AR076329A1 - 4-azetidinil-1-heteroaril ciclohexanos sustituidos antagonistas de ccr2, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos en el tratamiento de diabetes, obesidad y otras enfermedades. - Google Patents
4-azetidinil-1-heteroaril ciclohexanos sustituidos antagonistas de ccr2, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos en el tratamiento de diabetes, obesidad y otras enfermedades.Info
- Publication number
- AR076329A1 AR076329A1 ARP100101288A ARP100101288A AR076329A1 AR 076329 A1 AR076329 A1 AR 076329A1 AR P100101288 A ARP100101288 A AR P100101288A AR P100101288 A ARP100101288 A AR P100101288A AR 076329 A1 AR076329 A1 AR 076329A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- so2ch3
- 4alkyl
- benzo
- group
- Prior art date
Links
- 102100031151 C-C chemokine receptor type 2 Human genes 0.000 title 1
- 101710149815 C-C chemokine receptor type 2 Proteins 0.000 title 1
- 208000008589 Obesity Diseases 0.000 title 1
- 206010012601 diabetes mellitus Diseases 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 235000020824 obesity Nutrition 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 -O-pyridyl Chemical group 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 abstract 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 101100054666 Streptomyces halstedii sch3 gene Proteins 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 abstract 1
- 125000004536 indazol-1-yl group Chemical group N1(N=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- 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
- C07D417/08—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 alicyclic rings
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- 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
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- A—HUMAN NECESSITIES
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- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- C07D401/02—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 two hetero rings
- C07D401/08—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 two hetero rings linked by a carbon chain containing alicyclic rings
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
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- C07D405/08—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing alicyclic rings
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- C07D413/08—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 alicyclic rings
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- Pharmacology & Pharmacy (AREA)
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- General Health & Medical Sciences (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
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Abstract
Reivindicacion 1: Un compuesto de formula (1) X es H, F, OH, o NH2; R1 es formulas (2), -O-benzoisotiazol-3-ilo, -O-benzoisoxazolilo, -O-benzotiazolilo, -O-benzoxazolilo, -O-benzofurilo, -O-indolilo, -O-benzoimidazolilo, -O-indazolilo, -O-furilo, -O-imidazolilo, -O-oxazolilo, -O-isoxazolilo, -O-tiofenilo, -O-benzotiofenilo, -O-tiazolilo, -O-isotiazolilo, -O-piridazilo, -O-pirazolilo, -O-pirrolilo, -O-benzo[1,3]dioxolilo, -O-pirimidilo, indazol-1-ilo, -O-piridilo, imidazol-1-ilo, piridon-1-ilo, pirimidon-1-ilo, pirazol-1-ilo, indol-1-ilo, piridaz-1-ilo, o pirrol-1-ilo; alternativamente, R1 y X pueden tomarse conjuntamente con su carbono adjunto para formar un anillo seleccionado del grupo que consiste de formulas 3 a 7 y en donde en formula 7 cualquier R1 puede ser sustituido con hasta dos grupos metilo, o un sustituyente seleccionado del grupo que consiste de: alquilo de OC1-4, cicloalquilo de OC3-6, OCH2CF3, OCH2Ph, F, I, CN, CI, OCF3, CF3, CH2CN, alquilo C1-4, CH2CF3, N(alquilo C1-4)2, alquilo C1-4OH, Si(CH3)3, :::-x-, (CH3)3Si-:::-z, SCH3, S(O)CH3, pirrolidinilo de SO2CH3, OH, NH2, NHCN, CO2H, CONH2, alquilo de NHCO2C1-4, N(SO2CH3)2, NHSO2CH3, NHC(O)CF3, alquilo de NHC1-4, NHCO2H, alquilo de NHCO2C1-4, NHCOC1-4alquilo, NHCONH2, alquilo de NHCONHC1-4 y Br; R2 es alquilo C1-4, NH2, NO2, NHCH2CH2OH, alquilo de N(C1-4)2, N(SO2CH3)2, CN, F, CI, Br, CF3, cicloalquilo, heterociclilo, OCF3, OCF2H, CF2H, o alquilo de OC1-4; R3 es H, F, CI, CF3, o OC1-4alquilo; alternativamente, R2 y R3 pueden tomarse juntos con su fenilo adjunto para formar un grupo benzo[1,3]dioxolilo, 2,3-dihidro-benzofuranilo, o 2,3-dihidro-benzo[1,4]dioxinilo; R4 es H, OC1-4alquilo, o F; y solvatos, hidratos, tautomeros y sales farmacéuticamente aceptables de éstos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17022509P | 2009-04-17 | 2009-04-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076329A1 true AR076329A1 (es) | 2011-06-01 |
Family
ID=42169493
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101288A AR076329A1 (es) | 2009-04-17 | 2010-04-19 | 4-azetidinil-1-heteroaril ciclohexanos sustituidos antagonistas de ccr2, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos en el tratamiento de diabetes, obesidad y otras enfermedades. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8324186B2 (es) |
| EP (1) | EP2419418B1 (es) |
| JP (1) | JP5685581B2 (es) |
| KR (1) | KR20120006051A (es) |
| CN (1) | CN102459226B (es) |
| AR (1) | AR076329A1 (es) |
| AU (1) | AU2010236336B2 (es) |
| BR (1) | BRPI1016205A2 (es) |
| CA (1) | CA2758929A1 (es) |
| ES (1) | ES2541607T3 (es) |
| MX (1) | MX2011010963A (es) |
| NZ (1) | NZ595433A (es) |
| TW (1) | TW201102379A (es) |
| WO (1) | WO2010121036A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20110928A1 (es) | 2008-12-10 | 2012-01-05 | Janssen Pharmaceutica Nv | Derivados de 4-azetidinil-1-heteroaril-ciclohexanol como antagonistas de ccr2 |
| EP2419417B1 (en) * | 2009-04-16 | 2015-03-25 | Janssen Pharmaceutica NV | 4-azetidinyl-1-heteroaryl-cyclohexane antagonists of ccr2 |
| AU2010236346B2 (en) | 2009-04-17 | 2015-01-22 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-phenyl-cyclohexane antagonists of CCR2 |
| CN102459226B (zh) | 2009-04-17 | 2014-09-17 | 詹森药业有限公司 | Ccr2的4-氮杂环丁烷基-1-杂原子连接的-环己烷拮抗剂 |
| TW201211027A (en) * | 2010-06-09 | 2012-03-16 | Janssen Pharmaceutica Nv | Cyclohexyl-azetidinyl antagonists of CCR2 |
| AU2011268375B2 (en) | 2010-06-17 | 2015-02-05 | Janssen Pharmaceutica Nv | Cyclohexyl-azetidinyl antagonists of CCR2 |
| WO2013060865A1 (en) | 2011-10-28 | 2013-05-02 | Galderma Research & Development | New leukocyte infiltrate markers for rosacea and uses thereof |
| EP3059225A4 (en) * | 2013-10-17 | 2017-09-06 | Shionogi & Co., Ltd. | Novel alkylene derivative |
| US20230174633A1 (en) * | 2020-03-30 | 2023-06-08 | Memorial Sloan Kettering Cancer Center | Methods and compositions for modulating lipid storage in adipose tissue |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6037354A (en) | 1997-06-18 | 2000-03-14 | Merck & Co., Inc. | Alpha 1a adrenergic receptor antagonists |
| AU734892B2 (en) | 1997-06-18 | 2001-06-28 | Merck & Co., Inc. | Alpha 1a adrenergic receptor antagonists |
| CA2378499A1 (en) | 1999-08-04 | 2001-02-15 | Teijin Limited | Cyclic amine ccr3 antagonists |
| US6245799B1 (en) | 1999-11-08 | 2001-06-12 | American Home Products Corp | [(Indol-3-yl)-cycloalkyl]-3-substituted azetidines for the treatment of central nervous system disorders |
| EP1228065A1 (en) | 1999-11-08 | 2002-08-07 | Wyeth | (indol-3-yl)-cycloalkyl]-3-substituted azetidines for the treatment of central nervous system disorders |
| CA2432369A1 (en) | 2000-12-20 | 2002-08-08 | Bristol-Myers Squibb Pharma Company | Cyclic derivatives as modulators of chemokine receptor activity |
| UA87449C2 (ru) * | 2002-11-27 | 2009-07-27 | Инсайт Корпорейшн | Производные 3-аминопиролидина как модуляторы рецепторов хемокина |
| US7834021B2 (en) | 2002-11-27 | 2010-11-16 | Incyte Corporation | 3-aminopyrrolidine derivatives as modulators of chemokine receptors |
| GB0417801D0 (en) * | 2004-08-10 | 2004-09-15 | Novartis Ag | Organic compounds |
| EP1802602A1 (en) | 2004-09-28 | 2007-07-04 | Janssen Pharmaceutica N.V. | Substituted dipiperdine ccr2 antagonists |
| PA8653301A1 (es) * | 2004-11-22 | 2006-11-09 | Incyte Corp Incyte Corp | Sales de la n-[2-({(3r)-1-[trans-4-hidroxi-4-(6-metoxipiridin-3-il) ciclohexil)pirrolidin |
| GB0513747D0 (en) | 2005-07-06 | 2005-08-10 | Merck Sharp & Dohme | Therapeutic compounds |
| WO2007053498A1 (en) | 2005-11-01 | 2007-05-10 | Millennium Pharmaceuticals, Inc. | Compounds useful as antagonists of ccr2 |
| US20070197590A1 (en) | 2006-01-31 | 2007-08-23 | Demong Duane E | Substituted dipiperidine ccr2 antagonists |
| EP2280766A1 (en) * | 2007-12-11 | 2011-02-09 | CytoPathfinder, Inc. | Carboxamide compounds and their use as chemokine receptor agonists |
| PE20110928A1 (es) | 2008-12-10 | 2012-01-05 | Janssen Pharmaceutica Nv | Derivados de 4-azetidinil-1-heteroaril-ciclohexanol como antagonistas de ccr2 |
| EP2419417B1 (en) | 2009-04-16 | 2015-03-25 | Janssen Pharmaceutica NV | 4-azetidinyl-1-heteroaryl-cyclohexane antagonists of ccr2 |
| CN102459226B (zh) | 2009-04-17 | 2014-09-17 | 詹森药业有限公司 | Ccr2的4-氮杂环丁烷基-1-杂原子连接的-环己烷拮抗剂 |
| AU2010236346B2 (en) | 2009-04-17 | 2015-01-22 | Janssen Pharmaceutica Nv | 4-azetidinyl-1-phenyl-cyclohexane antagonists of CCR2 |
-
2010
- 2010-04-15 CN CN201080027621.9A patent/CN102459226B/zh not_active Expired - Fee Related
- 2010-04-15 MX MX2011010963A patent/MX2011010963A/es active IP Right Grant
- 2010-04-15 NZ NZ595433A patent/NZ595433A/en not_active IP Right Cessation
- 2010-04-15 WO PCT/US2010/031255 patent/WO2010121036A1/en not_active Ceased
- 2010-04-15 CA CA2758929A patent/CA2758929A1/en not_active Abandoned
- 2010-04-15 EP EP10714151.7A patent/EP2419418B1/en active Active
- 2010-04-15 JP JP2012506227A patent/JP5685581B2/ja not_active Expired - Fee Related
- 2010-04-15 KR KR1020117026820A patent/KR20120006051A/ko not_active Withdrawn
- 2010-04-15 US US12/760,855 patent/US8324186B2/en not_active Expired - Fee Related
- 2010-04-15 AU AU2010236336A patent/AU2010236336B2/en not_active Ceased
- 2010-04-15 ES ES10714151.7T patent/ES2541607T3/es active Active
- 2010-04-15 BR BRPI1016205A patent/BRPI1016205A2/pt not_active Application Discontinuation
- 2010-04-16 TW TW099111900A patent/TW201102379A/zh unknown
- 2010-04-19 AR ARP100101288A patent/AR076329A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US8324186B2 (en) | 2012-12-04 |
| MX2011010963A (es) | 2011-11-02 |
| CN102459226B (zh) | 2014-09-17 |
| US20100267668A1 (en) | 2010-10-21 |
| ES2541607T3 (es) | 2015-07-22 |
| TW201102379A (en) | 2011-01-16 |
| NZ595433A (en) | 2013-12-20 |
| AU2010236336A1 (en) | 2011-11-03 |
| KR20120006051A (ko) | 2012-01-17 |
| BRPI1016205A2 (pt) | 2016-04-19 |
| EP2419418B1 (en) | 2015-04-15 |
| CN102459226A (zh) | 2012-05-16 |
| AU2010236336B2 (en) | 2015-01-15 |
| CA2758929A1 (en) | 2010-10-21 |
| JP2012524110A (ja) | 2012-10-11 |
| WO2010121036A1 (en) | 2010-10-21 |
| EP2419418A1 (en) | 2012-02-22 |
| JP5685581B2 (ja) | 2015-03-18 |
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