AU2016379417B2 - Inhibitors of glucocorticoid receptor - Google Patents
Inhibitors of glucocorticoid receptor Download PDFInfo
- Publication number
- AU2016379417B2 AU2016379417B2 AU2016379417A AU2016379417A AU2016379417B2 AU 2016379417 B2 AU2016379417 B2 AU 2016379417B2 AU 2016379417 A AU2016379417 A AU 2016379417A AU 2016379417 A AU2016379417 A AU 2016379417A AU 2016379417 B2 AU2016379417 B2 AU 2016379417B2
- Authority
- AU
- Australia
- Prior art keywords
- optionally substituted
- alkyl
- carbocyclyl
- heterocyclyl
- cancer
- 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.)
- Ceased
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
- C07J1/0096—Alkynyl derivatives
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
-
- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0003—Androstane derivatives
- C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/006—Ketals at position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/008—Ketals at position 17
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
- C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
- C07K16/2827—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against B7 molecules, e.g. CD80, CD86
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2020256460A AU2020256460A1 (en) | 2015-12-23 | 2020-10-19 | Inhibitors of glucocorticoid receptor |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562387293P | 2015-12-23 | 2015-12-23 | |
| US62/387,293 | 2015-12-23 | ||
| PCT/US2016/068448 WO2017112909A1 (en) | 2015-12-23 | 2016-12-22 | Inhibitors of glucocorticoid receptor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2020256460A Division AU2020256460A1 (en) | 2015-12-23 | 2020-10-19 | Inhibitors of glucocorticoid receptor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2016379417A1 AU2016379417A1 (en) | 2018-07-19 |
| AU2016379417B2 true AU2016379417B2 (en) | 2020-09-24 |
Family
ID=59091255
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016379417A Ceased AU2016379417B2 (en) | 2015-12-23 | 2016-12-22 | Inhibitors of glucocorticoid receptor |
| AU2020256460A Abandoned AU2020256460A1 (en) | 2015-12-23 | 2020-10-19 | Inhibitors of glucocorticoid receptor |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2020256460A Abandoned AU2020256460A1 (en) | 2015-12-23 | 2020-10-19 | Inhibitors of glucocorticoid receptor |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11208432B2 (enExample) |
| EP (1) | EP3394079A4 (enExample) |
| JP (2) | JP6995757B2 (enExample) |
| CN (1) | CN108713023B (enExample) |
| AU (2) | AU2016379417B2 (enExample) |
| CA (1) | CA3009525A1 (enExample) |
| WO (1) | WO2017112909A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017112904A1 (en) | 2015-12-23 | 2017-06-29 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
| EP3394078A4 (en) | 2015-12-23 | 2019-11-27 | Oric Pharmaceuticals, Inc. | INHIBITORS OF THE GLUCOCORTICIDE RECEPTOR |
| JP6995757B2 (ja) * | 2015-12-23 | 2022-01-17 | オリック ファーマシューティカルズ,インク. | グルココルチコイド受容体の阻害剤 |
| WO2018068021A1 (en) | 2016-10-07 | 2018-04-12 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
| TW202010502A (zh) * | 2018-04-11 | 2020-03-16 | 美商歐瑞克製藥公司 | 包含糖皮質激素受體拮抗劑之固體形式與調配物及其用途 |
