EA202090450A1 - Антагонисты рецептора кортикотропин-рилизинг фактора - Google Patents
Антагонисты рецептора кортикотропин-рилизинг фактораInfo
- Publication number
- EA202090450A1 EA202090450A1 EA202090450A EA202090450A EA202090450A1 EA 202090450 A1 EA202090450 A1 EA 202090450A1 EA 202090450 A EA202090450 A EA 202090450A EA 202090450 A EA202090450 A EA 202090450A EA 202090450 A1 EA202090450 A1 EA 202090450A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- corticotropin
- receptor antagonists
- releasing factor
- dimethylpyrazolo
- ethylpropyl
- Prior art date
Links
- 102000012289 Corticotropin-Releasing Hormone Human genes 0.000 title 1
- 108010022152 Corticotropin-Releasing Hormone Proteins 0.000 title 1
- 239000000055 Corticotropin-Releasing Hormone Substances 0.000 title 1
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 206010010356 Congenital anomaly Diseases 0.000 abstract 1
- 210000004404 adrenal cortex Anatomy 0.000 abstract 1
- 206010020718 hyperplasia Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- XVAWSBAQNIXMIO-UHFFFAOYSA-N tildacerfont Chemical compound CC1=NN2C(C(CC)CC)=CC(C)=NC2=C1C(=C(N=1)Cl)SC=1N1CCOCC1 XVAWSBAQNIXMIO-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- 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
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- 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
- A61P15/08—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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
-
- 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762545406P | 2017-08-14 | 2017-08-14 | |
| PCT/US2018/046760 WO2019036503A1 (en) | 2017-08-14 | 2018-08-14 | CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA202090450A1 true EA202090450A1 (ru) | 2020-09-24 |
Family
ID=65362494
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202090450A EA202090450A1 (ru) | 2017-08-14 | 2018-08-14 | Антагонисты рецептора кортикотропин-рилизинг фактора |
Country Status (11)
| Country | Link |
|---|---|
| US (9) | US20210361664A1 (https=) |
| EP (1) | EP3628005A4 (https=) |
| JP (3) | JP7398963B2 (https=) |
| KR (2) | KR20250022913A (https=) |
| CN (2) | CN118845788A (https=) |
| AU (2) | AU2018317398A1 (https=) |
| BR (1) | BR112020002967A2 (https=) |
| CA (1) | CA3064464A1 (https=) |
| EA (1) | EA202090450A1 (https=) |
| MX (2) | MX2019015320A (https=) |
| WO (1) | WO2019036503A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015112642A1 (en) | 2014-01-21 | 2015-07-30 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia |
| CN118845788A (zh) | 2017-08-14 | 2024-10-29 | 云杉生物科学公司 | 促肾上腺皮质激素释放因子受体拮抗剂 |
| EP4438124A3 (en) | 2018-04-27 | 2024-12-18 | Spruce Biosciences, Inc. | Methods for treating testicular and ovarian adrenal rest tumors |
| CA3121920A1 (en) | 2018-12-07 | 2020-06-11 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| TW202116324A (zh) * | 2019-07-19 | 2021-05-01 | 美商雲杉生物科技股份有限公司 | 治療先天性腎上腺增生之方法 |
| JP7623365B2 (ja) | 2019-09-27 | 2025-01-28 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | Ｃｒｆ受容体アンタゴニストおよび使用方法 |
| BR112023002497A2 (pt) * | 2020-08-12 | 2023-05-02 | Spruce Biosciences Inc | Métodos e composições para tratamento da síndrome dos ovários policísticos |
| JP2023540223A (ja) * | 2020-08-26 | 2023-09-22 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | Ｃｒｆ受容体アンタゴニストおよび使用方法 |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
| WO2025188842A1 (en) * | 2024-03-08 | 2025-09-12 | Spruce Biosciences, Inc. | Amorphous solid dispersion of tildacerfont formulations |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE177101T1 (de) | 1992-12-17 | 1999-03-15 | Pfizer | Pyrrolopyrimidine als crf antagonisten |
| JP3356291B2 (ja) | 1996-02-07 | 2002-12-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｃｒｆレセプター拮抗薬としてのピラゾロピリミジン類 |
| IL127871A0 (en) | 1996-07-24 | 1999-10-28 | Du Pont Pharm Co | Azolo triazines and pyrimidines |
| HU228962B1 (en) | 1996-07-24 | 2013-07-29 | Bristol Myers Squibb Pharma Co | Azolo triazines, pharmaceutical compositions containing them and use of the compounds |
| IL127566A0 (en) | 1996-08-28 | 1999-10-28 | Pfizer | Substituted 6,5-hetero- bicyclic derivatives |
| EP1049699B1 (en) | 1998-01-28 | 2004-04-21 | Bristol-Myers Squibb Pharma Company | Pyrazolotriazines as crf antagonists |
| IL137019A (en) | 1998-01-28 | 2010-11-30 | Du Pont Pharm Co | 2,7 - dimethyl - 4 - (substituted amino) - 8 - arylpyrazolo [1,5-a] triazine derivatives and pharmaceutical compositions containing them |
| EP1040831A3 (en) | 1999-04-02 | 2003-05-02 | Pfizer Products Inc. | Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death |
| WO2000059908A2 (en) | 1999-04-06 | 2000-10-12 | Du Pont Pharmaceuticals Company | Pyrazolopyrimidines as crf antagonists |
| EP1218381B1 (en) | 1999-09-30 | 2006-12-06 | Neurogen Corporation | AMINO SUBSTITUTED PYRAZOLO¬1,5-a|-1,5-PYRIMIDINES AND PYRAZOLO¬1,5-a|-1,3,5-TRIAZINES |
| JP2003516353A (ja) | 1999-12-08 | 2003-05-13 | ファルマシア コーポレイション | ヴァルデコキシブ組成物 |
| BR0208357A (pt) | 2001-03-13 | 2004-06-29 | Bristol Myers Squibb Pharma Co | Composto, composição farmacêutica, método de antagonização de um receptor de fator de liberação de corticotropina (crf), método de tratamento de disfunção, método de triagem de ligantes, método de detecção de receptores de crf, método de inibição da ligação de crf, artigo industrializado e usos do composto |
| US20050085479A1 (en) | 2003-08-27 | 2005-04-21 | Pharmacia Corporation | Mediated central nervous system compositions of a cyclooxygenase-2 selective inhibitor and a corticotropin releasing factor antagonist for the treatment of ischemic disorders or injury |
| CA2547639A1 (en) | 2003-12-02 | 2005-06-16 | B&B Beheer Nv | Use of d4 and 5-ht2a antagonists, inverse agonists or partial agonists |
| CA2550948A1 (en) | 2003-12-22 | 2005-07-14 | Sb Pharmco Puerto Rico Inc. | Crf receptor antagonists and methods relating thereto |
| WO2005079868A2 (en) | 2004-02-13 | 2005-09-01 | Sb Pharmco Puerto Rico Inc | Crf receptor antagonists, their preparations, their pharmaceutical composition and their uses |
| WO2005079807A1 (en) | 2004-02-13 | 2005-09-01 | Pfizer Products Inc. | Therapeutic combinations of atypical antipsychotics with corticotropin releasing factor antagonists |
| WO2006124047A2 (en) * | 2004-08-13 | 2006-11-23 | Emisphere Technologies, Inc. | Pharmaceutical formulations containing microparticles or nanoparticles of a delivery agent |
| AU2006227300B2 (en) | 2005-03-21 | 2012-02-02 | Eli Lilly And Company | Imidazopyridazine compounds |
| CN101516835A (zh) | 2006-07-19 | 2009-08-26 | 俄亥俄州立大学研究基金会 | 选择性雄激素受体调节剂、它们的类似物和衍生物以及它们的用途 |
| EP2094709B1 (en) * | 2006-09-20 | 2010-09-15 | Eli Lilly And Company | Thiazole pyrazolopyrimidines as crf1 receptor antagonists |
| AU2007297481B2 (en) | 2006-09-20 | 2012-03-08 | Eli Lilly And Company | Thiophene pyrazolopyrimidine compounds |
| US8952207B2 (en) | 2007-09-11 | 2015-02-10 | The University Of Houston System | Copper-catalyzed C—H bond arylation |
| US8318813B2 (en) | 2007-09-13 | 2012-11-27 | Lcs Group, Llc | Method of treating binge eating disorder |
| WO2010039678A1 (en) | 2008-10-02 | 2010-04-08 | Eli Lilly And Company | Thiazolyl-pyrazolopyrimidine compounds as synthetic intermediates and related synthetic processes |
| EP4718073A2 (en) * | 2008-12-24 | 2026-04-01 | Quest Diagnostics Investments Incorporated | Mass spectrometry assay for congenital adrenal hyperplasia |
| PL2519230T3 (pl) * | 2009-12-31 | 2019-05-31 | Marius Pharmaceuticals Llc | Modulacja rozpuszczalności, stabilności, absorpcji, metabolizmu i profilu farmakokinetycznego leków lipofilowych przez sterole |
| US9750568B2 (en) | 2012-03-08 | 2017-09-05 | Medtronic Ardian Luxembourg S.A.R.L. | Ovarian neuromodulation and associated systems and methods |
| HK1207304A1 (en) | 2012-04-23 | 2016-01-29 | Hmnc Value Gmbh | Crhr1 antagonists for use in the treatment of patients having crh overactivity |
| WO2015112642A1 (en) * | 2014-01-21 | 2015-07-30 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia |
| AU2016242867B2 (en) | 2015-03-31 | 2020-11-05 | May Health Us Inc. | Methods and systems for the manipulation of ovarian tissues |
| CN118845788A (zh) | 2017-08-14 | 2024-10-29 | 云杉生物科学公司 | 促肾上腺皮质激素释放因子受体拮抗剂 |
| EA202090321A1 (ru) | 2017-08-14 | 2020-09-24 | Спрюс Биосайнсес, Инк. | Антагонисты рецептора кортикотропин-рилизинг фактора |
| EP4438124A3 (en) | 2018-04-27 | 2024-12-18 | Spruce Biosciences, Inc. | Methods for treating testicular and ovarian adrenal rest tumors |
| CA3121920A1 (en) | 2018-12-07 | 2020-06-11 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| US20200255436A1 (en) | 2019-02-12 | 2020-08-13 | Spruce Biosciences, Inc. | Corticotropin releasing factor receptor antagonists |
| TW202116324A (zh) | 2019-07-19 | 2021-05-01 | 美商雲杉生物科技股份有限公司 | 治療先天性腎上腺增生之方法 |
| BR112023002497A2 (pt) | 2020-08-12 | 2023-05-02 | Spruce Biosciences Inc | Métodos e composições para tratamento da síndrome dos ovários policísticos |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
| MX2024006064A (es) | 2021-11-19 | 2024-05-30 | Spruce Biosciences Inc | Composicion cristalina de tildacerfont y metodos de uso y preparacion de la misma. |
-
2018
- 2018-08-14 CN CN202410709847.0A patent/CN118845788A/zh active Pending
- 2018-08-14 JP JP2019572817A patent/JP7398963B2/ja active Active
- 2018-08-14 MX MX2019015320A patent/MX2019015320A/es unknown
- 2018-08-14 EP EP18846689.0A patent/EP3628005A4/en active Pending
- 2018-08-14 CN CN201880038569.3A patent/CN110996943A/zh active Pending
- 2018-08-14 KR KR1020257004457A patent/KR20250022913A/ko active Pending
- 2018-08-14 WO PCT/US2018/046760 patent/WO2019036503A1/en not_active Ceased
- 2018-08-14 BR BR112020002967-0A patent/BR112020002967A2/pt not_active Application Discontinuation
- 2018-08-14 CA CA3064464A patent/CA3064464A1/en active Pending
- 2018-08-14 KR KR1020207004095A patent/KR20200040761A/ko not_active Ceased
- 2018-08-14 AU AU2018317398A patent/AU2018317398A1/en not_active Abandoned
- 2018-08-14 US US16/639,541 patent/US20210361664A1/en not_active Abandoned
- 2018-08-14 EA EA202090450A patent/EA202090450A1/ru unknown
-
2019
- 2019-04-18 US US16/388,620 patent/US10849908B2/en active Active
- 2019-12-16 MX MX2023000501A patent/MX2023000501A/es unknown
-
2020
- 2020-10-05 US US17/063,592 patent/US11344557B2/en active Active
- 2020-10-22 US US17/078,054 patent/US11007201B2/en active Active
-
2021
- 2021-06-25 US US17/359,411 patent/US11351177B2/en active Active
- 2021-06-25 US US17/359,414 patent/US11311549B2/en active Active
-
2022
- 2022-01-27 US US17/586,228 patent/US20220143037A1/en not_active Abandoned
- 2022-12-09 US US18/078,649 patent/US20230321112A1/en active Pending
-
2023
- 2023-01-13 AU AU2023200189A patent/AU2023200189B2/en active Active
- 2023-04-26 US US18/307,718 patent/US12115166B2/en active Active
- 2023-09-08 JP JP2023146415A patent/JP7573080B2/ja active Active
-
2024
- 2024-10-11 JP JP2024179270A patent/JP2025020148A/ja active Pending
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