AR081830A1 - Activadores de guanilato ciclasa soluble, composiciones farmaceuticas que los comprenden y sus usos - Google Patents

Activadores de guanilato ciclasa soluble, composiciones farmaceuticas que los comprenden y sus usos

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Publication number
AR081830A1
AR081830A1 ARP110101824A ARP110101824A AR081830A1 AR 081830 A1 AR081830 A1 AR 081830A1 AR P110101824 A ARP110101824 A AR P110101824A AR P110101824 A ARP110101824 A AR P110101824A AR 081830 A1 AR081830 A1 AR 081830A1
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AR
Argentina
Prior art keywords
crd2
alkyl
cycloalkyl
heteroaryl
aryl
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ARP110101824A
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English (en)
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Merck Sharp & Dohme
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Publication of AR081830A1 publication Critical patent/AR081830A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Una sal farmacéuticamente aceptable de la misma, son capaces de modular la producción del cuerpo del guanosín monofosfato cíclico (GMPc) y son generalmente adecuados para la terapia y profilaxis de las enfermedades que están asociadas con un equilibrio perturbado del GMPc. Se refiere además a los procesos para preparar compuestos de fórmula (1) o una sal farmacéuticamente aceptable del mismo, para su uso en la terapia y profilaxis de las enfermedades arriba mencionadas y para la preparación de productos farmacéuticos destinados a este fin, y a preparaciones farmacéuticas que comprendan compuestos de fórmula (1) o una sal farmacéuticamente aceptable de los mismos.Reivindicación 1: Un compuesto que tiene la fórmula estructural (1), o una sal farmacéuticamente aceptable del mismo, en donde: el anillo A es un heteroarilo seleccionado entre el grupo de fórmulas (2); en donde * indica unión con el anillo de pirimidinilo y ** indica unión con el -CH2-R2 de la fórmula estructural (1); cada X1, X2, X3 y X4 es independientemente N o CH, con la condición de que no más de dos de X1, X2, X3 y X4 sean N; cada Rx y Ry es independientemente H, cicloalquilo C3-10 o alquilo C1-6; R1 es independientemente -H, halo, OR, -alquilo C1-6, arilo, heterociclilo, heteroarilo, -cicloalquilo C3-10, -CN, -NRaC(O)Rb o -C(O)NRaRb, dichos arilo, heteroarilo y cicloalquilo se encuentran opcionalmente sustituidos por uno a tres sustituyentes seleccionados entre halo, -alquilo C1-6, -OR, -CN y -CF3; R2 es -(CRd2)t-alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -(CRd2)tOR, -(CRd2)tSR, -(CRd2)tCF3, -(CRd2)t-cicloalquilo C3-10, -(CRd2)t-arilo, -(CRd2)t-heterociclilo o -(CRd2)t-heteroarilo, estando dichos alquilo, cicloalquilo, arilo, heterociclilo y heteroarilo opcionalmente sustituidos por uno a tres sustituyentes seleccionados entre halo, -alquilo C1-6, -CF3, -CN y -OR; R3 es -(CRd2)t-arilo, -(CRd2)t-heteroarilo, -(CRd2)t-heterociclilo, -(CRd2)t-cicloalquilo C3-10, -(CRd2)tCN, -(CRd2)t-C(O)NRaRb, -(CRd2)t-NRaC(O)Rb, -(CRd2)t-C(S)NRaRb, -(CRd2)t-C(O)ORa, -(CRd2)t-NRaC(O)NRb, -(CRd2)t-NRaC(O)ORa, -(CRd2)t-NRaRb, u -ORa, dichos arilo, heteroarilo o heterociclilo están opcionalmente sustituidos por uno a tres sustituyentes seleccionados entre R5; R4 es en -alquilo C1-6, cicloalquilo C3-10, halo o CF3; cada R5 es independientemente halo, OR, CN, -(CRd2)tCF3, S(O)pRc, -(CRd2)t-cicloalquilo C3-10 o alquilo C1-6, dicho alquilo y cicloalquilo se encuentra opcionalmente sustituidos por uno a tres sustituyentes seleccionados entre halo y OR; cada R6 es independientemente halo, -alquilo C1-6, OR, CN, CF3, arilo o heteroarilo, donde dichos alquilo, arilo o heteroarilo están opcionalmente sustituidos por halo, alquilo C1-6 o CF3; R es independientemente -H, -alquilo C1-6, -CF3 o arilo; Ra y Rb son independientemente -H, -alquilo C1-6, arilo, heteroarilo, heterociclilo o -(CH2)0-3-cicloalquilo C3-10, donde dichos alquilo, heteroarilo, heterociclilo y cicloalquilo están opcionalmente sustituidos por uno a tres sustituyentes seleccionados R6; opcionalmente, cuando Ra y Rb son -alquilo C1-6 y están unidos al mismo átomo de nitrógeno, Ra y Rb pueden ciclarse para formar un anillo cicloalquilo C3-6; Rc es independientemente -alquilo C1-6, -CF3 o arilo; Rd es independientemente halo, -CF3 o -alquilo C1-6; m es un número entero seleccionado entre 1, 2 ó 3; p es un número entero seleccionado independientemente entre 0, 1 ó 2; y t es un número entero seleccionado independientemente entre 0, 1, 2, 3 ó 4.
ARP110101824A 2010-05-27 2011-05-27 Activadores de guanilato ciclasa soluble, composiciones farmaceuticas que los comprenden y sus usos AR081830A1 (es)

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US34906510P 2010-05-27 2010-05-27

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US (1) US9365574B2 (es)
EP (1) EP2575473B1 (es)
JP (2) JP5409961B2 (es)
KR (2) KR101499308B1 (es)
CN (1) CN103096718B (es)
AR (1) AR081830A1 (es)
AU (1) AU2011258436B2 (es)
BR (1) BR112012030177B1 (es)
CA (1) CA2800541C (es)
CL (1) CL2012003317A1 (es)
CO (1) CO6640255A2 (es)
CR (1) CR20120599A (es)
DO (1) DOP2012000300A (es)
EA (1) EA023254B1 (es)
ES (1) ES2564503T3 (es)
GT (1) GT201200320A (es)
HN (1) HN2012002555A (es)
IL (1) IL223259A0 (es)
MA (1) MA34330B1 (es)
MX (1) MX2012013774A (es)
NI (1) NI201200172A (es)
NZ (1) NZ603884A (es)
PE (1) PE20130222A1 (es)
SG (1) SG185777A1 (es)
TN (1) TN2012000544A1 (es)
TW (1) TW201202245A (es)
UA (1) UA107112C2 (es)
WO (1) WO2011149921A1 (es)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2566963T3 (es) 2007-11-21 2016-04-18 Oregon Health & Science University Anticuerpos monoclonales anti-factor XI y métodos de uso de los mismos
AU2009322836B2 (en) 2008-11-25 2013-04-04 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
EP2373691B1 (en) 2008-12-18 2019-01-23 Oregon Health&Science University Anti-fxi antibodies and methods of use
EP2549875B1 (en) 2010-03-25 2015-05-13 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
JP5940062B2 (ja) * 2010-07-09 2016-06-29 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 環縮合4−アミノピリミジンおよび可溶性グアニル酸シクラーゼの刺激剤としてのその使用
WO2012004258A1 (de) 2010-07-09 2012-01-12 Bayer Pharma Aktiengesellschaft Annellierte pyrimidine und triazine und ihre verwendung zur behandlung bzw. prophylaxe von herz-kreislauf-erkrankungen
DE102010040233A1 (de) 2010-09-03 2012-03-08 Bayer Schering Pharma Aktiengesellschaft Bicyclische Aza-Heterocyclen und ihre Verwendung
US20140171434A1 (en) 2011-01-11 2014-06-19 Bayer Pharma Aktiengessellschaft Substituted imidazopyridines and imidazopyridazines and the use thereof
