UA80571C2 - Quinolinyl-pyrrolopyrazoles - Google Patents
Quinolinyl-pyrrolopyrazoles Download PDFInfo
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- UA80571C2 UA80571C2 UAA200504767A UA2005004767A UA80571C2 UA 80571 C2 UA80571 C2 UA 80571C2 UA A200504767 A UAA200504767 A UA A200504767A UA 2005004767 A UA2005004767 A UA 2005004767A UA 80571 C2 UA80571 C2 UA 80571C2
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- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
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US42889302P | 2002-11-22 | 2002-11-22 | |
PCT/US2003/032747 WO2004048382A1 (en) | 2002-11-22 | 2003-11-10 | Quinolinyl-pyrrolopyrazoles |
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UA80571C2 true UA80571C2 (en) | 2007-10-10 |
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UAA200504767A UA80571C2 (en) | 2002-11-22 | 2003-10-11 | Quinolinyl-pyrrolopyrazoles |
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JP (1) | JP4542906B2 (xx) |
KR (1) | KR101057282B1 (xx) |
CN (1) | CN100345852C (xx) |
AT (1) | ATE341550T1 (xx) |
AU (1) | AU2003291643B2 (xx) |
BR (1) | BR0315337A (xx) |
CA (1) | CA2501322C (xx) |
CO (1) | CO5570677A2 (xx) |
CR (1) | CR7830A (xx) |
CY (1) | CY1106283T1 (xx) |
DE (1) | DE60308893T2 (xx) |
DK (1) | DK1565471T3 (xx) |
EA (1) | EA008387B1 (xx) |
EC (1) | ECSP055807A (xx) |
EG (1) | EG25822A (xx) |
ES (1) | ES2273046T3 (xx) |
HK (1) | HK1081948A1 (xx) |
HR (1) | HRP20050436B1 (xx) |
IL (1) | IL168190A (xx) |
MX (1) | MXPA05005432A (xx) |
NO (1) | NO331403B1 (xx) |
NZ (1) | NZ538942A (xx) |
PL (1) | PL227840B1 (xx) |
PT (1) | PT1565471E (xx) |
UA (1) | UA80571C2 (xx) |
WO (1) | WO2004048382A1 (xx) |
ZA (1) | ZA200503121B (xx) |
Families Citing this family (33)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004050659A1 (en) * | 2002-11-27 | 2004-06-17 | Eli Lilly And Company | Novel compounds as pharmaceutical agents |
CA2616196C (en) | 2005-07-22 | 2012-08-21 | 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 |
ES2647472T3 (es) | 2006-10-03 | 2017-12-21 | Genzyme Corporation | Anticuerpos contra TGF-BETA para uso en el tratamiento de lactantes con riesgo de desarrollar displasia broncopulmonar |
ES2559521T3 (es) * | 2006-10-16 | 2016-02-12 | Thesan Pharmaceuticals, Inc. | Pirazolil tienopiridinas terapéuticas |
CN103140474A (zh) | 2010-07-02 | 2013-06-05 | 吉里德科学公司 | 治疗aids的萘-2-基乙酸衍生物 |
EA201291301A1 (ru) | 2010-07-02 | 2013-05-30 | Джилид Сайэнс, Инк. | Производные 2-хинолинилуксусной кислоты в качестве противовирусных соединений против вич |
US8871744B2 (en) | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
AU2012245187B2 (en) | 2011-04-21 | 2016-06-30 | 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 |
AU2011379972B2 (en) | 2011-10-26 | 2016-05-12 | 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 |
NZ622769A (en) | 2012-04-20 | 2017-06-30 | Gilead Sciences Inc | Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection |
US10023640B2 (en) | 2012-10-05 | 2018-07-17 | 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 |
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 |
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 |
CN109548403A (zh) * | 2016-07-07 | 2019-03-29 | 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 |
EP3827010A4 (en) | 2018-07-23 | 2022-03-16 | Brise Pharmaceuticals Co., Ltd. | BISPHOSPHONATE-DRUG CONJUGATES |
EA202191619A1 (ru) | 2018-12-27 | 2021-09-28 | Нексис Терапьютикс, Инк. | Производные (пиридин-2-ил)амина в качестве ингибиторов tgfбета r1 (alk5) для лечения злокачественных новообразований |
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 |
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 |
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 |
CA3170142A1 (en) | 2020-02-19 | 2021-08-26 | Nammi Therapeutics, Inc. | Formulated and/or co-formulated liposome compositions containing tfgb antagonist prodrugs useful in the treatment of cancer and methods thereof |
Family Cites Families (4)
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 |
ES2222919T3 (es) * | 1999-08-27 | 2005-02-16 | Abbott Laboratories | Compuestos sulfonilfenilpirazoles utiles como inhibidores de cox-2. |
SK287857B6 (sk) * | 2001-05-24 | 2012-01-04 | Eli Lilly And Company | Novel pyrrole derivatives as pharmaceutical agents |
CA2506799A1 (en) | 2002-11-21 | 2004-06-10 | Eli Lilly And Company | Mixed lineage kinase modulators |
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- 2003-11-10 DK DK03768531T patent/DK1565471T3/da active
- 2003-11-10 CN CNB2003801038400A patent/CN100345852C/zh not_active Expired - Fee Related
- 2003-11-10 EP EP03768531A patent/EP1565471B1/en not_active Expired - Lifetime
- 2003-11-10 MX MXPA05005432A patent/MXPA05005432A/es active IP Right Grant
- 2003-11-10 WO PCT/US2003/032747 patent/WO2004048382A1/en active IP Right Grant
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- 2003-11-10 CA CA2501322A patent/CA2501322C/en not_active Expired - Fee Related
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- 2003-11-10 DE DE60308893T patent/DE60308893T2/de not_active Expired - Lifetime
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- 2003-11-10 KR KR1020057009199A patent/KR101057282B1/ko not_active IP Right Cessation
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- 2003-11-10 AU AU2003291643A patent/AU2003291643B2/en not_active Ceased
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