ECSP15053445A - Derivados de la pirazolopirrolidina y su uso en el tratamiento de enfermedades - Google Patents
Derivados de la pirazolopirrolidina y su uso en el tratamiento de enfermedadesInfo
- Publication number
- ECSP15053445A ECSP15053445A ECIEPI201553445A ECPI201553445A ECSP15053445A EC SP15053445 A ECSP15053445 A EC SP15053445A EC IEPI201553445 A ECIEPI201553445 A EC IEPI201553445A EC PI201553445 A ECPI201553445 A EC PI201553445A EC SP15053445 A ECSP15053445 A EC SP15053445A
- Authority
- EC
- Ecuador
- Prior art keywords
- methyl
- pat055716a
- fluoro
- methoxy
- chloro
- Prior art date
Links
- GUOAGGANPURUME-UHFFFAOYSA-N 1,4,5,6-tetrahydropyrrolo[3,2-c]pyrazole Chemical class N1N=CC2=C1CCN2 GUOAGGANPURUME-UHFFFAOYSA-N 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 16
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 5
- 125000001153 fluoro group Chemical group F* 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- -1 -CH2F Chemical group 0.000 abstract 3
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 abstract 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 abstract 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 abstract 1
- 125000001246 bromo group Chemical group Br* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 150000003839 salts Chemical class 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
- A61K31/435—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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
RESUMEN DE LA INVENCIÓN De acuerdo con un primer aspecto de la invención, se proporciona un compuesto de la fórmula (I) o una sal farmacéuticamente aceptable del mismo, 20 (I) 4 PAT055716A en donde el anillo C se selecciona a partir de i. y ii. ; 5 A se selecciona a partir de: , , , , , , y . 10 B se selecciona a partir de 5 PAT055716A , y . R3 se selecciona a partir de H, metilo, etilo, -CH2F,-CF3, isopropilo,-OH, etoxilo, metoxilo, ciclopropilo,-CH2OCH3 y-CH2OH; 5 R4a se selecciona a partir de H, alquilo(C1-C4), cicloalquilo(C3-C6),-(CH2)2-OH,-(CH2)2-OCH3,- C(O)-NH(CH3),-C(O)-N(CH3)2, , , , 10 y ; R4b se selecciona a partir de H, alquilo (C1-C4), cicloalquilo(C3-C6),-(CH2)2-OH,-(CH2)2-OCH3, -(CH2)2-O-CH2-CF3,-(CH2)-CH(OH)-CF3,,-C(O)-NH(CH3),-C(O)-N(CH3)2, 6 PAT055716A , , , , , , y ; R5 es H; 5 R1 se selecciona a partir de H, metilo, cloro y flúor; R2 se selecciona a partir de bromo, chloro, fluoro,-O-CF3 y-CF3; R2a 10 es fluoro; R8 es metilo; R15, R16, R18 y R21 son todos metoxilo; 15 R17 es metilo o metoxilo; R22, R23, R26, R27, R28, R30, R32 y R33 son todos metilo; R24 20 es metilo o CHF2; R25 es metilo o-NR9R10; R29 es H o metilo; 25 R31 es H, metilo o metoxilo; 7 PAT055716A R34 es H o metilo; R9 es H o metilo; R10 5 es H, metilo o-C(O)-(C1-C3)alquilo; R35 es H, metilo,-C(O)CH3 o-C(O)OCH2CH3; y 10 * indica el punto de unión al resto de la molécula; con la condición que 15 Cuando el anillo C es i: , A es; , R1 se selecciona a partir de metilo, cloro y flúor, 20 B es: R2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13169364 | 2013-05-27 | ||
| EP13177673 | 2013-07-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP15053445A true ECSP15053445A (es) | 2017-10-31 |
Family
ID=50979827
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECIEPI201553445A ECSP15053445A (es) | 2013-05-27 | 2015-12-22 | Derivados de la pirazolopirrolidina y su uso en el tratamiento de enfermedades |
