NO20053045L - Kinolyl-pyrrol-pyrazoler. - Google Patents

Kinolyl-pyrrol-pyrazoler.

Info

Publication number
NO20053045L
NO20053045L NO20053045A NO20053045A NO20053045L NO 20053045 L NO20053045 L NO 20053045L NO 20053045 A NO20053045 A NO 20053045A NO 20053045 A NO20053045 A NO 20053045A NO 20053045 L NO20053045 L NO 20053045L
Authority
NO
Norway
Prior art keywords
pyrazoles
pyrrolo
quinolyl
pyrrolole
blpyrazole
Prior art date
Application number
NO20053045A
Other languages
English (en)
Other versions
NO331403B1 (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.)
Filing date
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

Links

Classifications

    • 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

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)
  • 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)

Abstract

Forbindelsene fmner anvendelse ved behandling av kanser. H,N Formel II 2-(6-metyl-pyridin-2-yl)-3-[fi-amido-klnoIin-4-yl)-S,6-dih}dro-4H-pyrrololl,2- blpyrazol
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 true NO20053045L (no) 2005-06-21
NO331403B1 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 (29)

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

Families Citing this family (33)

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US7405299B2 (en) * 2002-11-27 2008-07-29 Eli Lilly And Company Compounds as pharmaceutical agents
WO2007018818A1 (en) 2005-07-22 2007-02-15 Eli Lilly And Company A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole 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
PL2083863T3 (pl) 2006-10-03 2015-08-31 Genzyme Corp Przeciwciała przeciwko TGF-beta do stosowania w leczeniu niemowląt obarczonych ryzykiem rozwinięcia się dysplazji oskrzelowo-płucnej
MX2009003157A (es) * 2006-10-16 2009-04-03 Pfizer Prod Inc Pirazoliltienopiridinas terapeuticas.
PE20130525A1 (es) 2010-07-02 2013-05-05 Gilead Sciences Inc Derivados de acido 2 quinolinil acetico como compuestos antivirales frente a vih
MA34397B1 (fr) 2010-07-02 2013-07-03 Gilead Sciences Inc Dérivés d'acide napht-2-ylacétique dans le traitement du sida
US8871744B2 (en) 2010-07-21 2014-10-28 B & G Partyers, LLC Compounds and methods for selectively targeting tumor-associated mucins
CA2833377C (en) 2011-04-21 2019-02-12 Gilead Sciences, Inc. Benzothiazole compounds and their pharmaceutical use
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
CA2853484C (en) 2011-10-26 2018-08-21 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
JP6449772B2 (ja) 2012-10-05 2019-01-09 カドモン コーポレイション，リミティド ライアビリティ カンパニー ヒト抗ｖｅｇｆｒ２／ｋｄｒ抗体
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
EP3277673B1 (en) 2015-04-01 2022-05-04 Rigel Pharmaceuticals, Inc. Tgf-beta inhibitors
CN108602829A (zh) 2015-12-15 2018-09-28 百时美施贵宝公司 Cxcr4受体拮抗剂
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
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
US10995083B2 (en) 2017-03-21 2021-05-04 Hangzhou Solipharma Co., Ltd. Cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole, preparation method therefor, and pharmaceutical composition
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
CN112867724B (zh) 2018-07-23 2024-06-04 熙源安健医药(北京)有限公司 二膦酸盐药物缀合物
BR112021007006A2 (pt) 2018-12-27 2021-08-10 Nexys Therapeutics, Inc. derivados de (piridin-2-il)amina como inibidores de tgf-beta r1(alk5) para o tratamento de câncer
US20220177978A1 (en) 2019-04-02 2022-06-09 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
EP4087657A1 (en) 2020-01-08 2022-11-16 Synthis Therapeutics, Inc. Alk5 inhibitor conjugates and uses thereof
EP4096716A1 (en) 2020-02-19 2022-12-07 Nammi Therapeutics, Inc. Formulated and/or co-formulated liposome compositions containing tgfb antagonist prodrugs useful in the treatment of cancer and methods thereof

Family Cites Families (4)

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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
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
PT1397364E (pt) * 2001-05-24 2007-10-22 Lilly Co Eli Novos derivados de pirrole como agentes farmacêuticos
WO2004048383A1 (en) 2002-11-21 2004-06-10 Eli Lilly And Company Mixed lineage kinase modulators

Also Published As

Publication number Publication date
EA008387B1 (ru) 2007-04-27
CA2501322C (en) 2011-05-10
CR7830A (es) 2005-06-20
EP1565471B1 (en) 2006-10-04
WO2004048382A1 (en) 2004-06-10
DE60308893T2 (de) 2007-03-15
EG25822A (en) 2012-08-23
CY1106283T1 (el) 2011-10-12
NO331403B1 (no) 2011-12-19
US7265225B2 (en) 2007-09-04
CN1714090A (zh) 2005-12-28
MXPA05005432A (es) 2005-08-03
UA80571C2 (en) 2007-10-10
HRP20050436A2 (en) 2005-10-31
HRP20050436B1 (hr) 2013-11-08
EA200500859A1 (ru) 2005-10-27
KR101057282B1 (ko) 2011-08-16
CN100345852C (zh) 2007-10-31
JP4542906B2 (ja) 2010-09-15
PL227840B1 (pl) 2018-01-31
ATE341550T1 (de) 2006-10-15
AU2003291643B2 (en) 2010-05-13
ZA200503121B (en) 2006-07-26
DE60308893D1 (de) 2006-11-16
DK1565471T3 (da) 2007-02-05
PL376797A1 (pl) 2006-01-09
PT1565471E (pt) 2007-01-31
JP2006514012A (ja) 2006-04-27
EP1565471A1 (en) 2005-08-24
ES2273046T3 (es) 2007-05-01
CA2501322A1 (en) 2004-06-10
BR0315337A (pt) 2005-08-16
US20080027102A1 (en) 2008-01-31
US7834029B2 (en) 2010-11-16
ECSP055807A (es) 2005-08-11
CO5570677A2 (es) 2005-10-31
NZ538942A (en) 2007-01-26
AU2003291643A1 (en) 2004-06-18
HK1081948A1 (en) 2006-05-26
US20060040983A1 (en) 2006-02-23
KR20050083945A (ko) 2005-08-26
IL168190A (en) 2011-01-31

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