AR092869A1 - Alcoxipirazoles como activadores de guanilato ciclasa soluble - Google Patents
Alcoxipirazoles como activadores de guanilato ciclasa solubleInfo
- Publication number
- AR092869A1 AR092869A1 ARP130103197A ARP130103197A AR092869A1 AR 092869 A1 AR092869 A1 AR 092869A1 AR P130103197 A ARP130103197 A AR P130103197A AR P130103197 A ARP130103197 A AR P130103197A AR 092869 A1 AR092869 A1 AR 092869A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- ome
- aryl
- compounds
- optionally substituted
- Prior art date
Links
- 239000012190 activator Substances 0.000 title 1
- 230000001351 cycling effect Effects 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- -1 -OH Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- 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
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- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- 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
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- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/08—Bridged systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Vascular Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
Abstract
También composiciones farmacéuticas que comprenden estos compuestos, métodos para usar estos compuestos en el tratamiento de varias enfermedades y trastornos, procesos para preparar estos compuestos e intermediarios útiles en estos procesos. Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1) en donde: A es un grupo heterociclilo saturado de 5 - 7 miembros que contiene un nitrógeno y, opcionalmente, un oxígeno, en donde un carbono del grupo heterociclilo se sustituye opcionalmente con uno o dos grupos seleccionados de alquilo C₁₋₃ y oxo; R¹ es alquilo C₁₋₄ opcionalmente sustituido con un grupo metoxi; R² se selecciona de H, F, Cl, alquilo C₁₋₃ -CN, -OMe y -CF₃; R³ se selecciona de H y -CH₃; R⁴ se selecciona de H, F, -CH₃ y -OMe; R⁵ se selecciona de H, Cl, -CH₃, -CH₂CH₃, -CF₃, F y -OMe; R⁶ se fija al nitrógeno en A y se selecciona de H, alquilo C₁₋₆, -(CH₂)ₙ-cicloalquilo C₃₋₆, -C(O)alquilo C₁₋₆, -(CH₂)ₙ-heterociclilo, -(CH₂)ₙ-aril-(CH₂)ₙ-heteroarilo, -SO₂-arilo, SO₂-alquilo C₁₋₆, en donde alquilo C₁₋₆, -(CH₂)ₙ-heterociclilo, -(CH₂)ₙ-cicloalquilo, -(CH₂)ₙ-arilo y -(CH₂)ₙ-heteroarilo se sustituyen opcionalmente con 1 a 4 grupos seleccionados independientemente de alquilo C₁₋₃, halógeno, alcoxi C₁₋₃, -CF₃, -OH, oxo, -(CH₂)₁₋₃O(CH₂)₂₋₃OH y SO₂CH₃; R⁷ se selecciona de H, -CH₃, -CH₂CH₃, -CF₃, F y -CN; n es 0, 1 ó 2; o una sal de aquel.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261697899P | 2012-09-07 | 2012-09-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR092869A1 true AR092869A1 (es) | 2015-05-06 |
Family
ID=49170904
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP130103197A AR092869A1 (es) | 2012-09-07 | 2013-09-06 | Alcoxipirazoles como activadores de guanilato ciclasa soluble |
Country Status (38)
Country | Link |
---|---|
US (2) | US8906904B2 (es) |
EP (1) | EP2892891B1 (es) |
JP (1) | JP5970134B2 (es) |
KR (1) | KR101692707B1 (es) |
CN (1) | CN104619695B (es) |
AP (1) | AP2015008231A0 (es) |
AR (1) | AR092869A1 (es) |
AU (1) | AU2013312931B2 (es) |
BR (1) | BR112015004529B1 (es) |
CA (1) | CA2880494C (es) |
CL (2) | CL2015000255A1 (es) |
CY (1) | CY1122610T1 (es) |
DK (1) | DK2892891T3 (es) |
EA (1) | EA027244B1 (es) |
EC (1) | ECSP15012804A (es) |
ES (1) | ES2748798T3 (es) |
GE (1) | GEP20176631B (es) |
HK (1) | HK1210164A1 (es) |
HR (1) | HRP20191755T1 (es) |
HU (1) | HUE046996T2 (es) |
IL (1) | IL236987A (es) |
LT (1) | LT2892891T (es) |
MA (1) | MA37891B1 (es) |
MD (1) | MD4425C1 (es) |
MX (1) | MX338887B (es) |
NZ (1) | NZ703989A (es) |
PE (1) | PE20151001A1 (es) |
PH (1) | PH12015500457B1 (es) |
PL (1) | PL2892891T3 (es) |
PT (1) | PT2892891T (es) |
RS (1) | RS59394B1 (es) |
SG (2) | SG11201500861QA (es) |
SI (1) | SI2892891T1 (es) |
TN (1) | TN2015000054A1 (es) |
TW (1) | TWI586661B (es) |
UA (1) | UA115881C2 (es) |
UY (1) | UY35012A (es) |
WO (1) | WO2014039434A1 (es) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SG11201500861QA (en) * | 2012-09-07 | 2015-04-29 | Boehringer Ingelheim Int | Alkoxy pyrazoles as soluble guanylate cyclase activators |
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 |
US9353090B2 (en) * | 2014-07-22 | 2016-05-31 | Boehringer Ingelheim International Gmbh | Heterocyclic carboxylic acids as activators of soluble guanylate cyclase |
JP2018537488A (ja) | 2015-12-18 | 2018-12-20 | ノバルティス アーゲー | インダン誘導体、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 |
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) |
WO2019211081A1 (en) | 2018-04-30 | 2019-11-07 | Bayer Aktiengesellschaft | The use of sgc activators and sgc stimulators for the treatment of cognitive impairment |
EA202092680A1 (ru) | 2018-05-15 | 2021-04-13 | Байер Акциенгезельшафт | 1,3-тиазол-2-ил-замещенные бензамиды для лечения заболеваний, ассоциированных с сенситизацией нервных волокон |
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 |
EA202190193A1 (ru) | 2018-07-12 | 2021-06-16 | Бёрингер Ингельхайм Интернациональ Гмбх | Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы |
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) |
CN112079712B (zh) * | 2020-09-18 | 2022-12-13 | 江苏美迪克化学品有限公司 | 一种对乙烯基水杨酸的制备方法 |
EP4011873A1 (en) | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
GB202102895D0 (en) | 2021-03-01 | 2021-04-14 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
CN118900690A (zh) * | 2022-03-21 | 2024-11-05 | 勃林格殷格翰国际有限公司 | 用于治疗门脉高压的可溶性鸟苷酸环化酶活化剂 |
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 |
US20240174653A1 (en) | 2022-11-04 | 2024-05-30 | Boehringer Ingelheim International Gmbh | Soluble guanylate cyclate activators for treating systemic sclerosis |
WO2024123847A1 (en) | 2022-12-09 | 2024-06-13 | Boehringer Ingelheim International Gmbh | Solid forms of a sgc activator |
WO2025036839A1 (en) | 2023-08-16 | 2025-02-20 | Boehringer Ingelheim International Gmbh | Soluble guanylate cyclase activators for treating clinically significant portal hypertension and decompensated cirrhosis |
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GB9824310D0 (en) * | 1998-11-05 | 1998-12-30 | Univ London | Activators of soluble guanylate cyclase |
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