JP2017519835A5 - - Google Patents
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- JP2017519835A5 JP2017519835A5 JP2017520035A JP2017520035A JP2017519835A5 JP 2017519835 A5 JP2017519835 A5 JP 2017519835A5 JP 2017520035 A JP2017520035 A JP 2017520035A JP 2017520035 A JP2017520035 A JP 2017520035A JP 2017519835 A5 JP2017519835 A5 JP 2017519835A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- compound according
- pharmaceutical composition
- cycloalkyl
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 39
- 229910052739 hydrogen Inorganic materials 0.000 claims description 35
- 239000001257 hydrogen Substances 0.000 claims description 35
- 125000000217 alkyl group Chemical group 0.000 claims description 31
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 24
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 17
- 150000002431 hydrogen Chemical group 0.000 claims description 15
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 13
- 229910052760 oxygen Inorganic materials 0.000 claims description 13
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 13
- 238000002347 injection Methods 0.000 claims description 12
- 239000007924 injection Substances 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims description 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 9
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 125000005843 halogen group Chemical group 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- -1 C 1 -C 4 alkyl Chemical group 0.000 claims description 7
- 208000010412 Glaucoma Diseases 0.000 claims description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 125000003545 alkoxy group Chemical group 0.000 claims description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 230000004410 intraocular pressure Effects 0.000 claims description 4
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 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 claims description 4
- 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 claims description 2
- 239000000556 agonist Substances 0.000 claims description 2
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 claims description 2
- 239000002876 beta blocker Substances 0.000 claims description 2
- 229940097320 beta blocking agent Drugs 0.000 claims description 2
- 239000011203 carbon fibre reinforced carbon Substances 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
- 238000007918 intramuscular administration Methods 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 230000000394 mitotic effect Effects 0.000 claims description 2
- 239000004090 neuroprotective agent Substances 0.000 claims description 2
- 238000007911 parenteral administration Methods 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 239000002243 precursor Substances 0.000 claims description 2
- 150000003180 prostaglandins Chemical class 0.000 claims description 2
- 210000003786 sclera Anatomy 0.000 claims description 2
- 229960003310 sildenafil Drugs 0.000 claims description 2
- 229940127296 soluble guanylate cyclase stimulator Drugs 0.000 claims description 2
- 238000007920 subcutaneous administration Methods 0.000 claims description 2
- 229960000835 tadalafil Drugs 0.000 claims description 2
- 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 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 230000000699 topical effect Effects 0.000 claims description 2
- 229960002381 vardenafil Drugs 0.000 claims description 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical group [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 description 3
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462020166P | 2014-07-02 | 2014-07-02 | |
| US62/020,166 | 2014-07-02 | ||
| US201562168627P | 2015-05-29 | 2015-05-29 | |
| US62/168,627 | 2015-05-29 | ||
| PCT/IB2015/055006 WO2016001875A1 (en) | 2014-07-02 | 2015-07-02 | Indane and indoline derivatives and the use thereof as soluble guanylate cyclase activators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017519835A JP2017519835A (ja) | 2017-07-20 |
