ECSP109957A - Derivados de pirimidinil-piridazinona. - Google Patents

Derivados de pirimidinil-piridazinona.

Info

Publication number
ECSP109957A
ECSP109957A EC2010009957A ECSP109957A ECSP109957A EC SP109957 A ECSP109957 A EC SP109957A EC 2010009957 A EC2010009957 A EC 2010009957A EC SP109957 A ECSP109957 A EC SP109957A EC SP109957 A ECSP109957 A EC SP109957A
Authority
EC
Ecuador
Prior art keywords
piridazinona
pirimidinil
derivatives
tumors
treatment
Prior art date
Application number
EC2010009957A
Other languages
English (en)
Inventor
Dieter Dorsch
Oliver Schadt
Andree Blaukat
Frank Stieber
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of ECSP109957A publication Critical patent/ECSP109957A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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Abstract

Los compuestos seleccionados del grupo de acuerdo con la reivindicación 1 son inhibidores de las tirosina quinasas, en especial de la Met-quinasa, y pueden utilizarse, por ejemplo, para el tratamiento de tumores...
EC2010009957A 2007-07-12 2010-02-10 Derivados de pirimidinil-piridazinona. ECSP109957A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102007032507A DE102007032507A1 (de) 2007-07-12 2007-07-12 Pyridazinonderivate
PCT/EP2008/003473 WO2009006959A1 (de) 2007-07-12 2008-04-29 Pyridazinonderivate

Publications (1)

Publication Number Publication Date
ECSP109957A true ECSP109957A (es) 2010-03-31

Family

ID=39638671

Family Applications (2)

Application Number Title Priority Date Filing Date
EC2010009953A ECSP109953A (es) 2007-07-12 2010-02-09 Derivados de piridazinona
EC2010009957A ECSP109957A (es) 2007-07-12 2010-02-10 Derivados de pirimidinil-piridazinona.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EC2010009953A ECSP109953A (es) 2007-07-12 2010-02-09 Derivados de piridazinona

Country Status (36)

