DE60308893T2 - Quinolinyl-pyrrolopyrazole - Google Patents

Quinolinyl-pyrrolopyrazole Download PDF

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Publication number
DE60308893T2
DE60308893T2 DE60308893T DE60308893T DE60308893T2 DE 60308893 T2 DE60308893 T2 DE 60308893T2 DE 60308893 T DE60308893 T DE 60308893T DE 60308893 T DE60308893 T DE 60308893T DE 60308893 T2 DE60308893 T2 DE 60308893T2
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DE
Germany
Prior art keywords
tgf
cell
cancer
pyrrolo
tumor
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.)
Expired - Lifetime
Application number
DE60308893T
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German (de)
English (en)
Other versions
DE60308893D1 (de
Inventor
Wade Douglas Frankfort BEIGHT
SCOTT Jason Indianapolis SAWYER
Michael Jonathan Fishers YINGLING
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Eli Lilly and Co
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Eli Lilly and Co
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Publication of DE60308893D1 publication Critical patent/DE60308893D1/de
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Publication of DE60308893T2 publication Critical patent/DE60308893T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DE60308893T 2002-11-22 2003-11-10 Quinolinyl-pyrrolopyrazole Expired - Lifetime DE60308893T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42889302P 2002-11-22 2002-11-22
US428893P 2002-11-22
PCT/US2003/032747 WO2004048382A1 (en) 2002-11-22 2003-11-10 Quinolinyl-pyrrolopyrazoles

Publications (2)

Publication Number Publication Date
DE60308893D1 DE60308893D1 (de) 2006-11-16
DE60308893T2 true DE60308893T2 (de) 2007-03-15

Family

ID=32393478

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60308893T Expired - Lifetime DE60308893T2 (de) 2002-11-22 2003-11-10 Quinolinyl-pyrrolopyrazole

Country Status (28)

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

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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
WO2004050659A1 (en) * 2002-11-27 2004-06-17 Eli Lilly And Company Novel compounds as pharmaceutical agents
PT1910370E (pt) * 2005-07-22 2015-06-30 Lilly Co Eli Um pirrolo[1,2-b]pirazole mono-hidratado substituído com piridina e quinolina como inibidor do 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
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.
ES2559521T3 (es) * 2006-10-16 2016-02-12 Thesan Pharmaceuticals, Inc. Pirazolil tienopiridinas terapéuticas
MX2012015097A (es) 2010-07-02 2013-05-28 Gilead Sciences Inc Derivados de acido naft-2-ilacetico para tratar 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
US20140308275A1 (en) 2011-07-27 2014-10-16 Inserm (Institut National De La Sante Et De La Recherche Medicale Methods for diagnosing and treating myhre syndrome
AU2011379972B2 (en) 2011-10-26 2016-05-12 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
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
UY34750A (es) 2012-04-20 2013-11-29 Gilead Sciences Inc ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
EA039595B1 (ru) 2012-10-05 2022-02-15 Кадмон Корпорейшн, Ллк Нуклеиновые кислоты, кодирующие человеческие анти-vegfr-2/kdr-антитела
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
US11786457B2 (en) 2015-01-30 2023-10-17 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
JP6856648B2 (ja) 2015-12-15 2021-04-07 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Cxcr4受容体アンタゴニスト
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
WO2018170724A1 (zh) 2017-03-21 2018-09-27 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
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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
WO2021167703A1 (en) 2020-02-19 2021-08-26 Nammi Therapeutics, Inc. Formulated and/or co-formulated liposome compositions containing tgfb antagonist prodrugs useful in the treatment of cancer and methods thereof
CN121712526A (zh) 2023-06-13 2026-03-20 辛瑟斯治疗股份有限公司 抗cd5抗体及其用途
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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
SK287857B6 (sk) * 2001-05-24 2012-01-04 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents
AU2003298611A1 (en) 2002-11-21 2004-06-18 Eli Lilly And Company Mixed lineage kinase modulators

Also Published As

Publication number Publication date
BR0315337A (pt) 2005-08-16
US20080027102A1 (en) 2008-01-31
ECSP055807A (es) 2005-08-11
CN100345852C (zh) 2007-10-31
CN1714090A (zh) 2005-12-28
CY1106283T1 (el) 2011-10-12
IL168190A (en) 2011-01-31
EG25822A (en) 2012-08-23
HRP20050436B1 (hr) 2013-11-08
NO331403B1 (no) 2011-12-19
WO2004048382A1 (en) 2004-06-10
EP1565471A1 (en) 2005-08-24
DE60308893D1 (de) 2006-11-16
CA2501322C (en) 2011-05-10
EA008387B1 (ru) 2007-04-27
US20060040983A1 (en) 2006-02-23
KR20050083945A (ko) 2005-08-26
DK1565471T3 (da) 2007-02-05
CA2501322A1 (en) 2004-06-10
JP4542906B2 (ja) 2010-09-15
PT1565471E (pt) 2007-01-31
US7265225B2 (en) 2007-09-04
ATE341550T1 (de) 2006-10-15
US7834029B2 (en) 2010-11-16
MXPA05005432A (es) 2005-08-03
KR101057282B1 (ko) 2011-08-16
HK1081948A1 (en) 2006-05-26
NZ538942A (en) 2007-01-26
EP1565471B1 (en) 2006-10-04
JP2006514012A (ja) 2006-04-27
EA200500859A1 (ru) 2005-10-27
ZA200503121B (en) 2006-07-26
NO20053045L (no) 2005-06-21
AU2003291643B2 (en) 2010-05-13
HRP20050436A2 (en) 2005-10-31
PL376797A1 (pl) 2006-01-09
PL227840B1 (pl) 2018-01-31
AU2003291643A1 (en) 2004-06-18
CR7830A (es) 2005-06-20
UA80571C2 (en) 2007-10-10
CO5570677A2 (es) 2005-10-31
ES2273046T3 (es) 2007-05-01

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8364 No opposition during term of opposition
8328 Change in the person/name/address of the agent

Representative=s name: KROHER, STROBEL RECHTS- UND PATENTANWAELTE, 80336

8328 Change in the person/name/address of the agent

Representative=s name: DR. SCHOEN & PARTNER, 80336 MUENCHEN