NO331403B1 - Forbindelse av kinolinyl-pyrrolopyrazoliner, farmasoytisk preparat og anvendelse derav - Google Patents

Forbindelse av kinolinyl-pyrrolopyrazoliner, farmasoytisk preparat og anvendelse derav Download PDF

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Publication number
NO331403B1
NO331403B1 NO20053045A NO20053045A NO331403B1 NO 331403 B1 NO331403 B1 NO 331403B1 NO 20053045 A NO20053045 A NO 20053045A NO 20053045 A NO20053045 A NO 20053045A NO 331403 B1 NO331403 B1 NO 331403B1
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Norway
Prior art keywords
tgf
compound
cell
tumor
cancer
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Application number
NO20053045A
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English (en)
Norwegian (no)
Other versions
NO20053045L (no
Inventor
Jason Scott Sawyer
Douglas Wade Beight
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.)
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Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of NO20053045L publication Critical patent/NO20053045L/no
Publication of NO331403B1 publication Critical patent/NO331403B1/no

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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)
  • 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)
NO20053045A 2002-11-22 2005-06-21 Forbindelse av kinolinyl-pyrrolopyrazoliner, farmasoytisk preparat og anvendelse derav NO331403B1 (no)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
NO20053045L NO20053045L (no) 2005-06-21
NO331403B1 true NO331403B1 (no) 2011-12-19

Family

ID=32393478

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20053045A NO331403B1 (no) 2002-11-22 2005-06-21 Forbindelse av kinolinyl-pyrrolopyrazoliner, farmasoytisk preparat og anvendelse derav

Country Status (28)

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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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
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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
KR101057282B1 (ko) 2011-08-16
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
UA80571C2 (en) 2007-10-10
PL227840B1 (pl) 2018-01-31
AU2003291643B2 (en) 2010-05-13

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