutical solid state forms |
| TWI539953B (zh) | 2008-04-28 | 2016-07-01 | 瑞波若斯治療學公司 | 用於治療乳癌之組成物和方法 |
| TW201002736A (en) | 2008-04-28 | 2010-01-16 | Repros Therapeutics Inc | Compositions and methods for treating progesterone-dependent conditions |
| WO2010110086A1 (ja) | 2009-03-27 | 2010-09-30 | 株式会社小松製作所 | 作業車両の省燃費制御装置および作業車両の省燃費制御方法 |
| US9074002B2 (en) | 2009-04-27 | 2015-07-07 | Cold Spring Harbor Laboratory | PTP1B inhibitors |
| US20110003753A1 (en) | 2009-06-01 | 2011-01-06 | Samuel Waxman Cancer Research Foundation | COMPOSITIONS AND METHODS FOR DISRUPTING THE FUNCTION OF THE TRANSCRIPTIONAL REPRESSOR COMPONENT Sin3A-PAH2 DOMAIN TO INDUCE DIFFERENTIATION AND GROWTH INHIBITION IN BREAST CANCER |
| MX2012000680A (es) | 2009-07-15 | 2012-02-28 | S Bio Pte Ltd | Sal de citrato de 9e-15-(2-pirrolidin-1-il-etoxi)-7,12,25-trioxa-1 9,21,24-triaza-tetraciclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2 ,4,9,14,16,18(26),20,22-nonaeno. |
| US20110293511A1 (en) | 2009-09-29 | 2011-12-01 | Terrance Grant Johns | Specific binding proteins and uses thereof |
| US8261855B2 (en) * | 2009-11-11 | 2012-09-11 | Flanders Electric, Ltd. | Methods and systems for drilling boreholes |
| JP5965844B2 (ja) | 2009-12-15 | 2016-08-10 | バインド セラピューティックス インコーポレイテッド | 高いガラス転移温度または高分子量のコポリマーを有する治療用ポリマーナノ粒子組成物 |
| SG183924A1 (en) * | 2010-03-22 | 2012-10-30 | Repros Therapeutics Inc | Compositions and methods for non-toxic delivery of antiprogestins |
| WO2012087983A1 (en) | 2010-12-20 | 2012-06-28 | The General Hospital Corporation | Polycomb-associated non-coding rnas |
| EP2638163B1 (en) | 2010-11-12 | 2017-05-17 | The General Hospital Corporation | Polycomb-associated non-coding rnas |
| US20140018404A1 (en) | 2010-12-16 | 2014-01-16 | Celgene Corporation | Controlled release oral dosage forms of poorly soluble drugs and uses thereof |
| JP2014510080A (ja) | 2011-03-09 | 2014-04-24 | セントローズ， エルエルシー | 細胞外標的化薬物複合体 |
| JP6118273B2 (ja) | 2011-03-11 | 2017-04-19 | セルジーン コーポレイション | 免疫関連疾患及び炎症性疾患の治療における３−（５−アミノ−２−メチル−４−オキソキナゾリン−３（４ｈ）−イル）ピペリジン−２，６−ジオンの使用 |
| ES2656988T3 (es) | 2011-04-15 | 2018-03-01 | J-Pharma Co., Ltd. | Biomarcador para el cáncer de mama |
| AU2012258087B2 (en) | 2011-05-13 | 2017-07-20 | Astellas Pharma Inc. | Antibodies for treatment of cancer expressing claudin 6 |
| US20130029953A1 (en) * | 2011-07-28 | 2013-01-31 | Klaus Nickisch | Progesterone antagonists |
| WO2013052652A1 (en) | 2011-10-04 | 2013-04-11 | Erard Gilles | Methods and systems for identifying and treating anti-progestin sensitive tumors |
| BR112014013709A2 (pt) | 2011-12-08 | 2017-08-22 | Fund Sales | Métodos, composições farmaceuticas, e kits, para tratar cânceres resitentes às antiprogestinas |
| US20130338016A1 (en) | 2012-04-17 | 2013-12-19 | Vala Sciences, Inc. | Method For Integrated Pathology Diagnosis And Digital Biomarker Pattern Analysis |
| AU2013252913A1 (en) | 2012-04-27 | 2014-11-27 | Regents Of The University Of Minnesota | Breast cancer prognosis, prediction of progesterone receptor subtype and|prediction of response to antiprogestin treatment based on gene expression |
| EP2877210A4 (en) | 2012-07-24 | 2016-06-29 | Cedars Sinai Medical Center | A NEW METHOD FOR DETECTING THE RESISTANCE TO CHEMOTHERAPY IN PATIENTS WITH LUNG CANCER |
| US20150320795A1 (en) | 2012-12-13 | 2015-11-12 | Roy JOSEE | Compositions and methods comprising polyethylene glycol and magnesium for treatment of neuronal injury |
| CA2904116C (en) * | 2013-03-12 | 2021-09-14 | Arno Therapeutics | Onapristone polymorphic forms and methods of use |
| US20140363425A1 (en) | 2013-03-13 | 2014-12-11 | J. Dinny Graham | Systems and methods for identifying cancers having activated progesterone receptors |
| US9096641B2 (en) | 2013-06-05 | 2015-08-04 | Evestra, Inc. | Imidazolyl progesterone antagonists |
| CN103483449A (zh) | 2013-08-20 | 2014-01-01 | 东北农业大学 | 两种scFv抗体、其编码基因及其在制备治疗或预防鸡传染性法氏囊病制剂中的应用 |
| US20150285803A1 (en) | 2014-04-08 | 2015-10-08 | Invivis Pharmaceuticals Inc. | Systems and methods for identifying progesterone receptor subtypes |
| 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 |
