MX2016005142A - Derivados de pirazolopirimidona o pirrolotriazona, metodo y preparacion de los mismos y aplicaciones farmaceuticas de los mismos. - Google Patents
Derivados de pirazolopirimidona o pirrolotriazona, metodo y preparacion de los mismos y aplicaciones farmaceuticas de los mismos.Info
- Publication number
- MX2016005142A MX2016005142A MX2016005142A MX2016005142A MX2016005142A MX 2016005142 A MX2016005142 A MX 2016005142A MX 2016005142 A MX2016005142 A MX 2016005142A MX 2016005142 A MX2016005142 A MX 2016005142A MX 2016005142 A MX2016005142 A MX 2016005142A
- Authority
- MX
- Mexico
- Prior art keywords
- same
- preparation
- derivatives
- pharmaceutical applications
- pirrolotriazona
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 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
- DOTPSQVYOBAWPQ-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-3-one Chemical compound N1=CN=C2C(=O)N=NC2=C1 DOTPSQVYOBAWPQ-UHFFFAOYSA-N 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
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
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- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Pregnancy & Childbirth (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (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
La presente invención proporciona derivados de pirazolopirimidona o pirrolotriazona, el método de preparación de los mismos, y las aplicaciones farmacéuticas de los mismos. Específicamente, la presente invención proporciona derivados de pirazolopirimidona o pirrolotriazona representados por una formula general (I) y las sales farmacéuticas de los mismos, el método de preparación de los mismos, y su uso como un antagonista de hormona liberadora de gonadotropina (GnRH) y, especialmente, como agentes terapéuticos para la endometriosis, en donde el definiciones de los sustituyentes en la formula general (I) son los mismos que las definiciones de la especificación.
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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2016005142A true MX2016005142A (es) | 2016-10-28 |
| MX380546B MX380546B (es) | 2025-03-12 |
Family
ID=53003302
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016005142A MX380546B (es) | 2013-10-30 | 2014-09-30 | Derivados de pirazolopirimidona o pirrolotriazona, metodo y preparacion de los mismos y aplicaciones farmaceuticas de los mismos. |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US10005781B2 (es) |
| EP (1) | EP3064498B1 (es) |
| JP (1) | JP6412563B2 (es) |
| CN (1) | CN104884457B (es) |
| AU (1) | AU2014344504C1 (es) |
| BR (1) | BR112016008799B1 (es) |
| CA (1) | CA2927641C (es) |
| CY (1) | CY1122196T1 (es) |
| DK (1) | DK3064498T3 (es) |
| ES (1) | ES2747839T3 (es) |
| HR (1) | HRP20191679T1 (es) |
| HU (1) | HUE046314T2 (es) |
| LT (1) | LT3064498T (es) |
| MX (1) | MX380546B (es) |
| PL (1) | PL3064498T3 (es) |
| PT (1) | PT3064498T (es) |
| RS (1) | RS59457B1 (es) |
| RU (1) | RU2674977C2 (es) |
| SI (1) | SI3064498T1 (es) |
| SM (1) | SMT201900573T1 (es) |
| TW (1) | TWI675838B (es) |
| WO (1) | WO2015062391A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2674977C2 (ru) * | 2013-10-30 | 2018-12-14 | Шанхай Хэнжуй Фармасьютикал Ко., Лтд. | Производные пиразолопиримидона или пирролотриазона, способ их получения и их фармацевтические применения |
| CN108778280B (zh) * | 2016-11-07 | 2021-07-27 | 江苏恒瑞医药股份有限公司 | 一种GnRH受体拮抗剂的多晶型及其制备方法 |
| JP2019535712A (ja) * | 2016-11-14 | 2019-12-12 | ジエンス ヘンルイ メデイシンカンパニー リミテッドＪｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．，Ｌｔｄ． | ＧｎＲＨ受容体アンタゴニストの結晶体およびその製造方法 |
