CO5570677A2 - Quinolinilpirrolopirazoles - Google Patents

Quinolinilpirrolopirazoles

Info

Publication number
CO5570677A2
CO5570677A2 CO05048136A CO05048136A CO5570677A2 CO 5570677 A2 CO5570677 A2 CO 5570677A2 CO 05048136 A CO05048136 A CO 05048136A CO 05048136 A CO05048136 A CO 05048136A CO 5570677 A2 CO5570677 A2 CO 5570677A2
Authority
CO
Colombia
Prior art keywords
pharmaceutically acceptable
compound according
prodrug
ester
acceptable salt
Prior art date
Application number
CO05048136A
Other languages
English (en)
Inventor
Sawyer Jason Scott
Jonathan Michael Yingling
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of CO5570677A2 publication Critical patent/CO5570677A2/es

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Classifications

    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

1.- Un compuesto según la fórmula II y las sales farmacéuticamente aceptables del mismo.2.- El compuesto que es 2-(6-metilpiridin-2-il)-3-[6-amidoquinolin-4-il)-5,6-dihidro-4H-pirrolo[1,2-b]pirazol y las sales farmacéuticamente aceptables del mismo.3.- Una formulación farmacéutica que comprende un compuesto según la reivindicación 1 o la sal, éster o profármaco farmacéuticamente aceptable del mismo, junto con un diluyente o vehículo farmacéuticamente aceptable.4.- El procedimiento de tratamiento de cáncer que comprende administrar a un paciente necesitado de ello una cantidad terapéuticamente eficaz de un compuesto según la reivindicación 1 o una sal, éster o profármaco farmacéuticamente aceptable del mismo.
CO05048136A 2002-11-22 2005-05-18 Quinolinilpirrolopirazoles CO5570677A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US42889302P 2002-11-22 2002-11-22

Publications (1)

Publication Number Publication Date
CO5570677A2 true CO5570677A2 (es) 2005-10-31

Family

ID=32393478

Family Applications (1)

Application Number Title Priority Date Filing Date
CO05048136A CO5570677A2 (es) 2002-11-22 2005-05-18 Quinolinilpirrolopirazoles

Country Status (29)

Country Link
US (2) US7265225B2 (es)
EP (1) EP1565471B1 (es)
JP (1) JP4542906B2 (es)
KR (1) KR101057282B1 (es)
CN (1) CN100345852C (es)
AT (1) ATE341550T1 (es)
AU (1) AU2003291643B2 (es)
BR (1) BR0315337A (es)
CA (1) CA2501322C (es)
CO (1) CO5570677A2 (es)
CR (1) CR7830A (es)
CY (1) CY1106283T1 (es)
DE (1) DE60308893T2 (es)
DK (1) DK1565471T3 (es)
EA (1) EA008387B1 (es)
EC (1) ECSP055807A (es)
EG (1) EG25822A (es)
ES (1) ES2273046T3 (es)
HK (1) HK1081948A1 (es)
HR (1) HRP20050436B1 (es)
IL (1) IL168190A (es)
MX (1) MXPA05005432A (es)
NO (1) NO331403B1 (es)
NZ (1) NZ538942A (es)
PL (1) PL227840B1 (es)
PT (1) PT1565471E (es)
UA (1) UA80571C2 (es)
WO (1) WO2004048382A1 (es)
ZA (1) ZA200503121B (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7405299B2 (en) * 2002-11-27 2008-07-29 Eli Lilly And Company Compounds as pharmaceutical agents
US7872020B2 (en) * 2005-07-22 2011-01-18 Eli Lilly And Company TGF-β inhibitors
WO2007039151A1 (en) * 2005-09-28 2007-04-12 Universität Zürich Blockers of transforming growth factor beta and its receptors for the treatment of infectious diseases
EP2083863B1 (en) 2006-10-03 2015-03-18 Genzyme Corporation Antibodies to tgf-beta for use in the treatment of infants at risk of developing bronchopulmonary dysplasia
EP2074128B1 (en) * 2006-10-16 2013-08-14 Medicis Pharmaceutical Corporation Therapeutic pyrazolyl thienopyridines
MA34397B1 (fr) 2010-07-02 2013-07-03 Gilead Sciences Inc Dérivés d'acide napht-2-ylacétique dans le traitement du sida
EP2588455B1 (en) 2010-07-02 2018-04-04 Gilead Sciences, Inc. 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
US8871744B2 (en) 2010-07-21 2014-10-28 B & G Partyers, LLC Compounds and methods for selectively targeting tumor-associated mucins
UA111841C2 (uk) 2011-04-21 2016-06-24 Гіліад Сайєнсіз, Інк. Сполуки бензотіазолу та їх фармацевтичне застосування
WO2013014262A1 (en) 2011-07-27 2013-01-31 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating myhre syndrome
WO2013062544A1 (en) 2011-10-26 2013-05-02 Seattle Children's Research Institute Cysteamine in the treatment of fibrotic disease
US9782452B2 (en) 2011-11-22 2017-10-10 Cornell University Methods for stimulating hematopoietic recovery by inhibiting TGFβ signaling
US9284323B2 (en) 2012-01-04 2016-03-15 Gilead Sciences, Inc. Naphthalene acetic acid derivatives against HIV infection
US9376392B2 (en) 2012-01-04 2016-06-28 Gilead Sciences, Inc. 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS
PE20141558A1 (es) 2012-04-20 2014-11-06 Gilead Sciences Inc Derivados de acido benzotiazol-6-il acetico y su uso para tratar una infeccion por vih
EA039595B1 (ru) 2012-10-05 2022-02-15 Кадмон Корпорейшн, Ллк Нуклеиновые кислоты, кодирующие человеческие анти-vegfr-2/kdr-антитела
EP2917365B1 (en) 2012-11-12 2020-03-11 Institució Catalana de Recerca i Estudis Avançats Methods and kits for the prognosis of colorectal cancer
TWI582083B (zh) 2014-10-07 2017-05-11 美國禮來大藥廠 胺基吡啶基氧基吡唑化合物
TWI704151B (zh) 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
US10822337B2 (en) 2015-04-01 2020-11-03 Rigel Pharmaceuticals, Inc. TGF-β inhibitorC
KR20180094036A (ko) 2015-12-15 2018-08-22 브리스톨-마이어스 스큅 컴퍼니 Cxcr4 수용체 길항제
US10604528B2 (en) 2016-07-07 2020-03-31 Crystal Pharmaceutical (Suzhou) Co., Ltd. Galunisertib crystalline form, preparation method thereof and use thereof
CN110582497B (zh) * 2017-03-17 2022-03-11 杭州领业医药科技有限公司 Galunisertib的晶型及其制备方法和药物组合物
CN110582279B (zh) * 2017-03-21 2023-07-14 杭州领业医药科技有限公司 2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的共晶,其制备方法和药物组合物
WO2019042383A1 (zh) * 2017-08-31 2019-03-07 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途
WO2019105082A1 (zh) * 2017-11-30 2019-06-06 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途
WO2019137027A1 (zh) * 2018-01-12 2019-07-18 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途
EP3827010A4 (en) 2018-07-23 2022-03-16 Brise Pharmaceuticals Co., Ltd. BISPHOSPHONATE-DRUG CONJUGATES
KR20210110316A (ko) 2018-12-27 2021-09-07 넥시스 테라퓨틱스 인코포레이티드 암의 치료를 위한 tgf-베타 r1(alk5) 억제제로서의(피리딘-2-일)아민 유도체
WO2020201362A2 (en) 2019-04-02 2020-10-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
CN113557236B (zh) * 2019-06-10 2022-05-10 中国科学院广州生物医药与健康研究院 一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物
WO2021142086A1 (en) 2020-01-08 2021-07-15 Synthis Therapeutics, Inc. Alk5 inhibitor conjugates and uses thereof
KR20220143063A (ko) 2020-02-19 2022-10-24 남미 테라퓨틱스, 인크. 암의 치료에 유용한 TGFβ 길항제 전구약물을 함유하는 제제화된 및/또는 공동-제제화된 리포솜 조성물 및 그의 방법

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
DK1206474T3 (da) * 1999-08-27 2004-10-04 Abbott Lab Sulfonylphenylpyrazolforbindelser anvendelige som cox-2-inhibitorer
SI1397364T1 (sl) * 2001-05-24 2007-12-31 Lilly Co Eli Novi pirolni derivati kot farmacevtske uäśinkovine
EP1567528A1 (en) 2002-11-21 2005-08-31 Eli Lilly And Company Mixed lineage kinase modulators

Also Published As

Publication number Publication date
US20080027102A1 (en) 2008-01-31
CY1106283T1 (el) 2011-10-12
AU2003291643B2 (en) 2010-05-13
DE60308893T2 (de) 2007-03-15
HRP20050436A2 (en) 2005-10-31
NO20053045L (no) 2005-06-21
JP2006514012A (ja) 2006-04-27
EA200500859A1 (ru) 2005-10-27
MXPA05005432A (es) 2005-08-03
KR101057282B1 (ko) 2011-08-16
EG25822A (en) 2012-08-23
KR20050083945A (ko) 2005-08-26
CA2501322A1 (en) 2004-06-10
DK1565471T3 (da) 2007-02-05
ES2273046T3 (es) 2007-05-01
HRP20050436B1 (hr) 2013-11-08
EP1565471B1 (en) 2006-10-04
JP4542906B2 (ja) 2010-09-15
DE60308893D1 (de) 2006-11-16
US7834029B2 (en) 2010-11-16
HK1081948A1 (en) 2006-05-26
NO331403B1 (no) 2011-12-19
WO2004048382A1 (en) 2004-06-10
ZA200503121B (en) 2006-07-26
PT1565471E (pt) 2007-01-31
ECSP055807A (es) 2005-08-11
CN100345852C (zh) 2007-10-31
EP1565471A1 (en) 2005-08-24
CR7830A (es) 2005-06-20
EA008387B1 (ru) 2007-04-27
IL168190A (en) 2011-01-31
AU2003291643A1 (en) 2004-06-18
ATE341550T1 (de) 2006-10-15
CA2501322C (en) 2011-05-10
UA80571C2 (en) 2007-10-10
US20060040983A1 (en) 2006-02-23
US7265225B2 (en) 2007-09-04
BR0315337A (pt) 2005-08-16
NZ538942A (en) 2007-01-26
CN1714090A (zh) 2005-12-28
PL376797A1 (pl) 2006-01-09
PL227840B1 (pl) 2018-01-31

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