KR101057282B1 - 퀴놀리닐-피롤로피라졸 - Google Patents

퀴놀리닐-피롤로피라졸 Download PDF

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Publication number
KR101057282B1
KR101057282B1 KR1020057009199A KR20057009199A KR101057282B1 KR 101057282 B1 KR101057282 B1 KR 101057282B1 KR 1020057009199 A KR1020057009199 A KR 1020057009199A KR 20057009199 A KR20057009199 A KR 20057009199A KR 101057282 B1 KR101057282 B1 KR 101057282B1
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South Korea
Prior art keywords
tgf
cancer
pyridin
cell
methyl
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Expired - Fee Related
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Korean (ko)
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KR20050083945A (ko
Inventor
더글라스 웨이드 베이트
제이슨 스코트 소여
조나단 마이클 윙글링
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일라이 릴리 앤드 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • 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)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020057009199A 2002-11-22 2003-11-10 퀴놀리닐-피롤로피라졸 Expired - Fee Related KR101057282B1 (ko)

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
KR20050083945A KR20050083945A (ko) 2005-08-26
KR101057282B1 true KR101057282B1 (ko) 2011-08-16

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KR1020057009199A Expired - Fee Related KR101057282B1 (ko) 2002-11-22 2003-11-10 퀴놀리닐-피롤로피라졸

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

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AR039241A1 (es) 2002-04-04 2005-02-16 Biogen Inc Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos
EP1567527A1 (en) * 2002-11-27 2005-08-31 Eli Lilly And Company Condensed pyrazolo derivatives
MX2008001020A (es) 2005-07-22 2008-03-25 Lilly Co Eli Un monohidrato de pirrolo[1-2-b]pirazol piridin quinolin substituido como inhibidor de factor de crecimiento de transformacion-beta (tgf-beta).
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
WO2008060371A1 (en) 2006-10-03 2008-05-22 Genzyme Corporation USE OF TGF-β ANTAGONISTS TO TREAT INFANTS AT RISK OF DEVELOPING BRONCHOPULMONARY DYSPLASIA
ES2435430T3 (es) * 2006-10-16 2013-12-19 Thesan Pharmaceuticals, Inc. Pirazolil tienopiridinas terapéuticas
US9102614B2 (en) 2010-07-02 2015-08-11 Gilead Sciences, Inc. Naphth-2-ylacetic acid derivatives to treat AIDS
WO2012003498A1 (en) 2010-07-02 2012-01-05 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
PE20141066A1 (es) 2011-04-21 2014-09-05 Gilead Sciences Inc Compuestos de benzotiazol
EP2737083A1 (en) 2011-07-27 2014-06-04 INSERM (Institut National de la Santé et de la Recherche Scientifique) Methods for diagnosing and treating myhre syndrome
BR112014009789A2 (pt) 2011-10-26 2017-04-25 Seattle Children's Res Inst cisteamina no tratamento da doença fibrótica
US9782452B2 (en) 2011-11-22 2017-10-10 Cornell University Methods for stimulating hematopoietic recovery by inhibiting TGFβ signaling
WO2013103738A1 (en) 2012-01-04 2013-07-11 Gilead Sciences, Inc. Napthalene 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
PH12014500842A1 (en) 2012-04-20 2014-06-09 Gilead Sciences Inc Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection
WO2014055998A1 (en) 2012-10-05 2014-04-10 Kadmon Corporation, Llc Human anti-vegfr-2/kdr antibodies
ES2791627T3 (es) 2012-11-12 2020-11-05 Inst Catalana Recerca Estudis Avancats Métodos y kits para el pronóstico del cáncer colorrectal
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
WO2016123573A1 (en) 2015-01-30 2016-08-04 President And Fellows Of Harvard College Peritumoral and intratumoral materials for cancer therapy
ES2918924T3 (es) 2015-04-01 2022-07-21 Rigel Pharmaceuticals Inc Inhibidores de TGF-beta
US10450318B2 (en) 2015-12-15 2019-10-22 Bristol-Myers Squibb Company CXCR4 receptor antagonists
WO2018006870A1 (zh) * 2016-07-07 2018-01-11 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途
US11111248B2 (en) 2017-03-17 2021-09-07 Hangzhou Solipharma Co., Ltd. Crystal form of 2-(6-methyl-pyridin-2-yl)-3-yl-[6-amido-quinolin-4-yl]-5,6-dihydro-4H-pyrrolo[1,2-B]pyrazole, preparation method therefor and pharmaceutical composition thereof
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
EP3827010B1 (en) 2018-07-23 2025-08-27 Brise Pharmaceuticals Co., Ltd. Bisphosphonate drug conjugates
CN113348167A (zh) 2018-12-27 2021-09-03 奈可萨斯医药有限公司 用于治疗癌症的作为TGF-βR1(ALK5)抑制剂的(吡啶-2-基)胺衍生物
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
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
JP2023509760A (ja) 2020-01-08 2023-03-09 シンシス セラピューティクス，インコーポレイテッド Ａｌｋ５阻害剤複合体およびその使用
AU2021223336A1 (en) 2020-02-19 2022-10-06 Nammi Therapeutics, Inc. Formulated and/or co-formulated liposome compositions containing TGFB antagonist prodrugs useful in the treatment of cancer and methods thereof
WO2024258967A1 (en) 2023-06-13 2024-12-19 Synthis Therapeutics, Inc. Anti-cd5 antibodies and their uses
GB202309553D0 (en) 2023-06-24 2023-08-09 Ucl Business Ltd Compostions and uses thereof

