HRP20050251A2 - Triazole derivatives as transforming growth factor (tfg) inhibitors - Google Patents
Triazole derivatives as transforming growth factor (tfg) inhibitors Download PDFInfo
- Publication number
- HRP20050251A2 HRP20050251A2 HR20050251A HRP20050251A HRP20050251A2 HR P20050251 A2 HRP20050251 A2 HR P20050251A2 HR 20050251 A HR20050251 A HR 20050251A HR P20050251 A HRP20050251 A HR P20050251A HR P20050251 A2 HRP20050251 A2 HR P20050251A2
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- phenyl
- heteroaryl
- cycloalkyl
- heterocycle
- Prior art date
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- 102000009618 Transforming Growth Factors Human genes 0.000 title description 16
- 108010009583 Transforming Growth Factors Proteins 0.000 title description 16
- 239000003112 inhibitor Substances 0.000 title description 8
- 229940042055 systemic antimycotics triazole derivative Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims description 99
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 89
- -1 hydroxy, oxo, mercapto Chemical class 0.000 claims description 54
- 150000003839 salts Chemical class 0.000 claims description 34
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 29
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 25
- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 229910052736 halogen Inorganic materials 0.000 claims description 21
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 21
- 239000000651 prodrug Substances 0.000 claims description 21
- 229940002612 prodrug Drugs 0.000 claims description 21
- 201000010099 disease Diseases 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 150000002367 halogens Chemical class 0.000 claims description 19
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 15
- 238000000034 method Methods 0.000 claims description 14
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 13
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 241001465754 Metazoa Species 0.000 claims description 11
- 125000001424 substituent group Chemical group 0.000 claims description 11
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 10
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- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 9
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- 150000002148 esters Chemical class 0.000 claims description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
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- 125000005842 heteroatom Chemical group 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 6
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- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims description 5
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- 201000011510 cancer Diseases 0.000 claims description 3
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 3
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 3
- 150000002431 hydrogen Chemical class 0.000 claims description 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims description 2
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- CSYSULGPHGCBQD-UHFFFAOYSA-N s-ethylisothiouronium diethylphosphate Chemical compound CCSC(N)=N.CCOP(O)(=O)OCC CSYSULGPHGCBQD-UHFFFAOYSA-N 0.000 description 1
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- 229930195734 saturated hydrocarbon Natural products 0.000 description 1
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- MEZLKOACVSPNER-GFCCVEGCSA-N selegiline Chemical compound C#CCN(C)[C@H](C)CC1=CC=CC=C1 MEZLKOACVSPNER-GFCCVEGCSA-N 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 description 1
- 229960002073 sertraline Drugs 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 1
- 229960002930 sirolimus Drugs 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 238000003797 solvolysis reaction Methods 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 230000003595 spectral effect Effects 0.000 description 1
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- 235000012222 talc Nutrition 0.000 description 1
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- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
- 229940063683 taxotere Drugs 0.000 description 1
- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000001984 thiazolidinyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- MIQPIUSUKVNLNT-UHFFFAOYSA-N tolcapone Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC(O)=C(O)C([N+]([O-])=O)=C1 MIQPIUSUKVNLNT-UHFFFAOYSA-N 0.000 description 1
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- 230000000699 topical effect Effects 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 229960002004 valdecoxib Drugs 0.000 description 1
- LNPDTQAFDNKSHK-UHFFFAOYSA-N valdecoxib Chemical compound CC=1ON=C(C=2C=CC=CC=2)C=1C1=CC=C(S(N)(=O)=O)C=C1 LNPDTQAFDNKSHK-UHFFFAOYSA-N 0.000 description 1
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- 229960004528 vincristine Drugs 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41207902P | 2002-09-18 | 2002-09-18 | |
| US48453503P | 2003-07-02 | 2003-07-02 | |
| PCT/IB2003/003825 WO2004026307A1 (en) | 2002-09-18 | 2003-09-08 | Triazole derivatives as transforming growth factor (tgf) inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20050251A2 true HRP20050251A2 (en) | 2005-10-31 |
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| HR20050251A HRP20050251A2 (en) | 2002-09-18 | 2005-03-17 | Triazole derivatives as transforming growth factor (tfg) inhibitors |
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| JP (1) | JP2006502236A (pt) |
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| CN (1) | CN1681502A (pt) |
| AP (1) | AP2005003260A0 (pt) |
| AR (1) | AR041276A1 (pt) |
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| EC (1) | ECSP055681A (pt) |
| HR (1) | HRP20050251A2 (pt) |
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| PE (1) | PE20050074A1 (pt) |
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| UY (1) | UY27981A1 (pt) |
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| AP2005003263A0 (en) | 2002-09-18 | 2005-03-31 | Pfizer Prod Inc | Pyrazole derivatives as transforming growth factor(TGF) inhibitors. |
| MXPA05002981A (es) | 2002-09-18 | 2005-06-22 | Pfizer Prod Inc | Nuevos compuestos de imidazol como inhibidores del factor de crecimiento transformante (tgf). |
| JP4518956B2 (ja) | 2002-09-18 | 2010-08-04 | ファイザー・プロダクツ・インク | トランスフォーミング成長因子（ｔｇｆ）阻害剤としての新規トリアゾールおよびオキサゾール化合物 |
| PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| DK1854789T3 (da) * | 2005-02-23 | 2013-10-21 | Shionogi & Co | Quinazolinderivat med tyrosin-kinase inhibitorisk aktivitet |
| EP1919881B1 (en) | 2005-07-25 | 2013-04-10 | Synta Pharmaceuticals Corp. | 1, 2, 3 -triazoles inhibitors of tubulin polymerization for the treatment of poliferative disorders |
| KR20080082618A (ko) * | 2005-12-16 | 2008-09-11 | 알콘, 인코퍼레이티드 | Ａｌｋ5 조절제를 사용한 안압의 조절 |
| DE102005061840A1 (de) | 2005-12-23 | 2007-06-28 | Merck Patent Gmbh | Triazolderivate |
| WO2008009077A2 (en) * | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections |
| US9259426B2 (en) | 2006-07-20 | 2016-02-16 | Gilead Sciences, Inc. | 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| US8871744B2 (en) | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
| WO2013078286A1 (en) | 2011-11-22 | 2013-05-30 | Cornell University | Methods for stimulating hematopoietic recovery by inhibiting tgf beta signaling |
| CA2926386C (en) | 2012-10-05 | 2021-11-09 | Kadmon Corporation, Llc | Human anti-vegfr-2/kdr antibodies |
