BR0009431A - Diaryl derivatives and their use as medicines - Google Patents

Diaryl derivatives and their use as medicines

Info

Publication number
BR0009431A
BR0009431A BR0009431-5A BR0009431A BR0009431A BR 0009431 A BR0009431 A BR 0009431A BR 0009431 A BR0009431 A BR 0009431A BR 0009431 A BR0009431 A BR 0009431A
Authority
BR
Brazil
Prior art keywords
nr5r6
optionally substituted
alkyl
hydrogen
halogen
Prior art date
Application number
BR0009431-5A
Other languages
Portuguese (pt)
Inventor
Paivi Jaana Kukkola
Original Assignee
Novartis Ag Novarts Sa Novarti
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 Novartis Ag Novarts Sa Novarti filed Critical Novartis Ag Novarts Sa Novarti
Publication of BR0009431A publication Critical patent/BR0009431A/en

Links

Classifications

    • 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
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • 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
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C317/22—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
    • C07C323/67—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfonamide groups, bound to the carbon skeleton
    • 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
    • C07D295/04—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • 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
    • C07D295/22—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 with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Abstract

"DERIVADOS DIARILA E SEU USO COMO MEDICAMENTOS". Compostos da fórmula na qual W é 0, S, S(O) OU S(0)~ 2~; X é -S4, -S(O)R4, OU -S(0)~ 2~R4, S(0)~ 2~NR5R6; ou X é -C(O)NR5R6 com a condição de que -C(O)NR5R6 esteja localizado na posição 3', 4' ou 5'; Y é O ou H~ 2~; Z é hidrogênio, halogeno, hidróxi, alcóxi opcionalmente substituído, aralcóxi, acilóxi ou alcoxicarbonilóxi; R é hidrogênio, halogeno, trifluorometila, alquila inferior ou cicloalquila; R1 é hidróxi, aicóxi opcionalmente substituído, arilóxi, heteroarilóxi, aralquilóxi, cicloalcóxi, heteroaralcóxi ou -NR5R6; R2 é hidrogênio, halogeno ou alquila; R3 é halogeno ou alquila; R4 é alquila opcionalmente substituída, arila, aralquila, heteroaralquila ou heteroarila; R5, R6 e R7 são de modo independente hidrogênio, alquila opcionalmente substituída, cicloalquila, arila, aralquila, heteroarila, ou heteroaralquila; ou R5 e R6 combinados são alquileno opcionalmente interrompido por O, S, S(O), S(0)2 ou NR7 os quais junto com o átomo de nitrogênio ao qual estão ligados formam um anel de 5 a 7 membros; n representa zero ou um número inteiro de 1 a 4; sais farmaceuticamente aceitáveis dos mesmos; composições farmacêuticas compreendendo os compostos referidos; um método para prevenir e tratar doenças associadas com um desequilíbrio dos hormónios da tireóide, tal como hipotiroidismo e hipertiroidismo, obesidade, osteoporose e depressão, e, um método de reduzir os níveis de colesterol LDL e Lp(a) em mamíferos usando os compostos referidos."DIARIL DERIVATIVES AND THEIR USE AS MEDICINES". Compounds of the formula in which W is 0, S, S (O) OR S (0) ~ 2 ~; X is -S4, -S (O) R4, OR -S (0) ~ 2 ~ R4, S (0) ~ 2 ~ NR5R6; or X is -C (O) NR5R6 with the proviso that -C (O) NR5R6 is located at the 3 ', 4' or 5 'position; Y is O or H ~ 2 ~; Z is hydrogen, halogen, hydroxy, optionally substituted alkoxy, aralkoxy, acyloxy or alkoxycarbonyloxy; R is hydrogen, halogeno, trifluoromethyl, lower alkyl or cycloalkyl; R1 is hydroxy, optionally substituted aoxy, aryloxy, heteroaryloxy, aralkyloxy, cycloalkoxy, heteroaralkoxy or -NR5R6; R2 is hydrogen, halogen or alkyl; R3 is halogen or alkyl; R4 is optionally substituted alkyl, aryl, aralkyl, heteroaralkyl or heteroaryl; R5, R6 and R7 are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or R5 and R6 combined are alkylene optionally interrupted by O, S, S (O), S (0) 2 or NR7 which together with the nitrogen atom to which they are attached form a 5- to 7-membered ring; n represents zero or an integer from 1 to 4; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; a method to prevent and treat diseases associated with an imbalance of thyroid hormones, such as hypothyroidism and hyperthyroidism, obesity, osteoporosis and depression, and a method of reducing LDL and Lp (a) cholesterol levels in mammals using the compounds mentioned .

BR0009431-5A 1999-03-29 2000-03-27 Diaryl derivatives and their use as medicines BR0009431A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US28010599A 1999-03-29 1999-03-29
PCT/EP2000/002683 WO2000058279A1 (en) 1999-03-29 2000-03-27 Diaryl derivatives and their use as medicaments

Publications (1)

Publication Number Publication Date
BR0009431A true BR0009431A (en) 2002-01-08

Family

ID=23071698

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0009431-5A BR0009431A (en) 1999-03-29 2000-03-27 Diaryl derivatives and their use as medicines

Country Status (21)