DE102012200356A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Substituierte Imidazopyridine und Imidazopyridazine und ihre Verwendung
US9090610B2 (en) * 2011-04-21 2015-07-28 Bayer Intellectual Property Gmbh Fluoroalkyl-substituted pyrazolopyridines and use thereof
DE102012200357A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Fluoralkyl-substituierte Pyrazolopyridine und ihre Verwendung
RU2014103960A (ru) * 2011-07-06 2015-08-20 Байер Интеллектуэль Проперти Гмбх Гетероарилзамещенные пиразолопиридины и их применение в качестве стимуляторов растворимой гуанилатциклазы
DE102012200354A1 (de) 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Heteroaryl-substituierte Pyrazolopyridine und ihre Verwendung
BR112014005110A2 (pt) * 2011-09-02 2017-04-18 Bayer Ip Gmbh pirimidinas aneladas substituídas e utilização das mesmas
DE102012200351A1 (de) 2012-01-11 2013-07-11 Bayer Pharma Aktiengesellschaft Substituierte annellierte Pyrimidine und ihre Verwendung
CN102491974B (zh) 2011-12-12 2013-08-07 南京药石药物研发有限公司 1-(2-氟苄基)-1H-吡唑并[3,4-b]吡啶-3-甲脒盐酸盐的合成方法
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
DE102012200352A1 (de) * 2012-01-11 2013-07-11 Bayer Intellectual Property Gmbh Substituierte, annellierte Imidazole und Pyrazole und ihre Verwendung
ES2644781T3 (es) 2012-03-06 2017-11-30 Bayer Intellectual Property Gmbh Azabiciclos sustituidos y su uso
CN104684932B (zh) 2012-05-10 2019-03-12 拜耳药业股份公司 能够结合凝血因子XI和/或其活化形式因子XIa的抗体及其用途
JP6496246B2 (ja) 2012-10-05 2019-04-03 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. アルドステロンシンターゼインヒビター関連用途としてのインドリン化合物
US9624214B2 (en) 2012-11-05 2017-04-18 Bayer Pharma Aktiengesellschaft Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
PL2927231T3 (pl) * 2012-11-30 2018-01-31 Astellas Pharma Inc Związki imidazopirydyny
CA2901636A1 (en) 2013-02-21 2014-08-28 Adverio Pharma Gmbh Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate
KR20150121007A (ko) 2013-03-01 2015-10-28 바이엘 파마 악티엔게젤샤프트 트리플루오르메틸-치환된 고리-융합된 피리미딘 및 그의 용도
JP2016513129A (ja) 2013-03-01 2016-05-12 バイエル・ファルマ・アクティエンゲゼルシャフト ベンジル−置換ピラゾロピリジンおよびその使用
RS59981B1 (sr) 2013-03-15 2020-03-31 Cyclerion Therapeutics Inc Sgc stimulatori
US9776997B2 (en) 2013-06-04 2017-10-03 Bayer Pharma Aktiengesellschaft 3-aryl-substituted imidazo[1,2-A]pyridines and their use
JP2016523944A (ja) 2013-07-10 2016-08-12 バイエル・ファルマ・アクティエンゲゼルシャフト ベンジル−1H−ピラゾロ[3,4−b]ピリジンおよびその使用
WO2015088885A1 (en) * 2013-12-11 2015-06-18 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
WO2015088886A1 (en) * 2013-12-11 2015-06-18 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
JP2016540017A (ja) 2013-12-11 2016-12-22 アイアンウッド ファーマシューティカルズ インコーポレイテッド sGC刺激物質
EP3094327A1 (en) 2014-01-13 2016-11-23 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
CA2939793A1 (en) 2014-02-19 2015-08-27 Bayer Pharma Aktiengesellschaft 3-(pyrimidine-2-yl)imidazo[1,2-a]pyridines
US9796733B2 (en) 2014-06-04 2017-10-24 Merck Sharp & Dohme Corp. Imidazo-pyrazine derivatives useful as soluble guanylate cyclase activators
EP3186251A1 (de) 2014-08-29 2017-07-05 Bayer Pharma Aktiengesellschaft Substituierte annellierte pyrimidine und ihre verwendung
US20170240566A1 (en) 2014-08-29 2017-08-24 Bayer Pharma Aktiengesellschaft Amino-substituted annulated pyrimidines and use thereof
WO2016044445A2 (en) 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. sGC STIMULATORS
AU2015317824A1 (en) 2014-09-17 2017-03-23 Cyclerion Therapeutics, Inc. Pyrazole derivatives as sGC stimulators
CN107406421A (zh) 2014-09-17 2017-11-28 铁木医药有限公司 sGC刺激物
TW201625635A (zh) 2014-11-21 2016-07-16 默沙東藥廠 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物
CA2969268A1 (en) 2014-12-02 2016-06-09 Bayer Pharma Aktiengesellschaft Heteroaryl-substituted imidazo[1,2-a]pyridines and their use
TN2017000465A1 (en) 2015-05-06 2019-04-12 Bayer Pharma AG The use of sgc stimulators, sgc activators, alone and combinations with pde5 inhibitors for the treatment of digital ulcers (du) concomitant to systemic sclerosis (ssc)
WO2016191334A1 (en) 2015-05-27 2016-12-01 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
EP3310782B1 (en) * 2015-05-28 2021-12-01 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
HRP20201932T4 (hr) 2015-07-23 2024-02-16 Bayer Pharma Aktiengesellschaft Stimulatori / aktivatori topive gvanilat-ciklaze u kombinaciji s nep-inhibitorom i/ili angiotenzin aii-antagonistom i njihova uporaba
AU2016371762A1 (en) 2015-12-14 2018-06-21 Cyclerion Therapeutics, Inc. Use of sGC stimulators for the treatment of gastrointestinal sphincter dysfunction
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
WO2017121692A1 (de) 2016-01-15 2017-07-20 Bayer Pharma Aktiengesellschaft Substituierte sulfamide und ihre verwendung
WO2017121693A1 (de) 2016-01-15 2017-07-20 Bayer Pharma Aktiengesellschaft Substituierte thiazol- und thiadiazolamide und ihre verwendung
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
WO2017197555A1 (en) * 2016-05-16 2017-11-23 Merck Sharp & Dohme Corp. Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators
EP3458063A4 (en) * 2016-05-18 2020-02-26 Merck Sharp & Dohme Corp. METHODS OF USING TRIAZOLO-PYRAZINYL-SOLUBLE GUANYLATE CYCLASE ACTIVATORS FOR FIBROTIC DISORDERS
AU2017291826B2 (en) 2016-07-07 2021-10-21 Cyclerion Therapeutics, Inc. Phosphorus prodrugs of sGC stimulators
KR20230074840A (ko) 2016-07-07 2023-05-31 사이클리온 테라퓨틱스, 인크. sGC 자극제의 고체 형태
KR20230124760A (ko) 2016-09-02 2023-08-25 사이클리온 테라퓨틱스, 인크. 융합된 비시클릭 sGC 자극제
EP3525779B1 (de) 2016-10-11 2024-06-05 Bayer Pharma Aktiengesellschaft Kombination enthaltend den sgc stimulator vericuguat und den mineralcorticoid-rezeptor-antagonist finerenone
US11331308B2 (en) 2016-10-11 2022-05-17 Bayer Pharma Aktiengesellschaft Combination containing sGC activators and mineralocorticoid receptor antagonists
AU2017356887B2 (en) 2016-11-08 2022-06-30 Cyclerion Therapeutics, Inc. sGC stimulators
EP3538096B1 (en) 2016-11-08 2024-02-28 Tisento Therapeutics Inc. Treatment of cns diseases with sgc stimulators
US20190381039A1 (en) 2016-12-13 2019-12-19 Cyclerion Therapeutics, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF ESOPHAGEAL MOTILITY DISORDERS
ES2924359T3 (es) 2017-04-11 2022-10-06 Sunshine Lake Pharma Co Ltd Compuestos de indazol sustituidos con flúor y usos de los mismos
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)
CN111712247B (zh) 2017-12-19 2024-02-09 塞科里昂医疗股份有限公司 sGC刺激剂
MX2023004858A (es) 2018-03-07 2023-11-24 Cyclerion Therapeutics Inc Formas cristalinas de un estimulante de la guanilil ciclasa soluble (sgc).
WO2019211081A1 (en) 2018-04-30 2019-11-07 Bayer Aktiengesellschaft The use of sgc activators and sgc stimulators for the treatment of cognitive impairment
CA3100096A1 (en) 2018-05-15 2019-11-21 Bayer Aktiengesellschaft 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization
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
KR20210033444A (ko) 2018-06-04 2021-03-26 엑스사이언티아 엘티디 아데노신 수용체 길항제로서 피라졸로피리미딘 화합물
BR112021000358A2 (pt) 2018-07-11 2021-04-06 Cyclerion Therapeutics, Inc. Uso de estimulantes de sgc para o tratamento de distúrbios mitocondriais
MX2021005892A (es) 2018-11-28 2021-06-23 Topadur Pharma Ag Novedosos activadores de guanilato ciclasa soluble e inhibidores de fosfodiesterasa con modo de accion dual y usos de estos.
CN113330030A (zh) 2019-01-17 2021-08-31 拜耳公司 确定受试者是否适于用可溶性鸟苷酸环化酶(sGC)的激动剂治疗的方法
WO2020164008A1 (en) 2019-02-13 2020-08-20 Bayer Aktiengesellschaft Process for the preparation of porous microparticles
US12086719B2 (en) * 2019-10-11 2024-09-10 Royal Bank Of Canada System and method of machine learning using embedding networks
WO2021195403A1 (en) 2020-03-26 2021-09-30 Cyclerion Therapeutics, Inc. Deuterated sgc stimulators
US20230128032A1 (en) 2020-03-31 2023-04-27 Curtails Llc Early Drug Interventions to Reduce COVID-19 Related Respiratory Distress, Need for Respirator Assist and Death
CN111467350B (zh) * 2020-04-20 2021-03-19 黑龙江中医药大学 一种治疗乳腺炎的药物及其制备方法
WO2021245192A1 (en) 2020-06-04 2021-12-09 Topadur Pharma Ag Novel dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof
US20240207265A1 (en) 2021-04-20 2024-06-27 Tisento Therapeutics Inc. TREATMENT OF CNS DISEASES WITH sGC STIMULATORS
WO2022225903A1 (en) 2021-04-20 2022-10-27 Cyclerion Therapeutics, Inc. Sgc stimulators
US20240342187A1 (en) 2021-06-14 2024-10-17 Curtails Llc Use of nep inhibitors for the treatment of gastrointestinal sphincter disorders
WO2023018795A1 (en) 2021-08-11 2023-02-16 Curtails Llc Nep inhibitors for the treatment of laminitis
WO2024086179A1 (en) 2022-10-18 2024-04-25 Tisento Therapeutics, Inc. Pyrimidine sgc stimulators
WO2024086182A1 (en) 2022-10-18 2024-04-25 Tisento Therapeutics Inc. Treatment of mitochondrial diseases with sgc stimulators

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB876526A (en) 1957-12-24 1961-09-06 Geigy Ag J R Process for the production of new aminobenzoic acid derivatives and their use in pest control
DE4410997A1 (de) * 1994-03-30 1995-10-26 Isis Pharma Gmbh Pharmazeutische Zubereitungen und Arzneistoffe zur Prävention und Behandlung endothelialer Dysfunktionen
US5585381A (en) 1994-06-01 1996-12-17 Kureha Chemical Industry Co., Ltd. Pyrimidine derivatives and pharmaceutical composition
CN1082949C (zh) * 1995-06-06 2002-04-17 辉瑞大药厂 2,4-二氯吡啶类化合物转化为2-芳氧基-4-氯吡啶类化合物的方法
DE59713007D1 (de) 1996-10-14 2009-06-25 Bayer Healthcare Ag Neue heterocyclylmethyl-substituierte pyrazolderivate und ihre verwendung in der behandlung von herz-kreislauf-erkrankungen
DE19744026A1 (de) 1997-10-06 1999-04-08 Hoechst Marion Roussel De Gmbh Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE19744027A1 (de) 1997-10-06 1999-04-08 Hoechst Marion Roussel De Gmbh Substituierte Pyrazolo[3,4-b]pyridine, ihre Herstellung und Verwendung in Arzneimitteln
US6610497B1 (en) 1997-12-11 2003-08-26 Millennium Pharmaceuticals, Inc. Angiotensin converting enzyme homolog and therapeutic and diagnostic uses therefor
DE19756388A1 (de) 1997-12-18 1999-06-24 Hoechst Marion Roussel De Gmbh Substituierte 2-Aryl-4-amino-chinazoline
DE19834044A1 (de) * 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
DE19836697A1 (de) 1998-08-13 2000-02-17 Hoechst Marion Roussel De Gmbh Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
GB9824310D0 (en) 1998-11-05 1998-12-30 Univ London Activators of soluble guanylate cyclase
DE19904710A1 (de) 1999-02-05 2000-08-10 Aventis Pharma Gmbh Substituierte 4-Amino-2-aryl-tetrahydrochinazoline, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
US20010044445A1 (en) 1999-04-08 2001-11-22 Bamaung Nwe Y. Azole inhibitors of cytokine production
DE19943636A1 (de) 1999-09-13 2001-03-15 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE10021069A1 (de) 2000-04-28 2001-10-31 Bayer Ag Substituiertes Pyrazolderivat
DE10054278A1 (de) 2000-11-02 2002-05-08 Bayer Ag Verwendung von Stimulatoren der löslichen Guanylatcyclase zur Behandlung von Osteoporose
JP4295505B2 (ja) * 2000-11-22 2009-07-15 バイエル アクチェンゲゼルシャフト 新規なラクタム置換ピラゾロピリジン誘導体
AR031176A1 (es) 2000-11-22 2003-09-10 Bayer Ag Nuevos derivados de pirazolpiridina sustituidos con piridina
DE10057751A1 (de) 2000-11-22 2002-05-23 Bayer Ag Neue Carbamat-substituierte Pyrazolopyridinderivate
DE10057754A1 (de) 2000-11-22 2002-05-23 Bayer Ag Neue Sulfonamid-substituierte Pyrazolopyridinderivate
MXPA03008121A (es) 2001-03-15 2003-12-12 Basf Ag 5-fenilpirimidinas, metodos y productos intermedios para su produccion y uso de las mismas para controlar hongos patogenicos.
DE10122894A1 (de) 2001-05-11 2002-11-14 Bayer Ag Neue Sulfonat-substituierte Pyrazolopyridinderivate
CA2464333C (en) 2001-10-26 2011-07-26 University Of Connecticut Heteroindanes: a new class of potent cannabimimetic ligands
JP4359146B2 (ja) 2002-02-13 2009-11-04 エフ.ホフマン−ラ ロシュ アーゲー 新規なピリジン−およびピリミジン−誘導体
US20040048866A1 (en) 2002-03-08 2004-03-11 Teodozyj Kolasa Indazole derivatives that are activators of soluble guanylate cyclase
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
DE10222550A1 (de) 2002-05-17 2003-11-27 Bayer Ag Substituierte Benzyl-pyrazolopyridine
DE10232571A1 (de) 2002-07-18 2004-02-05 Bayer Ag 4-Aminosubstituierte Pyrimidinderivate
US7241803B2 (en) 2002-11-21 2007-07-10 New York Blood Center Compounds for inhibition of HIV infection by blocking HIV entry
US20040121994A1 (en) 2002-12-20 2004-06-24 Anderson Steven N. Novel amides that activate soluble guanylate cyclase
US20050038183A1 (en) 2003-08-14 2005-02-17 Dongchan Ahn Silicones having improved surface properties and curable silicone compositions for preparing the silicones
DE10351903A1 (de) 2003-11-06 2005-06-09 Bayer Healthcare Ag Neue Kombination
EP1616965A1 (en) * 2004-07-16 2006-01-18 AXXAM S.r.l. Methods and assays for detecting guanylate cyclase activity
CN100396678C (zh) 2004-11-16 2008-06-25 财团法人工业技术研究院 1-苯甲基-3-(5’-羟甲基-2’-呋喃基)吲唑的吲哚类似物的合成及用途
CA2611979A1 (en) 2005-06-15 2006-12-21 Pfizer Limited Substituted arylpyrazoles
BRPI0611798A2 (pt) 2005-06-15 2009-01-13 Pfizer Ltd compostos de arilpirazàis substituÍdos, sua composiÇço farmacÊutica e uso
AU2006261845C1 (en) 2005-06-27 2013-05-16 Exelixis Patent Company Llc Imidazole based LXR modulators
DE102005031575A1 (de) 2005-07-06 2007-01-11 Bayer Healthcare Ag Verwendung von Aktivatoren der löslichen Guanylatzyklase zur Förderung der Wundheilung
US20100016305A1 (en) 2005-07-18 2010-01-21 Bayer Healthcare Ag novel use of activators and stimulators of soluble guanylate cyclase for the prevention or treatment of renal disorders
DE102006043443A1 (de) * 2006-09-15 2008-03-27 Bayer Healthcare Ag Neue aza-bicyclische Verbindungen und ihre Verwendung
WO2008040753A1 (en) 2006-10-03 2008-04-10 Neurosearch A/S Indazolyl derivatives useful as potassium channel modulating agents
MX2009003821A (es) 2006-10-10 2009-05-25 Amgen Inc Compuestos de n-aril pirazol para usarse contra la diabetes.
EP1921067A1 (en) 2006-11-08 2008-05-14 Bayer Schering Pharma Aktiengesellschaft Indole and indazole derivatives as anti-inflammatory agents
DE102006054757A1 (de) 2006-11-21 2008-05-29 Bayer Healthcare Ag Neue aza-bicyclische Verbindungen und ihre Verwendung
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
WO2010015652A2 (en) 2008-08-07 2010-02-11 Smithkline Beecham Corporation Thiazole compounds as activators of soluble guanylate cyclase
AU2009322836B2 (en) 2008-11-25 2013-04-04 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
DE102009046115A1 (de) 2009-10-28 2011-09-08 Bayer Schering Pharma Aktiengesellschaft Substituierte 3-Phenylpropansäuren und ihre Verwendung
NZ602311A (en) 2010-03-18 2014-08-29 Pasteur Institut Korea Anti-infective compounds
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
WO2012004258A1 (de) * 2010-07-09 2012-01-12 Bayer Pharma Aktiengesellschaft Annellierte pyrimidine und triazine und ihre verwendung zur behandlung bzw. prophylaxe von herz-kreislauf-erkrankungen
JP5940062B2 (ja) * 2010-07-09 2016-06-29 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 環縮合4−アミノピリミジンおよび可溶性グアニル酸シクラーゼの刺激剤としてのその使用
DE102010040233A1 (de) * 2010-09-03 2012-03-08 Bayer Schering Pharma Aktiengesellschaft Bicyclische Aza-Heterocyclen und ihre Verwendung

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