| HUE049377T2 (hu) | 2013-03-14 | 2020-09-28 | Brigham & Womens Hospital Inc | Készítmények és eljárások epiteliális õssejtek expanziójára és tenyésztésére |
| PT3089971T (pt) | 2014-01-01 | 2020-09-03 | Medivation Tech Llc | Compostos e métodos de utilização |
| WO2016037016A1 (en) | 2014-09-03 | 2016-03-10 | The Brigham And Women's Hospital, Inc. | Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss |
| EP3722297A1 (en) | 2015-03-04 | 2020-10-14 | Gilead Sciences, Inc. | Toll-like receptor modulating 4,6-diamino-pyrido[3,2-d]pyrimidine compounds |
| CN108779437A (zh) | 2016-01-08 | 2018-11-09 | 麻省理工学院 | 分化的肠内分泌细胞和胰岛素产生细胞的制备 |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| AU2017318601B2 (en) | 2016-09-02 | 2020-09-03 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| WO2018045150A1 (en) | 2016-09-02 | 2018-03-08 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
| WO2018125746A1 (en) | 2016-12-30 | 2018-07-05 | Frequency Therapeutics, Inc. | 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
| CN112135613A (zh) | 2018-03-20 | 2020-12-25 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| US20210309679A1 (en) | 2018-07-23 | 2021-10-07 | Guangzhou Othrotx Co., Ltd. | Bisphosphonate drug conjugates |
| JP2021533788A (ja) | 2018-08-17 | 2021-12-09 | フリークエンシー セラピューティクス インコーポレイテッド | Ｊａｇ−１を上方制御することにより有毛細胞を生成するための組成物及び方法 |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| JP2022515652A (ja) | 2018-12-31 | 2022-02-21 | アイカーン スクール オブ メディシン アット マウント サイナイ | キナーゼ阻害剤化合物及び組成物ならびに使用方法 |
| TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TWI751517B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TW202115056A (zh) | 2019-06-28 | 2021-04-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑化合物的製備方法 |
| CN112694477B (zh) * | 2019-10-22 | 2024-02-06 | 四川科伦博泰生物医药股份有限公司 | 吡唑并环类化合物，包含其的药物组合物，其制备方法及其用途 |
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| JPS6058981A (ja) * | 1983-09-09 | 1985-04-05 | Takeda Chem Ind Ltd | ５−ピリジル−１，３−チアゾ−ル誘導体，その製造法およびそれを含んでなる医薬組成物 |
| JPS6025142A (ja) | 1983-07-21 | 1985-02-07 | Matsushita Electric Ind Co Ltd | 表示装置の電極製造方法 |
| DE3486009T2 (de) * | 1983-09-09 | 1993-04-15 | Takeda Chemical Industries Ltd | 5-pyridyl-1,3-thiazol-derivate, ihre herstellung und anwendung. |
| GB9201692D0 (en) * | 1992-01-27 | 1992-03-11 | Smithkline Beecham Intercredit | Compounds |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| IL132736A0 (en) | 1997-05-22 | 2001-03-19 | Searle & Co | 3(5)-Heteroaryl substituted pyrazoles as p38 kinase inhibitors |
| US6087381A (en) | 1997-05-22 | 2000-07-11 | G. D. Searle & Company | Pyrazole derivatives as p38 kinase inhibitors |
| US6436966B1 (en) * | 1997-10-27 | 2002-08-20 | Takeda Chemical Ind., Ltd. | Adenosine A3 receptor antagonists |
| EP1169317B1 (en) | 1999-04-09 | 2003-01-15 | SmithKline Beecham Corporation | Triarylimidazoles |
| JP2000302680A (ja) * | 1999-04-23 | 2000-10-31 | Takeda Chem Ind Ltd | 脳保護剤 |
| AU6471300A (en) * | 1999-08-06 | 2001-03-05 | Takeda Chemical Industries Ltd. | P38map kinase inhibitors |
| CO5271680A1 (es) | 2000-02-21 | 2003-04-30 | Smithkline Beecham Corp | Compuestos |
| GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
| PE20020506A1 (es) | 2000-08-22 | 2002-07-09 | Glaxo Group Ltd | Derivados de pirazol fusionados como inhibidores de la proteina cinasa |
| GB0027987D0 (en) | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
| AU2002225730A1 (en) | 2000-11-16 | 2002-05-27 | Smith Kline Beecham Corporation | Compounds |
| EP1354603A1 (en) * | 2000-12-26 | 2003-10-22 | Takeda Chemical Industries, Ltd. | Concomitant drugs |
| GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
| WO2002062775A1 (fr) * | 2001-02-02 | 2002-08-15 | Yamanouchi Pharmaceutical Co., Ltd. | Dérivé de 2-acylaminothiazole ou son sel |