Country Link
EP (1) EP1165502A1 (en)
JP (1) JP2002540189A (en)
KR (1) KR20010105394A (en)
CN (1) CN1345309A (en)
AU (1) AU4290800A (en)
BR (1) BR0009431A (en)
CA (1) CA2361016A1 (en)
CO (1) CO5160290A1 (en)
CZ (1) CZ20013449A3 (en)
HK (1) HK1042692A1 (en)
HU (1) HUP0200588A2 (en)
IL (1) IL144637A0 (en)
MX (1) MXPA01009843A (en)
NO (1) NO20014702D0 (en)
NZ (1) NZ514062A (en)
PE (1) PE20001587A1 (en)
PL (1) PL349355A1 (en)
RU (1) RU2001126579A (en)
SK (1) SK13812001A3 (en)
TR (1) TR200102225T2 (en)
WO (1) WO2000058279A1 (en)

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CN1515548A (en) 1999-03-01 2004-07-28 �Ʒ� Oxaminic acid used as thyroid gland receptor ligand and its derivative
US6790978B2 (en) 1999-03-29 2004-09-14 Novartis Ag Thyromimetic organic compounds
CA2400486C (en) 2000-02-17 2011-01-11 Bristol-Myers Squibb Company Aniline-derived ligands for the thyroid receptor
US6664291B2 (en) 2000-03-31 2003-12-16 Pfizer, Inc. Malonamic acids and derivatives thereof as thyroid receptor ligands
EP1268404B1 (en) * 2000-03-31 2008-01-02 Pfizer Products Inc. Malonamic acids and derivatives thereof as thyroid receptor ligands
AU4884701A (en) * 2000-05-12 2001-11-20 Kissei Pharmaceutical Co. Ltd. Malonanilic acid derivatives, medicinal compositions containing the same and usethereof
US6395784B1 (en) 2000-06-07 2002-05-28 Bristol-Myers Squibb Company Benzamide ligands for the thyroid receptor
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WO2002032408A2 (en) * 2000-10-20 2002-04-25 Novartis Ag Combinations of a thyromimetic compound and a statin
WO2002051805A1 (en) * 2000-12-27 2002-07-04 Bayer Aktiengesellschaft Indole derivatives as ligands of thyroid receptors
US6777442B2 (en) 2001-03-12 2004-08-17 Bayer Aktiengesellschaft Diphenyl derivatives
DE10122443A1 (en) * 2001-05-09 2002-11-14 Bayer Ag Amido-diphenyl derivatives
US6777443B2 (en) 2001-05-15 2004-08-17 Novartis Ag Dipeptide derivatives
DK1262177T3 (en) * 2001-05-31 2006-11-20 Pfizer Prod Inc Medical use of thyromimetic compounds for the treatment of hair loss and compositions
DE10131462A1 (en) * 2001-06-29 2003-01-09 Bayer Ag Phenol derivatives
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US6818766B2 (en) 2002-10-02 2004-11-16 Synthon Bv Process for making bicalutamide and intermediates thereof
CA2546601A1 (en) 2003-11-19 2005-06-09 Metabasis Therapeutics, Inc. Novel phosphorus-containing thyromimetics
US20080255240A1 (en) * 2004-05-05 2008-10-16 Novo Nordisk A/S Sulfonamide Derivatives
MX2007001215A (en) 2004-08-06 2007-04-17 Otsuka Pharma Co Ltd Aromatic compounds.
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US8236826B2 (en) 2005-12-05 2012-08-07 Otsuka Pharmaceutical Co., Ltd. Diarylether derivatives as antitumor agents
UA95978C2 (en) 2006-10-02 2011-09-26 Оцука Фармас'Ютікел Ко., Лтд. Stat3/5 activation inhibitor
WO2009133834A1 (en) * 2008-04-28 2009-11-05 塩野義製薬株式会社 Keto-amide derivative having inhibitory activity on endothelial lipase
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CN104193699B (en) * 2014-08-14 2016-05-25 嘉兴特科罗生物科技有限公司 A kind of micromolecular compound and synthetic method and application
CA3044059A1 (en) 2016-11-21 2018-05-24 Viking Therapeutics, Inc. Method of treating glycogen storage disease
EA201992703A1 (en) 2017-06-05 2020-04-15 Вайкинг Терапьютикс, Инк. COMPOSITIONS FOR TREATING FIBROSIS
CA3094167A1 (en) 2018-03-22 2019-09-26 Viking Therapeutics, Inc. Crystalline forms and methods of producing crystalline forms of a compound
CN112300133A (en) * 2019-07-31 2021-02-02 深圳微芯生物科技股份有限公司 Heterocyclic compound and application thereof

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Also Published As

Publication number Publication date
NO20014702L (en) 2001-09-27
IL144637A0 (en) 2002-05-23
KR20010105394A (en) 2001-11-28
PE20001587A1 (en) 2001-01-31
CZ20013449A3 (en) 2001-12-12
SK13812001A3 (en) 2002-04-04
HUP0200588A2 (en) 2002-07-29
NO20014702D0 (en) 2001-09-27
AU4290800A (en) 2000-10-16
CO5160290A1 (en) 2002-05-30
CN1345309A (en) 2002-04-17
EP1165502A1 (en) 2002-01-02
WO2000058279A1 (en) 2000-10-05
TR200102225T2 (en) 2002-01-21
CA2361016A1 (en) 2000-10-05
MXPA01009843A (en) 2002-05-06
HK1042692A1 (en) 2002-08-23
PL349355A1 (en) 2002-07-15
JP2002540189A (en) 2002-11-26
RU2001126579A (en) 2004-02-27
NZ514062A (en) 2001-09-28

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