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US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
EP1206474B1 (en) * 1999-08-27 2004-05-26 Abbott Laboratories Sulfonylphenylpyrazole compounds useful as cox-2 inhibitors
ES2289116T3 (es) 2001-05-24 2008-02-01 Eli Lilly And Company Nuevos derivados de pirrol como agentes farmaceuticos.
EP1567528A1 (en) 2002-11-21 2005-08-31 Eli Lilly And Company Mixed lineage kinase modulators

Also Published As

Publication number Publication date
DK1565471T3 (da) 2007-02-05
JP4542906B2 (ja) 2010-09-15
US7834029B2 (en) 2010-11-16
HK1081948A1 (en) 2006-05-26
EP1565471B1 (en) 2006-10-04
JP2006514012A (ja) 2006-04-27
CN1714090A (zh) 2005-12-28
CY1106283T1 (el) 2011-10-12
PL376797A1 (pl) 2006-01-09
US20080027102A1 (en) 2008-01-31
BR0315337A (pt) 2005-08-16
HRP20050436B1 (hr) 2013-11-08
ES2273046T3 (es) 2007-05-01
CN100345852C (zh) 2007-10-31
MXPA05005432A (es) 2005-08-03
EA200500859A1 (ru) 2005-10-27
DE60308893T2 (de) 2007-03-15
CO5570677A2 (es) 2005-10-31
KR20050083945A (ko) 2005-08-26
EA008387B1 (ru) 2007-04-27
IL168190A (en) 2011-01-31
ATE341550T1 (de) 2006-10-15
CR7830A (es) 2005-06-20
HRP20050436A2 (en) 2005-10-31
AU2003291643A1 (en) 2004-06-18
WO2004048382A1 (en) 2004-06-10
PT1565471E (pt) 2007-01-31
US20060040983A1 (en) 2006-02-23
EG25822A (en) 2012-08-23
NO20053045L (no) 2005-06-21
CA2501322A1 (en) 2004-06-10
DE60308893D1 (de) 2006-11-16
US7265225B2 (en) 2007-09-04
CA2501322C (en) 2011-05-10
ECSP055807A (es) 2005-08-11
EP1565471A1 (en) 2005-08-24
ZA200503121B (en) 2006-07-26
NZ538942A (en) 2007-01-26
NO331403B1 (no) 2011-12-19
UA80571C2 (en) 2007-10-10
PL227840B1 (pl) 2018-01-31
AU2003291643B2 (en) 2010-05-13

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