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 (enExample) |
| EP (1) | EP3628005A4 (enExample) |
| JP (3) | JP7398963B2 (enExample) |
| KR (2) | KR20200040761A (enExample) |
| CN (2) | CN118845788A (enExample) |
| AU (2) | AU2018317398A1 (enExample) |
| BR (1) | BR112020002967A2 (enExample) |
| CA (1) | CA3064464A1 (enExample) |
| EA (1) | EA202090450A1 (enExample) |
| MX (2) | MX2019015320A (enExample) |
| WO (1) | WO2019036503A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3155599A1 (en) | 2014-01-21 | 2015-07-30 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia |
| BR112020002967A2 (pt) | 2017-08-14 | 2020-08-11 | Spruce Biosciences, Inc. | antagonistas de receptor de fator de liberação de corticotropina |
| CN112423747A (zh) * | 2018-04-27 | 2021-02-26 | 云杉生物科学公司 | 用于治疗睾丸肾上腺残余瘤和卵巢肾上腺残余瘤的方法 |
| MA56226A (fr) | 2018-12-07 | 2022-04-20 | Neurocrine Biosciences Inc | Antagoniste du récepteur crf1, formulations pharmaceutiques et ses formes solides pour le traitement de l'hyperplasie surrénale congénitale |
| KR20220052927A (ko) * | 2019-07-19 | 2022-04-28 | 스프루스 바이오사이언시스 인코포레이티드 | 선천성 부신 증식증의 치료 방법 |
| CN118252829A (zh) | 2019-09-27 | 2024-06-28 | 纽罗克里生物科学有限公司 | Crf受体拮抗剂及使用方法 |
| EP4656192A2 (en) | 2020-08-12 | 2025-12-03 | Spruce Biosciences, Inc. | Tildacerfont and derivatives thereof for treating polycystic ovary syndrome |
| US20240024330A1 (en) * | 2020-08-26 | 2024-01-25 | Neurocrine Biosciences, Inc. | Crf receptor antagonists and methods of use |
| 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 |
|---|---|---|---|---|
| EP0674641B1 (en) | 1992-12-17 | 1999-03-03 | Pfizer Inc. | Pyrrolopyrimidines as crf antagonists |
| PL191271B1 (pl) | 1996-02-07 | 2006-04-28 | Neurocrine Biosciences Inc | Pochodna pirazolopirymidyny i jej zastosowanie oraz kompozycja farmaceutyczna |
| EA006626B1 (ru) | 1996-07-24 | 2006-02-24 | Дюпон Фармасьютикалз Компани | Азолопиримидины, фармацевтическая композиция и способ лечения |
| CZ299451B6 (cs) | 1996-07-24 | 2008-07-30 | Bristol-Myers Squibb Pharma Company | [1,5-a]-Pyrazolo-1,3,5- triaziny jejich použití afarmaceutické kompozice na jejich bázi |
| CA2263566C (en) | 1996-08-28 | 2003-09-09 | Pfizer Inc. | Substituted 6,5-hetero-bicyclic derivatives |
| 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 |
| ATE301657T1 (de) | 1998-01-28 | 2005-08-15 | Bristol Myers Squibb Pharma Co | Azolo-pyrimidine |
| EP1040831A3 (en) | 1999-04-02 | 2003-05-02 | Pfizer Products Inc. | Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death |
| AU4203500A (en) | 1999-04-06 | 2000-10-23 | Du Pont Pharmaceuticals Company | Pyrazolopyrimidines as crf antagonists |
| CN1377355A (zh) | 1999-09-30 | 2002-10-30 | 纽罗杰有限公司 | 氨基取代的吡唑并[1,5－a]－1,5－嘧啶和吡唑并[1,5－a]－1,3,5－三嗪 |
| CN1679556A (zh) | 1999-12-08 | 2005-10-12 | 法马西亚公司 | 维得克西组合物 |
| ATE355102T1 (de) | 2001-03-13 | 2006-03-15 | Bristol Myers Squibb Pharma Co | 4-(2-butylamino)-2,7-dimethyl-8-(2-methyl-6- methoxypyrid-3-yl) pyrazolo- 1,5-aö-1,3,5-triazin,seine enantiomeren und pharmazeutisch annehmbare salze als corticotropin-releasing-factor-rezeptor-ligande |
| 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 |
| AU2004309168B2 (en) | 2003-12-22 | 2009-04-23 | Neurocrine Biosciences Inc | CRF receptor antagonists and methods relating thereto |
| EP1718311A1 (en) | 2004-02-13 | 2006-11-08 | Pfizer Products Incorporated | Therapeutic combinations of atypical antipsychotics with corticotropin releasing factor antagonists |
| WO2005079868A2 (en) | 2004-02-13 | 2005-09-01 | Sb Pharmco Puerto Rico Inc | Crf receptor antagonists, their preparations, their pharmaceutical composition and their uses |
| EP1781257B1 (en) * | 2004-08-13 | 2018-12-19 | Emisphere Technologies, Inc. | Pharmaceutical formulations containing microparticles or nanoparticles of a delivery agent |
