AR097435A1 - 6-alquinilpiridinas - Google Patents

6-alquinilpiridinas

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Publication number
AR097435A1
AR097435A1 ARP140103170A ARP140103170A AR097435A1 AR 097435 A1 AR097435 A1 AR 097435A1 AR P140103170 A ARP140103170 A AR P140103170A AR P140103170 A ARP140103170 A AR P140103170A AR 097435 A1 AR097435 A1 AR 097435A1
Authority
AR
Argentina
Prior art keywords
alkyl
groups
independently
heteroaryl
halogen
Prior art date
Application number
ARP140103170A
Other languages
English (en)
Inventor
Madden James
Reiser Ulrich
Original Assignee
Boehringer Ingelheim Int
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Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR097435A1 publication Critical patent/AR097435A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • 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
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    • 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
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    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • 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
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P17/06Antipsoriatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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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    • 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
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    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/00Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
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    • 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
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
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  • Epidemiology (AREA)
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  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
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Abstract

Composiciones farmacéuticas que las contienen y su uso como medicamentos para el tratamiento y/o la prevención de enfermedades caracterizadas por proliferación celular excesiva o anormal y condiciones asociadas tales como cáncer. Reivindicación 1: Un compuesto caracterizado por la fórmula (1) en donde, R¹ está seleccionado de -alquilo C₁₋₃, -haloalquilo C₁₋₃ y -H; R² está seleccionado de -alquilo C₁₋₃ o -H; R²ᵃ está seleccionado de -alquilo C₁₋₃ o -H; R³ está seleccionado de fenilo y heteroarilo de 5 - 12 miembros, cada uno de cuyos grupos puede estar sustituido, opcional e independientemente, con uno o varios grupos seleccionados, de modo independiente, de R⁶ o R³ es heterociclilo aromático de 8 - 12 miembros, cada uno de cuyos grupos puede estar sustituido, opcional e independientemente, con uno o varios grupos seleccionados, de modo independiente, de =O y R⁶; R⁴ está seleccionado de fenilo y heteroarilo de 5 - 12 miembros, cada uno de cuyos grupos puede estar opcionalmente sustituido con uno o varios grupos seleccionados, de modo independiente, de R⁷ o R⁴ es heterociclilo aromático de 8 - 12 miembros, cada uno de cuyos grupos puede estar opcionalmente sustituido con uno o varios grupos seleccionados, de modo independiente, de =O y R⁷; R⁵ está seleccionado de -H, halógeno, -O-alquilo C₁₋₃ y heteroarilo de 5 - 6 miembros; R⁶ está seleccionado de halógeno, -alquilo C₁₋₃, -O-alquilo C₁₋₃, ciano, heteroarilo de 5 - 6 miembros, en donde el grupo heteroarilo puede estar opcionalmente sustituido con -alquilo C₁₋₃, -O-alquilo C₁₋₃ o halógeno; R⁷ está seleccionado de halógeno, -alquilo C₁₋₃, -haloalquilo C₁₋₃ y -O-alquilo C₁₋₃ o ciano; en donde los compuestos de la fórmula (1) pueden estar opcionalmente presentes en la forma de sales.
ARP140103170A 2013-08-23 2014-08-22 6-alquinilpiridinas AR097435A1 (es)

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US (1) US9278978B2 (es)
EP (1) EP3036228B1 (es)
JP (1) JP6338665B2 (es)
AR (1) AR097435A1 (es)
TW (1) TW201605798A (es)
UY (1) UY35710A (es)
WO (1) WO2015025019A1 (es)

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EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
AR101479A1 (es) 2014-08-11 2016-12-21 Boehringer Ingelheim Int Derivados de 6-alquinil-piridina
CN109153645B (zh) 2016-05-19 2022-06-21 勃林格殷格翰国际有限公司 制备6-炔基-吡啶衍生物的方法
JP2019522633A (ja) 2016-05-20 2019-08-15 ジェネンテック, インコーポレイテッド Protac抗体コンジュゲート及び使用方法
US20200046684A1 (en) 2017-03-31 2020-02-13 Boehringer Ingelheim International Gmbh Anticancer combination therapy
EP3886842A1 (en) 2018-11-26 2021-10-06 Debiopharm International SA Combination treatment of hiv infections
TW202043466A (zh) 2019-01-25 2020-12-01 德商百靈佳殷格翰國際股份有限公司 編碼ccl21之重組棒狀病毒
CA3151770A1 (en) 2019-09-25 2021-04-01 Silvano BRIENZA Dosing regimens for treatment of patients with locally advanced squamous cell carcinoma
PE20231293A1 (es) 2020-06-03 2023-08-22 Boehringer Ingelheim Int Rhabdovirus recombinante que codifica una proteina de fusion fc de dominio extracelular cd80
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

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ME02125B (me) 2004-04-07 2013-04-30 Novartis Ag Inhibitori protein apoptoze (iap)
CA2670728A1 (en) * 2006-12-07 2008-06-19 Novartis Ag Pyridine derivatives used as xiap inhibitors
DE102007036075A1 (de) * 2007-08-01 2009-02-05 Bayer Healthcare Ag Prodrugs und ihre Verwendung
US20110105436A1 (en) * 2008-03-10 2011-05-05 Auckland Uniservices Limited Heteroaryl compounds, compositions, and methods of use in cancer treatment
US8859541B2 (en) * 2012-02-27 2014-10-14 Boehringer Ingelheim International Gmbh 6-alkynylpyridines

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JP2016528273A (ja) 2016-09-15
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WO2015025019A1 (en) 2015-02-26
UY35710A (es) 2015-02-27
US20150057295A1 (en) 2015-02-26
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