JP2017519836A - シクロヘキセン−１−イル−ピリジン−２−イル−１ｈ−ピラゾール−４−カルボン酸誘導体、および可溶性グアニル酸シクラーゼ活性化剤としてのその使用 - Google Patents

シクロヘキセン−１−イル−ピリジン−２−イル−１ｈ−ピラゾール−４−カルボン酸誘導体、および可溶性グアニル酸シクラーゼ活性化剤としてのその使用 Download PDF

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JP2017519836A
JP2017519836A JP2017520036A JP2017520036A JP2017519836A JP 2017519836 A JP2017519836 A JP 2017519836A JP 2017520036 A JP2017520036 A JP 2017520036A JP 2017520036 A JP2017520036 A JP 2017520036A JP 2017519836 A JP2017519836 A JP 2017519836A
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methyl
ethyl
alkyl
mmol
hydrogen
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JP2017519836A5 (enExample
Inventor
マイケル アダムス，クリストファー
マイケル アダムス，クリストファー
ベランガー，デービッド
ビーバン，ダウグ
ボルダック，フィリップ
武 江原
武 江原
フェララ，ルシアナ
ジ，ナン
充典 加藤
充典 加藤
メレディス，エリック
宗人 茂木
宗人 茂木
ジェイ． パワーズ，ジェームズ
ジェイ． パワーズ，ジェームズ
プラサンナ，ガネーシュ
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ノバルティス アーゲー
ノバルティス アーゲー
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Publication of JP2017519836A publication Critical patent/JP2017519836A/ja
Publication of JP2017519836A5 publication Critical patent/JP2017519836A5/ja
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    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017520036A 2014-07-02 2015-07-02 シクロヘキセン−１−イル−ピリジン−２−イル−１ｈ−ピラゾール−４−カルボン酸誘導体、および可溶性グアニル酸シクラーゼ活性化剤としてのその使用 Ceased JP2017519836A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201462020187P 2014-07-02 2014-07-02
US62/020,187 2014-07-02
US201562127535P 2015-03-03 2015-03-03
US62/127,535 2015-03-03
US201562168651P 2015-05-29 2015-05-29
US62/168,651 2015-05-29
PCT/IB2015/055009 WO2016001878A1 (en) 2014-07-02 2015-07-02 Cyclohexen-1-yl-pyridin-2-yl-1h-pyrazole-4-carboxylic acid derivatives and the use thereof as soluble guanylate cyclase activators

Publications (2)

Publication Number Publication Date
JP2017519836A true JP2017519836A (ja) 2017-07-20
JP2017519836A5 JP2017519836A5 (enExample) 2018-08-09

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JP2017520036A Ceased JP2017519836A (ja) 2014-07-02 2015-07-02 シクロヘキセン−１−イル−ピリジン−２−イル−１ｈ−ピラゾール−４−カルボン酸誘導体、および可溶性グアニル酸シクラーゼ活性化剤としてのその使用

Country Status (6)

Country Link
US (1) US9957254B2 (enExample)
EP (1) EP3164396B1 (enExample)
JP (1) JP2017519836A (enExample)
CN (1) CN106470986A (enExample)
TW (1) TW201625586A (enExample)
WO (1) WO2016001878A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201625584A (zh) 2014-07-02 2016-07-16 諾華公司 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途
US10364256B2 (en) 2015-10-06 2019-07-30 Glaxosmithkline Intellectual Property Development Limited Biaryl pyrazoles as NRF2 regulators
EP3371167A1 (en) * 2015-10-06 2018-09-12 GlaxoSmithKline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as nrf2 regulators
US10316020B2 (en) 2015-12-18 2019-06-11 Novartis Ag Indane derivatives and the use thereof as soluble guanylate cyclase activators
JPWO2018016611A1 (ja) 2016-07-22 2019-05-09 トーアエイヨー株式会社 緑内障治療薬
CN109890379A (zh) 2016-10-11 2019-06-14 拜耳制药股份公司 包含sGC活化剂和盐皮质激素受体拮抗剂的组合产品
WO2019081456A1 (en) 2017-10-24 2019-05-02 Bayer Aktiengesellschaft USE OF SGC ACTIVATORS AND STIMULATORS COMPRISING A BETA2 SUBUNIT
EP3498298A1 (en) 2017-12-15 2019-06-19 Bayer AG The use of sgc stimulators and sgc activators alone or in combination with pde5 inhibitors for the treatment of bone disorders including osteogenesis imperfecta (oi)
CN112055584A (zh) 2018-04-30 2020-12-08 拜耳公司 sGC活化剂和sGC刺激剂用于治疗认知障碍的用途
CN112384213A (zh) 2018-05-15 2021-02-19 拜耳公司 用于治疗与神经纤维敏化有关的疾病的1,3-噻唑-2-基取代的苯甲酰胺
US11508483B2 (en) 2018-05-30 2022-11-22 Adverio Pharma Gmbh Method of identifying a subgroup of patients suffering from dcSSc which benefits from a treatment with sGC stimulators and sGC activators in a higher degree than a control group
US20220128561A1 (en) 2019-01-17 2022-04-28 Bayer Aktiengesellschaft Methods to determine whether a subject is suitable of being treated with an agonist of soluble gyanylyl cyclase (sgc)
TW202412753A (zh) 2022-06-09 2024-04-01 德商拜耳廠股份有限公司 用於治療女性心臟衰竭合併保留射出分率的可溶性鳥苷酸環化酶活化劑

