PE131099A1 - Compuestos terapeuticamente activos basados en el reemplazo bioisostero del catecol por el indazol en inhibidores de pde4 - Google Patents
Compuestos terapeuticamente activos basados en el reemplazo bioisostero del catecol por el indazol en inhibidores de pde4Info
- Publication number
- PE131099A1 PE131099A1 PE1998001040A PE00104098A PE131099A1 PE 131099 A1 PE131099 A1 PE 131099A1 PE 1998001040 A PE1998001040 A PE 1998001040A PE 00104098 A PE00104098 A PE 00104098A PE 131099 A1 PE131099 A1 PE 131099A1
- Authority
- PE
- Peru
- Prior art keywords
- indazol
- catecol
- alkyl
- group
- replacement
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title abstract 2
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title 1
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 abstract 2
- 208000027866 inflammatory disease Diseases 0.000 abstract 2
- 239000002571 phosphodiesterase inhibitor Substances 0.000 abstract 2
- 206010006458 Bronchitis chronic Diseases 0.000 abstract 1
- 208000011231 Crohn disease Diseases 0.000 abstract 1
- 206010014561 Emphysema Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 206010006451 bronchitis Diseases 0.000 abstract 1
- 208000007451 chronic bronchitis Diseases 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical class C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 210000000936 intestine Anatomy 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 230000000241 respiratory effect Effects 0.000 abstract 1
Classifications
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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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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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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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (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)
- Immunology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A UNA COMPOSICION QUE COMPRENDE UN INHIBIDOR DE LA FOSFODIESTERASA TIPO IV (PDE4) O UN INHIBIDOR DE LA PRODUCCION DE TNF; QUE EN SU ESCTRUCTURA PRESENTA UN INDAZOL COMO REEMPLAZO BIOISOSTERICO DE UN GRUPO CATECOL, DE PREFERENCIA A LOS COMPUESTOS IA o IB; R ES H, ALQUILO C1-C9, -(CH2)n-CICLOALQUILO C3-C10, -(Z1)b(Z2)cARILO C6-C10, ENTRE OTROS; n ES 0-2; R1 ES H, ALQUILO C1-C9, ALQUENILO C2-C3, FENILO, ENTRE OTROS; b Y c SON 0-1; Z1 ES ALQUILENO C1-C6, ALQUENILENO C2-C6; Z2 ES O, S, SO2, NR119; R2a Y R2b SON H PERO NO SIMULTANEAMENTE, O DE PREFERENCIA UN GRUPO IC o UN GRUPO IV; m ES 0-4; R113 ES DE PREFERENCIA CIANO; R114 Y R115 SON DE PREFERENCIA H; R116 ES METILO O ETILO SUSTITUIDO; X1 ES CR472R473, CR473; X2 ES CR475R477R478, CR477R478, ENTRE OTROS; R472 ES H, OH, BROMO, ENTRE OTROS; R473 ES CIANO, CIANOMETILO, BENCILOXI, ENTRE OTROS; R475 ES H, ALQUILO C1-C6; R477 ES R473, 2-OXO-PIRIDILO, ENTRE OTROS; R478 ES R475, CIANO, (CH2)p-ARILO, ENTRE OTROS; p ES 1-3. UN COMPUESTO PREFERIDO ES 1-(1-CICLOPENTIL-3-ETIL-1H-INDAZOL-6-IL)-4-OXOCICLOHEXANOCARBONITRILO, ENTRE OTROS. LA COMPOSICION PUEDE SER UTIL PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS Y AFECCIONES RESPIRATORIAS COMO INFLAMACION DE LAS ARTICULACIONES, ENFERMEDAD DE CROHN, ENFERMEDAD INFLAMATORIA DEL INTESTINO, ASMA, BRONQUITIS CRONICA, ENFISEMA PULMONAR
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6416097P | 1997-11-04 | 1997-11-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE131099A1 true PE131099A1 (es) | 1999-12-17 |
Family
ID=22053970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1998001040A PE131099A1 (es) | 1997-11-04 | 1998-11-03 | Compuestos terapeuticamente activos basados en el reemplazo bioisostero del catecol por el indazol en inhibidores de pde4 |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US6716978B2 (es) |
| EP (1) | EP1040100A1 (es) |
| JP (1) | JP2001521925A (es) |
| KR (1) | KR20010031783A (es) |
| CN (1) | CN1281441A (es) |
| AP (1) | AP1122A (es) |
| AR (1) | AR016413A1 (es) |
| AU (1) | AU754184B2 (es) |
| BG (1) | BG104391A (es) |
| BR (1) | BR9813938A (es) |
| CA (1) | CA2309175A1 (es) |
| CZ (1) | CZ20001623A3 (es) |
| DZ (1) | DZ2639A1 (es) |
| EA (1) | EA200000385A1 (es) |
| HN (1) | HN1998000172A (es) |
| HR (1) | HRP20000262A2 (es) |
| HU (1) | HUP0100330A3 (es) |
| ID (1) | ID24942A (es) |
| IL (1) | IL135714A0 (es) |
| IS (1) | IS5452A (es) |
| MA (1) | MA26562A1 (es) |
| NO (1) | NO20002127L (es) |
| NZ (1) | NZ503995A (es) |
| OA (1) | OA11353A (es) |
| PA (1) | PA8462601A1 (es) |
| PE (1) | PE131099A1 (es) |
| PL (1) | PL340799A1 (es) |
| SK (1) | SK6262000A3 (es) |
| TN (1) | TNSN98199A1 (es) |
| TR (1) | TR200001256T2 (es) |
| UY (1) | UY25232A1 (es) |
| WO (1) | WO1999023076A1 (es) |
| YU (1) | YU25400A (es) |
| ZA (1) | ZA9810042B (es) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL126745A (en) * | 1997-11-04 | 2003-09-17 | Pfizer Prod Inc | Methods of preparing 4-cyano-4- (substituted indazole) cyclohexanecarboxylic acids useful as pde4 inhibitors |
| UA71971C2 (en) | 1999-06-04 | 2005-01-17 | Agoron Pharmaceuticals Inc | Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases |
| TWI262914B (en) | 1999-07-02 | 2006-10-01 | Agouron Pharma | Compounds and pharmaceutical compositions for inhibiting protein kinases |
| US7141581B2 (en) | 1999-07-02 | 2006-11-28 | Agouron Pharmaceuticals, Inc. | Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use |
| PE20010306A1 (es) * | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| CA2398446A1 (en) | 2000-04-18 | 2001-10-25 | Agouron Pharmaceuticals, Inc. | Pyrazoles for inhibiting protein kinases |
| US6897231B2 (en) * | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| US7211594B2 (en) * | 2000-07-31 | 2007-05-01 | Signal Pharmaceuticals, Llc | Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith |
| ES2427930T3 (es) * | 2001-05-23 | 2013-11-04 | Mitsubishi Tanabe Pharma Corporation | Composición terapéutica para el tratamiento regenerativo de enfermedades de los cartílagos |
| US20060079540A1 (en) * | 2002-11-27 | 2006-04-13 | Altana Pharma Ag | Pde4 and pde3/4 inhibitors for use in the treatment of cachexia |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| JP2005089457A (ja) * | 2003-09-03 | 2005-04-07 | Yung Shin Pharmaceutical Industry Co Ltd | 骨成長を促進するまたは骨吸収を阻害するための薬剤組成物 |
| US6984652B2 (en) * | 2003-09-05 | 2006-01-10 | Warner-Lambert Company Llc | Gyrase inhibitors |
| CN104817534A (zh) * | 2004-03-03 | 2015-08-05 | 塔科达有限责任公司 | 新的羟基-6-杂芳基菲啶及其作为pde4抑制剂的用途 |
| US7432266B2 (en) * | 2004-10-15 | 2008-10-07 | Memory Pharmaceuticals Corporation | Phosphodiesterase 4 inhibitors |
| US7601847B2 (en) | 2004-10-26 | 2009-10-13 | Wyeth | Preparation and purification of 4-(indazol-3-yl)phenols |
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| DE2064304A1 (de) * | 1970-12-29 | 1972-07-20 | Agfa-Gevaert Ag, 5090 Leverkusen | Lichtempfindliches farbfotografisches Material |
| KR100188801B1 (ko) * | 1990-05-18 | 1999-06-01 | 엥겔하르트 라피체 | 이속사졸-4카복스아미드 및 하이드록시알킬리덴 시아노아세트아미드 및 이들 화합물을 함유하는 약제학적 조성물 |
| US5440038A (en) * | 1993-12-07 | 1995-08-08 | Miles Inc. | Process for the purification of substituted 4-amino-1,2,4-triazine-5-ones |
| US6005118A (en) * | 1996-05-03 | 1999-12-21 | Caron; Stephane | Methods of preparing 4-cyano-4 (substituted indazole) cyclohexane-carboxylic acids useful as PDE4 inhibitors |
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| SI0912558T1 (en) * | 1996-06-25 | 2003-10-31 | Pfizer Inc. | Substituted indazole derivatives and their use as phosphodiesterase (pde) type iv and tumor necrosis factor (tnf) inhibitors |
| EP0816357B1 (en) * | 1996-06-27 | 2002-01-09 | Pfizer Inc. | Substituted indazole derivatives |
| EA002113B1 (ru) * | 1996-09-04 | 2001-12-24 | Пфайзер Инк. | Производные индазола и их использование в качестве ингибиторов фосфодиэстеразы (фдэ) типа iv и продуцирования фактора некроза опухоли (фно) |
| WO1998050367A1 (en) * | 1997-05-08 | 1998-11-12 | Pfizer Products Inc. | Processes and intermediates for preparing substituted indazole derivatives |
| US6391872B1 (en) * | 1997-11-04 | 2002-05-21 | Pfizer Inc | Indazole bioisostere replacement of catechol in therapeutically active compounds |
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