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US (8) US8580781B2 (es)
EP (3) EP2164843B1 (es)
JP (2) JP5426543B2 (es)
KR (2) KR101553418B1 (es)
CN (2) CN101743241B (es)
AR (2) AR066543A1 (es)
AU (2) AU2008274670B2 (es)
BR (2) BRPI0814616B1 (es)
CA (2) CA2693600C (es)
CL (1) CL2008001392A1 (es)
CO (2) CO6170360A2 (es)
CY (3) CY1113137T1 (es)
DE (1) DE102007032507A1 (es)
DK (3) DK2164843T3 (es)
EA (2) EA016782B1 (es)
EC (2) ECSP109953A (es)
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Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007038957A1 (de) * 2007-08-17 2009-02-19 Merck Patent Gmbh 6-Thioxo-pyridazinderivate
DE102007041115A1 (de) * 2007-08-30 2009-03-05 Merck Patent Gmbh Thiadiazinonderivate
DE102007061963A1 (de) * 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
DE102008019907A1 (de) * 2008-04-21 2009-10-22 Merck Patent Gmbh Pyridazinonderivate
DE102008028905A1 (de) * 2008-06-18 2009-12-24 Merck Patent Gmbh 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate
DE102008037790A1 (de) * 2008-08-14 2010-02-18 Merck Patent Gmbh Bicyclische Triazolderivate
PT2361250E (pt) * 2008-12-22 2013-11-11 Merck Patent Gmbh Novas formas polimórficas de di-hidrogenofosfato de 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etoxi)-pirimidin-2-il]-benzil}-2h-piridazin-3-ona e processos de fabrico das mesmas
DE102008062826A1 (de) * 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
DE102009003954A1 (de) * 2009-01-07 2010-07-08 Merck Patent Gmbh Pyridazinonderivate
WO2010078897A1 (en) 2009-01-08 2010-07-15 Merck Patent Gmbh Novel polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof
EP2221053A1 (de) * 2009-02-20 2010-08-25 Albert-Ludwigs-Universität Freiburg Pharmazeutische Zusammensetzung enthaltend Hemmstoffe der Proteinmethyltransferase I und deren Verwendung zur Behandlung von Tumorerkrankungen
US20130315895A1 (en) 2010-07-01 2013-11-28 Takeda Pharmaceutical Company Limited COMBINATION OF A cMET INHIBITOR AND AN ANTIBODY TO HGF AND/OR cMET
DE102011101482B4 (de) 2011-05-13 2017-05-11 Thyssenkrupp Presta Aktiengesellschaft Sensoranordnung für eine drehbare Welle
RU2014141934A (ru) * 2012-03-19 2016-05-20 Мерк Патент Гмбх Комбинация производного 6-оксо-1,6-дигидро-пиридазина, которая обладает противораковым действием с другими противоопухолевыми соединениями
KR101842645B1 (ko) 2012-04-12 2018-03-29 한국화학연구원 신규한 히드라진온이 치환된 피리미딘 유도체 및 그의 용도
RU2684407C2 (ru) * 2012-10-11 2019-04-09 Мерк Патент Гмбх Комбинация производного 6-оксо-1,6-дигидро-пиридазина, имеющего противораковую активность, с мек ингибитором
RS56485B1 (sr) * 2012-11-02 2018-01-31 Merck Patent Gmbh 6-okso-1,6-dihidro-piridazin derivat za upotrebu u tretmanu hepatocelularnog karcinoma (hcc)
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
JP2016507496A (ja) * 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． ブロモドメイン阻害剤としての新規複素環式化合物
CN104968658B (zh) * 2013-02-07 2017-08-01 默克专利股份公司 哒嗪酮‑酰胺衍生物
EP3674300B1 (en) 2013-06-21 2022-10-12 Zenith Epigenetics Ltd. Novel bicyclic bromodomain inhibitors
EP3010918B1 (en) 2013-06-21 2018-08-15 Zenith Epigenetics Ltd. Novel substituted bicyclic compounds as bromodomain inhibitors
KR20160038008A (ko) 2013-07-31 2016-04-06 제니쓰 에피제네틱스 코포레이션 브로모도메인 억제제로서 신규 퀴나졸리논
CA2927567C (en) * 2013-10-18 2022-04-26 Celgene Quanticel Research, Inc. Bromodomain inhibitors
RS59067B1 (sr) * 2013-12-04 2019-09-30 Galmed Res & Development Ltd Soli aramchol-a
AU2014377079A1 (en) * 2014-01-07 2016-08-18 Merck Patent Gmbh A 6-oxo-1,6-dihydro-pyridazine derivative for the use for the treatment of renal cell carcinoma (RCC)
EP3091979A1 (en) * 2014-01-07 2016-11-16 Merck Patent GmbH Combination of a 6-oxo- 1,6-dihydro-pyridazine derivate having anti-cancer activity with gefitinib
US9919034B2 (en) 2014-03-28 2018-03-20 Tamir Biotechnology, Inc. Methods of treating and prophylactically protecting mammalian patients infected by viruses classified in Baltimore group V
BR112016022722B8 (pt) * 2014-04-01 2023-11-21 Merck Sharp & Dohme Composto, composição farmacêutica que o comprende e uso do mesmo
