CA3038875A1 - Treatment of prostate cancer - Google Patents
Treatment of prostate cancer Download PDFInfo
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- CA3038875A1 CA3038875A1 CA3038875A CA3038875A CA3038875A1 CA 3038875 A1 CA3038875 A1 CA 3038875A1 CA 3038875 A CA3038875 A CA 3038875A CA 3038875 A CA3038875 A CA 3038875A CA 3038875 A1 CA3038875 A1 CA 3038875A1
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Classifications
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- 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)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662402004P | 2016-09-30 | 2016-09-30 | |
| US201662402150P | 2016-09-30 | 2016-09-30 | |
| US62/402,150 | 2016-09-30 | ||
| US62/402,004 | 2016-09-30 | ||
| PCT/EP2017/074849 WO2018060463A2 (en) | 2016-09-30 | 2017-09-29 | Treatment of prostate cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3038875A1 true CA3038875A1 (en) | 2018-04-05 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3038875A Pending CA3038875A1 (en) | 2016-09-30 | 2017-09-29 | Treatment of prostate cancer |
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| HR (1) | HRP20241740T1 (show.php) |
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| MX (2) | MX2019003733A (show.php) |
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| SI (1) | SI3518932T1 (show.php) |
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|---|---|---|---|---|
| PL2900675T3 (pl) | 2012-09-28 | 2019-08-30 | Takeda Pharmaceutical Company Limited | Sposób wytwarzania pochodnej tienopirymidyny |
| FI3518932T3 (fi) | 2016-09-30 | 2025-02-03 | Sumitomo Pharma Switzerland Gmbh | Eturauhassyövän hoito |
| SI3518933T2 (sl) | 2016-09-30 | 2025-05-30 | Sumitomo Pharma Switzerland Gmbh | Metode zdravljenja materničnih miom in endometrioze |
| CN110194776B (zh) * | 2019-06-27 | 2021-05-28 | 四川伊诺达博医药科技有限公司 | 一种瑞卢戈利的合成方法 |
| JP7713934B2 (ja) * | 2019-10-10 | 2025-07-28 | スミトモ ファーマ スウィッツァーランド ゲーエムベーハー | Ｎ－（４－（１－（２，６－ジフルオロベンジル）－５－（（ジメチルアミノ）メチル）－３－（６－メトキシ－３－ピリダジニル）－２，４－ジオキソ－１，２，３，４－テトラヒドロチエノ［２，３－ｄ］ピリミジン－６－イル）フェニル）－Ｎ’－メトキシ尿素の結晶溶媒和形 |
| EP4041739A1 (en) * | 2019-10-10 | 2022-08-17 | Myovant Sciences GmbH | Crystalline forms of n-(4-(1-(2,6-difluorobenzyl)-5- ((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo- 1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'- methoxyurea |
| AU2021278303A1 (en) | 2020-05-29 | 2023-02-09 | Sumitomo Pharma Switzerland Gmbh | Combination solid oral dosage forms of gonadotropin-releasing hormone antagonists |
| US20230384316A1 (en) * | 2020-10-20 | 2023-11-30 | Baylor College Of Medicine | Multiplex metabolic markers in plasma for early detection of african american prostate cancer |
| JP2023549196A (ja) * | 2020-11-11 | 2023-11-22 | ミオバント サイエンシズ ゲーエムベーハー | レルゴリクスの投与方法 |
| EP4419530A1 (en) | 2021-10-18 | 2024-08-28 | Sumitomo Pharma Switzerland GmbH | Crystalline form of an ethanol solvate of n-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea |
| WO2023152611A1 (en) * | 2022-02-11 | 2023-08-17 | Aragon Pharmaceuticals, Inc. | Apalutamide and relugolix for the treatment of prostate cancer |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2710637B1 (fr) | 1993-09-28 | 1995-12-08 | Roquette Freres | Mannitol pulvérulent de friabilité modérée et son procédé de préparation. |
| RU2233284C2 (ru) | 1999-03-24 | 2004-07-27 | Такеда Кемикал Индастриз, Лтд. | Тиенопиримидиновые производные, способ их получения, фармацевтическая композиция и способ антагонизации гонадотропин-рилизинг гормона |
| TWI225863B (en) | 1999-03-24 | 2005-01-01 | Takeda Chemical Industries Ltd | Thienopyrimidine compounds, their production and use |
| CN1539836A (zh) | 2000-02-29 | 2004-10-27 | 武田药品工业株式会社 | 制备噻吩并嘧啶衍生物的方法 |
| US20050043315A1 (en) | 2002-01-02 | 2005-02-24 | Hideo Tsutsumi | Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them |
| EP1479684A4 (en) | 2002-01-30 | 2006-01-04 | Takeda Pharmaceutical | THIENOPYRIMIDINES, METHODS OF MAKING AND USING SAME |
| MY135609A (en) | 2002-02-26 | 2008-05-30 | Astrazeneca Ab | Pharmaceutical formulation of iressa comprising a water-soluble cellulose derivative |
| SI1591446T1 (sl) | 2003-01-29 | 2013-07-31 | Takeda Pharmaceutical Company Limited | Tienopiridinske spojine in njihova uporaba |
| HRP20080646T3 (en) | 2003-07-07 | 2009-01-31 | Neurocrine Biosciences | Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists |
| BRPI0613643A2 (pt) | 2005-07-22 | 2012-11-06 | Takeda Pharmaceutical | inibidor de ovulação prematura, método de inibir ovulação prematura e uso de um composto |
| EP2155194B1 (en) | 2007-04-06 | 2015-01-21 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| US8765948B2 (en) | 2007-11-07 | 2014-07-01 | Neurocrine Biosciences, Inc. | Processes for the preparation of uracil derivatives |
| JOP20090061B1 (ar) | 2008-02-11 | 2021-08-17 | Ferring Int Center Sa | طريقة معالجة سرطان البروستاتا بمضادات الهرمونات التناسلية GnRH |
| EP2329823A4 (en) | 2008-09-03 | 2013-04-03 | Takeda Pharmaceutical | PROCESS FOR INCREASING THE ABSORPTION ABILITY OF A PREPARATION AND PREPARATION WITH INCREASED ABSORPTION ABILITY |
| PL2900675T3 (pl) | 2012-09-28 | 2019-08-30 | Takeda Pharmaceutical Company Limited | Sposób wytwarzania pochodnej tienopirymidyny |
| EP3185881B1 (en) | 2014-08-26 | 2022-03-09 | Betanien Hospital | Methods, agents and compositions for treatment of inflammatory conditions |
| TWI744224B (zh) | 2015-02-26 | 2021-11-01 | 日商武田藥品工業股份有限公司 | 固形製劑 |
| CA3002791A1 (en) | 2015-09-01 | 2017-03-09 | Abbvie Inc. | Methods of administering elagolix |
| US20180044977A1 (en) | 2016-08-12 | 2018-02-15 | Raynor Mfg. Co. | Rolling door construction for controlling air leakage |
| FI3518932T3 (fi) | 2016-09-30 | 2025-02-03 | Sumitomo Pharma Switzerland Gmbh | Eturauhassyövän hoito |
| SI3518933T2 (sl) | 2016-09-30 | 2025-05-30 | Sumitomo Pharma Switzerland Gmbh | Metode zdravljenja materničnih miom in endometrioze |
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