TWI345974B - Pyridazine derivatives and their use in the inhibition of stearoyl-coa desaturase - Google Patents

Pyridazine derivatives and their use in the inhibition of stearoyl-coa desaturase

Info

Publication number
TWI345974B
TWI345974B TW093122736A TW93122736A TWI345974B TW I345974 B TWI345974 B TW I345974B TW 093122736 A TW093122736 A TW 093122736A TW 93122736 A TW93122736 A TW 93122736A TW I345974 B TWI345974 B TW I345974B
Authority
TW
Taiwan
Prior art keywords
stearoyl
inhibition
coa desaturase
pyridazine derivatives
pyridazine
Prior art date
Application number
TW093122736A
Other languages
English (en)
Other versions
TW200518753A (en
Inventor
Melwyn Abreo
Mikhail Chafeev
Nagasree Chakka
Sultan Chowdhury
Jian-Min Fu
Heinz W Gschwend
Mark W Holladay
Duanjie Hou
Rajender Kamboj
Vishnumurthy Kodumuru
Wenbao Li
Shifeng Liu
Vandna Raina
Sengen Sun
Shaoyi Sun
Serguei Sviridov
Chi Tu
Michael D Winther
Zaihui Zhang
Original Assignee
Xenon Pharmaceuticals Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34120234&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI345974(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Xenon Pharmaceuticals Inc filed Critical Xenon Pharmaceuticals Inc
Publication of TW200518753A publication Critical patent/TW200518753A/zh
Application granted granted Critical
Publication of TWI345974B publication Critical patent/TWI345974B/zh

Links

Classifications

    • 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
    • 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
    • A61K31/495—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW093122736A 2003-07-30 2004-07-29 Pyridazine derivatives and their use in the inhibition of stearoyl-coa desaturase TWI345974B (en)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US49109503P 2003-07-30 2003-07-30
US54681504P 2004-02-23 2004-02-23
US54678604P 2004-02-23 2004-02-23
US54689804P 2004-02-23 2004-02-23
US54682004P 2004-02-23 2004-02-23
US54693404P 2004-02-23 2004-02-23
US55349104P 2004-03-16 2004-03-16
US55341604P 2004-03-16 2004-03-16
US55340304P 2004-03-16 2004-03-16
US55340404P 2004-03-16 2004-03-16
US55344604P 2004-03-16 2004-03-16

Publications (2)

Publication Number Publication Date
TW200518753A TW200518753A (en) 2005-06-16
TWI345974B true TWI345974B (en) 2011-08-01

Family

ID=34120234

Family Applications (2)

Application Number Title Priority Date Filing Date
TW093122736A TWI345974B (en) 2003-07-30 2004-07-29 Pyridazine derivatives and their use in the inhibition of stearoyl-coa desaturase
TW099123172A TW201038270A (en) 2003-07-30 2004-07-29 Pyridazine derivatives and their use in the inhibition of stearoyl-CoA desaturase

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW099123172A TW201038270A (en) 2003-07-30 2004-07-29 Pyridazine derivatives and their use in the inhibition of stearoyl-CoA desaturase

Country Status (23)

Country Link
US (1) US7335658B2 (zh)
EP (3) EP3042895A1 (zh)
JP (1) JP4808616B2 (zh)
KR (1) KR100934554B1 (zh)
AR (1) AR047557A1 (zh)
AT (1) ATE527242T1 (zh)
AU (2) AU2004261252C1 (zh)
CA (1) CA2533899C (zh)
CY (1) CY1112178T1 (zh)
DK (1) DK1648874T3 (zh)
EC (1) ECSP066313A (zh)
ES (2) ES2568769T3 (zh)
HK (2) HK1097256A1 (zh)
HR (1) HRP20110974T1 (zh)
IL (1) IL173395A (zh)
MA (1) MA28011A1 (zh)
NO (1) NO332822B1 (zh)
NZ (1) NZ545265A (zh)
PL (1) PL1648874T3 (zh)
PT (1) PT1648874E (zh)
TN (1) TNSN06034A1 (zh)
TW (2) TWI345974B (zh)
WO (1) WO2005011655A2 (zh)

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040226056A1 (en) * 1998-12-22 2004-11-11 Myriad Genetics, Incorporated Compositions and methods for treating neurological disorders and diseases
US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
US7390813B1 (en) * 2001-12-21 2008-06-24 Xenon Pharmaceuticals Inc. Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents
AU2004261249B2 (en) * 2003-07-30 2008-09-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
TWI345974B (en) 2003-07-30 2011-08-01 Xenon Pharmaceuticals Inc Pyridazine derivatives and their use in the inhibition of stearoyl-coa desaturase
ES2377406T3 (es) * 2003-07-30 2012-03-27 Xenon Pharmaceuticals Inc. Derivados de la piperazina y su uso como agentes terapéuticos
US7759348B2 (en) * 2003-07-30 2010-07-20 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
CA2553968A1 (en) * 2004-01-23 2005-08-11 Amgen Inc. Vanilloid receptor ligands and their use in treatments of inflammatory and neuropathic pain
US7829712B2 (en) 2004-09-20 2010-11-09 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
BRPI0515483A (pt) 2004-09-20 2008-07-22 Xenon Pharmaceuticals Inc derivados heterocìclicos para o tratamento de doenças mediadas por enzimas estearoil-coa desaturase
AR051090A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
AR051294A1 (es) 2004-09-20 2007-01-03 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
AR051092A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa
CN101083993A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
BRPI0515499A (pt) * 2004-09-20 2008-07-29 Xenon Pharmaceuticals Inc derivados de piridina para a inibição de estearoil-coa-desaturase humana
CN101084207A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
CN101084212A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶介导剂的用途
GT200600046A (es) * 2005-02-09 2006-09-25 Terapia de combinacion
WO2006125179A1 (en) * 2005-05-19 2006-11-23 Xenon Pharmaceuticals Inc. Tricyclic compounds and their uses as therapeutic agents
WO2007044085A2 (en) * 2005-05-19 2007-04-19 Xenon Pharmaceuticals Inc. Heteroaryl compounds and their uses as therapeutic agents
WO2006125180A1 (en) * 2005-05-19 2006-11-23 Xenon Pharmaceuticals Inc. Piperazine derivatives and their uses as therapeutic agents
US8541457B2 (en) * 2005-06-03 2013-09-24 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-CoA desaturase inhibitors
WO2007005763A2 (en) * 2005-07-01 2007-01-11 Novartis Ag Combination of a renin inhibitor and an insulin secretion enhancer or an insulin sensitizer
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor
EP1966183A4 (en) * 2005-12-20 2010-12-29 Merck Frosst Canada Ltd HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A-DELTA-9-DESATURASE
US7989461B2 (en) * 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
WO2007136746A2 (en) * 2006-05-19 2007-11-29 Xenon Pharmaceuticals Inc. Macrocyclic compounds and their uses as stearoyl-coa desaturase
ES2358297T3 (es) 2006-06-05 2011-05-09 Novartis Ag Compuestos orgánicos.
KR20090040478A (ko) 2006-08-24 2009-04-24 노파르티스 아게 ２-(피라진-２-일)-티아졸 및 ２-(１Ｈ-피라졸-３-일)-티아졸 유도체, 및 대사, 심혈관 및 기타 장애의 치료를 위한 스테아로일-ＣｏＡ 데새투라제(ＳＣＤ) 억제제로서의 관련 화합물
US8246433B2 (en) * 2006-08-25 2012-08-21 Alma Mater Sports, Llc Team based fantasy sport contest
WO2008056687A1 (fr) * 2006-11-09 2008-05-15 Daiichi Sankyo Company, Limited Nouveau dérivé de spiropipéridine
US20080182851A1 (en) * 2006-11-20 2008-07-31 Glenmark Pharmaceuticals S.A. Acetylene derivatives as stearoyl coa desaturase inhibitors
US8575167B2 (en) 2007-02-06 2013-11-05 Takeda Pharmaceutical Company Limited Spiro compounds having stearoyl-CoA desaturase action