US9642794B2 (en) * 2014-08-18 2017-05-09 Tamir Biotechnology, Inc. Antiviral pharmaceutical for topical administration
US10835598B2 (en) 2014-08-18 2020-11-17 Orgenesis Inc. Prophylactic protection against viral infections, particularly HIV
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
TWI695837B (zh) 2014-12-04 2020-06-11 比利時商健生藥品公司 作為激酶調節劑之三唑並嗒
US10398774B2 (en) 2014-12-09 2019-09-03 INSERM (Institut National de la Santé et de la Recherche Médicale) Human monoclonal antibodies against AXL
CA2970394C (en) * 2014-12-11 2023-03-14 Merck Patent Gmbh Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with a quinazoline derivative
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
CA2970391A1 (en) * 2014-12-12 2016-06-16 Merck Patent Gmbh Combination of a 6-oxo-1,6-dihydro-pyridazine derivative having anti-cancer activity with an egfr inhibitor
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
WO2016135041A1 (en) 2015-02-26 2016-09-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Fusion proteins and antibodies comprising thereof for promoting apoptosis
WO2016192831A1 (en) 2015-05-29 2016-12-08 Merck Patent Gmbh Compositions of anions and cations with pharmacological activity
KR20180026455A (ko) 2015-06-15 2018-03-12 타미르 바이오테크놀로지 인코포레이티드 눈의 바이러스 감염의 치료를 위한 의약
ES2835301T3 (es) 2016-10-27 2021-06-22 Fujian Cosunter Pharmaceutical Co Ltd Compuesto de piridona como inhibidor de C-MET
KR20190078646A (ko) * 2016-11-18 2019-07-04 머크 샤프 앤드 돔 코포레이션 디아실글리세리드 o-아실트랜스퍼라제 2의 억제제로서 유용한 인다졸 유도체
KR102636384B1 (ko) 2017-08-04 2024-02-14 스카이호크 테라퓨틱스, 인코포레이티드 스플라이싱을 조절하는 방법 및 조성물
ES2946551T3 (es) 2017-10-17 2023-07-20 Palau Pharma S L U Síntesis de compuestos de 4-aminopirimidina
EP3719012B1 (en) 2017-11-24 2024-03-06 Medshine Discovery Inc. N-[4-[(2-amino-4-pyridinyl)oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-1,2,3,4-tetrahydro-2,4-dioxo-5-pyrimidinecarboxamide derivatives as c-met/axl inhibitors for the treatment of tumors
KR102374933B1 (ko) 2018-04-26 2022-03-15 푸젠 코선터 파마슈티컬 컴퍼니 리미티드 c-Met 억제제의 결정형과 이의 염 형태 및 제조 방법
CN108752322A (zh) * 2018-09-12 2018-11-06 广州新民培林医药科技有限公司 一种新型Tepotinib衍生物和制备方法及其在抗肿瘤药物中的应用
CN113272280A (zh) 2018-11-06 2021-08-17 艾知怀斯治疗学公司 哒嗪酮化合物及其用途
DK3877376T3 (da) 2018-11-06 2023-10-02 Edgewise Therapeutics Inc Pyridazinonforbindelser og anvendelser deraf
CA3118908A1 (en) 2018-11-06 2020-05-14 Edgewise Therapeutics, Inc. Pyridazinone compounds and uses thereof
EP3903828A4 (en) 2018-12-21 2022-10-05 Daiichi Sankyo Company, Limited COMBINATION OF AN ANTIBODY-DRUG CONJUGATE AND A KINASE INHIBITOR
KR102660608B1 (ko) * 2019-02-01 2024-04-26 지앙수 아오사이캉 파마수티칼 씨오., 엘티디. c-Met억제제로서 피리미디닐기를 포함하는 삼환식 화합물
KR20210135241A (ko) 2019-02-05 2021-11-12 스카이호크 테라퓨틱스, 인코포레이티드 스플라이싱을 조절하는 방법 및 조성물
KR20210135507A (ko) 2019-02-06 2021-11-15 스카이호크 테라퓨틱스, 인코포레이티드 스플라이싱을 조절하는 방법 및 조성물
AU2020240059A1 (en) * 2019-03-20 2021-10-28 Goldfinch Bio, Inc. Pyridazinones and methods of use thereof
DK3996688T3 (da) 2019-07-10 2023-11-27 Merck Patent Gmbh Farmaceutisk præparat
CN114174298B (zh) * 2019-08-14 2023-08-01 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
WO2022063869A2 (en) 2020-09-24 2022-03-31 Merck Patent Gmbh Compounds for the treatment of viral infections
KR102489160B1 (ko) * 2021-05-26 2023-01-18 주식회사 이노큐어테라퓨틱스 피페리딘디온 유도체
WO2022250350A1 (ko) * 2021-05-26 2022-12-01 주식회사 이노큐어테라퓨틱스 피페리딘디온 유도체
WO2022253935A1 (en) 2021-06-04 2022-12-08 Merck Patent Gmbh Compounds for the treatment of glioblastoma
WO2023091606A1 (en) * 2021-11-17 2023-05-25 Edgewise Therapeutics, Inc. Pyridazinone compounds and uses thereof
CN114394957B (zh) * 2021-12-24 2023-05-09 武汉九州钰民医药科技有限公司 Met抑制剂盐酸特泊替尼的制备方法
WO2024008929A1 (en) 2022-07-08 2024-01-11 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors in combination with hgf-receptor inhibitors for the treatment of cancer
CN115583939A (zh) * 2022-11-04 2023-01-10 苏州莱安医药化学技术有限公司 一种特泊替尼中间体的合成方法
CN116082309B (zh) * 2023-01-04 2023-10-24 广东莱恩医药研究院有限公司 嘧啶衍生物1d228盐酸盐晶型及其制备方法和应用
CN116768868B (zh) * 2023-08-15 2023-12-08 云南省药物研究所 一种哒嗪酮硫代衍生物及其制备方法和应用