Country Status (36)
| Country | Link |
|---|---|
| US (2) | US8975417B2 (es) |
| EP (1) | EP3004110B1 (es) |
| JP (1) | JP6181862B2 (es) |
| KR (1) | KR20160012196A (es) |
| CN (1) | CN105408335B (es) |
| AU (1) | AU2014272776C1 (es) |
| BR (1) | BR112015029512A8 (es) |
| CA (1) | CA2913223A1 (es) |
| CL (1) | CL2015003395A1 (es) |
| CR (1) | CR20150628A (es) |
| CU (1) | CU24350B1 (es) |
| CY (1) | CY1119490T1 (es) |
| DK (1) | DK3004110T3 (es) |
| EA (1) | EA029515B1 (es) |
| EC (1) | ECSP15053445A (es) |
| ES (1) | ES2651843T3 (es) |
| HR (1) | HRP20171613T1 (es) |
| HU (1) | HUE036674T2 (es) |
| IL (1) | IL242610A0 (es) |
| LT (1) | LT3004110T (es) |
| ME (1) | ME02906B (es) |
| MX (1) | MX364205B (es) |
| NO (1) | NO3004110T3 (es) |
| PE (1) | PE20160005A1 (es) |
| PH (2) | PH12015502628B1 (es) |
| PL (1) | PL3004110T3 (es) |
| PT (1) | PT3004110T (es) |
| RS (1) | RS56522B1 (es) |
| SG (1) | SG11201509474SA (es) |
| SI (1) | SI3004110T1 (es) |
| SV (1) | SV2015005115A (es) |
| TN (1) | TN2015000505A1 (es) |
| UA (1) | UA116017C2 (es) |
| UY (1) | UY35586A (es) |
| WO (1) | WO2014191896A1 (es) |
| ZA (1) | ZA201508259B (es) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2855483B1 (en) | 2012-05-24 | 2017-10-25 | Novartis AG | Pyrrolopyrrolidinone compounds |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| WO2014115080A1 (en) | 2013-01-22 | 2014-07-31 | Novartis Ag | Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction |
| EA035469B1 (ru) | 2013-03-15 | 2020-06-22 | Инсайт Холдингс Корпорейшн | Трициклические гетероциклы как ингибиторы белков бэт |
| AU2014272695B2 (en) * | 2013-05-28 | 2016-10-20 | Novartis Ag | Pyrazolo-pyrrolidin-4-one derivatives as BET inhibitors and their use in the treatment of disease |
| CN105473581B (zh) | 2013-06-21 | 2019-04-23 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的新取代的双环化合物 |
| KR102307566B1 (ko) | 2013-06-21 | 2021-10-05 | 제니쓰 에피제네틱스 리미티드 | 신규한 바이사이클릭 브로모도메인 억제제 |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CA2919948C (en) | 2013-07-31 | 2020-07-21 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| EP3290407B1 (en) | 2013-10-18 | 2020-01-01 | Celgene Quanticel Research, Inc | Bromodomain inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| SMT202000133T1 (it) | 2014-04-23 | 2020-05-08 | Incyte Corp | 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine bet |
| JP6599979B2 (ja) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
| HK1245246A1 (zh) | 2014-12-01 | 2018-08-24 | 恒翼生物医药科技(上海)有限公司 | 作为溴域抑制剂的取代吡啶酮 |
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| WO2017127930A1 (en) * | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| CA3013988A1 (en) | 2016-02-15 | 2017-08-24 | Cemm-Forschungszentrum Fur Molekulare Medizin Gmbh | Taf1 inhibitors for the therapy of cancer |
| CN109152843A (zh) | 2016-05-20 | 2019-01-04 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| EP3468559B1 (en) * | 2016-06-09 | 2023-11-22 | Dana Farber Cancer Institute, Inc. | Methods of use and pharmaceutical combinations of hdac inhibitors with bet inhibitors |
| CN109715625B (zh) | 2016-06-20 | 2022-04-19 | 因赛特公司 | Bet抑制剂的结晶固体形式 |
| CN113912586B (zh) | 2016-08-31 | 2023-04-07 | 江苏恒瑞医药股份有限公司 | 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用 |
| CN110225755A (zh) | 2016-11-14 | 2019-09-10 | 分子医学研究中心责任有限公司 | Brd4抑制剂和抗叶酸剂的组合用于治疗癌症 |
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