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 (Direct) | 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 (Direct) |
| EP (1) | EP3164395B1 (Direct) |
| JP (1) | JP2017519835A (Direct) |
| KR (1) | KR20170021345A (Direct) |
| CN (1) | CN106470985A (Direct) |
| AP (1) | AP2016009609A0 (Direct) |
| AU (1) | AU2015283617B2 (Direct) |
| BR (1) | BR112016030733A2 (Direct) |
| CA (1) | CA2953885A1 (Direct) |
| CL (1) | CL2016003329A1 (Direct) |
| CO (1) | CO2017000222A2 (Direct) |
| CR (1) | CR20170003A (Direct) |
| CU (1) | CU20160192A7 (Direct) |
| EA (1) | EA030634B1 (Direct) |
| EC (1) | ECSP17007208A (Direct) |
| ES (1) | ES2732758T3 (Direct) |
| GT (1) | GT201600269A (Direct) |
| IL (1) | IL249406A0 (Direct) |
| MX (1) | MX2016017325A (Direct) |
| PE (1) | PE20170323A1 (Direct) |
| PH (1) | PH12016502539A1 (Direct) |
| SG (1) | SG11201610226SA (Direct) |
| SV (1) | SV2016005351A (Direct) |
| TN (1) | TN2016000556A1 (Direct) |
| TW (1) | TW201625584A (Direct) |
| WO (1) | WO2016001875A1 (Direct) |
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 |
| JP2018529745A (ja) | 2015-10-06 | 2018-10-11 | 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 | Ｎｒｆ２レギュレーターとしてのビアリールピラゾール |
| AU2016370806A1 (en) * | 2015-12-18 | 2018-07-05 | 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 |
| US10682323B2 (en) | 2016-07-22 | 2020-06-16 | 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 |
| BR112020022340A2 (pt) | 2018-05-15 | 2021-02-02 | Bayer Aktiengesellschaft | benzamidas substituídas por 1,3-tiazol-2-il para o tratamento de doenças associadas com sensibilização de fibras nervosas |
| EP3574905A1 (en) | 2018-05-30 | 2019-12-04 | 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 |
| WO2020030489A1 (en) | 2018-08-06 | 2020-02-13 | Nicox S.A. | Nitric oxide releasing phosphodiesterase type 5 inhibitor |
| 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) |
| 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 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU228111B1 (en) | 1998-07-08 | 2012-11-28 | Sanofi Aventis Deutschland | Sulfur substituted sulfonylaminocarboxylic acid n-arylamides, their preparation, their use and pharmaceutical preparations comprising them |
| 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 |
| DE10110749A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Substituierte Aminodicarbonsäurederivate |
| DE10110750A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| 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 |
| CN101626688A (zh) * | 2006-12-11 | 2010-01-13 | 雷维瓦药品公司 | 茚满酮基胆碱酯酶抑制剂的组合物、合成和使用方法 |
| 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 |
| BRPI0816382A2 (pt) * | 2007-09-06 | 2015-02-24 | Merck Sharp & Dohme | Composto, composição, e, métodos para ativar a guanilato ciclase solúvel e para tratar ou previnir doenças |
| 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 |
| CA2720343A1 (en) | 2008-04-04 | 2009-10-08 | Takeda Pharmaceutical Company Limited | Heterocyclic derivative and use thereof |
| 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 |
| EP2401265B1 (en) * | 2009-02-26 | 2016-09-14 | Merck Sharp & Dohme Corp. | Derivatives of 1-pyri(mid)in-2-yl-pyrazole-4-carboxylic acid which are useful for therapy or prophylaxis of cardiovascular diseases |
| 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 |
| 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 |
| DK2531187T3 (en) | 2010-02-05 | 2015-11-09 | Adverio Pharma Gmbh | sGC stimulators OR sGC activators alone and in combination with PDE5 inhibitors for the treatment of cystic fibrosis |
| MA34249B1 (fr) | 2010-05-26 | 2013-05-02 | Bayer Ip Gmbh | Utilisation de stimulateurs de la sgc, d'activateurs de la sgc, seuls et en association avec des inhibiteurs de la pde5 en vue du traitement de la sclérodermie systémique |
| US20130158028A1 (en) | 2010-06-25 | 2013-06-20 | Bayer Intellectual Property Gmbh | Use of stimulators and activators of soluble guanylate cyclase for treating sickle-cell anemia and conserving blood substitutes |
| US8895583B2 (en) | 2010-10-28 | 2014-11-25 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| ES2544532T3 (es) | 2010-12-07 | 2015-09-01 | Bayer Intellectual Property Gmbh | Ácidos 1-bencilcicloalquilcarboxílicos sustituidos y su uso |
| EP2683710B1 (en) | 2011-03-10 | 2017-07-19 | 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 |
| JP5826393B2 (ja) | 2011-08-12 | 2015-12-02 | 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 |
| 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) |
| KR101692707B1 (ko) | 2012-09-07 | 2017-01-04 | 베링거 인겔하임 인터내셔날 게엠베하 | 가용성 구아닐레이트 사이클라제 활성제로서의 알콕시 피라졸 |
| 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 |
| RU2016112542A (ru) | 2013-09-05 | 2017-10-06 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Новые активаторы растворимой гуанилатциклазы и их применение |
| 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 CA CA2953885A patent/CA2953885A1/en not_active Abandoned
- 2015-07-02 CN CN201580036394.9A patent/CN106470985A/zh active Pending
- 2015-07-02 EA EA201692542A patent/EA030634B1/ru not_active IP Right Cessation
- 2015-07-02 TN TN2016000556A patent/TN2016000556A1/en unknown
- 2015-07-02 BR BR112016030733A patent/BR112016030733A2/pt not_active Application Discontinuation
- 2015-07-02 SG SG11201610226SA patent/SG11201610226SA/en unknown
- 2015-07-02 WO PCT/IB2015/055006 patent/WO2016001875A1/en not_active Ceased
- 2015-07-02 CR CR20170003A patent/CR20170003A/es unknown
- 2015-07-02 KR KR1020177002515A patent/KR20170021345A/ko not_active Withdrawn
- 2015-07-02 US US15/320,810 patent/US10208018B2/en active Active
- 2015-07-02 AU AU2015283617A patent/AU2015283617B2/en not_active Ceased
- 2015-07-02 MX MX2016017325A patent/MX2016017325A/es unknown
- 2015-07-02 AP AP2016009609A patent/AP2016009609A0/en unknown
- 2015-07-02 ES ES15742103T patent/ES2732758T3/es active Active
- 2015-07-02 EP EP15742103.3A patent/EP3164395B1/en active Active
- 2015-07-02 PE PE2016002818A patent/PE20170323A1/es unknown
- 2015-07-02 JP JP2017520035A patent/JP2017519835A/ja not_active Ceased
-
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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