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3853946A (en) 1971-11-11 1974-12-10 Hoffmann La Roche Process for the preparation of aminomethylene malononitrile
JPS5795964A (en) 1980-12-04 1982-06-15 Morishita Seiyaku Kk Preparation of 2-substituted-3(2h)-pyridazinone derivative
US4397854A (en) 1981-05-14 1983-08-09 Warner-Lambert Company Substituted 6-phenyl-3(2H)-pyridazinones useful as cardiotonic agents
IL115889A0 (en) 1994-11-14 1996-01-31 Rohm & Haas Pyridazinones and their use as fungicides
US5635494A (en) 1995-04-21 1997-06-03 Rohm And Haas Company Dihydropyridazinones and pyridazinones and their use as fungicides and insecticides
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE19604388A1 (de) 1996-02-07 1997-08-14 Merck Patent Gmbh Arylalkyl-diazinone
KR19990082463A (ko) 1996-02-13 1999-11-25 돈 리사 로얄 혈관 내피 성장 인자 억제제로서의 퀴나졸린유도체
WO1997032856A1 (en) 1996-03-05 1997-09-12 Zeneca Limited 4-anilinoquinazoline derivatives
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
JPH10259176A (ja) 1997-03-17 1998-09-29 Japan Tobacco Inc 血管新生阻害作用を有する新規アミド誘導体及びその用途
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
KR100626605B1 (ko) 1997-11-19 2006-09-22 코와 가부시키가이샤 신규 피리다진 유도체 및 이를 유효성분으로 하는 의약
TWI241295B (en) 1998-03-02 2005-10-11 Kowa Co Pyridazine derivative and medicine containing the same as effect component
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
AUPQ462299A0 (en) 1999-12-13 2000-01-13 Fujisawa Pharmaceutical Co., Ltd. Pyrazolopyridine compound and pharmaceutical use thereof
US6242461B1 (en) 2000-01-25 2001-06-05 Pfizer Inc. Use of aryl substituted azabenzimidazoles in the treatment of HIV and AIDS related diseases
DE10010422A1 (de) 2000-03-03 2001-09-06 Bayer Ag 6-Carboxyphenylpyridazinon-Derivate und ihre Verwendung
EP1289952A1 (en) 2000-05-31 2003-03-12 AstraZeneca AB Indole derivatives with vascular damaging activity
SK52003A3 (en) 2000-07-07 2003-07-01 Angiogene Pharm Ltd Colchinol derivatives as angiogenesis inhibitors, method for their preparation and pharmaceutical composition comprising the same
AU6623301A (en) 2000-07-07 2002-01-21 Angiogene Pharm Ltd Colchinol derivatives as vascular damaging agents
HUP0401984A3 (en) 2001-10-31 2005-06-28 Merck Patent Gmbh Use of type 4 phosphodiesterase inhibitors for preparation of pharmaceutical compositions and combination with other active ingredients
AU2003209321A1 (en) * 2002-01-18 2003-07-30 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
UA77526C2 (en) 2002-06-07 2006-12-15 Sanofi Aventis Substituted derivatives of 1-piperazineacylpiperidine, a method for the preparation thereof and their use in therapy
EP1572693A1 (en) 2002-12-20 2005-09-14 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
MXPA06000091A (es) 2003-07-02 2006-04-07 Sugen Inc Arilmetiltriazolo e imidazopirazinas como inhibidores de c-met.
US7959919B2 (en) * 2003-11-19 2011-06-14 Novelmed Therapeutics, Inc. Method of inhibiting factor B-mediated complement activation
TW200612918A (en) 2004-07-29 2006-05-01 Threshold Pharmaceuticals Inc Lonidamine analogs
US20070015771A1 (en) 2004-07-29 2007-01-18 Threshold Pharmaceuticals, Inc. Lonidamine analogs
US20070043057A1 (en) 2005-02-09 2007-02-22 Threshold Pharmaceuticals, Inc. Lonidamine analogs
WO2007044796A2 (en) 2005-10-11 2007-04-19 Nps Pharmaceuticals, Inc. Pyridazinone compounds as calcilytics
DE102005055354A1 (de) 2005-11-21 2007-10-31 Merck Patent Gmbh Substituierte 5-Phenyl-3,6-dihydro-2-oxo-6H-[1,3,4]thiadiazine
DE102005055355A1 (de) 2005-11-21 2007-10-31 Merck Patent Gmbh 3,6-Dihydro-2-oxo-6H-[1,3,4]thiadiazinderivate
BRPI0619252A2 (pt) 2005-11-30 2011-09-20 Vertex Pharma inibidores de c-met e seus usos
DE102005057924A1 (de) 2005-12-05 2007-06-06 Merck Patent Gmbh Pyridazinonderivate
ME02736B (me) 2005-12-21 2017-10-20 Janssen Pharmaceutica Nv Triazolopiridazini kao modulatori tirozin kinaze
WO2007130383A2 (en) 2006-04-28 2007-11-15 Northwestern University Compositions and treatments using pyridazine compounds and secretases
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
US20090099199A1 (en) 2007-10-16 2009-04-16 Joachim Nozulak Organic compounds