| CN118265717A (zh) * | 2022-03-31 | 2024-06-28 | 成都赛璟生物医药科技有限公司 | 一种cdk8抑制剂及其制备方法和用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5405979A (en) * | 1990-06-01 | 1995-04-11 | Schering Aktiengesellschaft | Process for the production of 10β-H-steroids |
| US5843931A (en) * | 1990-12-22 | 1998-12-01 | Shering Aktiengesellschaft | 6,7-modified 11β-aryl-4-oestrenes |
| US5843933A (en) * | 1989-06-23 | 1998-12-01 | Schering Aktiengesellschaft | 11β-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents |
| CN1222350A (zh) * | 1998-01-07 | 1999-07-14 | 沈志华 | 用于大月份引产的复合药物 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2528434B1 (fr) | 1982-06-11 | 1985-07-19 | Roussel Uclaf | Nouveaux 19-nor steroides substitues en 11b et eventuellement en 2, leur procede de preparation et leur application comme medicament |
| 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 |
| 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 |
| JP2785023B2 (ja) | 1987-12-30 | 1998-08-13 | ルセル―ユクラフ | 17α位置を置換された17β―OH―19―ノルステロイドの新誘導体、その製造方法、その薬剤としての使用及びそれを含有する製薬組成物 |
| JPH02188599A (ja) | 1988-11-16 | 1990-07-24 | Roussel Uclaf | 3―ケト―デルタ―4,9―19―ノルステロイドから誘導される新物質及びそれらよりなる薬剤 |
| FR2651435A1 (fr) | 1989-09-07 | 1991-03-08 | Roussel Uclaf | Nouvelle utilisation de composes anti-progestomimetiques. |
| DE69413829T2 (de) | 1993-08-04 | 1999-04-15 | Akzo Nobel N.V., Arnheim/Arnhem | Antiglucocorticoidsteroide zur behandlung von angststörungen |
| WO1995017192A1 (en) | 1993-12-22 | 1995-06-29 | The Salk Institute For Biological Studies | Methods for reducing multidrug resistance |
| WO1996023503A1 (de) | 1995-02-02 | 1996-08-08 | Schering Aktiengesellschaft | Progesteronantagonisten für die herstellung von arzneimitteln zur behandlung von dysfunktionellen uterinen blutungen |
| IL118974A (en) * | 1995-08-17 | 2001-09-13 | Akzo Nobel Nv | History 11 - (Transformed Phenyl) - Astra - 4, 9 - Diane, their preparation and pharmaceutical preparations containing them |
| 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 |
| US6512130B1 (en) | 2000-09-05 | 2003-01-28 | Council Of Scientific And Industrial Research | Mifepristone analogue, process for the preparation thereof and use thereof |
| EP1285927A3 (de) | 2001-08-16 | 2005-06-29 | Schering Aktiengesellschaft | Verwendung von Glucocorticoid-Rezeptorantagonisten zur Vorbeugung und Behandlung von Erkrankungen des männlichen Reproduktionssystems |
| US7250408B2 (en) | 2002-12-16 | 2007-07-31 | Bayer Schering Pharma Ag | Glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility |
| AU2007245022A1 (en) | 2006-03-29 | 2007-11-08 | The Regents Of The University Of California | Diarylthiohydantoin compounds |
| PL1989218T3 (pl) | 2006-02-17 | 2010-06-30 | Janssen Pharmaceutica Nv | Pochodne 17-fosforosteroidów użyteczne jako modulatory receptora progesteronowego |
| US8569274B2 (en) | 2007-04-20 | 2013-10-29 | Preglem S.A. | Progesterone antagonist and selective progesterone modulator in the treatment of excessive uterine bleeding |
| JP5804395B2 (ja) | 2011-02-03 | 2015-11-04 | ポップ テスト オンコロジー エルエルシー | 診断と治療のためのシステムおよび方法 |
| EP2545922A1 (en) | 2011-07-12 | 2013-01-16 | PregLem S.A. | Treatment of excessive menstrual bleeding associated with uterine fibroids |
| US20130029953A1 (en) | 2011-07-28 | 2013-01-31 | Klaus Nickisch | Progesterone antagonists |