JO2849B1 (en) 2007-02-13 2015-03-15 جانسين فارماسوتيكا ان. في Dopamine 2 receptor antagonists are rapidly hydrolyzed
JP2010520162A (ja) * 2007-02-28 2010-06-10 スミスクライン ビーチャム コーポレーション ステアロイル−ＣｏＡデサチュラーゼ阻害剤であるチアジアゾール誘導体
DK2148873T3 (da) * 2007-04-23 2012-11-26 Janssen Pharmaceutica Nv 4-alkoxypyridazinderivater som hurtigt dissocierende dopamin 2- receptorantagonister
US8933101B2 (en) * 2007-04-23 2015-01-13 Janssen Pharmaceutica Nv Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists
EP2142529B1 (en) 2007-04-27 2013-12-25 Purdue Pharma LP Trpv1 antagonists and uses thereof
CN101820757A (zh) 2007-06-01 2010-09-01 普林斯顿大学托管委员会 通过调节宿主细胞代谢途径治疗病毒感染
US7842696B2 (en) 2007-06-21 2010-11-30 Forest Laboratories Holdings Limited Piperazine derivatives as inhibitors of stearoyl-CoA desaturase
CN104292144B (zh) 2007-08-08 2017-05-17 台晟医药有限公司 苯氧基吡咯烷衍生物及其应用和组合物
RU2443699C2 (ru) * 2007-09-20 2012-02-27 Айрм Ллк Соединения и композиции в качестве модуляторов активности gpr119
WO2009037542A2 (en) 2007-09-20 2009-03-26 Glenmark Pharmaceuticals, S.A. Spirocyclic compounds as stearoyl coa desaturase inhibitors
EP2231619B1 (en) * 2007-12-11 2014-11-26 F. Hoffmann-La Roche AG Inhibitors of stearoyl-coa desaturase
WO2010012758A1 (en) 2008-07-31 2010-02-04 Janssen Pharmaceutica Nv Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists
US9168248B2 (en) 2009-02-17 2015-10-27 Merck Canada Inc. Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
WO2011011872A1 (en) 2009-07-28 2011-02-03 Merck Frosst Canada Ltd. Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase
WO2011014520A2 (en) 2009-07-29 2011-02-03 Irm Llc Compounds and compositions as modulators of gpr119 activity
US20130012709A1 (en) 2009-09-10 2013-01-10 Centre National De La Recherche Scientifique NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES
US8575168B2 (en) 2009-10-09 2013-11-05 Irm Llc Compounds and compositions as modulators of GPR119 activity
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
US8697739B2 (en) 2010-07-29 2014-04-15 Novartis Ag Bicyclic acetyl-CoA carboxylase inhibitors and uses thereof
RU2621708C2 (ru) 2011-06-22 2017-06-07 ПУРДЬЮ ФАРМА Эл. Пи. Антагонисты trpv1, включающие дигидроксигруппу в качестве заместителя, и их применение
EP2766000A2 (en) 2011-10-15 2014-08-20 F.Hoffmann-La Roche Ag Scd1 antagonists for treating cancer
WO2013144180A1 (en) * 2012-03-28 2013-10-03 Intervet International B.V. Heteroaryl compounds with cyclic bridging unit for use in the treatment helminth infection
CA2873817A1 (en) 2012-05-22 2013-11-28 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Selective inhibitors of undifferentiated cells
WO2014052619A1 (en) 2012-09-27 2014-04-03 Irm Llc Piperidine derivatives and compositions as modulators of gpr119 activity
SG10202110242YA (en) 2015-09-16 2021-10-28 Metacrine Inc Farnesoid x receptor agonists and uses thereof
EP3529245A4 (en) 2016-10-24 2020-12-23 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THE LATEST
EA201991650A1 (ru) 2017-01-06 2020-01-20 Юманити Терапьютикс, Инк. Способы лечения неврологических расстройств
CA3056019A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
US10961198B2 (en) 2017-03-15 2021-03-30 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
US11873298B2 (en) 2017-10-24 2024-01-16 Janssen Pharmaceutica Nv Compounds and uses thereof
PE20211496A1 (es) * 2018-05-09 2021-08-11 Lg Chemical Ltd Nuevo compuesto que presenta actividad inhibidora de enteropeptidasa
CN113056271A (zh) 2018-09-18 2021-06-29 梅塔科林公司 法尼醇x受体激动剂及其用途

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US667452A (en) * 1900-09-08 1901-02-05 John A Hendrickson Computing attachment for pumps.
US2985657A (en) * 1959-10-12 1961-05-23 Paul A J Janssen 1-(aroylalkyl)-4-heterocyclylpiperazines
AT340933B (de) * 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
US5001125A (en) 1984-03-26 1991-03-19 Janssen Pharmaceutica N.V. Anti-virally active pyridazinamines
ES8802151A1 (es) 1985-07-31 1988-04-01 Janssen Pharmaceutica Nv Un procedimiento para la preparacion de nuevos piridazinaminas.
AU1704588A (en) 1987-04-03 1988-11-02 Upjohn Company, The Amino-9,10-secosteroids
CA1338012C (en) 1987-04-27 1996-01-30 John Michael Mccall Pharmaceutically active amines
MY104343A (en) 1987-11-23 1994-03-31 Janssen Pharmaceutica Nv Novel pyridizinamine deravatives
US4994456A (en) 1989-03-01 1991-02-19 Nisshin Flour Milling Co., Ltd. Pyridinecarboxylic acid amide derivatives and pharmaceutical compositions comprising same
IL96891A0 (en) 1990-01-17 1992-03-29 Merck Sharp & Dohme Indole-substituted five-membered heteroaromatic compounds,their preparation and pharmaceutical compositions containing them
US5166147A (en) * 1990-07-09 1992-11-24 The Du Pont Merck Pharmaceutical Company 4-heteroaryl-and 4-aryl-1,4-dihydropyridine, derivatives with calcium agonist and alpha1 -antagonist activity
GB9019143D0 (en) * 1990-09-01 1990-10-17 Bp Chem Int Ltd Thixotropic compositions
EP0520292A1 (de) 1991-06-19 1992-12-30 Hoechst Aktiengesellschaft Chirale Azetidinon-Derivate und ihre Verwendung als Dotierstoffe in Flüssigkristallmischungen
DE4302051A1 (de) 1993-01-26 1994-07-28 Thomae Gmbh Dr K 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
WO1997026258A1 (en) 1996-01-15 1997-07-24 Janssen Pharmaceutica N.V. Angiogenesis inhibiting pyridazinamines
DE19614204A1 (de) 1996-04-10 1997-10-16 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
JPH107572A (ja) 1996-06-17 1998-01-13 Sumitomo Pharmaceut Co Ltd 腫瘍壊死因子産生阻害剤
AU8096798A (en) 1997-06-27 1999-01-19 Resolution Pharmaceuticals Inc. Dopamine d4 receptor ligands
ATE229945T1 (de) 1998-03-19 2003-01-15 Upjohn Co Zur behandlung von cmv infektionen geeignete 1,3, 4-thiadiazole
KR20010087738A (ko) * 1998-10-21 2001-09-21 다케다 야쿠힌 고교 가부시키가이샤 축합 피리다진 유도체, 이의 제조 방법 및 용도
AU1455500A (en) 1998-10-29 2000-05-22 Trega Biosciences, Inc. Oxadiazole, thiadiazole and triazole derivatives and combinatorial libraries thereof
AU2319100A (en) 1999-01-28 2000-08-18 Nippon Shinyaku Co. Ltd. Amide derivatives and drug compositions
JP4676062B2 (ja) 1999-01-29 2011-04-27 アボット・ラボラトリーズ ニコチン性アセチルコリン受容体リガンドとしてのジアザ２環式誘導体
DK1394150T3 (da) 1999-02-24 2011-03-21 Hoffmann La Roche 4-phenylpyridinderivater og deres anvendelse som NK-1-receptorantagonister
BR0009650A (pt) 1999-04-09 2002-01-02 Meiji Seika Kaisha Composto, composição farmacêutica, processos para inibir a secreção de uma lipoproteìna contendo apolipoproteìna b, para inibir a biossìntese de triglicerìdeos e para prevenir ou tratar hiperlipidemia, doenças arterioscleróticas e pancreatite, e, uso do composto
JP3637961B2 (ja) * 1999-09-16 2005-04-13 田辺製薬株式会社 芳香族含窒素六員環化合物
US6677452B1 (en) 1999-09-30 2004-01-13 Lion Bioscience Ag Pyridine carboxamide or sulfonamide derivatives and combinatorial libraries thereof
AU1887401A (en) 1999-12-14 2001-06-25 Nippon Shinyaku Co. Ltd. Medicinal composition
EP2172560A3 (en) * 2000-02-24 2010-09-29 Xenon Pharmaceuticals Inc. stearoyl-coa desaturase to identify triglyceride reducing therapeutic agents
JP2003527379A (ja) 2000-03-15 2003-09-16 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー Ｍｅｘ阻害物質としての５−アミド置換ジアリールアミン類
US20020045613A1 (en) 2000-04-27 2002-04-18 Heinz Pauls 1-aroyl-piperidinyl benzamidines
GB0013383D0 (en) 2000-06-01 2000-07-26 Glaxo Group Ltd Therapeutic benzamide derivatives
ATE374765T1 (de) * 2000-07-27 2007-10-15 Lilly Co Eli Substituierte heterocyclische amide
ATE402262T1 (de) 2000-09-26 2008-08-15 Xenon Pharmaceuticals Inc Verfahren und zusammensetzungen, die eine stearoyl-coa desuturase-hscd5 verwenden
DE10060412A1 (de) * 2000-12-05 2002-06-06 Bayer Ag DELTA1-Pyrroline
US20020169166A1 (en) 2001-03-09 2002-11-14 Cowart Marlon D. Benzimidazoles that are useful in treating sexual dysfunction
FR2823209B1 (fr) 2001-04-04 2003-12-12 Fournier Lab Sa Nouvelles thiohydantoines et leur utilisation en therapeutique
US6953801B2 (en) * 2001-05-22 2005-10-11 Neurogen Corporation Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues
CN1300114C (zh) 2001-06-15 2007-02-14 安斯泰来制药有限公司 苯基吡啶甲酰哌嗪衍生物
JP4186518B2 (ja) * 2001-06-15 2008-11-26 アステラス製薬株式会社 フェニルピリジン誘導体
JPWO2003037862A1 (ja) 2001-10-30 2005-02-17 日本新薬株式会社 アミド誘導体及び医薬
US6620811B2 (en) 2001-11-19 2003-09-16 Hoffmann-La Roche Inc. Isonicotin- and nicotinamide derivatives of benzothiazoles
US20050038035A1 (en) 2001-11-28 2005-02-17 Hisashi Takasugi Heterocyclic amide compounds as apolipoprotein b inhibitors
EP1456175A1 (en) 2001-12-07 2004-09-15 Eli Lilly And Company Substituted heterocyclic carboxamides with antithrombotic activity
BR0307429A (pt) 2002-02-05 2004-12-28 Novo Nordisk As Composto, uso do mesmo, composição farmacêutica, e, método para o tratamento de distúrbios ou doenças relacionadas com receptor de histamina h3
PL220783B1 (pl) * 2002-03-13 2016-01-29 Janssen Pharmaceutica Nv Pochodna sulfonylowa, jej zastosowanie i sposób wytwarzania oraz kompozycja farmaceutyczna
ATE521592T1 (de) 2002-03-13 2011-09-15 Janssen Pharmaceutica Nv Histone-deacetylase-inhibitoren
BR0307599A (pt) 2002-03-13 2005-02-01 Janssen Pharmaceutica Nv Derivados de sulfonilamino como inibidores de histona deacetilase
CA2483314A1 (en) 2002-04-25 2003-11-06 Pharmacia Corporation Piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
AU2003251933A1 (en) 2002-07-25 2004-02-16 Wisconsin Alumni Research Foundation Method for increasing insulin sensitivity and for treating and preventing type 2 diabetes
JP2006505570A (ja) 2002-10-17 2006-02-16 アムジエン・インコーポレーテツド ベンズイミダゾール誘導体およびそれのバニロイド受容体リガンドとしての使用
JP2004203871A (ja) 2002-12-13 2004-07-22 Yamanouchi Pharmaceut Co Ltd 医薬組成物
EP1590341B1 (en) 2003-01-17 2009-06-17 Warner-Lambert Company LLC 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
AU2004261249B2 (en) * 2003-07-30 2008-09-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
ES2377406T3 (es) 2003-07-30 2012-03-27 Xenon Pharmaceuticals Inc. Derivados de la piperazina y su uso como agentes terapéuticos
TWI345974B (en) 2003-07-30 2011-08-01 Xenon Pharmaceuticals Inc Pyridazine derivatives and their use in the inhibition of stearoyl-coa desaturase