CA2703653A1 (en) 2007-10-25 2009-04-30 Astrazeneca Ab Pyridine and pyrazine derivatives -083
CN101842359A (zh) 2007-10-31 2010-09-22 日产化学工业株式会社 哒嗪酮化合物和p2x7受体抑制剂
CL2008003407A1 (es) 2007-11-16 2010-01-11 Boehringer Ingelheim Int Compuestos derivados de aril- y heteroarilcarbonilo de heterobiciclo sustituido; composicion farmaceutica; procedimiento de preparacion; y su uso en el tratamiento y/o prevencion de trastornos metabolicos, mediado por la inhibicion de la enzima hsd-1.
MX2010006397A (es) 2007-12-21 2010-07-05 Hoffmann La Roche Compuestos heterociclicos antivirales.
GB0725059D0 (en) 2007-12-21 2008-01-30 Syngenta Participations Ag Novel pyridazine derivatives
US7816540B2 (en) 2007-12-21 2010-10-19 Hoffmann-La Roche Inc. Carboxyl- or hydroxyl-substituted benzimidazole derivatives
KR101204213B1 (ko) 2007-12-21 2012-11-26 에프. 호프만-라 로슈 아게 오렉신 수용체 길항제로서의 헤테로아릴 유도체
PE20091339A1 (es) 2007-12-21 2009-09-26 Glaxo Group Ltd Derivados de oxadiazol con actividad sobre receptores s1p1
CL2008003785A1 (es) 2007-12-21 2009-10-09 Du Pont Compuestos derivados de piridazina; composiciones herbicidas que comprenden a dichos compuestos; y método para controlar el crecimiento de la vegetación indeseada.
PE20091669A1 (es) 2007-12-21 2009-12-06 Exelixis Inc Benzofuropirimidinonas
KR20100099742A (ko) 2007-12-21 2010-09-13 아스트라제네카 아베 안드로겐 수용체 관련 병태의 치료에서 사용하기 위한 이환식 유도체
EP2072506A1 (de) 2007-12-21 2009-06-24 Bayer CropScience AG Thiazolyloxyphenylamidine oder Thiadiazolyloxyphenylamidine und deren Verwendung als Fungizide
DE102007061963A1 (de) 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
CA2709650C (en) 2007-12-21 2016-06-07 Palau Pharma, S.A. 4-aminopyrimidine derivatives as histamine h4 receptor antagonists
US8202996B2 (en) 2007-12-21 2012-06-19 Bristol-Myers Squibb Company Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide
EP2242483B1 (en) 2007-12-21 2013-02-20 Synthon B.V. Raloxifene composition
CN101538245B (zh) * 2008-03-18 2011-02-16 中国科学院上海药物研究所 一类哒嗪酮类化合物及其制备方法和制备药物的用途
DE102008019907A1 (de) 2008-04-21 2009-10-22 Merck Patent Gmbh Pyridazinonderivate
WO2009142732A2 (en) * 2008-05-20 2009-11-26 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
DE102008028905A1 (de) 2008-06-18 2009-12-24 Merck Patent Gmbh 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate
EP2323994A1 (en) * 2008-07-25 2011-05-25 Boehringer Ingelheim International GmbH Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
BRPI1013159A2 (pt) * 2009-03-30 2015-09-15 Sumitomo Chemical Co Uso de composto de piridazinona para controle de peste artrópode
AR082590A1 (es) * 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton

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IL203094A (en) 2013-08-29
US20130184260A1 (en) 2013-07-18
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CA2692867A1 (en) 2009-01-15
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BRPI0813707B1 (pt) 2022-02-22
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CA2693600A1 (en) 2009-01-15
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US20120295908A1 (en) 2012-11-22
BRPI0814616A2 (pt) 2015-01-27
JP5426543B2 (ja) 2014-02-26
SI2164843T1 (sl) 2015-02-27
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US20140128396A1 (en) 2014-05-08
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FR22C1024I1 (fr) 2022-07-22
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US20150133452A1 (en) 2015-05-14
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US8921357B2 (en) 2014-12-30
AU2008274670B2 (en) 2013-03-14
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JP5426544B2 (ja) 2014-02-26
EA017281B1 (ru) 2012-11-30
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EP2164843A1 (de) 2010-03-24
AR066543A1 (es) 2009-08-26
US9284300B2 (en) 2016-03-15
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AU2008274534A1 (en) 2009-01-15
IL203091A (en) 2013-10-31
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ES2614283T3 (es) 2017-05-30
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DE102007032507A1 (de) 2009-04-02
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