JP2017519025A5 - - Google Patents
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- JP2017519025A5 JP2017519025A5 JP2016574921A JP2016574921A JP2017519025A5 JP 2017519025 A5 JP2017519025 A5 JP 2017519025A5 JP 2016574921 A JP2016574921 A JP 2016574921A JP 2016574921 A JP2016574921 A JP 2016574921A JP 2017519025 A5 JP2017519025 A5 JP 2017519025A5
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- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- substituted
- cycloalkyl
- compound according
- 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.)
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 49
- 239000001257 hydrogen Substances 0.000 claims description 49
- 125000000217 alkyl group Chemical group 0.000 claims description 45
- 150000001875 compounds Chemical class 0.000 claims description 33
- 150000002431 hydrogen Chemical group 0.000 claims description 33
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 20
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 16
- -1 C 1 -C 4 alkyl Chemical group 0.000 claims description 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 14
- 229910052760 oxygen Inorganic materials 0.000 claims description 14
- 229910052757 nitrogen Inorganic materials 0.000 claims description 13
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 13
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 12
- 125000000623 heterocyclic group Chemical group 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 11
- 125000003545 alkoxy group Chemical group 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 125000005843 halogen group Chemical group 0.000 claims description 7
- 125000001072 heteroaryl group Chemical group 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 208000010412 Glaucoma Diseases 0.000 claims description 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 5
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 229920006395 saturated elastomer Polymers 0.000 claims description 5
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims description 4
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 230000004410 intraocular pressure Effects 0.000 claims description 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 3
- 125000004193 piperazinyl group Chemical group 0.000 claims description 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 2
- 239000000556 agonist Substances 0.000 claims description 2
- 125000005002 aryl methyl group Chemical group 0.000 claims description 2
- 239000002876 beta blocker Substances 0.000 claims description 2
- 229940097320 beta blocking agent Drugs 0.000 claims description 2
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 230000000394 mitotic effect Effects 0.000 claims description 2
- 239000004090 neuroprotective agent Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 150000003180 prostaglandins Chemical class 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000002347 injection Methods 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 description 4
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 description 2
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 description 2
- 229940122072 Carbonic anhydrase inhibitor Drugs 0.000 description 1
- 102100025027 E3 ubiquitin-protein ligase TRIM69 Human genes 0.000 description 1
- 101000830203 Homo sapiens E3 ubiquitin-protein ligase TRIM69 Proteins 0.000 description 1
- 241001024304 Mino Species 0.000 description 1
- SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 125000004965 chloroalkyl group Chemical group 0.000 description 1
- 238000002513 implantation Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 description 1
- 210000003786 sclera Anatomy 0.000 description 1
- 229960003310 sildenafil Drugs 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 229960000835 tadalafil Drugs 0.000 description 1
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229960002381 vardenafil Drugs 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462020182P | 2014-07-02 | 2014-07-02 | |
| US62/020,182 | 2014-07-02 | ||
| US201562168640P | 2015-05-29 | 2015-05-29 | |
| US62/168,640 | 2015-05-29 | ||
| PCT/IB2015/055007 WO2016001876A1 (en) | 2014-07-02 | 2015-07-02 | Thiophen-2-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 |
|---|---|
| JP2017519025A JP2017519025A (ja) | 2017-07-13 |
| JP2017519025A5 true JP2017519025A5 (enExample) | 2018-08-09 |
Family
ID=53724403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016574921A Withdrawn JP2017519025A (ja) | 2014-07-02 | 2015-07-02 | チオフェン−２−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) | US9765067B2 (enExample) |
| EP (1) | EP3164399A1 (enExample) |
| JP (1) | JP2017519025A (enExample) |
| CN (1) | CN106470989A (enExample) |
| TW (1) | TW201625601A (enExample) |
| WO (1) | WO2016001876A1 (enExample) |
Families Citing this family (14)
| 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 |
| WO2017201683A1 (en) | 2016-05-25 | 2017-11-30 | Merck Sharp & Dohme Corp. | Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists |
| 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 |
Family Cites Families (24)
| 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 |
| CN101939053A (zh) * | 2007-09-06 | 2011-01-05 | 默沙东公司 | 可溶性的鸟苷酸环化酶活化剂 |
| 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 |
| CA2753434C (en) | 2009-02-26 | 2014-07-15 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| 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 |
-
2015
- 2015-07-01 TW TW104121397A patent/TW201625601A/zh unknown
- 2015-07-02 US US15/320,813 patent/US9765067B2/en not_active Expired - Fee Related
- 2015-07-02 CN CN201580036308.4A patent/CN106470989A/zh not_active Withdrawn
- 2015-07-02 WO PCT/IB2015/055007 patent/WO2016001876A1/en not_active Ceased
- 2015-07-02 EP EP15742104.1A patent/EP3164399A1/en not_active Withdrawn
- 2015-07-02 JP JP2016574921A patent/JP2017519025A/ja not_active Withdrawn
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