| GB0102668D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| GB0102665D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| GB0102673D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| ES2237671T3 (es) | 2001-02-02 | 2005-08-01 | Smithkline Beecham Corporation | Derivados de pirazol contra la sobreexpresion de tgf. |
| EP1363904A1 (en) | 2001-02-02 | 2003-11-26 | Glaxo Group Limited | Pyrazoles as tgf inhibitors |
| GB0102672D0 (en) | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
| CA2450400A1 (en) * | 2001-06-11 | 2002-12-19 | Takeda Chemical Industries, Ltd. | Medicinal compositions |
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| GB0217780D0 (en) | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Compounds |
| AR040726A1 (es) | 2002-07-31 | 2005-04-20 | Smithkline Beecham Corp | Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento |
-
2003
- 2003-09-08 AP AP2005003260A patent/AP2005003260A0/xx unknown
- 2003-09-08 MX MXPA05002982A patent/MXPA05002982A/es unknown
- 2003-09-08 WO PCT/IB2003/003825 patent/WO2004026307A1/en active Application Filing
- 2003-09-08 PL PL03375974A patent/PL375974A1/xx not_active Application Discontinuation
- 2003-09-08 JP JP2004568900A patent/JP2006502236A/ja not_active Abandoned
- 2003-09-08 EA EA200500376A patent/EA200500376A1/ru unknown
- 2003-09-08 EP EP03797428A patent/EP1542685A1/en not_active Withdrawn
- 2003-09-08 CN CNA038221594A patent/CN1681502A/zh active Pending
- 2003-09-08 BR BR0314577-8A patent/BR0314577A/pt not_active IP Right Cessation
- 2003-09-08 KR KR1020057004575A patent/KR20050057393A/ko not_active Application Discontinuation
- 2003-09-08 CA CA002497971A patent/CA2497971A1/en not_active Abandoned
- 2003-09-08 OA OA1200500076A patent/OA12927A/en unknown
- 2003-09-08 AU AU2003260810A patent/AU2003260810A1/en not_active Abandoned
- 2003-09-16 UY UY27981A patent/UY27981A1/es not_active Application Discontinuation
- 2003-09-16 PE PE2003000947A patent/PE20050074A1/es not_active Application Discontinuation
- 2003-09-16 AR ARP030103360A patent/AR041276A1/es unknown
- 2003-09-17 US US10/667,183 patent/US7053095B2/en not_active Expired - Fee Related
- 2003-09-17 TW TW092125634A patent/TW200412346A/zh unknown
- 2003-09-17 PA PA20038583401A patent/PA8583401A1/es unknown
-
2005
- 2005-02-24 IS IS7713A patent/IS7713A/is unknown
- 2005-02-24 NO NO20051010A patent/NO20051010L/no unknown
- 2005-03-16 CO CO05024528A patent/CO5540390A2/es not_active Application Discontinuation
- 2005-03-17 HR HR20050251A patent/HRP20050251A2/hr not_active Application Discontinuation
- 2005-03-17 EC EC2005005681A patent/ECSP055681A/es unknown
- 2005-03-18 MA MA28156A patent/MA27442A1/fr unknown
-
2006
- 2006-02-07 US US11/349,481 patent/US20060128761A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| OA12927A (en) | 2006-10-13 |
| ECSP055681A (es) | 2005-05-30 |
| IS7713A (is) | 2005-02-24 |
| TW200412346A (en) | 2004-07-16 |
| EP1542685A1 (en) | 2005-06-22 |
| MXPA05002982A (es) | 2005-06-22 |
| AU2003260810A1 (en) | 2004-04-08 |
| BR0314577A (pt) | 2005-08-09 |
| EA200500376A1 (ru) | 2005-08-25 |
| MA27442A1 (fr) | 2005-07-01 |
| US7053095B2 (en) | 2006-05-30 |
| UY27981A1 (es) | 2004-04-30 |
| WO2004026307A1 (en) | 2004-04-01 |
| AP2005003260A0 (en) | 2005-03-31 |
| CN1681502A (zh) | 2005-10-12 |
| PA8583401A1 (es) | 2004-04-23 |
| AR041276A1 (es) | 2005-05-11 |
| CO5540390A2 (es) | 2005-07-29 |
| US20040110798A1 (en) | 2004-06-10 |
| NO20051010L (no) | 2005-05-31 |
| PE20050074A1 (es) | 2005-03-21 |
| KR20050057393A (ko) | 2005-06-16 |
| CA2497971A1 (en) | 2004-04-01 |
| PL375974A1 (en) | 2005-12-12 |
| JP2006502236A (ja) | 2006-01-19 |
| US20060128761A1 (en) | 2006-06-15 |
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