BRPI0412314B8 - composto 3-[2(r)-{hidroxicarbonilpropil-amino}-2-feniletil]-5-(2-flúor-3-metoxifenil)-1-[2-flúor-6-(trifluorometil)benzil]-6-metil-pirimidina-2,4(1h,3h)-diona, composição farmacêutica compreendendo dito composto e uso do mesmo para o tratamento de uma condição relacionada ao hormônio sexual - Google Patents
composto 3-[2(r)-{hidroxicarbonilpropil-amino}-2-feniletil]-5-(2-flúor-3-metoxifenil)-1-[2-flúor-6-(trifluorometil)benzil]-6-metil-pirimidina-2,4(1h,3h)-diona, composição farmacêutica compreendendo dito composto e uso do mesmo para o tratamento de uma condição relacionada ao hormônio sexualInfo
- Publication number
- BRPI0412314B8 BRPI0412314B8 BRPI0412314A BRPI0412314A BRPI0412314B8 BR PI0412314 B8 BRPI0412314 B8 BR PI0412314B8 BR PI0412314 A BRPI0412314 A BR PI0412314A BR PI0412314 A BRPI0412314 A BR PI0412314A BR PI0412314 B8 BRPI0412314 B8 BR PI0412314B8
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- fluoro
- pyrimidine
- treatment
- dione
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
-
- 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
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
- A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Anesthesiology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US48543403P | 2003-07-07 | 2003-07-07 | |
| US60/485,434 | 2003-07-07 | ||
| PCT/US2004/021593 WO2005007165A1 (en) | 2003-07-07 | 2004-07-06 | Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0412314A BRPI0412314A (pt) | 2006-08-22 |
| BRPI0412314B1 BRPI0412314B1 (pt) | 2019-03-06 |
| BRPI0412314B8 true BRPI0412314B8 (pt) | 2021-05-25 |
Family
ID=34079121
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0412314A BRPI0412314B8 (pt) | 2003-07-07 | 2004-07-06 | composto 3-[2(r)-{hidroxicarbonilpropil-amino}-2-feniletil]-5-(2-flúor-3-metoxifenil)-1-[2-flúor-6-(trifluorometil)benzil]-6-metil-pirimidina-2,4(1h,3h)-diona, composição farmacêutica compreendendo dito composto e uso do mesmo para o tratamento de uma condição relacionada ao hormônio sexual |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US7056927B2 (enExample) |
| EP (1) | EP1646389B1 (enExample) |
| JP (2) | JP4722844B2 (enExample) |
| KR (1) | KR101139148B1 (enExample) |
| CN (1) | CN100424078C (enExample) |
| AT (1) | ATE407679T1 (enExample) |
| AU (1) | AU2004257639B2 (enExample) |
| BR (1) | BRPI0412314B8 (enExample) |
| CA (1) | CA2531508C (enExample) |
| CY (1) | CY1108656T1 (enExample) |
| DE (1) | DE602004016516D1 (enExample) |
| DK (1) | DK1646389T3 (enExample) |
| EA (1) | EA010370B1 (enExample) |
| ES (1) | ES2314448T3 (enExample) |
| HR (1) | HRP20080646T3 (enExample) |
| IL (1) | IL172833A (enExample) |
| MX (1) | MXPA06000297A (enExample) |
| NO (1) | NO334897B1 (enExample) |
| NZ (1) | NZ544747A (enExample) |
| PL (1) | PL1646389T3 (enExample) |
| PT (1) | PT1646389E (enExample) |
| SI (1) | SI1646389T1 (enExample) |
| WO (1) | WO2005007165A1 (enExample) |
| ZA (1) | ZA200600475B (enExample) |
Families Citing this family (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2398018C (en) * | 2000-01-25 | 2011-10-18 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| CA2531508C (en) * | 2003-07-07 | 2013-10-08 | Neurocrine Biosciences, Inc. | Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists |
| ATE428427T1 (de) | 2003-07-07 | 2009-05-15 | Neurocrine Biosciences Inc | Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten |
| EP1644342B1 (en) * | 2003-07-07 | 2012-05-09 | Neurocrine Biosciences, Inc. | Arylpyrimidines useful for the treatment of sex hormone-related conditions such as endometriosis, prostate cancer and the like |
| EA013427B1 (ru) * | 2004-03-15 | 2010-04-30 | Такеда Фармасьютикал Компани Лимитед | Ингибиторы дипептидилпептидазы |
| NZ580457A (en) | 2007-04-06 | 2012-03-30 | Neurocrine Biosciences Inc | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| US8263588B2 (en) | 2007-04-06 | 2012-09-11 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| WO2009045370A2 (en) | 2007-09-28 | 2009-04-09 | Intrexon Corporation | Therapeutic gene-switch constructs and bioreactors for the expression of biotherapeutic molecules, and uses thereof |
| US8765948B2 (en) * | 2007-11-07 | 2014-07-01 | Neurocrine Biosciences, Inc. | Processes for the preparation of uracil derivatives |
| WO2011062437A2 (ko) * | 2009-11-20 | 2011-05-26 | 에스케이케미칼주식회사 | 고나도트로핀 방출 호르몬 수용체 길항제, 이의 제조방법 및 이를 함유하는 약제학적 조성물 |
| WO2014143669A1 (en) | 2013-03-15 | 2014-09-18 | AbbVie Inc . | Compositions for use in treating heavy menstrual bleeding and uterine fibroids |
| EP2881391A1 (en) | 2013-12-05 | 2015-06-10 | Bayer Pharma Aktiengesellschaft | Spiroindoline carbocycle derivatives and pharmaceutical compositions thereof |
| EP3185881B1 (en) | 2014-08-26 | 2022-03-09 | Betanien Hospital | Methods, agents and compositions for treatment of inflammatory conditions |
| WO2017221144A1 (en) * | 2016-06-20 | 2017-12-28 | Dr. Reddy's Laboratories Limited | Process for the preparation of elagolix sodium and its polymorph |
| WO2018015497A2 (en) | 2016-07-21 | 2018-01-25 | ObsEva S.A. | Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage |
| EP3503994B1 (de) | 2016-08-23 | 2024-03-06 | Swan Analytische Instrumente AG | Vorrichtung und verfahren zur elektrodeionisation einer flüssigkeit |
| ES2912929T5 (en) | 2016-09-30 | 2025-05-09 | Sumitomo Pharma Switzerland Gmbh | Methods of treating uterine fibroids and endometriosis |
| EP3518932B1 (en) | 2016-09-30 | 2024-11-13 | Sumitomo Pharma Switzerland GmbH | Treatment of prostate cancer |
| MA46353A (fr) | 2016-09-30 | 2019-08-07 | Myovant Sciences Gmbh | Méthodes de traitement de l'infertilité féminine |
| ES2983735T3 (es) | 2016-12-14 | 2024-10-24 | Purdue Research Foundation | Conjugados del receptor de la hormona liberadora de hormona luteinizante (LHRH-R) y usos de los mismos |
| EP3388421B1 (en) | 2017-04-13 | 2019-12-04 | Sandoz AG | Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist |
| WO2018189212A1 (en) | 2017-04-12 | 2018-10-18 | Sandoz Ag | Acid addition salts of an orally available gonadotropin-releasing hormone receptor antagonist |
| ES2770132T3 (es) | 2017-04-13 | 2020-06-30 | Sandoz Ag | Dispersión sólida amorfa de un antagonista del receptor de la hormona liberadora de gonadotropina disponible por vía oral |
| WO2018198086A1 (en) * | 2017-04-28 | 2018-11-01 | Lupin Limited | Process for the preparation of elagolix and pharmaceutically acceptable salts thereof |
| US11980621B2 (en) | 2017-06-05 | 2024-05-14 | Kissei Pharmaceutical Co., Ltd. | Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis |
| WO2018224063A2 (en) * | 2017-06-08 | 2018-12-13 | Zentiva, K.S. | Solid forms of elagolix |
| CA3073229A1 (en) * | 2017-08-18 | 2019-02-21 | Abbvie Inc. | Pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis |
| WO2019036712A1 (en) | 2017-08-18 | 2019-02-21 | Abbvie Inc. | PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT OF ENDOMETRIOSIS, UTERINE FIBROIDS, POLYKYSTIC OVARY SYNDROME OR ADENOMYOSIS |
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| CN107935863A (zh) * | 2017-11-30 | 2018-04-20 | 厦门海乐景生化有限公司 | Elagolix的关键原料化合物C的合成方法 |
| JP7200261B2 (ja) * | 2017-12-05 | 2023-01-06 | スージョウ ポンシュー ファーマテック カンパニー リミテッド | エラゴリクスを作製するプロセス |
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| EP3724167A1 (en) | 2017-12-11 | 2020-10-21 | Synthon B.V. | Process for preparing elagolix |
| CN109970663B (zh) * | 2017-12-27 | 2023-04-11 | 上海科胜药物研发有限公司 | 一种制备噁拉戈利中间体的方法 |
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| CA3104902A1 (en) * | 2018-07-23 | 2020-01-30 | Abbvie Inc. | Elagolix sodium compositions and processes |
| JP2021532160A (ja) * | 2018-08-01 | 2021-11-25 | アッヴィ・インコーポレイテッド | エラゴリックスに関する投与計画 |
| EP3572406A1 (en) | 2018-10-17 | 2019-11-27 | Sandoz Ag | Acid addition salt of elagolix and related compounds |
| MA54058A (fr) | 2018-10-29 | 2021-09-08 | ObsEva SA | Compositions et méthodes de traitement de l'endométriose interne et de l'endométriose rectovaginale |
| US20230067378A1 (en) | 2018-11-07 | 2023-03-02 | ObsEva S.A. | Compositions and methods for the treatment of estrogen-dependent disorders |
| CN109293634A (zh) * | 2018-12-04 | 2019-02-01 | 中国药科大学 | 恶拉戈利杂质的制备方法 |
| CN109651171A (zh) * | 2019-01-13 | 2019-04-19 | 苏州鹏旭医药科技有限公司 | 依拉戈利及其钠盐的中间体及其盐的制备方法和应用 |
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