| AU2018305633B2 (en) * | 2017-07-28 | 2022-11-24 | Jiangsu Hengrui Medicine Co., Ltd. | Method for preparing pyrimidone heteroaryl derivative and intermediate of pyrimidone heteroaryl 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 |
| TW202315622A (zh) * | 2021-08-30 | 2023-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種GnRH受體拮抗劑的結晶工藝 |
| 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 |
| JP7737490B2 (ja) * | 2023-02-24 | 2025-09-10 | 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 |
| US7569570B2 (en) * | 2002-01-30 | 2009-08-04 | Takeda Pharmaceutical Company Limited | Thienopyrimidines, process for preparing the same and use thereof |
| AU2003253165A1 (en) * | 2002-08-13 | 2004-02-25 | 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 |
| CN101076531A (zh) * | 2004-10-12 | 2007-11-21 | 解码遗传学公司 | 用于阻塞性血管疾病的羧酸迫位取代的双环化合物 |
| US7393827B2 (en) * | 2004-12-30 | 2008-07-01 | Diakine Therapeutics, Inc. | Pharmaceutical compositions and methods for restoring β-cell mass and function |
| EP1847541A4 (en) * | 2005-02-03 | 2009-12-30 | Takeda Pharmaceutical | CONDENSED PYRIMIDINE DERIVATIVE AND USE THEREOF |
| US20060211699A1 (en) | 2005-03-07 | 2006-09-21 | 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 |
| JPWO2010026993A1 (ja) | 2008-09-03 | 2012-02-02 | 武田薬品工業株式会社 | 製剤における吸収性改善方法および吸収性が改善された製剤 |
| BRPI1013559A2 (pt) * | 2009-03-23 | 2016-04-12 | Glenmark Pharmaceuticals Sa | compostos, composição farmacêutica, método de tratamento de doença ou condição associada à função trpa1 e respectivos usos |
| TW201130854A (en) | 2009-12-22 | 2011-09-16 | Bayer Schering Pharma Ag | Pyridinone derivatives and pharmaceutical compositions thereof |
| US9227971B2 (en) | 2010-01-19 | 2016-01-05 | 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 |
| EP3628320B1 (en) * | 2011-11-11 | 2022-03-16 | Gilead Apollo, LLC | Acc inhibitors and uses thereof |
| 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 |
| RU2674977C2 (ru) * | 2013-10-30 | 2018-12-14 | Шанхай Хэнжуй Фармасьютикал Ко., Лтд. | Производные пиразолопиримидона или пирролотриазона, способ их получения и их фармацевтические применения |
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2014
- 2014-09-30 RU RU2016119135A patent/RU2674977C2/ru active
- 2014-09-30 RS RSP20191238 patent/RS59457B1/sr unknown
- 2014-09-30 EP EP14858090.5A patent/EP3064498B1/en active Active
- 2014-09-30 PT PT148580905T patent/PT3064498T/pt unknown
- 2014-09-30 WO PCT/CN2014/087906 patent/WO2015062391A1/zh not_active Ceased
- 2014-09-30 DK DK14858090.5T patent/DK3064498T3/da active
- 2014-09-30 LT LTEP14858090.5T patent/LT3064498T/lt unknown
- 2014-09-30 CN CN201480003662.2A patent/CN104884457B/zh active Active
- 2014-09-30 SI SI201431353T patent/SI3064498T1/sl unknown
- 2014-09-30 MX MX2016005142A patent/MX380546B/es unknown
- 2014-09-30 BR BR112016008799-2A patent/BR112016008799B1/pt active IP Right Grant
- 2014-09-30 SM SM20190573T patent/SMT201900573T1/it unknown
- 2014-09-30 HU HUE14858090A patent/HUE046314T2/hu unknown
- 2014-09-30 CA CA2927641A patent/CA2927641C/en active Active
- 2014-09-30 JP JP2016522010A patent/JP6412563B2/ja active Active
- 2014-09-30 ES ES14858090T patent/ES2747839T3/es active Active
- 2014-09-30 AU AU2014344504A patent/AU2014344504C1/en active Active
- 2014-09-30 PL PL14858090T patent/PL3064498T3/pl unknown
- 2014-09-30 US US15/031,410 patent/US10005781B2/en active Active
- 2014-09-30 HR HRP20191679 patent/HRP20191679T1/hr unknown
- 2014-10-20 TW TW103136105A patent/TWI675838B/zh active
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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
- 2019-09-18 CY CY20191100975T patent/CY1122196T1/el unknown
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