BRPI0519597A2 - derivados de (3r, 6r)-3-(2, 3-diidro-1h-inden-2-il)-2, 5-piperazinadiona 1, 6-substituÍda como antagonistas de receptores de oxitocina para o tratamento de parto prematuro, dismenorrÉia e endometriose - Google Patents

derivados de (3r, 6r)-3-(2, 3-diidro-1h-inden-2-il)-2, 5-piperazinadiona 1, 6-substituÍda como antagonistas de receptores de oxitocina para o tratamento de parto prematuro, dismenorrÉia e endometriose

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Publication number
BRPI0519597A2
BRPI0519597A2 BRPI0519597-7A BRPI0519597A BRPI0519597A2 BR PI0519597 A2 BRPI0519597 A2 BR PI0519597A2 BR PI0519597 A BRPI0519597 A BR PI0519597A BR PI0519597 A2 BRPI0519597 A2 BR PI0519597A2
Authority
BR
Brazil
Prior art keywords
inden
dysmenorrhea
receptor antagonists
treatment
piperazinedione
Prior art date
Application number
BRPI0519597-7A
Other languages
English (en)
Inventor
Colin Andrew Leach
John Liddle
Simon Peace
Joanne Philp
Ian Edward David Smith
Lamont Roscoe Terrell
Jing Zhang
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of BRPI0519597A2 publication Critical patent/BRPI0519597A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61P15/06—Antiabortive agents; Labour repressants
    • 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
    • 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
    • A61P5/06—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

DERIVADOS DE (3R,6R)-3-(2,3-DIIDRO-1H-INDEN-2- IL)-2,5-PIPERAZINADIONA 1,6-SUBSTITUIDA COMO ANTAGONISTAS DE RECEPTORES DE OXITOCINA PARA O TRATAMENTO DE PARTO PRE-MATURO, DISMENORRÉIA E ENDOMETRIOSE. A presente invenção está relacionada com compostos de fórmula (I)
BRPI0519597-7A 2004-12-23 2005-12-22 derivados de (3r, 6r)-3-(2, 3-diidro-1h-inden-2-il)-2, 5-piperazinadiona 1, 6-substituÍda como antagonistas de receptores de oxitocina para o tratamento de parto prematuro, dismenorrÉia e endometriose BRPI0519597A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0428235.6A GB0428235D0 (en) 2004-12-23 2004-12-23 Novel compounds
PCT/GB2005/005007 WO2006067462A1 (en) 2004-12-23 2005-12-22 1,6 - substituted (3r,6r) -3- (2,3-dihydro-1h-inden-2-yl)-2,5-piperazinedione derivatives as oxytocin receptor antagonists for the treatment of pre-term labour, dysmenorrhea and endometriosis

Publications (1)

Publication Number Publication Date
BRPI0519597A2 true BRPI0519597A2 (pt) 2009-02-25

Family

ID=34113169

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0519597-7A BRPI0519597A2 (pt) 2004-12-23 2005-12-22 derivados de (3r, 6r)-3-(2, 3-diidro-1h-inden-2-il)-2, 5-piperazinadiona 1, 6-substituÍda como antagonistas de receptores de oxitocina para o tratamento de parto prematuro, dismenorrÉia e endometriose

Country Status (16)

Country Link
US (1) US20080242666A1 (pt)
EP (1) EP1831183A1 (pt)
JP (1) JP2008525408A (pt)
KR (1) KR20070090210A (pt)
CN (1) CN101128439A (pt)
AU (1) AU2005317886A1 (pt)
BR (1) BRPI0519597A2 (pt)
CA (1) CA2591827A1 (pt)
GB (1) GB0428235D0 (pt)
IL (1) IL183761A0 (pt)
MA (1) MA29091B1 (pt)
MX (1) MX2007007831A (pt)
NO (1) NO20073366L (pt)
RU (1) RU2007127834A (pt)
WO (1) WO2006067462A1 (pt)
ZA (1) ZA200703941B (pt)

