AR074583A1 - 4-azetidinil-1-heteroaril-ciclohexanol antagonistas del ccr2 - Google Patents
4-azetidinil-1-heteroaril-ciclohexanol antagonistas del ccr2Info
- Publication number
- AR074583A1 AR074583A1 ARP090104791A ARP090104791A AR074583A1 AR 074583 A1 AR074583 A1 AR 074583A1 AR P090104791 A ARP090104791 A AR P090104791A AR P090104791 A ARP090104791 A AR P090104791A AR 074583 A1 AR074583 A1 AR 074583A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- group
- pyridyl
- onyl
- Prior art date
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- 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
- C07D401/02—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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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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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- C07D405/14—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 three or more hetero rings
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- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
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- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
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- 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
- C07D413/08—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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- 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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- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
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- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
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Abstract
Composiciones farmacéuticas que comprenden los compuestos con la fórmula (1) y su uso para prevenir, tratar o aminorar síndromes, trastornos o enfermedades mediados por CCR2, por ejemplo, diabetes tipo II, obesidad o asma. Reivindicación 1: Un compuesto de fórmula (1) en donde R1 es como uno cualquiera de los grupos de fórmulas (2), piridil, óxido de N-piridil, 1H-pirid1n-2-onil, indolil, pirazinil, 3-H-tiazol-2-onil, pirimidil, benzooxazolil, oxazolil, tiazolil, isotiazolil, pirazolil, imidazolil, tiofenil, furil, [1,2,4]oxadiazolil o [1,3,4]tiadiazolil; en donde el piridil, óxido de N-piridil, pirimidil, pirazolil, imidazolil, tiofenil, o tiazolil se sustituye opcionalmente con un sustituyente seleccionado del grupo consistente de O-alquil C1-4, O-cicloalquil C3-6, OCH2CF3, OCH2Ph, F, CN, CH2CN, alquil C1-4, CH2CF3, N(alquil C1-4)2, alquil C1-4OH, Si(CH3)3, -C:::CH, SCH3, S(O)CH3, SO2CH3, pirrolidinil, OH, NH2, NHCN, CO2H, CONH2, NHCO2-alquil C1-4, N(SO2CH3)2, NHSO2CH3, NHC(O)CF3, NHalquil C1-4, NHCO2H, NHCO2alquil C1-4, NHCOalquil C1-4, NHCONH2, NHCONHalquil C1-4 y Br o el piridil puede sustituirse con un grupo OCH3 y un CH3; o en donde el pirimidil se sustituye opcionalmente con un grupo N(C1-4 alquil)2 o uno o dos grupos OCH3; o en donde el tiazolil se sustituye opcionalmente en dos átomos de carbono adyacentes para formar sistema bicíclico fusionado de benzotiazol-2-il, o en donde el benzotiazol-2-iI se sustituye opcionalmente con Br o OCH3; o en donde el 1H-piridin-2-onil se sustituye opcionalmente con un sustituyente seleccionado del grupo consistente de CH2CN, alquil C1-4, CH2CF3, y CH2CH2OH, o el 1H-piridin-2-onil puede sustituirse opcionalmente con hasta 2 grupos metilo; o en donde el [1,2,4)oxadiazolil se sustituye opcionalmente con cualquier átomo de carbono con CCl3, o pirrolidinil o, de forma alternativa, ambos hidrógenos en el átomo de carbono del [1,2,4]oxadiazolil pueden reemplazarse con un grupo oxo; R2 es alquil C1-4, NH2, NO2, NHCH2CH2OH, N(alquil C1-4)2, N(SO2CH3)2, CN, F, CI, Br, CF3, cicloalquil C3-6, heterociclil, OCF3, OCF2H, CF2H, o O-alquil C1-4; R3 es H, F, CI, CF3, o O-alquil C1-4, de forma alternativa, R2 y R3 pueden tomarse juntos con su fenil adjunto para formar un benzo[1,3]dioxolil, 2,3-dihidro-benzofuranil, o un grupo 2,3-dihidro-benzo[1,4]dioxinil; R4 es H, O-alquil C1-4 o F; y solvatos, hidratos, tautómeros, profármacos y sales farmacéuticamente o aceptables de éstos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12127208P | 2008-12-10 | 2008-12-10 | |