| AU2016235298B2 (en) | 2015-03-23 | 2021-03-11 | Evestra, Inc. | Novel cytotoxic agents that preferentially target leukemia inhibitory factor (LIF) for the treatment of malignancies and as new contraceptive agents |
| 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 |
| JP2019513706A (ja) | 2016-03-21 | 2019-05-30 | コンテキスト・バイオファーマ・インコーポレイテッド | オナプリストン代謝物質組成物及び方法 |
| WO2017192567A1 (en) | 2016-05-02 | 2017-11-09 | Tetragenetics, Inc. | ANTI-Kv1.3 ANTIBODIES, AND METHODS OF PRODUCTION AND USE THEREOF |
| WO2018067198A1 (en) | 2016-10-03 | 2018-04-12 | The Regents Of The University Of California | Inhibitory antibodies and methods of use thereof |
-
2015
- 2015-11-16 HK HK18106169.2A patent/HK1246653A1/zh unknown
- 2015-11-16 AU AU2015350241A patent/AU2015350241B2/en not_active Ceased
- 2015-11-16 CN CN201580062192.1A patent/CN106999501B/zh not_active Expired - Fee Related
- 2015-11-16 CA CA2966753A patent/CA2966753A1/en active Pending
- 2015-11-16 MX MX2017005163A patent/MX391191B/es unknown
- 2015-11-16 JP JP2017520520A patent/JP6655075B2/ja not_active Expired - Fee Related
- 2015-11-16 CN CN202110852562.9A patent/CN113559075A/zh active Pending
- 2015-11-16 RU RU2017112748A patent/RU2017112748A/ru not_active Application Discontinuation
- 2015-11-16 US US14/942,809 patent/US10786461B2/en not_active Expired - Fee Related
- 2015-11-16 KR KR1020177012909A patent/KR20170084086A/ko not_active Ceased
- 2015-11-16 EP EP15861014.7A patent/EP3247362A4/en not_active Withdrawn
- 2015-11-16 WO PCT/US2015/060940 patent/WO2016081383A1/en not_active Ceased
-
2020
- 2020-09-28 US US17/035,544 patent/US11672762B2/en active Active
-
2021
- 2021-08-18 AU AU2021218093A patent/AU2021218093A1/en not_active Abandoned
-
2023
- 2023-01-09 US US18/151,846 patent/US20230157960A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP3247362A4 (en) | 2018-10-10 |
| AU2015350241B2 (en) | 2021-05-20 |
| US20210220279A1 (en) | 2021-07-22 |
| CN106999501B (zh) | 2021-08-13 |
| EP3247362A1 (en) | 2017-11-29 |
| MX391191B (es) | 2025-03-21 |
| CN106999501A (zh) | 2017-08-01 |
| RU2017112748A3 (OSRAM) | 2019-06-26 |
| US20160166583A1 (en) | 2016-06-16 |
| RU2017112748A (ru) | 2018-12-19 |
| JP2017537883A (ja) | 2017-12-21 |
| US11672762B2 (en) | 2023-06-13 |
| WO2016081383A1 (en) | 2016-05-26 |
| HK1246653A1 (zh) | 2018-09-14 |
| AU2015350241A1 (en) | 2017-05-04 |
| CN113559075A (zh) | 2021-10-29 |
| US20230157960A1 (en) | 2023-05-25 |
| US10786461B2 (en) | 2020-09-29 |
| KR20170084086A (ko) | 2017-07-19 |
| JP6655075B2 (ja) | 2020-02-26 |
| MX2017005163A (es) | 2018-01-18 |
| AU2021218093A1 (en) | 2021-09-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20230157960A1 (en) | Onapristone extended-release compositions and methods | |
| Nguyen et al. | Evaluation of the effect of food and gastric pH on the single‐dose pharmacokinetics of cabozantinib in healthy adult subjects | |
| KR102158948B1 (ko) | 약물 전달 시스템 | |
| US20220323446A1 (en) | Sotorasib dosing regimen | |
| US20230270744A1 (en) | Methods of Administering Elagolix | |
| MX2007012081A (es) | Tableta que contiene hormonas esteroides. | |
| EP4340842B1 (en) | Sotorasib for use in the treatment of cancer | |
| US20250017932A1 (en) | Methods of Administering Elagolix | |
| HK40062842A (en) | Onapristone extended-release compositions and methods | |
| CN114340625B (zh) | 用雌激素受体-α抑制剂的口服剂型治疗癌症的方法 | |
| WO2023049363A1 (en) | Sotorasib and afatinib for treating cancer comprising a kras g12c mutation | |
| WO2022261025A1 (en) | Methods of treating cancer with a combination of sotorasib and trametinib | |
| TW202444376A (zh) | 治療癌症之方法 | |
| TW202206074A (zh) | 藥物配製物 | |
| EA048243B1 (ru) | Фармацевтический состав |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20201104 |
|
| EEER | Examination request |
Effective date: 20201104 |
|
| EEER | Examination request |
Effective date: 20201104 |
|
| EEER | Examination request |
Effective date: 20201104 |
|
| EEER | Examination request |
Effective date: 20201104 |
|
| EEER | Examination request |
Effective date: 20201104 |
|
| EEER | Examination request |
Effective date: 20201104 |
|
| EEER | Examination request |
Effective date: 20201104 |