HRP20220512T1 - Supstituirani pirazolopirimidini kao aktivatori glukocerebrozidaze - Google Patents
Supstituirani pirazolopirimidini kao aktivatori glukocerebrozidaze Download PDFInfo
- Publication number
- HRP20220512T1 HRP20220512T1 HRP20220512TT HRP20220512T HRP20220512T1 HR P20220512 T1 HRP20220512 T1 HR P20220512T1 HR P20220512T T HRP20220512T T HR P20220512TT HR P20220512 T HRP20220512 T HR P20220512T HR P20220512 T1 HRP20220512 T1 HR P20220512T1
- Authority
- HR
- Croatia
- Prior art keywords
- methyl
- c2alkyl
- pharmaceutical composition
- phenyl
- c4alkyl
- Prior art date
Links
- 108010017544 Glucosylceramidase Proteins 0.000 title claims 2
- APXRHPDHORGIEB-UHFFFAOYSA-N 1H-pyrazolo[4,3-d]pyrimidine Chemical class N1=CN=C2C=NNC2=C1 APXRHPDHORGIEB-UHFFFAOYSA-N 0.000 title 1
- 102000004547 Glucosylceramidase Human genes 0.000 title 1
- 239000012190 activator Substances 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- -1 cyano, nitro, amino Chemical group 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 101150028412 GBA gene Proteins 0.000 claims 2
- 208000015872 Gaucher disease Diseases 0.000 claims 2
- 206010064571 Gene mutation Diseases 0.000 claims 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- IDVNKENDKSWSGM-UHFFFAOYSA-N 5,7-dimethyl-n-quinolin-2-ylpyrazolo[1,5-a]pyrimidine-3-carboxamide Chemical compound C1=CC=CC2=NC(NC(=O)C=3C=NN4C(C)=CC(=NC4=3)C)=CC=C21 IDVNKENDKSWSGM-UHFFFAOYSA-N 0.000 claims 1
- CWYOCWBZXYMRSX-UHFFFAOYSA-N 5,7-dimethyl-n-quinolin-3-ylpyrazolo[1,5-a]pyrimidine-3-carboxamide Chemical compound C1=CC=CC2=CC(NC(=O)C=3C=NN4C(C)=CC(=NC4=3)C)=CN=C21 CWYOCWBZXYMRSX-UHFFFAOYSA-N 0.000 claims 1
- 102100033342 Lysosomal acid glucosylceramidase Human genes 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- MUEZEYDZQXQLNT-UHFFFAOYSA-N chembl1876337 Chemical compound N1=CC=C2C(NC(=O)C3=C4NC(=C)C=C(N4N=C3)C)=CC=CC2=C1 MUEZEYDZQXQLNT-UHFFFAOYSA-N 0.000 claims 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 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000000265 leukocyte Anatomy 0.000 claims 1
- MCQYBGOYJAACFA-UHFFFAOYSA-N n-(4-tert-butylcyclohexyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-carboxamide Chemical compound C=12N=C(C)C=C(C)N2N=CC=1C(=O)NC1CCC(C(C)(C)C)CC1 MCQYBGOYJAACFA-UHFFFAOYSA-N 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
Classifications
-
- 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
- A61K31/535—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
-
- 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
-
- 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)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42094610P | 2010-12-08 | 2010-12-08 | |
| EP18165005.2A EP3366688B1 (en) | 2010-12-08 | 2011-12-08 | Substituted pyrazolopyrimidines as glucocerebrosidase activators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20220512T1 true HRP20220512T1 (hr) | 2022-05-27 |
Family
ID=45498099
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20220512TT HRP20220512T1 (hr) | 2010-12-08 | 2011-12-08 | Supstituirani pirazolopirimidini kao aktivatori glukocerebrozidaze |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US9353117B2 (OSRAM) |
| EP (2) | EP2649075B1 (OSRAM) |
| JP (1) | JP6154746B2 (OSRAM) |
| KR (1) | KR101931224B1 (OSRAM) |
| CN (1) | CN103534255B (OSRAM) |
| AU (1) | AU2011338377B2 (OSRAM) |
| BR (1) | BR112013014242B1 (OSRAM) |
| CA (1) | CA2820362C (OSRAM) |
| CY (1) | CY1125186T1 (OSRAM) |
| DK (2) | DK2649075T3 (OSRAM) |
| ES (2) | ES2681218T3 (OSRAM) |
| HR (1) | HRP20220512T1 (OSRAM) |
| HU (1) | HUE038635T2 (OSRAM) |
| IL (2) | IL226767B (OSRAM) |
| LT (1) | LT3366688T (OSRAM) |
| MX (2) | MX385600B (OSRAM) |
| PL (2) | PL2649075T3 (OSRAM) |
| PT (2) | PT2649075T (OSRAM) |
| RS (1) | RS63320B1 (OSRAM) |
| RU (1) | RU2603637C2 (OSRAM) |
| SI (2) | SI2649075T1 (OSRAM) |
| TR (1) | TR201810523T4 (OSRAM) |
| WO (1) | WO2012078855A1 (OSRAM) |
| ZA (1) | ZA201304215B (OSRAM) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2649075T1 (sl) | 2010-12-08 | 2018-10-30 | The U.S.A. As Represented By The Secretary, Department Of Health And Human Services | Substituirani pirazolopirimidini kot aktivatorji glukocerebrozidaze |
| JP2014517079A (ja) | 2011-06-22 | 2014-07-17 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| US9845327B2 (en) * | 2011-06-22 | 2017-12-19 | The General Hospital Corporation | Treatment of proteinopathies |
| EP2723717A2 (en) | 2011-06-24 | 2014-04-30 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| MX2013015058A (es) | 2011-06-24 | 2014-01-20 | Amgen Inc | Antagonistas de melastatina 8 de potencial receptor transitorio y su uso en tratamientos. |
| WO2013059587A1 (en) * | 2011-10-20 | 2013-04-25 | Sirtris Pharmaceuticals, Inc. | Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| PT4190786T (pt) | 2012-12-07 | 2025-05-29 | Vertex Pharma | Compostos úteis como inibidores da quinase atr |
| JP2016512816A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な化合物 |
| JP2016512239A (ja) | 2013-03-15 | 2016-04-25 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な化合物 |
| EP2970286A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| MX389256B (es) | 2013-10-04 | 2025-03-20 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos y usos de los mismos. |
| US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CA2932757C (en) | 2013-12-06 | 2023-10-31 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| EA201691872A1 (ru) | 2014-03-19 | 2017-04-28 | Инфинити Фармасьютикалз, Инк. | Гетероциклические соединения для применения в лечении pi3k-гамма-опосредованных расстройств |
| KR102575125B1 (ko) | 2014-06-05 | 2023-09-07 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 저해제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]-피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물의 방사성표지된 유도체, 상기 화합물의 제조 및 이의 다양한 고체 형태 |
| RU2736219C2 (ru) | 2014-06-17 | 2020-11-12 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации ингибиторов снк1 и atr |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| MX2017005586A (es) | 2014-11-03 | 2017-06-19 | Bayer Pharma AG | Piperidinilpirazolopirimidinonas y utilización de las mismas. |
| US20180185368A1 (en) | 2014-11-06 | 2018-07-05 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| KR102662215B1 (ko) * | 2014-11-06 | 2024-05-02 | 비알 - 알&디 인베스트먼츠, 에스.에이. | 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도 |
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| EP3317282B1 (en) | 2015-07-01 | 2020-12-09 | Northwestern University | Substituted 4-methyl-pyrrolo[1.2-a]pyrimidine-8-carboxamide compounds and uses thereof for modulating glucocerebrosidase activity |
| WO2017040879A1 (en) * | 2015-09-04 | 2017-03-09 | Lysosomal Therapeutics Inc. | Thiazolo(3,2-a) pyrimidinone and other heterobicyclic pyrimidinone compounds for use in medical therapy |
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| KR20230104752A9 (ko) * | 2016-04-06 | 2024-11-15 | 비알 - 알&디 인베스트먼츠, 에스.에이. | 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물및 의학적 장애의 치료에서의 그의 용도 |
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| EP3452455A4 (en) * | 2016-05-05 | 2019-11-13 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO [1,2-] PYRIDINES, SUBSTITUTED IMIDAZO [1,2-] PYRAZINES, RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF ILLNESSES |
| WO2017192929A1 (en) * | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED PYRROLO[1,2-α]TRIAZINES AND RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| JP7164774B2 (ja) * | 2016-05-05 | 2022-11-02 | ビアル－アール・アンド・ディ・インベストメンツ・ソシエダーデ・アノニマ | 置換イミダゾ［１，２－ｂ］ピリダジン、置換イミダゾ［１，５－ｂ］ピリダジン、関連化合物、および医学的障害の治療におけるその使用 |
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