ATE548357T1 - Gonadotropin freisetzende hormon rezeptor antagonisten und ihre verwandten verfahren - Google Patents

Gonadotropin freisetzende hormon rezeptor antagonisten und ihre verwandten verfahren

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Publication number
ATE548357T1
ATE548357T1 AT01910362T AT01910362T ATE548357T1 AT E548357 T1 ATE548357 T1 AT E548357T1 AT 01910362 T AT01910362 T AT 01910362T AT 01910362 T AT01910362 T AT 01910362T AT E548357 T1 ATE548357 T1 AT E548357T1
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Austria
Prior art keywords
receptor antagonists
releasing hormone
related methods
hormone receptor
gonadotropin releasing
Prior art date
Application number
AT01910362T
Other languages
English (en)
Inventor
Yun-Fei Zhu
Chen Chen
Fabio Tucci
Zhiqiang Guo
Timothy Gross
Martin Rowbottom
R Struthers
Original Assignee
Neurocrine Biosciences Inc
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Filing date
Publication date
Application filed by Neurocrine Biosciences Inc filed Critical Neurocrine Biosciences Inc
Application granted granted Critical
Publication of ATE548357T1 publication Critical patent/ATE548357T1/de

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    • 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
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    • 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
    • C07D239/60—Three or more oxygen or sulfur atoms
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    • 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
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    • 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
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    • 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
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AT01910362T 2000-01-25 2001-01-25 Gonadotropin freisetzende hormon rezeptor antagonisten und ihre verwandten verfahren ATE548357T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17793300P 2000-01-25 2000-01-25
US23968300P 2000-10-11 2000-10-11
PCT/US2001/002740 WO2001055119A2 (en) 2000-01-25 2001-01-25 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

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ATE548357T1 true ATE548357T1 (de) 2012-03-15

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Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6608197B2 (en) * 2000-01-25 2003-08-19 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
SE0100567D0 (sv) * 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
JP2005504034A (ja) 2001-08-02 2005-02-10 ニューロクライン バイオサイエンシーズ， インコーポレイテッド ゴナドトロピン放出性ホルモンレセプターアンタゴニストとしてのピリジノン誘導体およびピリダジノン誘導体
JP2005505525A (ja) * 2001-08-02 2005-02-24 ニューロクライン バイオサイエンシーズ， インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法
WO2003086464A1 (en) * 2002-04-12 2003-10-23 Takeda Pharmaceutical Company Limited. Preventives/remedies for hotflash
EP1646389B1 (de) * 2003-07-07 2008-09-10 Neurocrine Biosciences, Inc. Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
JP4673847B2 (ja) * 2003-07-07 2011-04-20 ニューロクライン バイオサイエンシーズ，インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法
BRPI0412327A (pt) * 2003-07-07 2006-09-05 Neurocrine Biosciences Inc derivados de pirimidina-2,4-diona como antagonistas de receptor de hormÈnio liberador de gonadotropina
MXPA06001601A (es) 2003-08-13 2006-08-25 Takeda Pharmaceutical Derivados de 4-pirimidona y su uso como inhibidores de dipeptidilpeptidasa.
CN102079743B (zh) * 2004-03-15 2020-08-25 武田药品工业株式会社 二肽基肽酶抑制剂
US20080262005A1 (en) * 2004-05-14 2008-10-23 Neurocrine Biosciences, Inc. Uracil-Type Gonadotropin-Releasing Hormone Receptor Antagonists and Methods Related Thereto
EP1655288A1 (de) * 2004-11-05 2006-05-10 Institut Pasteur Aryl-pyrimidyl-Verbindungen, sie enthaltende pharmazeutische Zusammensetzungen und ihre Verwendung als antimikrobielle Mittel
NZ566799A (en) 2005-09-14 2011-04-29 Takeda Pharmaceutical Dipeptidyl peptidase inhibitors for treating diabetes
WO2007035629A2 (en) 2005-09-16 2007-03-29 Takeda Pharmaceutical Company Limited Process for the preparation of pyrimidinedione derivatives
WO2007122634A2 (en) * 2006-04-24 2007-11-01 Jubilant Biosys Limited Pyrimidinediones as tyrosine kinase inhibitors
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
CL2008000986A1 (es) 2007-04-06 2008-10-17 Neurocrine Biosciences Inc COMPUESTO DERIVADO DE HETEROCICLOS DE NITROGENO, AGONISTAS DEL RECEPTOR GnRH; COMPOSICION FARMACEUTICA QUE COMPRENDE A DICHO COMPUESTO; Y USO PARA TRATAR UNA AFECCION RELACIONADA CON LAS HORMONAS SEXUALES, ENDOMETRIOSIS, DISMENORREA, ENFERMEDAD DE OV
MX2009010828A (es) 2007-04-06 2009-10-29 Neurocrine Biosciences Inc Antagonistas del receptor de la hormona liberadora de gonadotropina y metodos relacionados con los mismos.
JP5352449B2 (ja) * 2007-04-18 2013-11-27 キッセイ薬品工業株式会社 縮合へテロ環誘導体、それを含有する医薬組成物及びその医薬用途
CA2682400A1 (en) * 2007-04-18 2008-11-06 Kissei Pharmaceutical Co., Ltd. Fused heterocyclic derivative, pharmaceutical composition comprising the derivative, and use of the composition for medical purposes
US8765948B2 (en) * 2007-11-07 2014-07-01 Neurocrine Biosciences, Inc. Processes for the preparation of uracil derivatives
DE102008030091B4 (de) * 2008-06-25 2011-03-03 Resprotect Gmbh Uracilderivate und deren Verwendung
WO2010029299A1 (en) * 2008-09-12 2010-03-18 Biolipox Ab Pyrimidinone derivaties for use as medicaments
JP5757956B2 (ja) * 2009-11-20 2015-08-05 エスケー ケミカルス シーオー．， エルティーディー．Ｓｋ Ｃｈｅｍｉｃａｌｓ Ｃｏ．， Ｌｔｄ． ゴナドトロピン放出ホルモン受容体拮抗剤、その製造方法及びそれを含む医薬組成物
TW201130854A (en) 2009-12-22 2011-09-16 Bayer Schering Pharma Ag Pyridinone derivatives and pharmaceutical compositions thereof
WO2012175514A1 (en) 2011-06-21 2012-12-27 Bayer Intellectual Property Gmbh Pyridinone derivatives and pharmaceutical compositions thereof
EP4223298A3 (de) 2013-03-15 2023-08-16 AbbVie Inc. Zusammensetzungen zur verwendung bei der behandlung von schweren menstruationsblutungen
AU2018243749A1 (en) * 2017-03-31 2019-11-21 Epizyme, Inc. Methods of using EHMT2 inhibitors
WO2018195450A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
TW201919632A (zh) 2017-08-18 2019-06-01 美商艾伯維有限公司 治療子宮內膜異位症、子宮纖維瘤、多囊性卵巢症候群或子宮腺肌症之醫藥調配物
SG11202001436YA (en) 2017-08-18 2020-03-30 Abbvie Inc Pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis
TW201912157A (zh) 2017-08-18 2019-04-01 美商艾伯維有限公司 治療子宮內膜異位症、子宮纖維瘤、多囊性卵巢症候群及子宮腺肌症之固體醫藥調配物
US11690854B2 (en) 2018-04-19 2023-07-04 Abbvie Inc. Methods of treating heavy menstrual bleeding
WO2020023459A1 (en) 2018-07-23 2020-01-30 Abbvie Inc. Elagolix sodium compositions and processes
JP2022518019A (ja) 2019-01-15 2022-03-11 ルパン インコーポレイテッド 重水素化エラゴリクス様組成物及び方法
CN111333586A (zh) * 2020-02-19 2020-06-26 诚达药业股份有限公司 一种含有6-甲基尿嘧啶结构化合物的制备方法
CN111333587B (zh) * 2020-04-11 2023-04-07 东莞市东阳光新药研发有限公司 取代的嘧啶-2,4(1h,3h)-二酮衍生物及其用途
CN113527213B (zh) * 2020-04-20 2023-01-03 上海英诺富成生物科技有限公司 促性激素释放激素受体拮抗剂及其用途
LT4122926T (lt) 2021-04-14 2025-07-25 Shionogi & Co., Ltd. Triazino dariniai, turintys virusų replikaciją slopinantį poveikį, ir juos apimanti farmacinė kompozicija

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2631625B1 (fr) * 1988-05-17 1992-10-16 Synthelabo Derives de phenyl-6 piperazinylalkyl-3 1h,3h-pyrimidinedione-2,4, leur preparation et leur application en therapeutique
US5140029A (en) 1989-01-09 1992-08-18 Janssen Pharmaceutica N.V. 2-aminopyrimidinone derivatives
US5476855A (en) * 1993-11-02 1995-12-19 Mahmoud H. el Kouni Enzyme inhibitors, their synthesis and methods for use
UY23948A1 (es) * 1995-02-08 2001-10-25 Takeda Chemical Industries Ltd Derivados de anillos condensados de tiofeno su producción y uso.
EP0828731A1 (de) 1995-06-01 1998-03-18 Takeda Chemical Industries, Ltd. TRICYCLISCHE DIAZEPINE VERWENDBAR ALS GnRH-REZEPTOR ANTAGONISTE
US5859014A (en) * 1995-06-09 1999-01-12 Syntex (U.S.A.) Inc. Pyrimidinedione, pyrimidinetrione, triazinedione and tetrahydroquinazolinedione derivatives as α1 -adrenergic receptor antagonists
ES2157366T3 (es) * 1995-06-09 2001-08-16 Hoffmann La Roche Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos.
AU7333396A (en) 1995-10-19 1997-05-07 Takeda Chemical Industries Ltd. Thienopyridine derivatives as gonadotropin releasing hormone antagonists
CA2229201A1 (en) 1995-10-19 1997-04-24 Satoshi Sasaki Quinoline derivatives, their production and use
WO1997021435A1 (en) 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
PL327146A1 (en) 1995-12-14 1998-11-23 Merck & Co Inc Antagonists of the gonadotrophin liberating hormone
KR19990072124A (ko) 1995-12-14 1999-09-27 애쉬톤 왈레이스 티 고나도트로핀 방출 호르몬의 길항제
US5849764A (en) 1995-12-14 1998-12-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US5780437A (en) 1995-12-14 1998-07-14 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997021707A1 (en) 1995-12-14 1997-06-19 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
JPH09286786A (ja) * 1996-04-18 1997-11-04 Nippon Paper Ind Co Ltd ピリミジン誘導体及びその抗腫瘍剤としての用途
WO1997044321A1 (en) 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
CA2254769A1 (en) 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997044041A1 (en) 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
EP0918522A4 (de) 1996-05-20 1999-08-18 Merck & Co Inc Antagonisten des gonadotropin-releasinghormons
EP0986385A4 (de) 1997-06-05 2001-05-16 Merck & Co Inc Antagonisten des gonadorelins
AU729663B2 (en) 1997-06-05 2001-02-08 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
EP0986550A1 (de) 1997-06-05 2000-03-22 Merck & Co., Inc. Antagonisten des gonadotropin freisetzenden hormons
WO1998055119A1 (en) 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US6313301B1 (en) 1997-08-13 2001-11-06 Takeda Chemical Industries, Ltd. Thienopyridine derivatives, their intermediates and production thereof
US6194419B1 (en) 1997-12-26 2001-02-27 Takeda Chemical Industries, Ltd. Nitrogen-containing heterocyclic compounds, their production and use
EP1067930A4 (de) 1998-04-02 2002-09-18 Merck & Co Inc Antagonisten des gonadoliberins
AU1345600A (en) * 1998-11-12 2000-06-05 Merck & Co., Inc. Pyrimidinedione derivatives useful as alpha 1a adrenoceptor antagonists
EP1185530A1 (de) 1999-05-14 2002-03-13 Neurocrine Biosciences, Inc. Imidazo- und pyrrolo[1,2-a]pyrimid-4-one als antagonisten des rezeptors für das gonadotropin freisetzende hormon
JP2002544263A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 抗凝血剤としての置換多環式アリールおよびヘテロアリールウラシル
ES1043085Y (es) * 1999-06-03 2001-02-01 Nueva Ceramica Arb Sa Teja planoconvexa
MXPA02003614A (es) 1999-10-15 2002-10-23 Neurocrine Biosciences Inc Antagonistas del receptor de la hormona liberadora de ganadotropina y metodos relacionados con los mismos..
US6608197B2 (en) * 2000-01-25 2003-08-19 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
JP4673847B2 (ja) * 2003-07-07 2011-04-20 ニューロクライン バイオサイエンシーズ，インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法
EP1646389B1 (de) * 2003-07-07 2008-09-10 Neurocrine Biosciences, Inc. Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
BRPI0412327A (pt) * 2003-07-07 2006-09-05 Neurocrine Biosciences Inc derivados de pirimidina-2,4-diona como antagonistas de receptor de hormÈnio liberador de gonadotropina

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US20020132820A1 (en) 2002-09-19
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US6872728B2 (en) 2005-03-29
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