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010538065A (ja) * 2007-09-06 2010-12-09 メルク・シャープ・エンド・ドーム・コーポレイション 可溶性グアニレートシクラーゼ活性化因子
JP2012519169A (ja) * 2009-02-26 2012-08-23 メルク・シャープ・エンド・ドーム・コーポレイション 可溶性グアニレートシクラーゼ活性化剤

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3786579B2 (ja) 1998-07-08 2006-06-14 サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 硫黄置換スルホニルアミノカルボン酸ｎ−アリールアミド、それらの製造、それらの使用、及びそれらを含む医薬製剤
EP1420023B1 (en) 2001-01-24 2006-12-06 Yung Shin Pharmaceutical Ind. Co., Ltd. Use of fused pyrazolyl compounds for the preparation of a medicament for treating hypertension
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
DE10216145A1 (de) 2002-04-12 2003-10-23 Bayer Ag Verwendung von Stimulatoren der löslichen Guanylatcyclase zur Behandlung von Glaukom
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
AU2007333586A1 (en) 2006-12-11 2008-06-19 Reviva Pharmaceuticals, Inc. Compositions, synthesis, and methods of using indanone based cholinesterase inhibitors
DE102007015035A1 (de) 2007-03-29 2008-10-02 Bayer Healthcare Ag Substituierte Dibenzoesäure-Derivate und ihre Verwendung
WO2009068652A1 (en) 2007-11-30 2009-06-04 Smithkline Beecham Corporation 2, 6-disubstituted pyridines and 2, 4-disubstituted pyrimidines as soluble guanylate cyclase activators
WO2009071504A1 (en) 2007-12-03 2009-06-11 Smithkline Beecham Corporation 2,6-disubstituted pyridines as soluble guanylate cyclase activators
CN102056907B (zh) 2008-04-04 2014-12-31 武田药品工业株式会社 杂环衍生物及其用途
DE102008018675A1 (de) 2008-04-14 2009-10-15 Bayer Schering Pharma Aktiengesellschaft Oxo-heterocyclisch substituierte Carbonsäure-Derivate und ihre Verwendung
DE102009012314A1 (de) 2009-03-09 2010-09-16 Bayer Schering Pharma Aktiengesellschaft Oxo-heterocyclisch substituierte Alkylcarbonsäuren und ihre Verwendung
DE102009046115A1 (de) 2009-10-28 2011-09-08 Bayer Schering Pharma Aktiengesellschaft Substituierte 3-Phenylpropansäuren und ihre Verwendung
WO2012058132A1 (en) 2010-10-28 2012-05-03 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
MX2013006053A (es) 2010-12-07 2013-06-18 Bayer Ip Gmbh Acidos 1-bencilcicloalquilcarboxilicos sustituidos y su uso.
WO2012122340A1 (en) 2011-03-10 2012-09-13 Boehringer Ingelheim International Gmbh Soluble guanylate cyclase activators
DE102011007272A1 (de) 2011-04-13 2012-10-18 Bayer Pharma Aktiengesellschaft Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung
US8815857B2 (en) 2011-08-12 2014-08-26 Boehringer Ingelheim International Gmbh Soluble guanylate cyclase activators
JP5565645B1 (ja) 2012-10-09 2014-08-06 Ｄｉｃ株式会社 バンプクッション
US10265314B2 (en) 2013-07-25 2019-04-23 Bayer Pharma Aktiengesellschaft SGC stimulators in combination with additional treatment for the therapy of cystic fibrosis
US20160214956A1 (en) 2013-09-05 2016-07-28 Glaxosmithkline Intellectual Property Development Limited Novel soluble guanylate cyclase activators and their use

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010538065A (ja) * 2007-09-06 2010-12-09 メルク・シャープ・エンド・ドーム・コーポレイション 可溶性グアニレートシクラーゼ活性化因子
JP2012519169A (ja) * 2009-02-26 2012-08-23 メルク・シャープ・エンド・ドーム・コーポレイション 可溶性グアニレートシクラーゼ活性化剤

Also Published As

Publication number Publication date
TW201625586A (zh) 2016-07-16
EP3164396B1 (en) 2019-01-16
CN106470986A (zh) 2017-03-01
EP3164396A1 (en) 2017-05-10
US9957254B2 (en) 2018-05-01
US20170197941A1 (en) 2017-07-13
WO2016001878A1 (en) 2016-01-07

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