| JP2017519835A5 true JP2017519835A5 (enExample) | 2018-08-09 |
Family
ID=53724402
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017520035A Ceased JP2017519835A (ja) | 2014-07-02 | 2015-07-02 | インダンおよびインドリン誘導体、ならびに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 (26)
| Country | Link |
|---|---|
| US (2) | US10208018B2 (enExample) |
| EP (1) | EP3164395B1 (enExample) |
| JP (1) | JP2017519835A (enExample) |
| KR (1) | KR20170021345A (enExample) |
| CN (1) | CN106470985A (enExample) |
| AP (1) | AP2016009609A0 (enExample) |
| AU (1) | AU2015283617B2 (enExample) |
| BR (1) | BR112016030733A2 (enExample) |
| CA (1) | CA2953885A1 (enExample) |
| CL (1) | CL2016003329A1 (enExample) |
| CO (1) | CO2017000222A2 (enExample) |
| CR (1) | CR20170003A (enExample) |
| CU (1) | CU20160192A7 (enExample) |
| EA (1) | EA030634B1 (enExample) |
| EC (1) | ECSP17007208A (enExample) |
| ES (1) | ES2732758T3 (enExample) |
| GT (1) | GT201600269A (enExample) |
| IL (1) | IL249406A0 (enExample) |
| MX (1) | MX2016017325A (enExample) |
| PE (1) | PE20170323A1 (enExample) |
| PH (1) | PH12016502539A1 (enExample) |
| SG (1) | SG11201610226SA (enExample) |
| SV (1) | SV2016005351A (enExample) |
| TN (1) | TN2016000556A1 (enExample) |
| TW (1) | TW201625584A (enExample) |
| WO (1) | WO2016001875A1 (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 |
| EP3359532A1 (en) | 2015-10-06 | 2018-08-15 | GlaxoSmithKline Intellectual Property Development Limited | Biaryl pyrazoles as nrf2 regulators |
| WO2017103888A1 (en) * | 2015-12-18 | 2017-06-22 | Novartis Ag | Indane derivatives and the use thereof as soluble guanylate cyclase activators |
| WO2017201683A1 (en) * | 2016-05-25 | 2017-11-30 | Merck Sharp & Dohme Corp. | Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists |
| AU2017300558B2 (en) * | 2016-07-22 | 2021-02-25 | Toa Eiyo Ltd. | Therapeutic agent for glaucoma |
| WO2018069148A1 (de) | 2016-10-11 | 2018-04-19 | Bayer Pharma Aktiengesellschaft | Kombination enthaltend sgc aktivatoren und mineralocorticoid-rezeptor-antagonisten |
| 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 |
| JP2021523201A (ja) | 2018-05-15 | 2021-09-02 | バイエル アクチェンゲゼルシャフトＢａｙｅｒ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 神経線維感作に関連する疾患を治療するための１，３−チアゾール−２−イル置換ベンズアミド |
| 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 |
| EP3833395A1 (en) | 2018-08-06 | 2021-06-16 | Nicox S.A. | Nitric oxide releasing phosphodiesterase type 5 inhibitor |
| 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) |
| CA3258617A1 (en) | 2022-06-09 | 2023-12-14 | Bayer Aktiengesellschaft | SOLUBLE GUANYLATE CYCLASE ACTIVATORS FOR USE IN THE TREATMENT OF HEART FAILURE WITH PRESERVED EJECTION FRACTION IN WOMEN |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100720844B1 (ko) | 1998-07-08 | 2007-05-25 | 사노피-아벤티스 도이칠란트 게엠베하 | 황 치환된 설포닐아미노카복실산 ｎ-아릴아미드, 이의 제조방법, 및 이를 함유하는 약제학적 제제 |
| 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 |
| CA2514733A1 (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 |
| EP2114166A4 (en) * | 2006-12-11 | 2011-05-25 | 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 |
| CA2697678C (en) | 2007-08-31 | 2015-06-23 | Kalsi Engineering, Inc. | Rotary seal with improved film distribution |
| CA2698332C (en) * | 2007-09-06 | 2012-08-21 | Merck Sharp & Dohme Corp. | Pyrazole derivatives as soluble guanylate cyclase activators |
| 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 |
| WO2009123316A1 (ja) | 2008-04-04 | 2009-10-08 | 武田薬品工業株式会社 | 複素環誘導体及びその用途 |
| DE102008018675A1 (de) | 2008-04-14 | 2009-10-15 | Bayer Schering Pharma Aktiengesellschaft | Oxo-heterocyclisch substituierte Carbonsäure-Derivate und ihre Verwendung |
| WO2010015653A1 (en) | 2008-08-07 | 2010-02-11 | Smithkline Beecham Corporation | Pyrimidine derivatives as activators of soluble guanylate cyclase |
| CN102414194A (zh) * | 2009-02-26 | 2012-04-11 | 默沙东公司 | 可溶性鸟苷酸环化酶激活剂 |
