AR070810A1 - Derivados de 1- bencil-3-hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1 cx3cr1 y p40 - Google Patents
Derivados de 1- bencil-3-hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1 cx3cr1 y p40Info
- Publication number
- AR070810A1 AR070810A1 ARP090100800A ARP090100800A AR070810A1 AR 070810 A1 AR070810 A1 AR 070810A1 AR P090100800 A ARP090100800 A AR P090100800A AR P090100800 A ARP090100800 A AR P090100800A AR 070810 A1 AR070810 A1 AR 070810A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- different
- same
- alkoxy
- Prior art date
Links
- 102100021943 C-C motif chemokine 2 Human genes 0.000 title abstract 3
- 101710155857 C-C motif chemokine 2 Proteins 0.000 title abstract 3
- 108090000835 CX3C Chemokine Receptor 1 Proteins 0.000 title abstract 3
- 102100039196 CX3C chemokine receptor 1 Human genes 0.000 title abstract 3
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- AKQDXNFPEFHRLS-UHFFFAOYSA-N (1-benzylindazol-3-yl)methanol Chemical class C12=CC=CC=C2C(CO)=NN1CC1=CC=CC=C1 AKQDXNFPEFHRLS-UHFFFAOYSA-N 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- 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
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
Abstract
Derivados de 1-bencil-3-hidroximetilindazol segun la formula (1) descritos en las reivindicaciones y a una composicion farmacéutica que los comprende, junto con un vehiculo farmacéuticamente aceptable. Además, se refiere a la utilizacion de derivadas de 1-bencil-3-hidroximetilindazol para la preparacion de una composicion farmacéutica que es activa en el tratamiento de enfermedades basadas en la expresion de MCP-1, CX3CR1 y p40, y a su utilizacion para tratar o prevenir enfermedades basadas en la expresion de MCP-1 CX3CR1 y p40. Reivindicacion 1: Compuesto de formula (1) en la que: A puede ser -X1- o -X1-OC(R9)(R10)-, en los que X1 puede ser un grupo alquilo C1-5, opcionalmente sustituido con unto o más grupos alquilo C1-5 o uno o más grupos alcoxi C1-3, y R9 y R10, que pueden ser iguales o diferentes entre sí, pueden ser hidrogeno, alquilo C1-5, o alcoxi C1-3, Y es OH; R1 y R2, que pueden ser iguales o diferentes entre sí, pueden ser hidrogeno, alquilo C1-5, o alcoxi C1-3; R3, R4 y R8, que pueden ser iguales o diferentes entre sí, pueden ser hidrogeno, alquilo C1-5, alcoxi C1-3, un átomo de halogeno, -OH, -N(R')(Rö), -N(R')CORö, -CN, -CONR'Rö, -SO2NR'Rö, -SO2R', nitro y trifluorometilo; con R' y Rö, que pueden ser iguales o diferentes entre sí, representados por hidrogeno y un grupo alquilo C1-5, R5 puede ser hidrogeno, alquilo C1-5, alcoxi C1-3, un átomo de halogeno, -OH, -N(R')(Rö), -N(R')CORö, nitro y trifluorometilo, o R5 junto con uno de entre R6 y R7 forma un anillo que presenta 5 o 6 átomos de carbono; con R' y Rö, que pueden ser iguales o diferentes entre sí, representados por hidrogeno y un grupo alquilo C1-5, R6 y R7, que pueden ser iguales o diferentes entre sí, pueden ser hidrogeno, alquilo C1-5, o juntos forman un grupo C=O, o uno de entre R6 y R7, junto con R5, forma un anillo que presenta 5 o 6 átomos de carbono, con la condicion de que cuando Y sea -OH, A sea diferente de alquilo C1, opcionalmente sustituido con uno o más alquilo C1-5, o alternativamente por lo menos uno de los grupos de R1 a R8 es diferente de hidrogeno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08425139 | 2008-03-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070810A1 true AR070810A1 (es) | 2010-05-05 |
Family
ID=39671487
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100800A AR070810A1 (es) | 2008-03-07 | 2009-03-06 | Derivados de 1- bencil-3-hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1 cx3cr1 y p40 |
| ARP090100801A AR070811A1 (es) | 2008-03-07 | 2009-03-06 | Derivados de 1- bencil-3- hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1, cx3cr1 y p40 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100801A AR070811A1 (es) | 2008-03-07 | 2009-03-06 | Derivados de 1- bencil-3- hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1, cx3cr1 y p40 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US7919518B2 (es) |
| EP (3) | EP2254869B1 (es) |
| JP (2) | JP5509101B2 (es) |
| KR (2) | KR101599867B1 (es) |
| CN (2) | CN101945855B (es) |
| AR (2) | AR070810A1 (es) |
| AU (2) | AU2009221089B2 (es) |
| BR (2) | BRPI0907977A2 (es) |
| CA (2) | CA2712703C (es) |
| CY (2) | CY1117584T1 (es) |
| DK (2) | DK2254869T3 (es) |
| EA (2) | EA018241B1 (es) |
| ES (2) | ES2569330T3 (es) |
| GE (2) | GEP20135912B (es) |
| HR (2) | HRP20160462T1 (es) |
| HU (1) | HUE027098T2 (es) |
| IL (3) | IL206893A0 (es) |
| LT (1) | LT2254869T (es) |
| MX (2) | MX2010009623A (es) |
| PL (2) | PL2254870T3 (es) |
| PT (1) | PT2254869T (es) |
| SG (1) | SG188177A1 (es) |
| SI (2) | SI2254870T1 (es) |
| UA (2) | UA103605C2 (es) |
| WO (2) | WO2009109618A2 (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7919518B2 (en) * | 2008-03-07 | 2011-04-05 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40 |
| DK2262778T5 (da) | 2008-03-07 | 2020-06-08 | Acraf | 1-benzyl-3-hydroxymethylindazolderivativer og brug deraf i behandling af sygdomme baseret på ekspression af mcp-1, cx3cr1 og p40 |
| CN101959866B (zh) | 2008-03-07 | 2013-10-02 | 方济各安吉利克化学联合股份有限公司 | 1-苄基-3-羟基甲基吲唑衍生物及其在治疗基于mcp-1和cx3cr1表达的疾病中的用途 |
| US8350052B2 (en) | 2009-08-03 | 2013-01-08 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Process for the preparation of 1-benzyl-3-hydroxymethyl-1H-indazole and its derivatives and required magnesium intermediates |
| UA108742C2 (uk) * | 2009-09-23 | 2015-06-10 | Фармацевтична композиція для лікування запальних захворювань, опосередкованих mcp-1 | |
| ES2656292T3 (es) * | 2012-05-01 | 2018-02-26 | Translatum Medicus Inc. | Métodos de tratamiento y diagnóstico de enfermedades oculares que causan ceguera |
| US8999292B2 (en) * | 2012-05-01 | 2015-04-07 | Translatum Medicus Inc. | Methods for treating and diagnosing blinding eye diseases |
| WO2013171316A1 (en) | 2012-05-18 | 2013-11-21 | Sanofi | Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation |
| KR20150010973A (ko) * | 2012-05-18 | 2015-01-29 | 사노피 | 피라졸 유도체 및 lpar5 길항제로서의 그의 용도 |
| AU2013342209B2 (en) | 2012-11-09 | 2016-05-26 | Colgate-Palmolive Company | Block copolymers for tooth enamel protection |
| WO2015173786A1 (en) * | 2014-05-15 | 2015-11-19 | Boyd Shelley Romayne | Compositions and methods for treating and diagnosing ocular disorders |
| KR102653599B1 (ko) | 2015-06-12 | 2024-04-01 | 베토어 엘엘씨 | 질환 치료용 mct4 저해제 |
| US20180221339A1 (en) * | 2015-06-16 | 2018-08-09 | Translatum Medicus, Inc. | Compositions and methods for treating and diagnosing ocular disorders |
| KR102615828B1 (ko) | 2016-12-12 | 2023-12-20 | 베토어 엘엘씨 | Mct4 의 헤테로시클릭 저해제 |
| GB201811169D0 (en) | 2018-07-06 | 2018-08-29 | Kancera Ab | New compounds |
| WO2020026471A1 (ja) * | 2018-07-31 | 2020-02-06 | 株式会社親広産業 | グルコース消費促進剤および解糖系促進剤 |
| JP6612004B1 (ja) * | 2018-07-31 | 2019-11-27 | 株式会社親広産業 | グルコース消費促進剤および解糖系促進剤 |
| CA3144861A1 (en) | 2019-06-25 | 2020-12-30 | Translatum Medicus, Inc. | Processes of making 2-((1-benzyl-1h-indazol-3-yl)methoxy)-2-methylpropanoic acid and its derivatives |
| CN113929627A (zh) * | 2021-10-19 | 2022-01-14 | 吕梁学院 | 一种宾达利的合成方法 |
| WO2024108386A1 (zh) * | 2022-11-22 | 2024-05-30 | 中国科学院深圳先进技术研究院 | 抗mcp1中和抗体在制备治疗神经退行性疾病引起的系统性炎症药物中的应用 |
| EP4662203A1 (en) * | 2023-02-10 | 2025-12-17 | Translatum Medicus Inc. | Bindarit conjugates, compositions and methods for treating ocular diseases or disorders |
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| US416359A (en) * | 1889-12-03 | Sash-fastener | ||
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| IT1230441B (it) * | 1989-02-07 | 1991-10-23 | Acraf | Eteri della serie dell'indazolo |
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| IT1293795B1 (it) | 1997-07-28 | 1999-03-10 | Angelini Ricerche Spa | Farmaco attivo nel ridurre la produzione di proteina mcp-1 |
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| AU2005304393B2 (en) | 2004-11-10 | 2012-09-27 | Synta Pharmaceuticals Corp. | IL-12 modulatory compounds |
| CA2587590A1 (en) | 2004-11-19 | 2006-06-08 | Synta Pharmaceuticals Corp. | Pyrimidine compounds and uses thereof |
| AR053347A1 (es) | 2005-04-06 | 2007-05-02 | Astrazeneca Ab | Derivados de [1,3]tiazolo[4,5-d]pirimidin-2(3h)-ona 5,7-sustituidos |
| UA90707C2 (en) | 2005-04-06 | 2010-05-25 | Астразенека Аб | Novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives |
| DK2262778T5 (da) | 2008-03-07 | 2020-06-08 | Acraf | 1-benzyl-3-hydroxymethylindazolderivativer og brug deraf i behandling af sygdomme baseret på ekspression af mcp-1, cx3cr1 og p40 |
| CN101959866B (zh) | 2008-03-07 | 2013-10-02 | 方济各安吉利克化学联合股份有限公司 | 1-苄基-3-羟基甲基吲唑衍生物及其在治疗基于mcp-1和cx3cr1表达的疾病中的用途 |
| US7919518B2 (en) | 2008-03-07 | 2011-04-05 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40 |
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