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GB0130677D0 (en) 2001-12-21 2002-02-06 Glaxo Group Ltd Medicaments and novel compounds
GB0314738D0 (en) 2003-06-24 2003-07-30 Glaxo Group Ltd Novel compounds
GB0414093D0 (en) 2004-06-23 2004-07-28 Glaxo Group Ltd Novel compounds
JP5544296B2 (ja) 2007-11-16 2014-07-09 ライジェル ファーマシューティカルズ， インコーポレイテッド 代謝障害のためのカルボキサミド、スルホンアミド、およびアミン化合物
ES2553340T3 (es) 2007-12-12 2015-12-07 Rigel Pharmaceuticals, Inc. Compuestos de carboxamida, sulfonamida y amina para trastornos metabólicos
JP5658138B2 (ja) 2008-04-23 2015-01-21 ライジェル ファーマシューティカルズ， インコーポレイテッド 代謝障害の処置のためのカルボキサミド化合物
JP5702293B2 (ja) 2008-11-10 2015-04-15 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な化合物
BRPI0924084B1 (pt) 2008-12-19 2021-12-21 Vertex Pharmaceuticals Incorporated Derivados de pirazina e composição farmacêutica que os compreende
US8716286B2 (en) 2009-10-30 2014-05-06 Glaxo Group Limited Crystalline forms of (3R, 6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione
WO2011143422A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of atr kinase
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013526538A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
US9062008B2 (en) 2010-05-12 2015-06-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
AU2011253025A1 (en) 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2011163527A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
JP5902172B2 (ja) 2010-09-08 2016-04-13 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 広範囲のインフルエンザ抗ウイルス薬としての新規ピペラジン類似体
WO2012138938A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
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JP2014522818A (ja) 2011-06-22 2014-09-08 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
JP2014517079A (ja) 2011-06-22 2014-07-17 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
SG10201606774UA (en) 2011-09-30 2016-10-28 Vertex Pharma Processes for making compounds useful as inhibitors of atr kinase
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
IN2014CN02501A (pt) 2011-09-30 2015-06-26 Vertex Pharma
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2014003796A (es) 2011-09-30 2015-01-16 Vertex Pharma Compuestos utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
EP2776421A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776422A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US20140044802A1 (en) 2012-04-05 2014-02-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
US20140057920A1 (en) 2012-08-23 2014-02-27 Boehringer Ingelheim International Gmbh Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
SMT202000713T1 (it) 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
CN107074863B (zh) 2014-06-05 2019-12-03 沃泰克斯药物股份有限公司 Atr激酶抑制剂的制备方法及其不同的固体形式
PL3157566T3 (pl) 2014-06-17 2019-10-31 Vertex Pharma Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr
KR102678021B1 (ko) 2015-09-30 2024-06-26 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물
CN107915672A (zh) * 2016-10-09 2018-04-17 浙江九洲药物科技有限公司 一种取代异吲哚啉化合物的制备方法
CN109305969B (zh) * 2017-07-27 2023-03-10 江苏恒瑞医药股份有限公司 哌嗪-2,5-二酮类衍生物、其制备方法及其在医药上的应用
US11505531B2 (en) 2018-08-07 2022-11-22 Uab Research Foundation Piperazine-2,5-diones as TGF-beta inhibitors
CN112745270B (zh) * 2020-12-30 2023-02-24 河北医科大学 新化合物及其制备苯唑草酮中间体的方法

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GB0130677D0 (en) * 2001-12-21 2002-02-06 Glaxo Group Ltd Medicaments and novel compounds
GB0314738D0 (en) * 2003-06-24 2003-07-30 Glaxo Group Ltd Novel compounds

Also Published As

Publication number Publication date
US20080242666A1 (en) 2008-10-02
WO2006067462A1 (en) 2006-06-29
ZA200703941B (en) 2008-12-31
GB0428235D0 (en) 2005-01-26
AU2005317886A1 (en) 2006-06-29
MX2007007831A (es) 2007-07-25
KR20070090210A (ko) 2007-09-05
CN101128439A (zh) 2008-02-20
RU2007127834A (ru) 2009-01-27
NO20073366L (no) 2007-09-21
MA29091B1 (fr) 2007-12-03
IL183761A0 (en) 2007-09-20
JP2008525408A (ja) 2008-07-17
EP1831183A1 (en) 2007-09-12
CA2591827A1 (en) 2006-06-29

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2160 DE 29/05/2012.