| 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 |
| KR101793304B1 (ko) | 2010-02-05 | 2017-11-02 | 아드베리오 파마 게엠베하 | 낭성 섬유증의 치료를 위한, 단독으로의 및 ＰＤＥ5 억제제와 조합된 ｓＧＣ 자극제 또는 ｓＧＣ 활성화제 |
| WO2011095553A1 (en) | 2010-02-05 | 2011-08-11 | Bayer Schering Pharma Aktiengesellschaft | Sgc stimulators or sgc activators in combination with pde5 inhbitors for the treatment of erectile dysfunction |
| CN103038232B (zh) | 2010-05-26 | 2016-01-20 | 阿德弗里奥药品有限责任公司 | 单独的和与PDE5抑制剂相组合的sGC刺激剂、sGC活化剂用于治疗系统性硬化症(SSc)的用途 |
| EP2585055A1 (de) | 2010-06-25 | 2013-05-01 | Bayer Intellectual Property GmbH | Verwendung von stimulatoren und aktivatoren der löslichen guanylatzyklase zur behandlung von sichelzellanämie und konservierung von blutersatzstoffen |
| EP2632551B1 (en) | 2010-10-28 | 2016-07-06 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| SG190296A1 (en) | 2010-12-07 | 2013-06-28 | Bayer Ip Gmbh | Substituted 1-benzylcycloalkylcarboxlic acids and use thereof |
| JP5715713B2 (ja) | 2011-03-10 | 2015-05-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 可溶性グアニル酸シクラーゼ活性化因子 |
| 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 |
| EP2594270A3 (en) | 2011-11-18 | 2013-07-31 | BIP Patents | The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc) |
| NZ703989A (en) | 2012-09-07 | 2017-04-28 | Boehringer Ingelheim Int | Alkoxy pyrazoles as soluble guanylate cyclase activators |
| WO2014057740A1 (ja) | 2012-10-09 | 2014-04-17 | 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 |
| JP2016530292A (ja) | 2013-09-05 | 2016-09-29 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | 新規な可溶性グアニル酸シクラーゼ活性剤およびそれらの使用 |
| WO2015095515A1 (en) | 2013-12-20 | 2015-06-25 | Novartis Ag | Sgc activators for the treatment of glaucoma |
| TW201625601A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 噻吩－２－基－吡啶－２－基－１ｈ－吡唑－４－羧酸衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| TW201625586A (zh) | 2014-07-02 | 2016-07-16 | 諾華公司 | 環己烯－１－基－吡啶－２－基－１ｈ－吡唑－４－羧酸衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途 |
| 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 |
-
2015
- 2015-07-01 TW TW104121398A patent/TW201625584A/zh unknown
- 2015-07-02 AP AP2016009609A patent/AP2016009609A0/en unknown
- 2015-07-02 KR KR1020177002515A patent/KR20170021345A/ko not_active Withdrawn
- 2015-07-02 AU AU2015283617A patent/AU2015283617B2/en not_active Ceased
- 2015-07-02 ES ES15742103T patent/ES2732758T3/es active Active
- 2015-07-02 CN CN201580036394.9A patent/CN106470985A/zh active Pending
- 2015-07-02 JP JP2017520035A patent/JP2017519835A/ja not_active Ceased
- 2015-07-02 PE PE2016002818A patent/PE20170323A1/es unknown
- 2015-07-02 CR CR20170003A patent/CR20170003A/es unknown
- 2015-07-02 MX MX2016017325A patent/MX2016017325A/es unknown
- 2015-07-02 US US15/320,810 patent/US10208018B2/en active Active
- 2015-07-02 SG SG11201610226SA patent/SG11201610226SA/en unknown
- 2015-07-02 BR BR112016030733A patent/BR112016030733A2/pt not_active Application Discontinuation
- 2015-07-02 WO PCT/IB2015/055006 patent/WO2016001875A1/en not_active Ceased
- 2015-07-02 TN TN2016000556A patent/TN2016000556A1/en unknown
- 2015-07-02 CA CA2953885A patent/CA2953885A1/en not_active Abandoned
- 2015-07-02 EA EA201692542A patent/EA030634B1/ru not_active IP Right Cessation
- 2015-07-02 EP EP15742103.3A patent/EP3164395B1/en active Active
-
2016
- 2016-12-06 IL IL249406A patent/IL249406A0/en unknown
- 2016-12-19 PH PH12016502539A patent/PH12016502539A1/en unknown
- 2016-12-22 SV SV2016005351A patent/SV2016005351A/es unknown
- 2016-12-23 GT GT201600269A patent/GT201600269A/es unknown
- 2016-12-26 CL CL2016003329A patent/CL2016003329A1/es unknown
- 2016-12-28 CU CUP2016000192A patent/CU20160192A7/es unknown
-
2017
- 2017-01-11 CO CONC2017/0000222A patent/CO2017000222A2/es unknown
- 2017-02-02 EC ECIEPI20177208A patent/ECSP17007208A/es unknown
-
2018
- 2018-12-11 US US16/216,420 patent/US10550102B2/en not_active Expired - Fee Related
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