JP6410819B2 - 置換オキソピリジン誘導体および第XIa因子/血漿としてのその使用 - Google Patents

置換オキソピリジン誘導体および第XIa因子/血漿としてのその使用 Download PDF

Info

Publication number
JP6410819B2
JP6410819B2 JP2016528481A JP2016528481A JP6410819B2 JP 6410819 B2 JP6410819 B2 JP 6410819B2 JP 2016528481 A JP2016528481 A JP 2016528481A JP 2016528481 A JP2016528481 A JP 2016528481A JP 6410819 B2 JP6410819 B2 JP 6410819B2
Authority
JP
Japan
Prior art keywords
formula
mmol
methyl
compound
represents hydrogen
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2016528481A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016525136A (ja
JP2016525136A5 (OSRAM
Inventor
レーリヒ,ズザンネ
ヒリツシユ,アレクサンダー
シユトラスブルガー,ユリア
ハイトマイアー,シユテフアン
シユミツト,マルテイナ・ヴイクトーリア
シユレマー,カール−ハインツ
ブーフミユラー,アンニヤ
ゲルデス,クリストフ
テラー,ヘンリツク
シエーフアー,マルテイナ
テルシユテーゲン,アードリアン
Original Assignee
バイエル ファーマ アクチエンゲゼルシャフト
バイエル ファーマ アクチエンゲゼルシャフト
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 バイエル ファーマ アクチエンゲゼルシャフト, バイエル ファーマ アクチエンゲゼルシャフト filed Critical バイエル ファーマ アクチエンゲゼルシャフト
Publication of JP2016525136A publication Critical patent/JP2016525136A/ja
Publication of JP2016525136A5 publication Critical patent/JP2016525136A5/ja
Application granted granted Critical
Publication of JP6410819B2 publication Critical patent/JP6410819B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Quinoline Compounds (AREA)
JP2016528481A 2013-07-23 2014-07-21 置換オキソピリジン誘導体および第XIa因子/血漿としてのその使用 Expired - Fee Related JP6410819B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13177605.6 2013-07-23
EP13177605 2013-07-23
PCT/EP2014/065608 WO2015011087A1 (de) 2013-07-23 2014-07-21 Substituierte oxopyridin-derivate und ihre verwendung als faktor xia / plasma

Publications (3)

Publication Number Publication Date
JP2016525136A JP2016525136A (ja) 2016-08-22
JP2016525136A5 JP2016525136A5 (OSRAM) 2017-08-17
JP6410819B2 true JP6410819B2 (ja) 2018-10-24

Family

ID=48803476

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016528481A Expired - Fee Related JP6410819B2 (ja) 2013-07-23 2014-07-21 置換オキソピリジン誘導体および第XIa因子/血漿としてのその使用

Country Status (7)