| EP1869049B1 (en) | 2005-03-21 | 2009-03-04 | 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 |
| CN101516886B (zh) | 2006-09-20 | 2012-02-29 | 伊莱利利公司 | 噻吩吡唑并嘧啶化合物 |
| JP5161226B2 (ja) * | 2006-09-20 | 2013-03-13 | イーライ リリー アンド カンパニー | Ｃｒｆ１受容体アンタゴニストとしてのチアゾールピラゾロピリミジン |
| US8952207B2 (en) | 2007-09-11 | 2015-02-10 | The University Of Houston System | Copper-catalyzed C—H bond arylation |
| WO2009035473A2 (en) | 2007-09-13 | 2009-03-19 | Sanfilippo Louis C | Method of treating binge eating disorder, obesity resulting from binge eating behavior and depressive disorders |
| KR101357392B1 (ko) | 2008-10-02 | 2014-02-03 | 일라이 릴리 앤드 캄파니 | 합성 중간체로서의 티아졸릴-피라졸로피리미딘 화합물 및 관련 합성 방법 |
| EP2384437B1 (en) * | 2008-12-24 | 2018-12-12 | Quest Diagnostics Investments Incorporated | Mass spectrometry assay for pregnenolone and 17-hydroxypregnenolone |
| US20110160168A1 (en) * | 2009-12-31 | 2011-06-30 | Differential Drug Development Associates, Llc | Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols |
| AU2013230781B2 (en) | 2012-03-08 | 2015-12-03 | Medtronic Af Luxembourg S.A.R.L. | Ovarian neuromodulation and associated systems and methods |
| EP2841068B8 (en) | 2012-04-23 | 2019-03-06 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Crhr1 antagonists for use in the treatment of patients having crh overactivity |
| CA3155599A1 (en) * | 2014-01-21 | 2015-07-30 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia |
| JP6712279B2 (ja) | 2015-03-31 | 2020-06-17 | ジーバ メディカル， インコーポレイテッド | 卵巣組織の操作のための方法およびシステム |
| KR102644781B1 (ko) | 2017-08-14 | 2024-03-06 | 스프루스 바이오사이언시스 인코포레이티드 | 코티코트로핀 방출 인자 수용체 길항제 |
| BR112020002967A2 (pt) | 2017-08-14 | 2020-08-11 | Spruce Biosciences, Inc. | antagonistas de receptor de fator de liberação de corticotropina |
| CN112423747A (zh) | 2018-04-27 | 2021-02-26 | 云杉生物科学公司 | 用于治疗睾丸肾上腺残余瘤和卵巢肾上腺残余瘤的方法 |
| MA56226A (fr) | 2018-12-07 | 2022-04-20 | Neurocrine Biosciences Inc | Antagoniste du récepteur crf1, formulations pharmaceutiques et ses formes solides pour le traitement de l'hyperplasie surrénale congénitale |
| US20200255436A1 (en) | 2019-02-12 | 2020-08-13 | Spruce Biosciences, Inc. | Corticotropin releasing factor receptor antagonists |
| KR20220052927A (ko) | 2019-07-19 | 2022-04-28 | 스프루스 바이오사이언시스 인코포레이티드 | 선천성 부신 증식증의 치료 방법 |
| EP4656192A2 (en) | 2020-08-12 | 2025-12-03 | Spruce Biosciences, Inc. | Tildacerfont and derivatives thereof for treating polycystic ovary syndrome |
| EP4402142A4 (en) | 2021-11-19 | 2025-07-23 | Spruce Biosciences Inc | CRYSTALLINE COMPOSITION OF TILDACERFONT AND ITS METHODS OF USE AND PREPARATION |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
-
2018
- 2018-08-14 BR BR112020002967-0A patent/BR112020002967A2/pt not_active Application Discontinuation
- 2018-08-14 KR KR1020207004095A patent/KR20200040761A/ko not_active Ceased
- 2018-08-14 MX MX2019015320A patent/MX2019015320A/es unknown
- 2018-08-14 EA EA202090450A patent/EA202090450A1/ru unknown
- 2018-08-14 AU AU2018317398A patent/AU2018317398A1/en not_active Abandoned
- 2018-08-14 CN CN202410709847.0A patent/CN118845788A/zh active Pending
- 2018-08-14 US US16/639,541 patent/US20210361664A1/en not_active Abandoned
- 2018-08-14 CN CN201880038569.3A patent/CN110996943A/zh active Pending
- 2018-08-14 CA CA3064464A patent/CA3064464A1/en active Pending
- 2018-08-14 EP EP18846689.0A patent/EP3628005A4/en active Pending
- 2018-08-14 WO PCT/US2018/046760 patent/WO2019036503A1/en not_active Ceased
- 2018-08-14 JP JP2019572817A patent/JP7398963B2/ja active Active
- 2018-08-14 KR KR1020257004457A patent/KR20250022913A/ko active Pending
-
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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