CY1122196T1 - Παραγωγα πυραζολοπυριμιδονης ή πυρρολοτριαζονης, μεθοδος παρασκευης αυτων και φαρμακευτικες εφαρμογες αυτων - Google Patents
Παραγωγα πυραζολοπυριμιδονης ή πυρρολοτριαζονης, μεθοδος παρασκευης αυτων και φαρμακευτικες εφαρμογες αυτωνInfo
- Publication number
- CY1122196T1 CY1122196T1 CY20191100975T CY191100975T CY1122196T1 CY 1122196 T1 CY1122196 T1 CY 1122196T1 CY 20191100975 T CY20191100975 T CY 20191100975T CY 191100975 T CY191100975 T CY 191100975T CY 1122196 T1 CY1122196 T1 CY 1122196T1
- Authority
- CY
- Cyprus
- Prior art keywords
- pyrazolopyrimidone
- preparation
- pharmaceutical applications
- pyrrolotriazone
- derivatives
- Prior art date
Links
- DOTPSQVYOBAWPQ-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-3-one Chemical compound N1=CN=C2C(=O)N=NC2=C1 DOTPSQVYOBAWPQ-UHFFFAOYSA-N 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title abstract 2
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 abstract 2
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 abstract 2
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 abstract 2
- 229940035638 gonadotropin-releasing hormone Drugs 0.000 abstract 2
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- 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
- 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
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
-
- 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
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- 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
-
- 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
- A61P17/10—Anti-acne agents
-
- 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
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- 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
- 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
- A61P5/24—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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pregnancy & Childbirth (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Η παρούσα εφεύρεση παρέχει παράγωγα πυραζολοπυριμιδόνης ή πυρρολοτριαζόνης, μέθοδο παρασκευής αυτών και φαρμακευτικές εφαρμογές αυτών. Συγκεκριμένα, η παρούσα εφεύρεση παρέχει παράγωγα πυραζολοπυριμιδόνης ή πυρρολοτριαζόνης που παριστάνονται με έναν γενικό τύπο (I) και φαρμακευτικά άλατα αυτών, μέθοδο παρασκευής αυτών και χρήση αυτών ως έναν ανταγωνιστή ορμόνης αποδέσμευσης γοναδοτροπίνης (GnRH) και ειδικά ως θεραπευτικούς παράγοντες για την ενδομητρίωση, όπου οι ορισμοί των υποκατάστατων στον γενικό τύπο (I) είναι οι ίδιοι όπως οι ορισμοί στην περιγραφή.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310525956 | 2013-10-30 | ||
| PCT/CN2014/087906 WO2015062391A1 (zh) | 2013-10-30 | 2014-09-30 | 吡唑并嘧啶酮类或吡咯并三嗪酮类衍生物、其制备方法及其在医药上的应用 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1122196T1 true CY1122196T1 (el) | 2020-11-25 |
Family
ID=53003302
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20191100975T CY1122196T1 (el) | 2013-10-30 | 2019-09-18 | Παραγωγα πυραζολοπυριμιδονης ή πυρρολοτριαζονης, μεθοδος παρασκευης αυτων και φαρμακευτικες εφαρμογες αυτων |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US10005781B2 (el) |
| EP (1) | EP3064498B1 (el) |
| JP (1) | JP6412563B2 (el) |
| CN (1) | CN104884457B (el) |
| AU (1) | AU2014344504C1 (el) |
| BR (1) | BR112016008799B1 (el) |
| CA (1) | CA2927641C (el) |
| CY (1) | CY1122196T1 (el) |
| DK (1) | DK3064498T3 (el) |
| ES (1) | ES2747839T3 (el) |
| HR (1) | HRP20191679T1 (el) |
| HU (1) | HUE046314T2 (el) |
| LT (1) | LT3064498T (el) |
| MX (1) | MX2016005142A (el) |
| PL (1) | PL3064498T3 (el) |
| PT (1) | PT3064498T (el) |
| RS (1) | RS59457B1 (el) |
| RU (1) | RU2674977C2 (el) |
| SI (1) | SI3064498T1 (el) |
| TW (1) | TWI675838B (el) |
| WO (1) | WO2015062391A1 (el) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112016008799B1 (pt) * | 2013-10-30 | 2023-02-23 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Derivados de pirazolopirimidona ou pirrolotriazona, seus intermediários, seus usos, seus processos de preparação, e composição farmacêutica |
| TWI751220B (zh) * | 2016-11-07 | 2022-01-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種ＧｎＲＨ受體拮抗劑的多晶型及其製備方法 |
| CA3040026A1 (en) * | 2016-11-14 | 2018-05-17 | Jiangsu Hengrui Medicine Co., Ltd. | Crystalline form of gnrh receptor antagonist and preparation method therefor |
| EP3660017A4 (en) * | 2017-07-28 | 2020-12-30 | Jiangsu Hengrui Medicine Co., Ltd. | PROCESS FOR PREPARATION OF A HETERARYL PYRIMIDONE DERIVATIVE AND INTERMEDIATE OF A HETERARYL PYRIMIDONE DERIVATIVE |
| CN109970662B (zh) * | 2017-12-27 | 2023-06-30 | 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 |
| TW202302592A (zh) * | 2021-04-02 | 2023-01-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | GnRH受體拮抗劑的結晶形式及其製備方法 |
| CN115260211B (zh) * | 2021-04-29 | 2024-02-06 | 长春金赛药业有限责任公司 | 含噻吩稠环类衍生物、药物组合物及其制备方法和应用 |
| CN117769424A (zh) * | 2021-08-30 | 2024-03-26 | 江苏恒瑞医药股份有限公司 | 一种GnRH受体拮抗剂的结晶工艺 |
| CN115141809B (zh) * | 2022-08-30 | 2023-05-02 | 南京诺唯赞生物科技股份有限公司 | 一种检测gnrh结合蛋白生物学活性的方法及试剂盒 |
| JP2024120882A (ja) * | 2023-02-24 | 2024-09-05 | 日本たばこ産業株式会社 | 置換ピラゾロピリミジン化合物及びその医薬用途 |
| WO2024177126A1 (ja) * | 2023-02-24 | 2024-08-29 | 日本たばこ産業株式会社 | ６－アルコキシピラゾロピリミジン化合物及びその医薬用途 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5171835A (en) | 1988-10-21 | 1992-12-15 | The Administrators Of The Tulane Educational Fund | LHRH antagonists |
| US20020065309A1 (en) | 1999-08-04 | 2002-05-30 | Ge Peng | Novel Bicyclic and tricyclic pyrrolidine derivatives as GnRH antagonists |
| JP5072166B2 (ja) * | 2002-01-30 | 2012-11-14 | 武田薬品工業株式会社 | チエノピリミジン化合物、その製造法および用途 |
| EP1479684A4 (en) * | 2002-01-30 | 2006-01-04 | Takeda Pharmaceutical | THIENOPYRIMIDINES, PROCESS FOR THEIR PRODUCTION AND THEIR USE |
| WO2004014916A1 (en) * | 2002-08-13 | 2004-02-19 | Warner-Lambert Company Llc | Pyrimidine fused bicyclic metalloproteinase inhibitors |
| JP4039574B2 (ja) * | 2003-01-29 | 2008-01-30 | 武田薬品工業株式会社 | チエノピリミジン化合物およびその用途 |
| US7714017B2 (en) * | 2004-10-12 | 2010-05-11 | Decode Genetics, Ehf | Carboxylic acid peri-substituted bicyclics for occlusive artery disease |
| EP1841448A2 (en) * | 2004-12-30 | 2007-10-10 | Diakine Therapeutics, Inc. | Pharmaceutical compositions and methods for restoring beta-cell mass and function |
| WO2006083005A1 (ja) * | 2005-02-03 | 2006-08-10 | Takeda Pharmaceutical Company Limited | 縮合ピリミジン誘導体およびその用途 |
