DE69907210T2 - Glucocorticoid- und thyroidhormonrezeptor-liganden zur behandlung von stoffwechselkrankheiten - Google Patents

Glucocorticoid- und thyroidhormonrezeptor-liganden zur behandlung von stoffwechselkrankheiten Download PDF

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Publication number
DE69907210T2
DE69907210T2 DE69907210T DE69907210T DE69907210T2 DE 69907210 T2 DE69907210 T2 DE 69907210T2 DE 69907210 T DE69907210 T DE 69907210T DE 69907210 T DE69907210 T DE 69907210T DE 69907210 T2 DE69907210 T2 DE 69907210T2
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Prior art keywords
isopropyl
dibromo
methoxyphenoxy
phenyl
acetic acid
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Expired - Fee Related
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DE69907210T
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German (de)
English (en)
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DE69907210D1 (de
Inventor
Theresa Apelqvist
Patrick Goede
Erik Holmgren
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Karo Healthcare AB
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Karo Bio AB
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Anticipated expiration legal-status Critical
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/78—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C217/80—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings
    • C07C217/82—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring
    • C07C217/90—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring the oxygen atom of at least one of the etherified hydroxy groups being further bound to a carbon atom of a six-membered aromatic ring, e.g. amino-diphenylethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/56—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having carbon atoms of carboxamide groups bound to carbon atoms of carboxyl groups, e.g. oxamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • C07C59/66—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
    • C07C59/68—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/76—Unsaturated compounds containing keto groups
    • C07C59/90—Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/32—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing keto groups
    • C07C65/40—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing keto groups containing singly bound oxygen-containing groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/734—Ethers
    • C07C69/736—Ethers the hydroxy group of the ester being etherified with a hydroxy compound having the hydroxy group bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/84—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
    • C07C69/92—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)
DE69907210T 1998-08-05 1999-08-04 Glucocorticoid- und thyroidhormonrezeptor-liganden zur behandlung von stoffwechselkrankheiten Expired - Fee Related DE69907210T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9816935 1998-08-05
GBGB9816935.2A GB9816935D0 (en) 1998-08-05 1998-08-05 Novel glucocortoid and thyroid receptor ligands for the treatment of metabolic disorders
PCT/IB1999/001447 WO2000007972A1 (en) 1998-08-05 1999-08-04 Glucocorticoid and thyroid hormone receptor ligands for the treatment of metabolic disorders

Publications (2)

Publication Number Publication Date
DE69907210D1 DE69907210D1 (de) 2003-05-28
DE69907210T2 true DE69907210T2 (de) 2004-02-19

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ID=10836671

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69907210T Expired - Fee Related DE69907210T2 (de) 1998-08-05 1999-08-04 Glucocorticoid- und thyroidhormonrezeptor-liganden zur behandlung von stoffwechselkrankheiten

Country Status (26)

Country Link
US (1) US6492424B1 (enExample)
EP (1) EP1102739B1 (enExample)
JP (1) JP2002522407A (enExample)
KR (1) KR20010072113A (enExample)
CN (1) CN1311767A (enExample)
AT (1) ATE238267T1 (enExample)
AU (1) AU753376B2 (enExample)
BG (1) BG105214A (enExample)
BR (1) BR9912742A (enExample)
CA (1) CA2339194A1 (enExample)
DE (1) DE69907210T2 (enExample)
DK (1) DK1102739T3 (enExample)
ES (1) ES2193730T3 (enExample)
GB (1) GB9816935D0 (enExample)
HU (1) HUP0103222A3 (enExample)
ID (1) ID28805A (enExample)
IL (1) IL141106A0 (enExample)
MX (1) MXPA01001047A (enExample)
NO (1) NO20010610L (enExample)
PL (1) PL345824A1 (enExample)
SE (1) SE1102739T5 (enExample)
SI (1) SI20579A (enExample)
SK (1) SK942001A3 (enExample)
TR (1) TR200100274T2 (enExample)
WO (1) WO2000007972A1 (enExample)
ZA (1) ZA200100832B (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60012700T2 (de) * 1999-03-01 2005-07-28 Pfizer Products Inc., Groton Oxamsäure und deren derivate als liganden der thyroid-rezeptoren
US6599942B1 (en) 1999-03-29 2003-07-29 Novartis Ag Thyromimetic organic compounds
US6790978B2 (en) 1999-03-29 2004-09-14 Novartis Ag Thyromimetic organic compounds
GB9928805D0 (en) * 1999-12-07 2000-02-02 Karobio Ab Compounds active at the Glucocorticoid and Thyroid Hormone Receptors
US6664291B2 (en) 2000-03-31 2003-12-16 Pfizer, Inc. Malonamic acids and derivatives thereof as thyroid receptor ligands
DE10038007A1 (de) * 2000-08-04 2002-02-14 Bayer Ag Neue Amino-und Amido-Diphenylether für Arzneimittel
ES2246292T3 (es) 2000-10-30 2006-02-16 Pfizer Products Inc. Moduladores de receptor glucocorticoide.
AU2001216038A1 (en) * 2000-11-14 2002-05-27 Alcon Laboratories Inc. Treatment of glaucoma and ocular hypertension
GB0029100D0 (en) * 2000-11-29 2001-01-10 Karobio Ab Compounds active at the glucocorticoid receptor
GB0029102D0 (en) * 2000-11-29 2001-01-10 Karobio Ab Compounds active at the glucocorticoid receptor
US6583180B2 (en) 2001-02-14 2003-06-24 Abbott Laboratories Glucocorticoid receptor modulators
US6777442B2 (en) * 2001-03-12 2004-08-17 Bayer Aktiengesellschaft Diphenyl derivatives
GB0111861D0 (en) * 2001-05-15 2001-07-04 Karobio Ab Novel compounds
GB0120691D0 (en) * 2001-08-24 2001-10-17 Karobio Ab Novel Compounds
WO2003018515A2 (en) * 2001-08-24 2003-03-06 Karo Bio Ab Prime ring substituted thyroid receptor antagonists for the treatment of cardiac and metabolic disorders
EP1430017A2 (en) 2001-09-26 2004-06-23 Theravance, Inc. Substituted phenol compounds useful for anesthesia and sedation
EP1297833B1 (en) 2001-09-26 2005-12-21 Pfizer Products Inc. Indole carboxylic acids as thyroid receptor ligands
CA2473886C (en) 2002-01-22 2012-08-21 The Regents Of The University Of California Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof
US7230031B2 (en) 2002-01-30 2007-06-12 Kissei Pharmaceutical Co., Ltd. Thyroid hormone receptor ligand, medicinal compositions containing the same and use thereof
GB0215978D0 (en) * 2002-07-10 2002-08-21 Karobio Ab Novel compounds
AU2002951977A0 (en) 2002-10-10 2002-10-24 Leo Engineering Pty Ltd Improvements to two-part vessels
CA2546601A1 (en) * 2003-11-19 2005-06-09 Metabasis Therapeutics, Inc. Novel phosphorus-containing thyromimetics
GB0406378D0 (en) * 2004-03-22 2004-04-21 Karobio Ab Novel pharmaceutical compositions
US20090232879A1 (en) * 2005-05-26 2009-09-17 Metabasis Therapeutics, Inc. Thyromimetics for the Treatment of Fatty Liver Diseases
US20090028925A1 (en) * 2005-05-26 2009-01-29 Erion Mark D Novel Phosphinic Acid-Containing Thyromimetics
JP2011518169A (ja) * 2008-04-15 2011-06-23 オステオジェネックス インコーポレイティド 骨増殖を変化させるための化合物及び方法
CN110198719A (zh) 2016-11-21 2019-09-03 维京治疗公司 治疗糖原贮积病的方法
EA201992703A1 (ru) 2017-06-05 2020-04-15 Вайкинг Терапьютикс, Инк. Композиции для лечения фиброза
AU2019238090B2 (en) 2018-03-22 2024-08-01 Viking Therapeutics, Inc. Crystalline forms and methods of producing crystalline forms of a compound
US12102646B2 (en) 2018-12-05 2024-10-01 Viking Therapeutics, Inc. Compositions for the treatment of fibrosis and inflammation

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0580550T3 (da) * 1992-07-21 1998-02-02 Ciba Geigy Ag Oxamidsyrederivater som hypercholesterolæmiske midler
EP1143948A3 (en) * 1998-06-08 2002-09-11 Karo Bio Ab Liver-selective glucocorticoid antagonist for treating diabetes

Also Published As

Publication number Publication date
HUP0103222A3 (en) 2002-12-28
AU753376B2 (en) 2002-10-17
CN1311767A (zh) 2001-09-05
BR9912742A (pt) 2001-05-02
ATE238267T1 (de) 2003-05-15
PL345824A1 (en) 2002-01-14
TR200100274T2 (tr) 2001-09-21
DK1102739T3 (da) 2003-08-18
US6492424B1 (en) 2002-12-10
GB9816935D0 (en) 1998-09-30
IL141106A0 (en) 2002-02-10
SK942001A3 (en) 2001-12-03
ID28805A (id) 2001-07-05
JP2002522407A (ja) 2002-07-23
EP1102739A1 (en) 2001-05-30
SE1102739T3 (enExample) 2003-08-12
AU5188199A (en) 2000-02-28
CA2339194A1 (en) 2000-02-17
DE69907210D1 (de) 2003-05-28
SE1102739T5 (enExample) 2003-09-16
HUP0103222A2 (hu) 2002-01-28
NO20010610L (no) 2001-04-04
BG105214A (en) 2001-12-29
EP1102739B1 (en) 2003-04-23
MXPA01001047A (es) 2002-09-02
WO2000007972A1 (en) 2000-02-17
SI20579A (sl) 2001-12-31
NO20010610D0 (no) 2001-02-05
KR20010072113A (ko) 2001-07-31
ES2193730T3 (es) 2003-11-01
ZA200100832B (en) 2001-10-31

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