AR108179A2 - Compuestos de pirrolo[2,3-d]pirimidina y sus usos para el tratamiento de diversos tipos de cáncer por medio de la modulación de la actividad de la cinasa de proteína tirosina - Google Patents
Compuestos de pirrolo[2,3-d]pirimidina y sus usos para el tratamiento de diversos tipos de cáncer por medio de la modulación de la actividad de la cinasa de proteína tirosinaInfo
- Publication number
- AR108179A2 AR108179A2 ARP170100874A ARP170100874A AR108179A2 AR 108179 A2 AR108179 A2 AR 108179A2 AR P170100874 A ARP170100874 A AR P170100874A AR P170100874 A ARP170100874 A AR P170100874A AR 108179 A2 AR108179 A2 AR 108179A2
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- cycloalkyl
- heterocyclyl
- heteroaryl
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 title 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 title 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical class C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 1
- 229940100514 Syk tyrosine kinase inhibitor Drugs 0.000 title 1
- 201000011510 cancer Diseases 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 12
- 125000001072 heteroaryl group Chemical group 0.000 abstract 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 125000003107 substituted aryl group Chemical group 0.000 abstract 4
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 150000002894 organic compounds Chemical class 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- -1 C3− cycloalkyl 8 Chemical group 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 150000001875 compounds Chemical class 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
- 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
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000004944 pyrrolopyrimidines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
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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
- A61K31/495—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
-
- 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
- A61K31/495—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
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/495—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
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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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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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A—HUMAN NECESSITIES
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- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Pregnancy & Childbirth (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
Abstract
La presente solicitud describe compuestos orgánicos que son útiles para el tratamiento, la prevención, y/o el alivio de enfermedades; en particular se describen compuestos de pirrolo-pirimidina y sus derivados, que inhiben a las cinasas de proteína. Los compuestos orgánicos son útiles en el tratamiento de enfermedades proliferativas. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable o solvato del mismo, caracterizado porque: la línea punteada indica un enlace doble; A es N o CR⁵, en donde R⁵ es hidrógeno o alquilo C₁₋₃; R² y R³ se seleccionan cada uno independientemente a partir del grupo que consiste en hidrógeno, hidroxilo, alquilo C₁₋₃, cicloalquilo C₃₋₈, heterociclilo, arilo, heteroarilo, alquilo C₁₋₃ sustituido, cicloalquilo C₃₋₈ sustituido, heterociclilo sustituido, arilo sustituido, y heteroarilo sustituido; R⁴ es seleccionado del grupo que consiste de C(H)(CH₂CH₃)₂, C(H)(CH₂CH₃)Ph, CH₂CH₃, ciclopropilo, ciclopentilo o ciclohexilo; X es N o CR¹¹, e Y es CR¹²; R¹¹ es seleccionado del grupo que consiste de halógeno, hidrógeno, alquilo C₁₋₃, alcoxi C₁₋₃, CN, C=NOH, C=NOCH₃, C(O)H, C(O)alquilo C₁₋₃, cicloalquilo C₃₋₈, heterociclilo, arilo, heteroarilo, alquilo C₁₋₃ substituido, cicloalquilo C₃₋₈ substituido, heterociclilo substituido, arilo substituido, heteroarilo substituido, -BNR¹³R¹⁴, -BOR¹³, -BC(O)R¹³, -BC(O)OR¹³, -BC(O)NR¹³R¹⁴; donde B es un enlace, alquilo C₁₋₃ o alquilo C₁₋₃ ramificado; donde R¹³ y R¹⁴ son cada uno, independientemente, seleccionados del grupo que consiste de hidrógeno, alquilo C₁₋₃, cicloalquilo C₃₋₈, heterociclilo, arilo, heteroarilo, alquilo substituido, cicloalquilo substituido, heterociclilo substituido, arilo substituido, y heteroarilo substituido y R¹² es -BC(O)NR¹³R¹⁴; donde B es un enlace, alquilo C₁₋₃ o alquilo C₁₋₃ ramificado; donde R¹³ y R¹⁴ son cada una, independientemente, seleccionados del grupo que consiste de hidrógeno, alquilo C₁₋₃, cicloalquilo C₃₋₈, heterociclilo, arilo, heteroarilo, alquilo substituido, cicloalquilo substituido, heterociclilo substituido, arilo substituido, y heteroarilo substituido.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80860506P | 2006-05-26 | 2006-05-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR108179A2 true AR108179A2 (es) | 2018-07-25 |
Family
ID=38779335
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070102252A AR061124A1 (es) | 2006-05-26 | 2007-05-24 | Compuestos de pirrolo[2, 3 - d]pirimidina y sus usos para el tratamiento de diversos tipos de cancer por medio de la modulacion de la actividad de la cinasa de proteina tirosina. |
| ARP170100874A AR108179A2 (es) | 2006-05-26 | 2017-04-05 | Compuestos de pirrolo[2,3-d]pirimidina y sus usos para el tratamiento de diversos tipos de cáncer por medio de la modulación de la actividad de la cinasa de proteína tirosina |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070102252A AR061124A1 (es) | 2006-05-26 | 2007-05-24 | Compuestos de pirrolo[2, 3 - d]pirimidina y sus usos para el tratamiento de diversos tipos de cancer por medio de la modulacion de la actividad de la cinasa de proteina tirosina. |
Country Status (38)
| Country | Link |
|---|---|
| US (2) | US8324225B2 (es) |
| EP (1) | EP2029145B1 (es) |
| JP (2) | JP2009538341A (es) |
| KR (1) | KR101466412B1 (es) |
| CN (1) | CN101594871B (es) |
| AR (2) | AR061124A1 (es) |
| AU (1) | AU2007267645C1 (es) |
| BR (1) | BRPI0712816B8 (es) |
| CA (1) | CA2652044C (es) |
| CL (1) | CL2007001504A1 (es) |
| CR (1) | CR10433A (es) |
| CU (1) | CU23831B1 (es) |
| EA (1) | EA016301B1 (es) |
| EC (1) | ECSP088910A (es) |
| ES (1) | ES2623133T3 (es) |
| GE (1) | GEP20115283B (es) |
| GT (1) | GT200800258A (es) |
| HN (1) | HN2008001752A (es) |
| HR (1) | HRP20170631T1 (es) |
| IL (1) | IL195086A (es) |
| JO (1) | JO3235B1 (es) |
| MA (1) | MA30557B1 (es) |
| ME (1) | ME00486B (es) |
| MX (1) | MX2008015076A (es) |
| MY (1) | MY150650A (es) |
| NO (1) | NO343182B1 (es) |
| NZ (1) | NZ572549A (es) |
| PE (1) | PE20080263A1 (es) |
| PL (1) | PL2029145T3 (es) |
| PT (1) | PT2029145T (es) |
| SG (1) | SG172632A1 (es) |
| SM (1) | SMP200800069B (es) |
| TN (1) | TNSN08481A1 (es) |
| TW (1) | TWI398252B (es) |
| UA (1) | UA95632C2 (es) |
| UY (1) | UY30369A1 (es) |
| WO (1) | WO2007140222A2 (es) |
| ZA (1) | ZA200809382B (es) |
Families Citing this family (195)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI3184526T1 (sl) | 2005-12-13 | 2019-03-29 | Incyte Holdings Corporation | Derivati pirolo(2,3-D)pirimidina kot inhibitorji Janus kinaze |
| US7989459B2 (en) | 2006-02-17 | 2011-08-02 | Pharmacopeia, Llc | Purinones and 1H-imidazopyridinones as PKC-theta inhibitors |
| US7919490B2 (en) | 2006-10-04 | 2011-04-05 | Wyeth Llc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| WO2008043019A1 (en) | 2006-10-04 | 2008-04-10 | Pharmacopeia, Inc | 8-substituted 2-(benzimidazolyl) purine derivatives for immunosuppression |
| US7902187B2 (en) | 2006-10-04 | 2011-03-08 | Wyeth Llc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| MX2009013402A (es) | 2007-06-13 | 2010-02-24 | Incyte Corp | Sales de inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3-d]piri midin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo. |
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