Also Published As

Publication number Publication date
US7335658B2 (en) 2008-02-26
HRP20110974T1 (hr) 2012-01-31
KR20060036107A (ko) 2006-04-27
CA2533899A1 (en) 2005-02-10
HK1097256A1 (en) 2007-06-22
CA2533899C (en) 2011-01-04
MA28011A1 (fr) 2006-07-03
WO2005011655A3 (en) 2005-03-24
EP2316827A1 (en) 2011-05-04
TNSN06034A1 (en) 2007-10-03
AU2004261252C1 (en) 2009-09-17
AR047557A1 (es) 2006-01-25
DK1648874T3 (da) 2012-01-23
EP3042895A1 (en) 2016-07-13
PL1648874T3 (pl) 2012-04-30
TW201038270A (en) 2010-11-01
AU2004261252A1 (en) 2005-02-10
ES2568769T3 (es) 2016-05-04
AU2009201788B2 (en) 2012-04-05
ES2375134T3 (es) 2012-02-27
NO20060981L (no) 2006-05-02
AU2004261252B2 (en) 2009-02-05
EP2316827B1 (en) 2016-01-27
EP1648874A2 (en) 2006-04-26
NZ545265A (en) 2009-11-27
AU2009201788A1 (en) 2009-05-28
IL173395A (en) 2013-03-24
JP4808616B2 (ja) 2011-11-02
EP1648874B1 (en) 2011-10-05
PT1648874E (pt) 2011-12-23
IL173395A0 (en) 2006-06-11
HK1226399A1 (zh) 2017-09-29
JP2007500717A (ja) 2007-01-18
ECSP066313A (es) 2006-07-28
KR100934554B1 (ko) 2009-12-29
US20050065143A1 (en) 2005-03-24
NO332822B1 (no) 2013-01-21
CY1112178T1 (el) 2015-12-09
WO2005011655A2 (en) 2005-02-10
ATE527242T1 (de) 2011-10-15
TW200518753A (en) 2005-06-16

Similar Documents

Publication Publication Date Title
TWI345974B (en) Pyridazine derivatives and their use in the inhibition of stearoyl-coa desaturase
TWI349551B (en) Thiophenepyrimidinone derivatives and their use in therapy
HK1041697A1 (zh) 苯並雜環和它們作為mek抑制劑的用途
IL175278A0 (en) Pyridazin-3(2h)-one derivatives and their use as pde4 inhibitors
ZA200600387B (en) Hydrolytically-resistant bornon-containing therapeutics and methods of use
IL178012A0 (en) Diphenyl-indol-2-on compounds and their use in the treatment of cancer
AU2002223599A1 (en) Pyrimidinone derivatives and their use in the treatment of atherosclerosis
HK1089155A1 (en) Novel cyanopyridine derivatives useful in the treatment of cancer and other disorders
HK1162948A1 (zh) 哈米特林 衍生物及其在治療癌症中的應用
EP1465615A4 (en) TRICYCLIC BISENONE DERIVATIVES AND METHODS OF USE
IL171501A (en) Genetically engineered cutaneous microorganisms and their use
AP2006003820A0 (en) Piperazin derivatives and their use in controllingpests
EP1586332A4 (en) COMBINED USE OF CARNOSINAS INHIBITOR WITH L-CARNOSINES AND COMPOSITION
ZA200410409B (en) Use of thio-oxindole derivatives in treatment of hormonerelated conditions
IL166733A0 (en) The use of fermented wheatgerm in the feeding and veterinary practice
HK1105288A1 (en) Flavopereirine and alstonine combinations in the treatment and prevention of prostate cancer
PL352333A1 (en) Dihydrobenzodiazepines and use of same in treatment of dislipidemia
GB9912159D0 (en) Improvements in and relating to the treatment of water
AU2003217421A8 (en) Prostate specific genes and the use thereof in design or therapeutics
GB0207411D0 (en) Azole compounds and their therapeutic use
AU2003216367A8 (en) Biglycan and related therapeutics and methods of use
IL162941A0 (en) Carboxamidine derivatives and their use in the treatment of vascular diseases
SG110107A1 (en) Compound and use in treatment
AU2003244455A1 (en) Piperidylcarboxamide derivatives and their use in the treatment of tachykinim-mediated diseases
EP1757286A4 (en) USE OF 1-N-BUTYLPHTALIDE FOR THE PREVENTION OR TREATMENT OF DEMENTIA

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees