AR058779A1 - Derivados de tiazol y oxazol como inhibidores de ptp-1b, composiciones farmaceuticas - Google Patents
Derivados de tiazol y oxazol como inhibidores de ptp-1b, composiciones farmaceuticasInfo
- Publication number
- AR058779A1 AR058779A1 ARP060104051A ARP060104051A AR058779A1 AR 058779 A1 AR058779 A1 AR 058779A1 AR P060104051 A ARP060104051 A AR P060104051A AR P060104051 A ARP060104051 A AR P060104051A AR 058779 A1 AR058779 A1 AR 058779A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- aryl
- iii
- halo
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 102100033001 Tyrosine-protein phosphatase non-receptor type 1 Human genes 0.000 title abstract 2
- 101710128896 Tyrosine-protein phosphatase non-receptor type 1 Proteins 0.000 title abstract 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 125000001475 halogen functional group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 abstract 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 abstract 2
- -1 cyano, amino, carboxy Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- PMPVIKIVABFJJI-UHFFFAOYSA-N Cyclobutane Chemical compound C1CCC1 PMPVIKIVABFJJI-UHFFFAOYSA-N 0.000 abstract 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 235000010290 biphenyl Nutrition 0.000 abstract 1
- 239000004305 biphenyl Substances 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
- C07F9/6539—Five-membered 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or 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
- C07D263/48—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente también comprende un proceso para preparar dicho compuesto, composiciones farmacéuticas y métodos para el tratamiento o la prevención de enfermedades causadas por la PTP-1B. Composiciones farmacéuticas. Reivindicación 1: Un compuesto representado por la fórmula (1) donde: A es un miembro seleccionado del grupo formado por las fórmulas (2) a (38); B es un resto seleccionado del grupo de fórmulas (39); L se selecciona entre -NH-, -NH-CH₂-, -NH-CH(CH₃)-, -NH-CH-C(O)NH-, -NH-CH₂-CH₂-, -NHNH-, -NH-CH(COOH)-CH₂, -N(CH₂COOH)-; C es un miembro seleccionado del grupo formado por (i) fenilo, (ii) naftilo, (iii) indolilo, (iv) tiazolilo, y (v) bencimidazolilo; Y se selecciona del grupo formado por las fórmulas (40) a (43); p es 1, 2 ó 3; R¹ se selecciona del grupo formado por: i) H, ii) -CH₂COOR⁴, iii) -X(CH₂)ₙ-arilo, donde n se selecciona entre 0, 1 ó 2, y X se selecciona entre S, NH u O, iv) -S-alquilo, v) -OR⁴, vi) OCH₂-cicloalquilo, donde cicloalquilo se selecciona entre ciclopropilo, ciclobutilo, ciclopentilo, ciclohexilo, cicloheptilo o ciclooctilo, vii) -CH₂CONH₂, viii) -CN, ix) halo, x) alquilo, xi) -SO₂-arilo, xii) -CF₃, xiii) -CO₂R⁴, xiv) -CO-alquilo, xv) -NH₂, xvi) -NO₂, xvii) -CH₂CONH-PhCH₂COOR⁴, xviii) tetrazolilo, xix) triazolilo, xx) pirrolilo, xxi) bencimidazolilo, xxii) pirazolilo, xxiii) ftalamoilo, xxiv) fenilo opcionalmente sustituido con uno o más grupos seleccionados entre ciano, amino, carboxi, halo, nitro, alquilo, hidroxilo, -O-alquilo, xxv) bifenilo, xxvi) -OCH₂CO₂R⁴, xxvii) piridilo, xxviii) tienilo, xxix) dimetilamino, xxx) -CH₂OH, xxxi) -CF₂H, xxxii) -SO₂NHR⁴, xxxiii) NHCO-alquilo, xxxiv) -OCF₃, o es un resto seleccionado del grupo de fórmulas (44), donde X es como se definió anteriormente; R² y R³ son seleccionados independientemente del grupo formado por: i) H, ii) -CH₂COOR⁴, iii) -S-alquilo, iv) -OR⁴, v) -CH₂CONH₂, vi) -CN, vii) halo, viii) alquilo, ix) -CF₃, x) -COOR⁴, xi) arilo, xii) -CO-alquilo, xiii) -NH₂, xiv) -NO₂, xv) -CF₂H, xvi) tienilo, xvii) NHCO-alquilo, y xviii) -OCF₃; R⁴ se selecciona entre H o alquilo; R⁵ se selecciona del grupo formado por i) -COOR⁴, donde R⁴ es como se definió anteriormente, ii) -C(O)C(O)OH, o iii) un compuesto de fórmula (45), donde Z se selecciona entre arilo o heteroarilo, opcionalmente sustituido por un grupo seleccionado independientemente entre H, alquilo, halo, nitro, -OR⁴, CF₃ y CONHR⁴, iv) un resto de fórmula (46), v) un resto de fórmula (47), vi) -CONHOH, vii) -SO₂NHCO-alquilo, viii) -SO₂NH-alquilo, ix) -CONHSO₂-alquilo, x) OH, xi) -NHCO-alquilo, y xii) -SO₂NHR⁴; R⁶ se selecciona del grupo formado por i) H, ii) -OR⁴, iii) alquilo, iv) halo, v) heterociclilo, vi) -S-alquilo, vii) -S-arilo, viii) -COOH, ix) bencilo, y x) heteroarilo; R⁷ se selecciona del grupo formado por: i) alquilo, ii) H, y iii) halo; o R⁶ y R⁷ juntos pueden formar un anillo cicloalcano seleccionado del grupo de ciclopentano, ciclohexano, ciclobutano; R⁸ y R⁹ son seleccionados independientemente del grupo formado por: i) H, ii) halo, iii) -OR⁴, iv) alquilo, v) -CONHR⁴, vi) -COOR⁴, y vii) -CO-alquilo; R¹⁰ se selecciona del grupo formado por: i) alquilo, ó ii) arilo; R¹¹ se selecciona del grupo formado por: i) H, ii) alquilo, y iii) arilo; y con la condición de que: a) cuando R⁵ es -C(O)C(O)OH, entonces Y es el resto de fórmula (40), y p es nulo; b) cuando A es fenilo y está sustituido por R¹ en la posición cuarta entonces R¹ no es -X(CH₂)ₙ-arilo; o una sal farmacéuticamente aceptable o prodroga del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN860KO2005 | 2005-09-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058779A1 true AR058779A1 (es) | 2008-02-20 |
Family
ID=37547001
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104051A AR058779A1 (es) | 2005-09-16 | 2006-09-15 | Derivados de tiazol y oxazol como inhibidores de ptp-1b, composiciones farmaceuticas |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20090088432A1 (es) |
| EP (1) | EP1934192A1 (es) |
| JP (1) | JP2009508848A (es) |
| KR (1) | KR20080056730A (es) |
| CN (1) | CN101268060A (es) |
| AR (1) | AR058779A1 (es) |
| AU (1) | AU2006290250A1 (es) |
| BR (1) | BRPI0616217A2 (es) |
| CA (1) | CA2622518A1 (es) |
| RU (1) | RU2008114836A (es) |
| TW (1) | TW200745066A (es) |
| WO (1) | WO2007032028A1 (es) |
| ZA (1) | ZA200802078B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ551027A (en) | 2004-04-08 | 2011-01-28 | Targegen Inc | Benzotriazine inhibitors of kinases |
| JP5275628B2 (ja) | 2004-08-25 | 2013-08-28 | ターゲジェン インコーポレーティッド | 複素環式化合物および使用方法 |
| CN101274918A (zh) * | 2007-03-30 | 2008-10-01 | 中国科学院上海药物研究所 | 一类取代五元杂环化合物,其制备方法和医学用途 |
| US20160331729A9 (en) | 2007-04-11 | 2016-11-17 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| US11241420B2 (en) | 2007-04-11 | 2022-02-08 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| JP2011510067A (ja) | 2008-01-25 | 2011-03-31 | トレント・ファーマシューティカルズ・リミテッド | 組合せ医薬品 |
| WO2009109999A1 (en) * | 2008-03-03 | 2009-09-11 | Lupin Limited | Novel protein tyrosine phosphatase - ib inhibitors |
| WO2010122979A1 (ja) * | 2009-04-20 | 2010-10-28 | Ｓｂｉバイオテック株式会社 | チアゾリジノン誘導体 |
| GB201121794D0 (en) * | 2011-12-19 | 2012-02-01 | Isis Innovation | PIM kinase inhibitors |
| CN102617564B (zh) * | 2012-01-19 | 2015-04-29 | 西安交通大学 | 一种化合物及其制备方法 |
| CN102617563B (zh) * | 2012-01-19 | 2015-04-29 | 西安交通大学 | 一种化合物及其制备方法 |
| CN104059060B (zh) * | 2014-05-30 | 2017-08-01 | 西安交通大学 | 一种5‑(1h‑吲哚‑3‑亚甲基)‑1,3‑噻唑烷‑4‑酮类衍生物及其合成方法和应用 |
| CN104016942B (zh) * | 2014-06-16 | 2016-02-24 | 天津医科大学 | 噻唑啉酮类衍生物及其药物组合物与应用 |
| KR20170124602A (ko) | 2015-03-13 | 2017-11-10 | 포르마 세라퓨틱스 인크. | Hdac8 억제제로서의 알파-신나미드 화합물 및 조성물 |
| EP3445749B1 (en) * | 2016-04-18 | 2022-12-21 | Novartis AG | Compounds and compositions for treating conditions associated with nlrp activity |
| KR101911785B1 (ko) * | 2016-08-09 | 2018-10-26 | 세종대학교 산학협력단 | Ampk 억제기능에 기반한 뇌졸중 치료용 약학적 조성물 |
| WO2018030762A1 (ko) * | 2016-08-09 | 2018-02-15 | 세종대학교산학협력단 | Ampk 억제기능에 기반한 뇌졸중 치료용 약학적 조성물 |
| CN106946744B (zh) * | 2017-03-17 | 2019-05-24 | 上海交通大学 | 一种新型ptp1b酶抑制剂及其制备方法和应用 |
| CN112336719A (zh) * | 2020-10-19 | 2021-02-09 | 济南大学 | 一种噻唑衍生物作为α-葡萄糖苷酶抑制剂及其应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004047760A2 (en) | 2002-11-22 | 2004-06-10 | Smithkline Beecham Corporation | Novel chemical compounds |
| WO2005082901A1 (en) | 2004-02-25 | 2005-09-09 | Smithkline Beecham Corporation | Novel chemical compounds |
| AU2005259512A1 (en) | 2004-07-01 | 2006-01-12 | F. Hoffmann-La Roche Ag | Thiazolinone unsubstituted quinolines |
| JP2008516905A (ja) | 2004-10-14 | 2008-05-22 | エフ．ホフマン−ラ ロシュ アーゲー | Ｃｄｋ１抗増殖活性を有する１，５−ナフチリジンアゾリジノン |
| CA2583311A1 (en) | 2004-10-14 | 2006-04-20 | F. Hoffmann-La Roche Ag | Quinazolinylmethylenethiazolinones as cdk1 inhibitors |
| CA2583271C (en) | 2004-10-22 | 2014-05-20 | Exelixis, Inc. | Benzylthiazolone inhibitors of estrogen-related receptors (err) |
-
2006
- 2006-09-14 TW TW095134013A patent/TW200745066A/zh unknown
- 2006-09-15 WO PCT/IN2006/000368 patent/WO2007032028A1/en not_active Ceased
- 2006-09-15 AU AU2006290250A patent/AU2006290250A1/en not_active Abandoned
- 2006-09-15 BR BRPI0616217-7A patent/BRPI0616217A2/pt not_active IP Right Cessation
- 2006-09-15 CA CA002622518A patent/CA2622518A1/en not_active Abandoned
- 2006-09-15 US US11/992,016 patent/US20090088432A1/en not_active Abandoned
- 2006-09-15 EP EP06796203A patent/EP1934192A1/en not_active Withdrawn
- 2006-09-15 AR ARP060104051A patent/AR058779A1/es not_active Application Discontinuation
- 2006-09-15 RU RU2008114836/04A patent/RU2008114836A/ru not_active Application Discontinuation
- 2006-09-15 JP JP2008530756A patent/JP2009508848A/ja active Pending
- 2006-09-15 CN CNA2006800341349A patent/CN101268060A/zh active Pending
- 2006-09-15 KR KR1020087009160A patent/KR20080056730A/ko not_active Ceased
-
2008
- 2008-03-05 ZA ZA200802078A patent/ZA200802078B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20090088432A1 (en) | 2009-04-02 |
| AU2006290250A1 (en) | 2007-03-22 |
| KR20080056730A (ko) | 2008-06-23 |
| ZA200802078B (en) | 2009-08-26 |
| BRPI0616217A2 (pt) | 2011-06-14 |
| EP1934192A1 (en) | 2008-06-25 |
| TW200745066A (en) | 2007-12-16 |
| RU2008114836A (ru) | 2009-10-27 |
| WO2007032028A1 (en) | 2007-03-22 |
| CA2622518A1 (en) | 2007-03-22 |
| WO2007032028A8 (en) | 2008-07-17 |
| JP2009508848A (ja) | 2009-03-05 |
| CN101268060A (zh) | 2008-09-17 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR058779A1 (es) | Derivados de tiazol y oxazol como inhibidores de ptp-1b, composiciones farmaceuticas | |
| US8293929B2 (en) | Processes and intermediates | |
| AR066972A1 (es) | Derivados azapeptidicos | |
| PE20212023A1 (es) | Compuestos, composiciones y metodos | |
| AR087127A1 (es) | Compuestos que se unen a fxr (nr1h4) y modulan su actividad | |
| NO20090760L (no) | Nye tricykliske spiropiperidinforbindelser, deres synteser og deres anvendelser som modulatorer av kemokinreseptor-aktivitet | |
| DOP2009000201A (es) | Derivados de 3-amino-pirrolo[3,4-c]pirazol-5(1h, 4h, 6h)carbaldehido como inhibidores pkc | |
| EA200870358A1 (ru) | 2-(циклический амино) пиримидоновые производные в качестве ингибиторов tpk1 | |
| AR074359A1 (es) | Compuestos heterociclicos sustituidos como moduladores de canales ionicos | |
| AR083501A1 (es) | 1-(heterociclo carbonil)piperidinas | |
| AR087792A1 (es) | Compuestos heterociclicos tetraciclicos y metodos para el uso de los mismos en el tratamiento de enfermedades virales | |
| AR062797A1 (es) | Derivados de piperidina como inhibidores de renina, composiciones farmaceuticas. | |
| US7109357B2 (en) | Process and intermediates for making substituted aspartic acid acetals | |
| CO2021014210A2 (es) | Compuestos de pirrol | |
| AR035728A1 (es) | Proceso perfeccionado para la sintesis de carbapenem | |
| CO6400145A2 (es) | Derivados de 2-piridin-2-il pirazol-3(2h) -ona, su preparción y su aplicación terapeútica | |
| AR123583A1 (es) | Composiciones y métodos para el tratamiento de la infección por coronavirus | |
| EA201071272A1 (ru) | Новые производные аминокислот, способ их получения и применение | |
| PE20240213A1 (es) | Compuestos como moduladores de bis-fosfoglicerato mutasa para el tratamiento de la anemia de celulas falciforme | |
| AR121554A1 (es) | Azálidos de urea inmunoduladores | |
| AR123170A1 (es) | Inhibidores atr y usos de estos | |
| ES2383861B1 (es) | Procedimiento de síntesis de intermedios de crambescidinas, de cimipronidina y de sus derivados. | |
| AR045028A1 (es) | Derivados de tiadiazola 1,2,5-substituidos pesticidas | |
| AR116568A1 (es) | Inhibidores de udp glicosiltransferasa y métodos de uso | |
| AU2014224107A1 (en) | Processes and intermediates for the preparation of aspartic acetal caspase inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |