AR097325A1 - Pirroles anillados - Google Patents

Pirroles anillados

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Publication number
AR097325A1
AR097325A1 ARP140103037A ARP140103037A AR097325A1 AR 097325 A1 AR097325 A1 AR 097325A1 AR P140103037 A ARP140103037 A AR P140103037A AR P140103037 A ARP140103037 A AR P140103037A AR 097325 A1 AR097325 A1 AR 097325A1
Authority
AR
Argentina
Prior art keywords
polysubstituted
substituted
monosubstituted
unsubstituted
case
Prior art date
Application number
ARP140103037A
Other languages
English (en)
Inventor
Dr Voss Felix
Dr Wachten Sebastian
Dr Oberbrsch Stefan
Dr Nordhoff Sonja
Dr Ritter Stefanie
Dr Kless Achim
Original Assignee
Gruenenthal Gmbh
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of AR097325A1 publication Critical patent/AR097325A1/es

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Classifications

    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente se relaciona con compuestos de pirroloheterociclilo bicíclicos sustituidos que son útiles como inhibidores de ICRAC, con composiciones farmacéuticas que contienen a estos compuestos y con estos compuestos para su uso en el tratamiento y/o la profilaxis de enfermedades y/o trastornos inflamatorios y autoinmunes. Reivindicación 1: Un compuesto de fórmula (1), donde A¹ y A² representan un enlace directo o C(=O), con la condición de que 0 ó 1 de A¹ y A² representa C(=O); m y n en forma independiente denotan 0, 1, 2 ó 3, con la condición de que la suma [n + m] es 1, 2, 3 ó 4; R¹ denota H, F, Cl, Br, I, CN, CF₃, CF₂H, CFH₂, CO₂H, CO₂R¹³, R¹³, OH, O-R¹³, NH₂, N(H)R¹³, N(R¹³)₂; R² representa entre 0 y 4 sustituyentes, cada uno seleccionado en forma independiente entre F, Cl, Br, CN, CF₃, CF₂H, CFH₂, R¹³, OH, O-R¹³, NH₂, N(H)R¹³ y N(R¹³)₂; Ar¹ representa fenilo o heteroarilo de 5 ó 6 miembros, en cada caso no sustituido o sustituido con uno, dos, tres o cuatro sustituyentes, seleccionados en forma independiente entre F, Cl, Br, CN, CF₅, CF₂H CFH₂, R¹³ y O-R¹³; o C₃₋₆-cicloalquilo o heterocicloalquilo de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido; Ar² representa fenilo o heteroarilo de 5 ó 6 miembros, donde dicho fenilo o dicho heteroarilo puede no estar sustituido o estar monosustituido o polisustituido y puede estar condensado con un anillo de 4, 5, 6 ó 7 miembros, que puede ser carbocíclico o heterocíclico, donde dicho anillo condensado puede ser saturado, parcialmente insaturado o aromático y puede no estar sustituido o estar monosustituido o polisustituido; y cada R¹³ en forma independiente en cada caso denota C₁₋₈-alquilo, no sustituido o monosustituido o polisustituido; o C₃₋₆-cicloalquilo o heterocicloalquilo de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido; o C₃₋₆-cicloalquilo o heterocicloalquilo de entre 3 y 7 miembros, en cada caso no sustituido o monosustituido o polisustituido, y en cada caso conectado a través de un grupo C₁₋₄-alifático, no sustituido o monosustituido o polisustituido; opcionalmente en forma de un único estereoisómero o una mezcla de estereoisómeros, en forma del compuesto libre o una sal aceptable para uso fisiológico del mismo o un solvato aceptable para uso fisiológico del mismo.
ARP140103037A 2013-08-13 2014-08-13 Pirroles anillados AR097325A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13004028 2013-08-13

Publications (1)

Publication Number Publication Date
AR097325A1 true AR097325A1 (es) 2016-03-09

Family

ID=48985546

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140103037A AR097325A1 (es) 2013-08-13 2014-08-13 Pirroles anillados

Country Status (4)

Country Link
US (1) US20160151337A1 (es)
EP (1) EP3033342A1 (es)
AR (1) AR097325A1 (es)
WO (1) WO2015022073A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6704398B2 (ja) 2015-01-28 2020-06-03 バイエル ファーマ アクチエンゲゼルシャフト 4H−ピロロ[3,2−c]ピリジン−4−オン誘導体
CA2994596A1 (en) 2015-08-05 2017-02-09 Bayer Pharma Aktiengesellschaft 1h-pyrrol-3-amines
JP6400247B1 (ja) * 2015-11-16 2018-10-03 ロンザ・リミテッド 1−メチル−3−(トリフルオロメチル)−1h−ピラゾール−5−オールの調製方法
CN107325067B (zh) * 2017-05-03 2020-05-12 广州中医药大学 磷酸二酯酶4抑制剂桑辛素m衍生物及其用途
EP3412658A1 (en) * 2017-06-09 2018-12-12 Solvay Sa Processes for the manufacture of sulfur-substitued pyrazole derivatives
EP3700904B1 (en) 2017-10-24 2023-07-19 Bayer AG 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
JP2022508468A (ja) 2018-09-14 2022-01-19 ルヒゼン ファーマスティカルズ アクツィエンゲゼルシャフト Crac阻害剤およびコルチコステロイドを含む組成物ならびにそれらの使用方法
WO2020161257A1 (en) 2019-02-07 2020-08-13 Bayer Aktiengesellschaft 3-amino-2-[2-(acylamino)pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one as csnk1 inhibitors
WO2020216773A1 (en) 2019-04-24 2020-10-29 Bayer Aktiengesellschaft 4h-pyrrolo[3,2-c]pyridin-4-one compounds
MA55751A (fr) 2019-04-24 2022-03-02 Bayer Ag Composés de 4h-pyrrolo[3,2-c]pyridin-4-one
CA3137611A1 (en) 2019-04-24 2020-10-29 Bayer Aktiengesellschaft 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CA3177214A1 (en) 2020-03-31 2021-10-07 Bayer Aktiengesellschaft 3-(anilino)-2-[3-(3-alkoxy-pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one derivatives as egfr inhibitors for the treatment of cancer
WO2022023337A1 (en) 2020-07-29 2022-02-03 Bayer Aktiengesellschaft Substituted pyrrolo-pyridinone derivatives and therapeutic uses thereof
US20230322767A1 (en) 2020-07-29 2023-10-12 Bayer Aktiengesellschaft Aryl substituted pyrrolo-pyridinones and therapeutic uses thereof
CN115850178A (zh) * 2022-12-28 2023-03-28 宁夏格瑞精细化工有限公司 一种1-甲基-3-(三氟甲基)-1h-吡唑-5-醇的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7071207B2 (en) * 2001-09-24 2006-07-04 Bayer Pharmaceuticals Corporation Preparation and use of 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives for treatment of obesity
BR112012006630A2 (pt) * 2009-09-24 2016-05-03 Hoffmann La Roche derivados em indol como moduladores dos canais de cálcio ativados para liberação de cálcio (crac)

Also Published As

Publication number Publication date
WO2015022073A1 (en) 2015-02-19
EP3033342A1 (en) 2016-06-22
US20160151337A1 (en) 2016-06-02

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