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

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
methyl
ethyl
alkyl
mmol
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.)
Ceased
Application number
JP2017520036A
Other languages
English (en)
Japanese (ja)
Other versions
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
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
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 ノバルティス アーゲー, ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2017519836A publication Critical patent/JP2017519836A/ja
Publication of JP2017519836A5 publication Critical patent/JP2017519836A5/ja
Ceased legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (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

Family

ID=53724404

Family Applications (1)

Application Number Title Priority Date Filing Date
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
US10351530B2 (en) * 2015-10-06 2019-07-16 Glaxosmithkline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as NRF2 regulators
US10364256B2 (en) 2015-10-06 2019-07-30 Glaxosmithkline Intellectual Property Development Limited Biaryl pyrazoles as NRF2 regulators
CN108473470A (zh) 2015-12-18 2018-08-31 诺华股份有限公司 作为可溶性鸟苷酸环化酶激活剂的茚满衍生物及其用途
EP3489219B1 (en) 2016-07-22 2020-12-16 TOA Eiyo Ltd. Therapeutic agent for glaucoma
US11331308B2 (en) 2016-10-11 2022-05-17 Bayer Pharma Aktiengesellschaft Combination containing sGC activators and mineralocorticoid receptor antagonists
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
MA52616A (fr) 2018-05-15 2021-03-24 Bayer Ag Benzamides à substitution 1,3-thiazol-2-yl pour le traitement de maladies associées à la sensibilisation de fibres nerveuses
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
WO2020148379A1 (en) 2019-01-17 2020-07-23 Bayer Aktiengesellschaft Methods to determine whether a subject is suitable of being treated with an agonist of soluble guanylyl cyclase (sgc)
CN119300815A (zh) 2022-06-09 2025-01-10 拜耳公司 用于治疗女性射血分数保留型心力衰竭的可溶性鸟苷酸环化酶激活剂

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
CZ302691B6 (cs) 1998-07-08 2011-09-07 Sanofi - Aventis Deutschland GmbH N-Arylamidová sloucenina, zpusob její prípravy, farmaceutický prostredek tuto slouceninu obsahující, tato sloucenina pro použití jako aktivátor a pro použití k terapii nebo profylaxi
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
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
DE10216145A1 (de) 2002-04-12 2003-10-23 Bayer Ag Verwendung von Stimulatoren der löslichen Guanylatcyclase zur Behandlung von Glaukom
RU2478619C2 (ru) 2006-12-11 2013-04-10 Ривайва Фармасьютикалс, Инк. Композиции, синтез и способы применения ингибиторов холинэстеразы на основе инданона
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
PE20091258A1 (es) 2007-12-03 2009-09-12 Smithkline Beecham Corp Derivados de piridina como activadores de la guanilato ciclasa soluble
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
JP5989660B2 (ja) 2010-12-07 2016-09-07 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH 置換1−ベンジルシクロアルキルカルボン酸およびその使用
US8569339B2 (en) 2011-03-10 2013-10-29 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
WO2013025425A1 (en) 2011-08-12 2013-02-21 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
WO2015011086A1 (en) 2013-07-25 2015-01-29 Bayer Pharma Aktiengesellschaft Sgc stimulators or sgc activators and pde5 inhibitors in combination with additional treatment for the therapy of cystic fibrosis
RU2016112542A (ru) 2013-09-05 2017-10-06 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Новые активаторы растворимой гуанилатциклазы и их применение

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

Similar Documents

Publication Publication Date Title
EP3164396B1 (en) Cyclohexen-1-yl-pyridin-2-yl-1h-pyrazole-4-carboxylic acid derivatives and the use thereof as soluble guanylate cyclase activators
US10550102B2 (en) Indane and indoline derivatives and the use thereof as soluble guanylate cyclase activators
US9765067B2 (en) Thiophen-2-yl-pyridin-2-yl-1H-pyrazole-4-carboxylic acid derivatives and the use thereof as soluble guanylate cyclase activators
JP2016505512A (ja) Pde4のヘテロアリール阻害剤
CN105085482B (zh) 取代的哌嗪化合物及其使用方法和用途
KR20160121572A (ko) 오렉신 수용체 길항제로서의 1,2-치환된 사이클로펜탄
JP2021519269A (ja) ピペラジンアザスピロ誘導体
US10316020B2 (en) Indane derivatives and the use thereof as soluble guanylate cyclase activators
JP2025179155A (ja) Sstr4アゴニストとしてのn-ヘテロアリールアルキル-2-(ヘテロシクリル及びヘテロシクリルメチル)アセトアミド誘導体
WO2025074305A1 (en) N-(1-(aminomethyl)cyclopropyl)(aryl or heteroaryl) carboxamide derivatives

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180629

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180629

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20190219

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190221

A045 Written measure of dismissal of application [lapsed due to lack of payment]

Free format text: JAPANESE INTERMEDIATE CODE: A045

Effective date: 20190625