| WO2006096785A1 (en) | 2005-03-07 | 2006-09-14 | Wyeth | Quinoxaline dihydrohalide dihydrates and synthetic methods therefor |
| CN101468988A (zh) * | 2007-12-26 | 2009-07-01 | 上海恒瑞医药有限公司 | 哌嗪类衍生物,其制备方法及其在医药上的应用 |
| EP2329823A4 (en) | 2008-09-03 | 2013-04-03 | Takeda Pharmaceutical | METHOD FOR IMPROVING CAPACITY OF PREPARATION TO BE ABSORBED AND PREPARATION WHICH CAPACITY TO BE ABSORBED IS IMPROVED |
| MX2011009824A (es) * | 2009-03-23 | 2012-01-25 | Glenmark Pharmaceuticals Sa | Derivados de pirimidina-diona fusionados como moduladores del trpa1. |
| TW201130854A (en) | 2009-12-22 | 2011-09-16 | Bayer Schering Pharma Ag | Pyridinone derivatives and pharmaceutical compositions thereof |
| WO2011090935A1 (en) | 2010-01-19 | 2011-07-28 | Merck Sharp & Dohme Corp. | PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS |
| CN102807568B (zh) | 2011-05-31 | 2015-11-25 | 正大天晴药业集团股份有限公司 | 噻二唑衍生物类dpp-iv抑制剂 |
| WO2012175514A1 (en) | 2011-06-21 | 2012-12-27 | Bayer Intellectual Property Gmbh | Pyridinone derivatives and pharmaceutical compositions thereof |
| PL3628320T3 (pl) * | 2011-11-11 | 2022-07-25 | Gilead Apollo, Llc | Inhibitory acc i ich zastosowania |
| MX357841B (es) * | 2012-02-28 | 2018-07-26 | Tiumbio Co Ltd | Antagonistas de los receptores de la hormona liberadora de gonadotropina, método para la preparación de éstos y composición farmacéutica que los contienen. |
| CN102807569B (zh) * | 2012-08-21 | 2015-02-25 | 四川大学 | 一种镇静催眠的化合物及其制备方法和用途 |
| BR112016008799B1 (pt) * | 2013-10-30 | 2023-02-23 | Shanghai Hengrui Pharmaceutical Co., Ltd. | Derivados de pirazolopirimidona ou pirrolotriazona, seus intermediários, seus usos, seus processos de preparação, e composição farmacêutica |
-
2014
- 2014-09-30 BR BR112016008799-2A patent/BR112016008799B1/pt active IP Right Grant
- 2014-09-30 ES ES14858090T patent/ES2747839T3/es active Active
- 2014-09-30 JP JP2016522010A patent/JP6412563B2/ja active Active
- 2014-09-30 EP EP14858090.5A patent/EP3064498B1/en active Active
- 2014-09-30 AU AU2014344504A patent/AU2014344504C1/en active Active
- 2014-09-30 PT PT148580905T patent/PT3064498T/pt unknown
- 2014-09-30 CA CA2927641A patent/CA2927641C/en active Active
- 2014-09-30 US US15/031,410 patent/US10005781B2/en active Active
- 2014-09-30 HU HUE14858090A patent/HUE046314T2/hu unknown
- 2014-09-30 WO PCT/CN2014/087906 patent/WO2015062391A1/zh active Application Filing
- 2014-09-30 CN CN201480003662.2A patent/CN104884457B/zh active Active
- 2014-09-30 RU RU2016119135A patent/RU2674977C2/ru active
- 2014-09-30 RS RSP20191238 patent/RS59457B1/sr unknown
- 2014-09-30 DK DK14858090.5T patent/DK3064498T3/da active
- 2014-09-30 SI SI201431353T patent/SI3064498T1/sl unknown
- 2014-09-30 LT LTEP14858090.5T patent/LT3064498T/lt unknown
- 2014-09-30 PL PL14858090T patent/PL3064498T3/pl unknown
- 2014-09-30 MX MX2016005142A patent/MX2016005142A/es unknown
- 2014-10-20 TW TW103136105A patent/TWI675838B/zh active
-
2018
- 2018-05-02 US US15/969,098 patent/US10344034B2/en active Active
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2019
- 2019-05-20 US US16/416,418 patent/US10633388B2/en active Active
- 2019-09-17 HR HRP20191679 patent/HRP20191679T1/hr unknown
- 2019-09-18 CY CY20191100975T patent/CY1122196T1/el unknown
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