| PT3111950T (pt) | 2012-02-24 | 2021-10-19 | Univ Chicago | Métodos e composições relacionadas com antagonismo recetor de glucocorticoide e cancro da próstata |
| EP2641602A1 (en) | 2012-03-23 | 2013-09-25 | PregLem S.A. | Method for treating gynecological diseases |
| US9096641B2 (en) | 2013-06-05 | 2015-08-04 | Evestra, Inc. | Imidazolyl progesterone antagonists |
| EP3079475B1 (en) | 2013-12-11 | 2020-10-07 | Sloan-kettering Institute For Cancer Research | Glucocorticoid inhibitors for treatment of prostate cancer |
| CN104530166B (zh) | 2014-12-04 | 2016-08-24 | 陕西汉江药业集团股份有限公司 | 选择性还原4,6-共轭双烯-3-酮甾体化合物的方法 |
| WO2017112904A1 (en) | 2015-12-23 | 2017-06-29 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
| EP3394078A4 (en) | 2015-12-23 | 2019-11-27 | Oric Pharmaceuticals, Inc. | INHIBITORS OF THE GLUCOCORTICIDE RECEPTOR |
| JP6995757B2 (ja) * | 2015-12-23 | 2022-01-17 | オリック ファーマシューティカルズ,インク. | グルココルチコイド受容体の阻害剤 |
| WO2018068021A1 (en) | 2016-10-07 | 2018-04-12 | Oric Pharmaceuticals, Inc. | Inhibitors of glucocorticoid receptor |
| WO2018227129A1 (en) | 2017-06-09 | 2018-12-13 | Regents Of The University Of Minnesota | Skin care formulations and skin cancer treatment |
| TW202010502A (zh) | 2018-04-11 | 2020-03-16 | 美商歐瑞克製藥公司 | 包含糖皮質激素受體拮抗劑之固體形式與調配物及其用途 |
-
2016
- 2016-12-22 JP JP2018533668A patent/JP6995757B2/ja not_active Expired - Fee Related
- 2016-12-22 AU AU2016379417A patent/AU2016379417B2/en not_active Ceased
- 2016-12-22 CA CA3009525A patent/CA3009525A1/en active Pending
- 2016-12-22 EP EP16880126.4A patent/EP3394079A4/en not_active Withdrawn
- 2016-12-22 US US16/065,627 patent/US11208432B2/en active Active
- 2016-12-22 WO PCT/US2016/068448 patent/WO2017112909A1/en not_active Ceased
- 2016-12-22 CN CN201680082460.0A patent/CN108713023B/zh not_active Expired - Fee Related
-
2020
- 2020-10-19 AU AU2020256460A patent/AU2020256460A1/en not_active Abandoned
-
2021
- 2021-09-10 JP JP2021147955A patent/JP2022003045A/ja active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5843933A (en) * | 1989-06-23 | 1998-12-01 | Schering Aktiengesellschaft | 11β-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents |
| US5405979A (en) * | 1990-06-01 | 1995-04-11 | Schering Aktiengesellschaft | Process for the production of 10β-H-steroids |
| US5843931A (en) * | 1990-12-22 | 1998-12-01 | Shering Aktiengesellschaft | 6,7-modified 11β-aryl-4-oestrenes |
| CN1222350A (zh) * | 1998-01-07 | 1999-07-14 | 沈志华 | 用于大月份引产的复合药物 |
Non-Patent Citations (1)
| Title |
|---|
| GEISLER, J. et al., "An efficient synthesis of 11beta-(4-Aminophenyl)spiro [estr-4-ene-17beta, 2' (5'H)-furan]-3, 5'-di one", Tetrahedron, (2000-08-25), vol. 56, no. 35, doi:doi:10.1016/S0040-4020(00)00602-5, pages 6489 - 6492 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3394079A4 (en) | 2019-08-21 |
| AU2016379417A1 (en) | 2018-07-19 |
| JP6995757B2 (ja) | 2022-01-17 |
| AU2020256460A1 (en) | 2020-11-12 |
| JP2019500376A (ja) | 2019-01-10 |
| JP2022003045A (ja) | 2022-01-11 |
| CA3009525A1 (en) | 2017-06-29 |
| US20210002324A1 (en) | 2021-01-07 |
| CN108713023B (zh) | 2021-10-26 |
| CN108713023A (zh) | 2018-10-26 |
| EP3394079A1 (en) | 2018-10-31 |
| US11208432B2 (en) | 2021-12-28 |
| WO2017112909A1 (en) | 2017-06-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |