HRP20040202A2 - Tieno[2,3-d]pyrimidines with combined lh and fsh agonistic activity - Google Patents
Tieno[2,3-d]pyrimidines with combined lh and fsh agonistic activity Download PDFInfo
- Publication number
- HRP20040202A2 HRP20040202A2 HR20040202A HRP20040202A HRP20040202A2 HR P20040202 A2 HRP20040202 A2 HR P20040202A2 HR 20040202 A HR20040202 A HR 20040202A HR P20040202 A HRP20040202 A HR P20040202A HR P20040202 A2 HRP20040202 A2 HR P20040202A2
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- Croatia
- Prior art keywords
- pyrimidine
- thieno
- methylthio
- amino
- tert
- Prior art date
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- 150000001447 alkali salts Chemical class 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 150000001448 anilines Chemical class 0.000 description 1
- 230000002513 anti-ovulatory effect Effects 0.000 description 1
- HGQULGDOROIPJN-UHFFFAOYSA-N azetidin-1-ium;chloride Chemical compound Cl.C1CNC1 HGQULGDOROIPJN-UHFFFAOYSA-N 0.000 description 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 238000011953 bioanalysis Methods 0.000 description 1
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- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 230000001593 cAMP accumulation Effects 0.000 description 1
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- 150000001805 chlorine compounds Chemical class 0.000 description 1
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- 239000003086 colorant Substances 0.000 description 1
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- 239000003085 diluting agent Substances 0.000 description 1
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- 229940000406 drug candidate Drugs 0.000 description 1
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- 229940079360 enema for constipation Drugs 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- PVBRSNZAOAJRKO-UHFFFAOYSA-N ethyl 2-sulfanylacetate Chemical compound CCOC(=O)CS PVBRSNZAOAJRKO-UHFFFAOYSA-N 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- UAYKGOMDUQLCJS-UHFFFAOYSA-N ethylsulfanyl acetate Chemical compound CCSOC(C)=O UAYKGOMDUQLCJS-UHFFFAOYSA-N 0.000 description 1
- 230000004720 fertilization Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 230000008217 follicular development Effects 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
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- 239000008187 granular material Substances 0.000 description 1
- 239000005090 green fluorescent protein Substances 0.000 description 1
- 150000004820 halides Chemical class 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 239000000960 hypophysis hormone Substances 0.000 description 1
- FDGQSTZJBFJUBT-UHFFFAOYSA-N hypoxanthine Chemical class O=C1NC=NC2=C1NC=N2 FDGQSTZJBFJUBT-UHFFFAOYSA-N 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 238000002513 implantation Methods 0.000 description 1
- 238000000099 in vitro assay Methods 0.000 description 1
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- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 238000004020 luminiscence type Methods 0.000 description 1
- 230000029849 luteinization Effects 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 210000001161 mammalian embryo Anatomy 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 238000013160 medical therapy Methods 0.000 description 1
- 230000021121 meiosis Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 102000006240 membrane receptors Human genes 0.000 description 1
- 108020004084 membrane receptors Proteins 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- SDDKIZNHOCEXTF-UHFFFAOYSA-N methyl carbamimidothioate Chemical compound CSC(N)=N SDDKIZNHOCEXTF-UHFFFAOYSA-N 0.000 description 1
- NNBBQNFHCVVQHZ-UHFFFAOYSA-N methyl carbamimidothioate;sulfuric acid Chemical compound CSC(N)=N.OS(O)(=O)=O NNBBQNFHCVVQHZ-UHFFFAOYSA-N 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000003595 mist Substances 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 238000010369 molecular cloning Methods 0.000 description 1
- 239000006199 nebulizer Substances 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 238000010534 nucleophilic substitution reaction Methods 0.000 description 1
- 210000000287 oocyte Anatomy 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 210000002394 ovarian follicle Anatomy 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 230000027758 ovulation cycle Effects 0.000 description 1
- 210000004681 ovum Anatomy 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- RLOWWWKZYUNIDI-UHFFFAOYSA-N phosphinic chloride Chemical compound ClP=O RLOWWWKZYUNIDI-UHFFFAOYSA-N 0.000 description 1
- UHZYTMXLRWXGPK-UHFFFAOYSA-N phosphorus pentachloride Chemical compound ClP(Cl)(Cl)(Cl)Cl UHZYTMXLRWXGPK-UHFFFAOYSA-N 0.000 description 1
- 239000002281 placental hormone Substances 0.000 description 1
- 229920001184 polypeptide Polymers 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 230000035484 reaction time Effects 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000027272 reproductive process Effects 0.000 description 1
- 238000006798 ring closing metathesis reaction Methods 0.000 description 1
- 239000008237 rinsing water Substances 0.000 description 1
- 238000007127 saponification reaction Methods 0.000 description 1
- 238000002741 site-directed mutagenesis Methods 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 150000003432 sterols Chemical class 0.000 description 1
- 235000003702 sterols Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
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- 239000000126 substance Substances 0.000 description 1
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- 239000000829 suppository Substances 0.000 description 1
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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)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Reproductive Health (AREA)
- Diabetes (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01203327 | 2001-09-04 | ||
| PCT/EP2002/009647 WO2003020726A1 (en) | 2001-09-04 | 2002-08-29 | Thieno[2,3-d]pyrimidines with combined lh and fsh agonistic activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20040202A2 true HRP20040202A2 (en) | 2004-08-31 |
Family
ID=8180876
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20040202A HRP20040202A2 (en) | 2001-09-04 | 2004-03-01 | Tieno[2,3-d]pyrimidines with combined lh and fsh agonistic activity |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US7317006B2 (hu) |
| EP (1) | EP1427733B1 (hu) |
| JP (1) | JP4262092B2 (hu) |
| KR (1) | KR100900018B1 (hu) |
| CN (1) | CN1246324C (hu) |
| AR (1) | AR036407A1 (hu) |
| AT (1) | ATE345345T1 (hu) |
| AU (1) | AU2002337035B2 (hu) |
| BR (1) | BR0211938A (hu) |
| CA (1) | CA2456901C (hu) |
| CY (1) | CY1106012T1 (hu) |
| DE (1) | DE60216128T2 (hu) |
| DK (1) | DK1427733T3 (hu) |
| ES (1) | ES2275005T3 (hu) |
| HR (1) | HRP20040202A2 (hu) |
| HU (1) | HUP0401444A3 (hu) |
| IL (1) | IL160084A0 (hu) |
| IS (1) | IS2424B (hu) |
| MX (1) | MXPA04002045A (hu) |
| NO (1) | NO20040927L (hu) |
| NZ (1) | NZ531340A (hu) |
| PE (1) | PE20030439A1 (hu) |
| PL (1) | PL368502A1 (hu) |
| PT (1) | PT1427733E (hu) |
| RU (1) | RU2298011C2 (hu) |
| TW (1) | TWI228508B (hu) |
| WO (1) | WO2003020726A1 (hu) |
| ZA (1) | ZA200401455B (hu) |
Families Citing this family (12)
| 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 |
| CA2741030A1 (en) | 2008-10-20 | 2010-04-29 | Marvin C. Gershengorn | 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 |
| JP5965387B2 (ja) | 2010-04-08 | 2016-08-03 | アメリカ合衆国 | Ｔｓｈ受容体用のインバースアゴニストおよびニュートラルアンタゴニスト |
| RU2619091C2 (ru) * | 2015-10-13 | 2017-05-11 | Министерство Промышленности И Торговли Рф | Цилиндрический термоэмиссионный катод |
| WO2023239854A2 (en) * | 2022-06-08 | 2023-12-14 | 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 DE DE60216128T patent/DE60216128T2/de not_active Expired - Lifetime
- 2002-08-29 DK DK02772230T patent/DK1427733T3/da active
- 2002-08-29 HU HU0401444A patent/HUP0401444A3/hu unknown
- 2002-08-29 NZ NZ531340A patent/NZ531340A/en unknown
- 2002-08-29 IL IL16008402A patent/IL160084A0/xx 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 RU RU2004110042/04A patent/RU2298011C2/ru not_active IP Right Cessation
- 2002-08-29 BR BR0211938-2A patent/BR0211938A/pt not_active IP Right Cessation
- 2002-08-29 US US10/488,482 patent/US7317006B2/en not_active Expired - Lifetime
- 2002-08-29 PT PT02772230T patent/PT1427733E/pt unknown
- 2002-08-29 MX MXPA04002045A patent/MXPA04002045A/es active IP Right Grant
- 2002-08-29 PL PL02368502A patent/PL368502A1/xx not_active Application Discontinuation
- 2002-08-29 AT AT02772230T patent/ATE345345T1/de not_active IP Right Cessation
- 2002-08-29 JP JP2003524996A patent/JP4262092B2/ja not_active Expired - Fee Related
- 2002-08-29 ES ES02772230T patent/ES2275005T3/es not_active Expired - Lifetime
- 2002-08-29 WO PCT/EP2002/009647 patent/WO2003020726A1/en active IP Right Grant
- 2002-08-29 CA CA2456901A patent/CA2456901C/en not_active Expired - Fee Related
- 2002-08-29 CN CNB028172604A patent/CN1246324C/zh not_active Expired - Fee Related
- 2002-08-29 KR KR1020047003095A patent/KR100900018B1/ko not_active IP Right Cessation
- 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
- 2004-03-01 HR HR20040202A patent/HRP20040202A2/hr not_active Application Discontinuation
- 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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