RU2004110042A - Тиено[2,3-d] пиримидины с комбинированной агонистической активностью lh и fsh - Google Patents
Тиено[2,3-d] пиримидины с комбинированной агонистической активностью lh и fsh Download PDFInfo
- Publication number
- RU2004110042A RU2004110042A RU2004110042/04A RU2004110042A RU2004110042A RU 2004110042 A RU2004110042 A RU 2004110042A RU 2004110042/04 A RU2004110042/04 A RU 2004110042/04A RU 2004110042 A RU2004110042 A RU 2004110042A RU 2004110042 A RU2004110042 A RU 2004110042A
- Authority
- RU
- Russia
- Prior art keywords
- thieno
- pyrimidine
- acetamido
- methylthio
- carboxamide
- Prior art date
Links
- DDWBRNXDKNIQDY-UHFFFAOYSA-N thieno[2,3-d]pyrimidine Chemical class N1=CN=C2SC=CC2=C1 DDWBRNXDKNIQDY-UHFFFAOYSA-N 0.000 title claims 4
- 230000001270 agonistic effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000035558 fertility Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 208000021267 infertility disease Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- GKPIFULDHDHNBW-UHFFFAOYSA-N thieno[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=CN=C2SC(C(=O)N)=CC2=C1 GKPIFULDHDHNBW-UHFFFAOYSA-N 0.000 claims 1
- 0 CC(C)(C)NC(c([s]c1nc(SC)nc(-c2cccc(NC(CN(*)*)=O)c2)c11)c1N)=O Chemical compound CC(C)(C)NC(c([s]c1nc(SC)nc(-c2cccc(NC(CN(*)*)=O)c2)c11)c1N)=O 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- 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
- A61P5/06—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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (6)
1. Производные тиено[2,3-d]пиримидина общей формулы I
(I)
или их фармацевтически приемлемые соли, где R1 и R2 вместе с атомом азота, к которому они присоединены, образуют кольцо, имеющее от 2 до 6 атомов углерода, необязательно содержащее один или более гетероатомов, выбранных из N, O и/или S.
2. Соединение, выбранное из группы, включающей трет-бутил-5-амино-2-метилтио-4-(3-(2-(азетидин-1-ил)-ацетамидо)-фенил)-тиено[2,3-d]пиримидин-6-карбоксамид; трет-бутил-5-амино-2-метилтио-4-(3-(2-морфолин-4-ил)-ацетамидо)-фенил)-тиено[2,3-d]пиримидин-6-карбоксамид; трет-бутил-5-амино-2-метилтио-4-(3-(2-(тиоморфолин-4-ил)-ацетамидо)-фенил)-тиено[2,3-d]пиримидин-6-карбоксамид; трет-бутил-5-амино-2-метилтио-4-(3-(2-(пиперидин-1-ил)-ацетамидо)-фенил)-тиено[2,3-d]пиримидин-6-карбоксамид; трет-бутил-5-амино-2-метилтио-4-(3-(2-(пирролидин-1-ил)-ацетамидо)-фенил)-тиено[2,3-d]пиримидин-6-карбоксамид или трет-бутил-5-амино-2-метилтио-4-(3-(2-(пиперазин-1-ил)-ацетамидо)-фенил)-тиено[2,3-d]пиримидин-6-карбоксамид.
3. Соединение по пп.1 и 2 для применения в терапии.
4. Фармацевтическая композиция, содержащая производное тиено[2,3-d]пиримидина по пп.1 и 2 или его фармацевтически приемлемую соль или сольват, в смеси с фармацевтически приемлемым вспомогательным веществом.
5. Применение производных тиено[2,3-d]пиримидина по пп.1 и 2 или их фармацевтически приемлемых солей или сольватов для изготовления медикаментов для регулирования фертильности.
6. Способ лечения нарушений фертильности у пациентов, нуждающихся в этом, путем введения эффективного количества соединения по пп.1 и 2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01203327.0 | 2001-09-04 | ||
| EP01203327 | 2001-09-04 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2004110042A true RU2004110042A (ru) | 2005-08-20 |
| RU2298011C2 RU2298011C2 (ru) | 2007-04-27 |
Family
ID=8180876
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004110042/04A RU2298011C2 (ru) | 2001-09-04 | 2002-08-29 | Производные тиено[2,3-d]пиримидина и их применение для лечения нарушений фертильности |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US7317006B2 (ru) |
| EP (1) | EP1427733B1 (ru) |
| JP (1) | JP4262092B2 (ru) |
| KR (1) | KR100900018B1 (ru) |
| CN (1) | CN1246324C (ru) |
| AR (1) | AR036407A1 (ru) |
| AT (1) | ATE345345T1 (ru) |
| AU (1) | AU2002337035B2 (ru) |
| BR (1) | BR0211938A (ru) |
| CA (1) | CA2456901C (ru) |
| CY (1) | CY1106012T1 (ru) |
| DE (1) | DE60216128T2 (ru) |
| DK (1) | DK1427733T3 (ru) |
| ES (1) | ES2275005T3 (ru) |
| HR (1) | HRP20040202A2 (ru) |
| HU (1) | HUP0401444A3 (ru) |
| IL (1) | IL160084A0 (ru) |
| IS (1) | IS2424B (ru) |
| MX (1) | MXPA04002045A (ru) |
| NO (1) | NO20040927L (ru) |
| NZ (1) | NZ531340A (ru) |
| PE (1) | PE20030439A1 (ru) |
| PL (1) | PL368502A1 (ru) |
| PT (1) | PT1427733E (ru) |
| RU (1) | RU2298011C2 (ru) |
| TW (1) | TWI228508B (ru) |
| WO (1) | WO2003020726A1 (ru) |
| ZA (1) | ZA200401455B (ru) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6890923B2 (en) * | 2002-12-16 | 2005-05-10 | Astrazeneca Ab | Compounds |
| GB0315950D0 (en) * | 2003-06-11 | 2003-08-13 | Xention Discovery Ltd | Compounds |
| GB0525164D0 (en) * | 2005-12-09 | 2006-01-18 | Xention Discovery Ltd | Compounds |
| CN100430403C (zh) * | 2006-10-13 | 2008-11-05 | 中国科学院上海有机化学研究所 | 3-芳基-5,6-取代噻吩并嘧啶-4-羰基-2-巯基乙腈、合成方法和用途 |
| US20090118276A1 (en) * | 2007-11-02 | 2009-05-07 | Wyeth | Thienopyrimidines, thienopyridines, and pyrrolopyrimidines as b-raf inhibitors |
| TWI389913B (zh) * | 2008-09-08 | 2013-03-21 | Lg Life Sciences Ltd | 并合雜環化合物 |
| WO2010047674A1 (en) | 2008-10-20 | 2010-04-29 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Low molecular weight thyroid stimulating hormone receptor (tshr) agonists |
| GB0905525D0 (en) | 2009-03-31 | 2009-05-13 | Univ Leiden | Compounds and uses |
| BR112012018108A2 (pt) | 2010-01-22 | 2015-10-20 | Bayer Ip Gmbh | combinações acaricidas e/ou inseticidas de ingredientes ativos |
| CA2789818A1 (en) | 2010-04-08 | 2011-10-13 | The United States Of America, As Represented By The Secretary, Departmen T Of Health And Human Services | Inverse agonists and neutral antagonists for the tsh receptor |
| WO2016029372A1 (en) | 2014-08-27 | 2016-03-03 | The Procter & Gamble Company | Wearable article having elastic belt |
| WO2016029375A1 (en) | 2014-08-27 | 2016-03-03 | The Procter & Gamble Company | Wearable article having elastic belt |
| RU2619091C2 (ru) * | 2015-10-13 | 2017-05-11 | Министерство Промышленности И Торговли Рф | Цилиндрический термоэмиссионный катод |
| EP3439600B1 (en) | 2016-04-08 | 2022-06-22 | The Procter & Gamble Company | Wearable article having artwork |
| AU2023282849A1 (en) * | 2022-06-08 | 2025-01-09 | Icahn School Of Medicine At Mount Sinai | Method of treating obesity with a luteinizing hormone receptor agonist |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2054784T3 (es) | 1987-08-08 | 1994-08-16 | Akzo Nv | Un metodo para la fabricacion de un implante. |
| TW564247B (en) | 1999-04-08 | 2003-12-01 | Akzo Nobel Nv | Bicyclic heteraromatic compound |
-
2002
- 2002-07-22 TW TW091116284A patent/TWI228508B/zh not_active IP Right Cessation
- 2002-08-29 AT AT02772230T patent/ATE345345T1/de not_active IP Right Cessation
- 2002-08-29 DK DK02772230T patent/DK1427733T3/da active
- 2002-08-29 CA CA2456901A patent/CA2456901C/en not_active Expired - Fee Related
- 2002-08-29 DE DE60216128T patent/DE60216128T2/de not_active Expired - Lifetime
- 2002-08-29 JP JP2003524996A patent/JP4262092B2/ja not_active Expired - Fee Related
- 2002-08-29 MX MXPA04002045A patent/MXPA04002045A/es active IP Right Grant
- 2002-08-29 PT PT02772230T patent/PT1427733E/pt unknown
- 2002-08-29 CN CNB028172604A patent/CN1246324C/zh not_active Expired - Fee Related
- 2002-08-29 BR BR0211938-2A patent/BR0211938A/pt not_active IP Right Cessation
- 2002-08-29 AU AU2002337035A patent/AU2002337035B2/en not_active Ceased
- 2002-08-29 EP EP02772230A patent/EP1427733B1/en not_active Expired - Lifetime
- 2002-08-29 WO PCT/EP2002/009647 patent/WO2003020726A1/en not_active Ceased
- 2002-08-29 PL PL02368502A patent/PL368502A1/xx not_active Application Discontinuation
- 2002-08-29 NZ NZ531340A patent/NZ531340A/en unknown
- 2002-08-29 KR KR1020047003095A patent/KR100900018B1/ko not_active Expired - Fee Related
- 2002-08-29 ES ES02772230T patent/ES2275005T3/es not_active Expired - Lifetime
- 2002-08-29 US US10/488,482 patent/US7317006B2/en not_active Expired - Lifetime
- 2002-08-29 RU RU2004110042/04A patent/RU2298011C2/ru not_active IP Right Cessation
- 2002-08-29 HU HU0401444A patent/HUP0401444A3/hu unknown
- 2002-08-29 IL IL16008402A patent/IL160084A0/xx not_active IP Right Cessation
- 2002-08-29 HR HR20040202A patent/HRP20040202A2/hr not_active Application Discontinuation
- 2002-09-02 AR ARP020103309A patent/AR036407A1/es unknown
- 2002-09-03 PE PE2002000840A patent/PE20030439A1/es not_active Application Discontinuation
-
2004
- 2004-01-29 IS IS7130A patent/IS2424B/is unknown
- 2004-02-23 ZA ZA200401455A patent/ZA200401455B/en unknown
- 2004-03-03 NO NO20040927A patent/NO20040927L/no not_active Application Discontinuation
-
2007
- 2007-02-13 CY CY20071100189T patent/CY1106012T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PC4A | Invention patent assignment |
Effective date: 20070621 |
|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20090830 |