PE20160201A1 - Bencil-1h-pirazol[3,4-b]piridinas y su uso - Google Patents
Bencil-1h-pirazol[3,4-b]piridinas y su usoInfo
- Publication number
- PE20160201A1 PE20160201A1 PE2016000026A PE2016000026A PE20160201A1 PE 20160201 A1 PE20160201 A1 PE 20160201A1 PE 2016000026 A PE2016000026 A PE 2016000026A PE 2016000026 A PE2016000026 A PE 2016000026A PE 20160201 A1 PE20160201 A1 PE 20160201A1
- Authority
- PE
- Peru
- Prior art keywords
- fluorine
- represents hydrogen
- methyl
- oxides
- salts
- Prior art date
Links
- RQMWVVBHJMUJNZ-UHFFFAOYSA-N 4-chloropyridin-2-amine Chemical compound NC1=CC(Cl)=CC=N1 RQMWVVBHJMUJNZ-UHFFFAOYSA-N 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 5
- 229910052731 fluorine Chemical group 0.000 abstract 5
- 239000011737 fluorine Chemical group 0.000 abstract 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 2
- 239000000460 chlorine Chemical group 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- YNVRFTUDHPLHJD-UHFFFAOYSA-N 1-benzylpyrazolo[3,4-b]pyridine Chemical class N1=CC2=CC=CN=C2N1CC1=CC=CC=C1 YNVRFTUDHPLHJD-UHFFFAOYSA-N 0.000 abstract 1
- GTPVKNOAYNWRKA-UHFFFAOYSA-N 3-[1-[(2,3-difluorophenyl)methyl]-5-fluoro-6-methylpyrazolo[3,4-b]pyridin-3-yl]-7,7-dimethyl-5h-pyrrolo[2,3-e][1,2,4]triazin-6-one Chemical compound N1=C(C=2N=C3C(C(C(=O)N3)(C)C)=NN=2)C=2C=C(F)C(C)=NC=2N1CC1=CC=CC(F)=C1F GTPVKNOAYNWRKA-UHFFFAOYSA-N 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- C07D519/04—Dimeric indole alkaloids, e.g. vincaleucoblastine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente solicitud se relaciona con bencil-1 H-pirazolo[3,4-b]piridinas de formula (I), en la que R1 representa hidrogeno o fluor, R2 representa hidrogeno o fluor, R3 representa hidrogeno, cloro o fluor, R4 representa hidrogeno, cloro, fluor o metilo, con la condicion de que por lo menos dos de los radicales R1, R2, R3 o R4 son diferentes de hidrogeno, R5 representa hidrogeno o fluor, R6 representa metilo, R7 representa metilo, o R6 y R7 junto con el atomo de carbono al que se unen forman un anillo ciclopropilo, y los oxidos N, sales, solvatos, sales de los oxidos N y solvatos de los oxidos N o sales de los mismos. Es compuesto preferido: 3-[1-(2,3-difluorobencil)-5-fluoro-6-metil- 1 H-pirazolo[3,4-b]piridin-3-il]-7, 7 -dimetil-5, 7 -dihidro-6H-pirrolo[2,3-e][1,2,4]triazin-6-ona; entre otros. Dichos compuestos son utiles para el tratamiento de enfermedades cardiovasculares.
Applications Claiming Priority (10)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13175896 | 2013-07-10 | ||
| EP13175889 | 2013-07-10 | ||
| EP13175895 | 2013-07-10 | ||
| EP13175904 | 2013-07-10 | ||
| EP13175894 | 2013-07-10 | ||
| EP13175899 | 2013-07-10 | ||
| EP13175890 | 2013-07-10 | ||
| EP13175892 | 2013-07-10 | ||
| EP13175903 | 2013-07-10 | ||
| EP13175898 | 2013-07-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160201A1 true PE20160201A1 (es) | 2016-05-06 |
Family
ID=51162805
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000026A PE20160201A1 (es) | 2013-07-10 | 2014-07-08 | Bencil-1h-pirazol[3,4-b]piridinas y su uso |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9605008B2 (es) |
| EP (1) | EP3019506A1 (es) |
| JP (1) | JP2016523944A (es) |
| KR (1) | KR20160030541A (es) |
| CN (1) | CN105745215A (es) |
| AP (1) | AP2016008970A0 (es) |
| AU (1) | AU2014289312A1 (es) |
| CA (1) | CA2917682A1 (es) |
| CL (1) | CL2016000030A1 (es) |
| CU (1) | CU20160004A7 (es) |
| DO (1) | DOP2016000006A (es) |
| EA (1) | EA201600096A1 (es) |
| GT (1) | GT201600002A (es) |
| IL (1) | IL243525A0 (es) |
| MX (1) | MX2016000258A (es) |
| PE (1) | PE20160201A1 (es) |
| PH (1) | PH12016500065A1 (es) |
| SG (1) | SG11201600038UA (es) |
| TN (1) | TN2016000006A1 (es) |
| TW (1) | TW201542569A (es) |
| UY (1) | UY35652A (es) |
| WO (1) | WO2015004105A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102012200349A1 (de) | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte annellierte Pyrimidine und Triazine und ihre Verwendung |
| JP6748113B2 (ja) | 2015-05-06 | 2020-08-26 | バイエル・ファルマ・アクティエンゲゼルシャフト | 全身性硬化症（ＳＳｃ）に付随する指潰瘍（ＤＵ）を治療するための単独のまたはＰＤＥ５阻害剤と組み合わせたｓＧＣ刺激剤、ｓＧＣ活性化剤の使用 |
| CA2989740C (en) | 2015-07-23 | 2023-07-11 | Bayer Pharma Aktiengesellschaft | Stimulators and/or activators of soluble guanylate cyclase (sgc) in combination with an inhibitor of neutral endopeptidase (nep inhibitor) and/or an angiotensin aii antagonist and the use thereof |
| WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
| WO2017121700A1 (de) | 2016-01-15 | 2017-07-20 | Bayer Pharma Aktiengesellschaft | 1,3-disubstituierte 1h-pyrazolo[3,4-b]pyridin- derivate und ihre verwendung als stimulatoren der löslichen guanylatcyclase |
| WO2017121692A1 (de) | 2016-01-15 | 2017-07-20 | Bayer Pharma Aktiengesellschaft | Substituierte sulfamide und ihre verwendung |
| ES2985316T3 (es) | 2016-10-11 | 2024-11-05 | Bayer Pharma AG | Combinación que contiene el estimulador sGC vericuguat y el antagonista de los receptores de corticoides minerales finerenona |
| 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 |
| EP3609883B1 (en) | 2017-04-11 | 2022-06-29 | Sunshine Lake Pharma Co., Ltd. | Fluorine-substituted indazole compounds and uses thereof |
| WO2018234488A1 (en) | 2017-06-23 | 2018-12-27 | Basf Se | Substituted cyclopropyl derivatives |
| TW202015676A (zh) | 2018-05-15 | 2020-05-01 | 德商拜耳廠股份有限公司 | 經1,3-噻唑-2-基取代之苯甲醯胺用於治療與神經纖維敏化作用相關疾病之用途 |
| WO2020164008A1 (en) | 2019-02-13 | 2020-08-20 | Bayer Aktiengesellschaft | Process for the preparation of porous microparticles |
| US11884672B2 (en) | 2019-05-14 | 2024-01-30 | Vertex Pharmaceuticals Incorporated | Modulators of alpha-1 antitrypsin |
| CN120754115A (zh) * | 2025-05-23 | 2025-10-10 | 远大医药（中国）有限公司 | 一种含依普利酮组合物及其药物制剂、制备方法和用途 |
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| JPS63139949A (ja) | 1986-12-02 | 1988-06-11 | Fuji Photo Film Co Ltd | 新規ピラゾロン染料 |
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| GB9314412D0 (en) | 1993-07-13 | 1993-08-25 | Rhone Poulenc Agriculture | New compositions of matter |
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| JP2011513483A (ja) | 2008-03-10 | 2011-04-28 | バーテックス ファーマシューティカルズ インコーポレイテッド | タンパク質キナーゼの阻害剤として有用なピリミジンおよびピリジン |
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| KR20140019004A (ko) | 2010-05-27 | 2014-02-13 | 머크 샤프 앤드 돔 코포레이션 | 가용성 구아닐레이트 시클라제 활성화제 |
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| DE102010043380A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Benzyl-substituierte Carbamate und ihre Verwendung |
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| EP2699578B1 (de) | 2011-04-21 | 2016-04-20 | Bayer Intellectual Property GmbH | Fluoralkyl-substituierte pyrazolopyridine und ihre verwendung |
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| EP2729476B1 (de) | 2011-07-06 | 2017-08-23 | Bayer Intellectual Property GmbH | Heteroaryl-substituierte pyrazolopyridine und ihre verwendung als stimulatoren der löslichen guanylatcyclase |
| EP2763990B1 (en) | 2011-09-01 | 2017-02-22 | F. Hoffmann-La Roche AG | Pyrrolopyrazine kinase inhibitors |
| SG11201400083VA (en) | 2011-09-02 | 2014-06-27 | Bayer Ip Gmbh | Substituted annellated pyrimidine and the use thereof |
| DE102012200352A1 (de) * | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte, annellierte Imidazole und Pyrazole und ihre Verwendung |
| DE102012200360A1 (de) | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte Triazine und ihre Verwendung |
| DE102012200349A1 (de) * | 2012-01-11 | 2013-07-11 | Bayer Intellectual Property Gmbh | Substituierte annellierte Pyrimidine und Triazine und ihre Verwendung |
| WO2013131923A1 (de) | 2012-03-06 | 2013-09-12 | Bayer Intellectual Property Gmbh | Substituierte azabicyclen und ihre verwendung |
| CN105026405B (zh) | 2013-03-01 | 2017-08-08 | 拜耳制药股份公司 | 苄基‑取代的吡唑并吡啶及其用途 |
| AU2014222739A1 (en) | 2013-03-01 | 2015-09-03 | Bayer Pharma Aktiengesellschaft | Trifluormethyl-substituted ring-fused pyrimidines and use thereof |
| CN105899510A (zh) | 2013-08-08 | 2016-08-24 | 拜耳制药股份公司 | 取代的咪唑并[1,2-a]吡嗪羧酰胺及其用途 |
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2014
- 2014-07-08 PE PE2016000026A patent/PE20160201A1/es not_active Application Discontinuation
- 2014-07-08 WO PCT/EP2014/064547 patent/WO2015004105A1/de not_active Ceased
- 2014-07-08 KR KR1020167003065A patent/KR20160030541A/ko not_active Withdrawn
- 2014-07-08 CN CN201480049852.8A patent/CN105745215A/zh active Pending
- 2014-07-08 US US14/903,347 patent/US9605008B2/en not_active Expired - Fee Related
- 2014-07-08 EA EA201600096A patent/EA201600096A1/ru unknown
- 2014-07-08 TW TW103123391A patent/TW201542569A/zh unknown
- 2014-07-08 EP EP14736803.9A patent/EP3019506A1/de not_active Withdrawn
- 2014-07-08 AU AU2014289312A patent/AU2014289312A1/en not_active Abandoned
- 2014-07-08 MX MX2016000258A patent/MX2016000258A/es unknown
- 2014-07-08 CA CA2917682A patent/CA2917682A1/en not_active Abandoned
- 2014-07-08 AP AP2016008970A patent/AP2016008970A0/xx unknown
- 2014-07-08 TN TN2016000006A patent/TN2016000006A1/en unknown
- 2014-07-08 UY UY0001035652A patent/UY35652A/es not_active Application Discontinuation
- 2014-07-08 SG SG11201600038UA patent/SG11201600038UA/en unknown
- 2014-07-08 JP JP2016524789A patent/JP2016523944A/ja active Pending
-
2016
- 2016-01-07 DO DO2016000006A patent/DOP2016000006A/es unknown
- 2016-01-08 PH PH12016500065A patent/PH12016500065A1/en unknown
- 2016-01-08 GT GT201600002A patent/GT201600002A/es unknown
- 2016-01-08 CL CL2016000030A patent/CL2016000030A1/es unknown
- 2016-01-10 IL IL243525A patent/IL243525A0/en unknown
- 2016-01-11 CU CUP2016000004A patent/CU20160004A7/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| GT201600002A (es) | 2018-12-19 |
| US20160145271A1 (en) | 2016-05-26 |
| DOP2016000006A (es) | 2016-02-15 |
| SG11201600038UA (en) | 2016-02-26 |
| JP2016523944A (ja) | 2016-08-12 |
| CU20160004A7 (es) | 2016-06-29 |
| CN105745215A (zh) | 2016-07-06 |
| US9605008B2 (en) | 2017-03-28 |
| TW201542569A (zh) | 2015-11-16 |
| IL243525A0 (en) | 2016-02-29 |
| AU2014289312A1 (en) | 2016-02-11 |
| WO2015004105A1 (de) | 2015-01-15 |
| CL2016000030A1 (es) | 2016-08-19 |
| AP2016008970A0 (en) | 2016-01-31 |
| PH12016500065A1 (en) | 2016-07-04 |
| CA2917682A1 (en) | 2015-01-15 |
| EP3019506A1 (de) | 2016-05-18 |
| KR20160030541A (ko) | 2016-03-18 |
| UY35652A (es) | 2015-01-30 |
| EA201600096A1 (ru) | 2016-10-31 |
| TN2016000006A1 (en) | 2017-07-05 |
| MX2016000258A (es) | 2016-04-28 |
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