US16729509P | 2009-04-07 | 2009-04-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR074583A1 true AR074583A1 (es) | 2011-01-26 |
Family
ID=41510894
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090104791A AR074583A1 (es) | 2008-12-10 | 2009-12-10 | 4-azetidinil-1-heteroaril-ciclohexanol antagonistas del ccr2 |
Country Status (28)
Country | Link |
---|---|
US (1) | US8450304B2 (es) |
EP (1) | EP2376475B1 (es) |
JP (1) | JP5782381B2 (es) |
KR (1) | KR20110094325A (es) |
CN (1) | CN102317278B (es) |
AR (1) | AR074583A1 (es) |
AU (1) | AU2009324723B2 (es) |
BR (1) | BRPI0923237A2 (es) |
CA (1) | CA2745969C (es) |
CL (1) | CL2011001427A1 (es) |
CO (1) | CO6331470A2 (es) |
CR (1) | CR20110381A (es) |
EA (1) | EA018997B1 (es) |
EC (1) | ECSP11011124A (es) |
ES (1) | ES2555004T3 (es) |
HN (1) | HN2011001606A (es) |
IL (1) | IL213250A0 (es) |
MX (1) | MX2011006226A (es) |
NI (1) | NI201100117A (es) |
NZ (1) | NZ593172A (es) |
PA (1) | PA8853001A1 (es) |
PE (1) | PE20110928A1 (es) |
SG (1) | SG171998A1 (es) |
SV (1) | SV2011003944A (es) |
TW (1) | TW201033204A (es) |
UY (1) | UY32312A (es) |
WO (1) | WO2010068663A1 (es) |
ZA (1) | ZA201105056B (es) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5782381B2 (ja) | 2008-12-10 | 2015-09-24 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | Ccr2の4−アゼチジニル−1−ヘテロアリール−シクロヘキサノールアンタゴニスト |
KR20120061060A (ko) * | 2009-04-16 | 2012-06-12 | 얀센 파마슈티카 엔.브이. | Ccr2의 4-아제티디닐-1-헤테로아릴-사이클로헥산 길항제 |
EP2419419B1 (en) * | 2009-04-17 | 2014-12-03 | Janssen Pharmaceutica NV | 4-azetidinyl-1-phenyl-cyclohexane antagonists of ccr2 |
BRPI1016205A2 (pt) * | 2009-04-17 | 2016-04-19 | Janssen Pharmaceutica Nv | compostos de cicloexano ligado a 4-azetidinil-1-heteroátomo antagonistas de ccr2 |
TW201211027A (en) * | 2010-06-09 | 2012-03-16 | Janssen Pharmaceutica Nv | Cyclohexyl-azetidinyl antagonists of CCR2 |
MX2012014934A (es) * | 2010-06-17 | 2013-05-20 | Janssen Pharmaceutica Nv | Antagonistas de ciclohexilacetindinilo del receptor de la citocina quimioatrayente 2. |
CA2852160A1 (en) | 2011-10-28 | 2013-05-02 | Galderma Research & Development | New leukocyte infiltrate markers for rosacea and uses thereof |
CN108135168B (zh) | 2015-05-21 | 2021-07-20 | 凯莫森特里克斯股份有限公司 | Ccr2调节剂 |
MX2020003192A (es) | 2017-09-25 | 2020-07-29 | Chemocentryx Inc | Terapia de combinacion usando un antagonista del receptor de quimiocina tipo 2 (ccr2) y un inhibidor de pd-1/pd-l1. |
CN107793404A (zh) * | 2017-11-07 | 2018-03-13 | 全椒先奇医药科技有限公司 | 一种治疗缺血性脑损伤药物组合物及其应用 |
US20190269664A1 (en) | 2018-01-08 | 2019-09-05 | Chemocentryx, Inc. | Methods of treating solid tumors with ccr2 antagonists |
JP7442141B2 (ja) | 2018-01-08 | 2024-03-04 | ケモセントリックス,インコーポレイティド | Ccr2アンタゴニストによる固形腫瘍の治療方法 |
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US7576089B2 (en) | 2003-12-18 | 2009-08-18 | Incyte Corporation | 3-cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors |
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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 |
JP5782381B2 (ja) | 2008-12-10 | 2015-09-24 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap | Ccr2の4−アゼチジニル−1−ヘテロアリール−シクロヘキサノールアンタゴニスト |
KR20120061060A (ko) * | 2009-04-16 | 2012-06-12 | 얀센 파마슈티카 엔.브이. | Ccr2의 4-아제티디닐-1-헤테로아릴-사이클로헥산 길항제 |
EP2419419B1 (en) * | 2009-04-17 | 2014-12-03 | Janssen Pharmaceutica NV | 4-azetidinyl-1-phenyl-cyclohexane antagonists of ccr2 |
BRPI1016205A2 (pt) | 2009-04-17 | 2016-04-19 | Janssen Pharmaceutica Nv | compostos de cicloexano ligado a 4-azetidinil-1-heteroátomo antagonistas de ccr2 |
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