AU2003291643B2 - Quinolinyl-pyrrolopyrazoles - Google Patents

Quinolinyl-pyrrolopyrazoles Download PDF

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Publication number
AU2003291643B2
AU2003291643B2 AU2003291643A AU2003291643A AU2003291643B2 AU 2003291643 B2 AU2003291643 B2 AU 2003291643B2 AU 2003291643 A AU2003291643 A AU 2003291643A AU 2003291643 A AU2003291643 A AU 2003291643A AU 2003291643 B2 AU2003291643 B2 AU 2003291643B2
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AU
Australia
Prior art keywords
tgf
pharmaceutically acceptable
compound according
compound
acceptable salt
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2003291643A
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English (en)
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AU2003291643A1 (en
Inventor
Douglas Wade Beight
Jason Scott Sawyer
Jonathan Michael Yingling
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Eli Lilly and Co
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Eli Lilly and Co
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Filing date
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Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of AU2003291643A1 publication Critical patent/AU2003291643A1/en
Application granted granted Critical
Publication of AU2003291643B2 publication Critical patent/AU2003291643B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K31/41Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2003291643A 2002-11-22 2003-11-10 Quinolinyl-pyrrolopyrazoles Ceased AU2003291643B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42889302P 2002-11-22 2002-11-22
US60/428,893 2002-11-22
PCT/US2003/032747 WO2004048382A1 (en) 2002-11-22 2003-11-10 Quinolinyl-pyrrolopyrazoles

Publications (2)

Publication Number Publication Date
AU2003291643A1 AU2003291643A1 (en) 2004-06-18
AU2003291643B2 true AU2003291643B2 (en) 2010-05-13

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2003291643A Ceased AU2003291643B2 (en) 2002-11-22 2003-11-10 Quinolinyl-pyrrolopyrazoles

Country Status (29)

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AU2003290734A1 (en) * 2002-11-27 2004-06-23 Eli Lilly And Company Novel compounds as pharmaceutical agents
RS53999B1 (en) 2005-07-22 2015-10-30 Eli Lilly And Company PIRIDIN HINOLIN SUBSTITUTED PIROLO [1,2-B] PIRAZOLE MONOHYDRATE AS TGF-BETA INHIBITOR
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
MX2009003518A (es) 2006-10-03 2009-08-25 Genzyme Corp Uso de antagonistas de tgf-beta para tratar a los infantes en riesgo de desarrollar displasia brocopulmonar.
ES2435430T3 (es) * 2006-10-16 2013-12-19 Thesan Pharmaceuticals, Inc. Pirazolil tienopiridinas terapéuticas
UY33480A (es) 2010-07-02 2012-02-29 Gilead Sciences Inc Compuestos terapeuticos, composicion farmaceutica que lo comprende, metodo de tratamiento y su uso para la manufactura de un medicamento.
AP2013006707A0 (en) 2010-07-02 2013-02-28 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
ES2615734T3 (es) 2011-04-21 2017-06-08 Gilead Sciences, Inc. Compuestos de benzotiazol y su uso farmacéutico
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
WO2013078286A1 (en) 2011-11-22 2013-05-30 Cornell University Methods for stimulating hematopoietic recovery by inhibiting tgf beta signaling
WO2013103724A1 (en) 2012-01-04 2013-07-11 Gilead Sciences, Inc. 2- (tert - butoxy) -2- (7 -methylquinolin- 6 - yl) acetic acid derivatives for treating aids
WO2013103738A1 (en) 2012-01-04 2013-07-11 Gilead Sciences, Inc. Napthalene acetic acid derivatives against hiv infection
US9096586B2 (en) 2012-04-20 2015-08-04 Gilead Sciences, Inc. Therapeutic compounds
ES2781974T3 (es) 2012-10-05 2020-09-09 Kadmon Corp Llc Anticuerpos humanos anti-VEGFR-2/KDR
US20150289795A1 (en) 2012-11-12 2015-10-15 Institució Catalana De Recerca I Estudis Avançats Methods and kits for the prognosis of colorectal cancer
JO3336B1 (ar) 2014-10-07 2019-03-13 Lilly Co Eli مركبات أمينو بيريديلوكسي بيرازول
TWI704151B (zh) 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
EP3277673B1 (en) 2015-04-01 2022-05-04 Rigel Pharmaceuticals, Inc. Tgf-beta inhibitors
WO2017106291A1 (en) 2015-12-15 2017-06-22 Bristol-Myers Squibb Company Cxcr4 receptor antagonists
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WO2018165979A1 (zh) * 2017-03-17 2018-09-20 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
WO2020019108A1 (en) 2018-07-23 2020-01-30 Guangzhou Othrotx Co., Ltd. Bisphosphonate drug conjugates
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JP2022527972A (ja) 2019-04-02 2022-06-07 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 前悪性病変を有する患者において癌を予測及び予防する方法
WO2020248908A1 (zh) * 2019-06-10 2020-12-17 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
AU2021205893A1 (en) 2020-01-08 2022-06-23 Synthis Therapeutics, Inc. ALK5 inhibitor conjugates and uses thereof
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WO2002094833A1 (en) * 2001-05-24 2002-11-28 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents

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JP2003508401A (ja) * 1999-08-27 2003-03-04 アボット・ラボラトリーズ Cox−2阻害薬として有用なスルホニルフェニルピラゾール化合物
JP2006522735A (ja) 2002-11-21 2006-10-05 イーライ リリー アンド カンパニー ミックス系統キナーゼモジュレータ

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WO2002094833A1 (en) * 2001-05-24 2002-11-28 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents

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Publication number Publication date
PT1565471E (pt) 2007-01-31
EG25822A (en) 2012-08-23
EA008387B1 (ru) 2007-04-27
IL168190A (en) 2011-01-31
CN100345852C (zh) 2007-10-31
CR7830A (es) 2005-06-20
HK1081948A1 (en) 2006-05-26
DK1565471T3 (da) 2007-02-05
JP2006514012A (ja) 2006-04-27
EA200500859A1 (ru) 2005-10-27
CA2501322C (en) 2011-05-10
HRP20050436B1 (hr) 2013-11-08
ECSP055807A (es) 2005-08-11
CY1106283T1 (el) 2011-10-12
CO5570677A2 (es) 2005-10-31
US7834029B2 (en) 2010-11-16
DE60308893D1 (de) 2006-11-16
MXPA05005432A (es) 2005-08-03
UA80571C2 (en) 2007-10-10
PL376797A1 (pl) 2006-01-09
CA2501322A1 (en) 2004-06-10
CN1714090A (zh) 2005-12-28
NO20053045L (no) 2005-06-21
KR20050083945A (ko) 2005-08-26
US20060040983A1 (en) 2006-02-23
US20080027102A1 (en) 2008-01-31
AU2003291643A1 (en) 2004-06-18
NO331403B1 (no) 2011-12-19
KR101057282B1 (ko) 2011-08-16
JP4542906B2 (ja) 2010-09-15
WO2004048382A1 (en) 2004-06-10
PL227840B1 (pl) 2018-01-31
DE60308893T2 (de) 2007-03-15
BR0315337A (pt) 2005-08-16
EP1565471A1 (en) 2005-08-24
ES2273046T3 (es) 2007-05-01
EP1565471B1 (en) 2006-10-04
US7265225B2 (en) 2007-09-04
HRP20050436A2 (en) 2005-10-31
ZA200503121B (en) 2006-07-26
ATE341550T1 (de) 2006-10-15
NZ538942A (en) 2007-01-26

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