Country Link
US (2) US9475809B2 (OSRAM)
EP (1) EP3024822B1 (OSRAM)
JP (1) JP6410819B2 (OSRAM)
CN (1) CN105555767B (OSRAM)
CA (1) CA2918814C (OSRAM)
ES (1) ES2633248T3 (OSRAM)
WO (1) WO2015011087A1 (OSRAM)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2978751B1 (en) 2013-03-25 2018-12-05 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
US9475809B2 (en) * 2013-07-23 2016-10-25 Bayer Pharma Aktiengesellschaft Substituted oxopyridine derivatives and use thereof as factor xia/plasma
NO2760821T3 (OSRAM) 2014-01-31 2018-03-10
KR20240017118A (ko) 2014-01-31 2024-02-06 브리스톨-마이어스 스큅 컴퍼니 인자 XIa 억제제로서의 헤테로시클릭 P2' 기를 갖는 마크로사이클
EP3189047B1 (en) 2014-09-04 2018-12-26 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
EP3197896B1 (de) 2014-09-24 2019-01-30 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
US10414731B2 (en) 2014-09-24 2019-09-17 Bayer Pharma Aktiengesellschaft Substituted oxopyridine derivatives
WO2016046157A1 (de) 2014-09-24 2016-03-31 Bayer Pharma Aktiengesellschaft Faktor xia hemmende pyridobenzazepin- und pyridobenzazocin-derivate
ES2722425T3 (es) 2014-09-24 2019-08-12 Bayer Pharma AG (2H)-2-Oxopiridinas como inhibidores del factor XIa para el tratamiento de enfermedades trombóticas
WO2016046156A1 (de) 2014-09-24 2016-03-31 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
JO3703B1 (ar) 2015-07-09 2021-01-31 Bayer Pharma AG مشتقات أوكسوبيريدين مستبدلة
EP3344618A1 (de) 2015-09-04 2018-07-11 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
EP3371162B1 (en) 2015-10-29 2022-01-26 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
EP3500556B1 (en) 2016-08-22 2023-08-02 Merck Sharp & Dohme LLC Pyridine-1-oxide derivatives and their use as factor xia inhibitors
CN106831761B (zh) * 2016-12-14 2019-02-12 浙江工业大学 顺式四氢-1H-吡咯并[3,4-b]吡啶-2,5(3H,6H)-二酮的合成方法
MX2020010635A (es) 2018-04-10 2020-10-28 Bayer Pharma AG Un derivado de oxopiridina sustituido.
KR20210106504A (ko) 2018-12-21 2021-08-30 바이엘 악티엔게젤샤프트 치환된 옥소피리딘 유도체
US20220144848A1 (en) 2018-12-21 2022-05-12 Bayer Aktiengesellschaft Substituted oxopyridine derivatives
CN110105276A (zh) * 2019-06-24 2019-08-09 红河学院 一种2-喹啉酮化合物及其制备方法
CN112778273B (zh) * 2019-11-11 2022-08-23 江西济民可信集团有限公司 环酮并吡啶酮类化合物及其制备方法和用途
CN112778277B (zh) * 2019-11-11 2024-04-02 江西济民可信集团有限公司 环酮并吡啶酮联杂芳环化合物及其制备方法和用途
CN113135930B (zh) * 2020-01-17 2023-11-17 上海济煜医药科技有限公司 呋喃并吡啶酮咪唑化合物及其制备方法和用途
CN113135929B (zh) * 2020-01-17 2024-04-19 江西济民可信集团有限公司 呋喃并吡啶酮酰胺化合物及其制备方法和用途
US11845748B2 (en) 2021-03-18 2023-12-19 Janssen Pharmaceutica Nv Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11919881B2 (en) 2021-03-18 2024-03-05 Janssen Pharmaceutica Nv Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11814364B2 (en) 2021-03-18 2023-11-14 Janssen Pharmaceutica Nv Pyridine N-oxide derivatives useful as factor XIa inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0407342A3 (en) * 1989-07-06 1991-07-10 Ciba-Geigy Ag Pyrimidine derivatives
CN101891680B (zh) * 2004-06-24 2014-10-29 沃泰克斯药物股份有限公司 Atp-结合弹夹转运蛋白的调控剂
GB0420722D0 (en) * 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
JP5236293B2 (ja) * 2005-01-13 2013-07-17 ブリストル−マイヤーズ スクイブ カンパニー Xia因子阻害剤としての置換ビアリール化合物
ES2365815T3 (es) * 2005-12-14 2011-10-11 Bristol-Myers Squibb Company Análogos de arilpropionamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor xia.
EP2102189B1 (en) * 2006-12-15 2015-07-29 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
JP5419706B2 (ja) 2006-12-20 2014-02-19 タケダ カリフォルニア インコーポレイテッド グルコキナーゼアクチベーター
WO2009076337A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
US8268820B2 (en) * 2009-03-26 2012-09-18 Hoffmann-La Roche Inc. 2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds
CA2813911A1 (en) * 2010-10-07 2012-04-12 Takeda Pharmaceutical Company Limited 1,4-oxazepane derivatives
DK2794597T3 (en) * 2011-12-21 2018-01-15 Ono Pharmaceutical Co PYRIDINON AND PYRIMIDINON DERIVATIVES AS FACTOR XIA INHIBITORS
US9475809B2 (en) * 2013-07-23 2016-10-25 Bayer Pharma Aktiengesellschaft Substituted oxopyridine derivatives and use thereof as factor xia/plasma

Also Published As

Publication number Publication date
ES2633248T3 (es) 2017-09-20
US9475809B2 (en) 2016-10-25
CA2918814A1 (en) 2015-01-29
US20170035739A1 (en) 2017-02-09
WO2015011087A1 (de) 2015-01-29
US9918969B2 (en) 2018-03-20
CN105555767A (zh) 2016-05-04
JP2016525136A (ja) 2016-08-22
CN105555767B (zh) 2018-03-23
EP3024822B1 (de) 2017-05-03
EP3024822A1 (de) 2016-06-01
CA2918814C (en) 2021-10-12
US20160152613A1 (en) 2016-06-02

Similar Documents

Publication Publication Date Title
US9918969B2 (en) Substituted oxopyridine derivatives and use thereof as factor XIa/plasma
JP6368367B2 (ja) 置換オキソピリジン誘導体
JP6633045B2 (ja) 置換されたオキソピリジン誘導体およびそれの心血管障害の治療における使用
CN106687458B (zh) 取代的氧代吡啶衍生物
US10138236B2 (en) Factor xia-inhibiting pyridobenzazepine and pyridobenzazocine derivatives
US10071995B2 (en) Substituted oxopyridine derivatives
US10077265B2 (en) Substituted oxopyridine derivatives
US10414731B2 (en) Substituted oxopyridine derivatives
US20180250280A1 (en) Substituted oxopyridine derivatives
JP2018509426A (ja) 血栓症の治療のための因子XIa阻害剤としてのオキソピリジン誘導体
HK1237777A1 (en) Substituted oxopyridine derivatives
HK1227852A1 (en) Substituted oxopyridine derivatives
HK1218749B (en) Substituted oxopyridine derivatives and use thereof in the treatment of cardiovascular disorders

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170706

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170706

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20180529

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180605

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180822

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20180904

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20180925

R150 Certificate of patent or registration of utility model

Ref document number: 6410819

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees