JP2017527598A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017527598A5 JP2017527598A5 JP2017514842A JP2017514842A JP2017527598A5 JP 2017527598 A5 JP2017527598 A5 JP 2017527598A5 JP 2017514842 A JP2017514842 A JP 2017514842A JP 2017514842 A JP2017514842 A JP 2017514842A JP 2017527598 A5 JP2017527598 A5 JP 2017527598A5
- Authority
- JP
- Japan
- Prior art keywords
- injury
- compound according
- disease
- alkyl
- disorder
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- -1 5-fluoro - pyrid -2-yl Chemical group 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 8
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 150000002367 halogens Chemical group 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 7
- 238000011282 treatment Methods 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- 150000003839 salts Chemical group 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 229910052739 hydrogen Inorganic materials 0.000 claims description 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 125000001769 aryl amino group Chemical group 0.000 claims description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 208000014674 injury Diseases 0.000 claims 15
- 208000027418 Wounds and injury Diseases 0.000 claims 11
- 230000006378 damage Effects 0.000 claims 11
- 208000035475 disorder Diseases 0.000 claims 9
- 208000020431 spinal cord injury Diseases 0.000 claims 7
- 208000029028 brain injury Diseases 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 208000015114 central nervous system disease Diseases 0.000 claims 4
- 230000000069 prophylactic effect Effects 0.000 claims 4
- 230000008733 trauma Effects 0.000 claims 4
- 206010061218 Inflammation Diseases 0.000 claims 3
- 210000003169 central nervous system Anatomy 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims 3
- 231100000317 environmental toxin Toxicity 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000003449 preventive effect Effects 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 1
- 208000024412 Friedreich ataxia Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000001089 Multiple system atrophy Diseases 0.000 claims 1
- 102000029797 Prion Human genes 0.000 claims 1
- 108091000054 Prion Proteins 0.000 claims 1
- 241000283080 Proboscidea <mammal> Species 0.000 claims 1
- 206010057430 Retinal injury Diseases 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 208000008675 hereditary spastic paraplegia Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 5
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 5
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 5
- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical compound C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 description 4
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 4
- PCLIMKBDDGJMGD-UHFFFAOYSA-N N-bromosuccinimide Chemical compound BrN1C(=O)CCC1=O PCLIMKBDDGJMGD-UHFFFAOYSA-N 0.000 description 4
- JRNVZBWKYDBUCA-UHFFFAOYSA-N N-chlorosuccinimide Chemical compound ClN1C(=O)CCC1=O JRNVZBWKYDBUCA-UHFFFAOYSA-N 0.000 description 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 4
- ZCSHNCUQKCANBX-UHFFFAOYSA-N lithium diisopropylamide Chemical compound [Li+].CC(C)[N-]C(C)C ZCSHNCUQKCANBX-UHFFFAOYSA-N 0.000 description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 3
- MZRVEZGGRBJDDB-UHFFFAOYSA-N N-Butyllithium Chemical compound [Li]CCCC MZRVEZGGRBJDDB-UHFFFAOYSA-N 0.000 description 3
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 description 3
- DTQVDTLACAAQTR-UHFFFAOYSA-N trifluoroacetic acid Substances OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 3
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 description 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 description 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 description 2
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 description 2
- 208000010877 cognitive disease Diseases 0.000 description 2
- 235000019439 ethyl acetate Nutrition 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 208000003532 hypothyroidism Diseases 0.000 description 2
- 230000002989 hypothyroidism Effects 0.000 description 2
- 230000009245 menopause Effects 0.000 description 2
- XHXFXVLFKHQFAL-UHFFFAOYSA-N phosphoryl trichloride Chemical compound ClP(Cl)(Cl)=O XHXFXVLFKHQFAL-UHFFFAOYSA-N 0.000 description 2
- 238000011321 prophylaxis Methods 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- FYSNRJHAOHDILO-UHFFFAOYSA-N thionyl chloride Chemical compound ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 description 2
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 2
- CYPYTURSJDMMMP-WVCUSYJESA-N (1e,4e)-1,5-diphenylpenta-1,4-dien-3-one;palladium Chemical compound [Pd].[Pd].C=1C=CC=CC=1\C=C\C(=O)\C=C\C1=CC=CC=C1.C=1C=CC=CC=1\C=C\C(=O)\C=C\C1=CC=CC=C1.C=1C=CC=CC=1\C=C\C(=O)\C=C\C1=CC=CC=C1 CYPYTURSJDMMMP-WVCUSYJESA-N 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- 208000037853 Abnormal uterine bleeding Diseases 0.000 description 1
- 201000000736 Amenorrhea Diseases 0.000 description 1
- 206010001928 Amenorrhoea Diseases 0.000 description 1
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 1
- 201000005670 Anovulation Diseases 0.000 description 1
- 206010002659 Anovulatory cycle Diseases 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 206010003805 Autism Diseases 0.000 description 1
- 208000020706 Autistic disease Diseases 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 206010007559 Cardiac failure congestive Diseases 0.000 description 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- 102000004076 Dopamine D1 Receptors Human genes 0.000 description 1
- 108090000511 Dopamine D1 Receptors Proteins 0.000 description 1
- 101001117089 Drosophila melanogaster Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1 Proteins 0.000 description 1
- 208000012661 Dyskinesia Diseases 0.000 description 1
- 206010057671 Female sexual dysfunction Diseases 0.000 description 1
- 208000001914 Fragile X syndrome Diseases 0.000 description 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010020880 Hypertrophy Diseases 0.000 description 1
- 206010027339 Menstruation irregular Diseases 0.000 description 1
- 208000016285 Movement disease Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 208000005107 Premature Birth Diseases 0.000 description 1
- 206010036590 Premature baby Diseases 0.000 description 1
- 206010036618 Premenstrual syndrome Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 description 1
- 208000005793 Restless legs syndrome Diseases 0.000 description 1
- 206010039085 Rhinitis allergic Diseases 0.000 description 1
- 201000001880 Sexual dysfunction Diseases 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 208000000323 Tourette Syndrome Diseases 0.000 description 1
- 208000016620 Tourette disease Diseases 0.000 description 1
- 206010044565 Tremor Diseases 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 231100000540 amenorrhea Toxicity 0.000 description 1
- 239000000908 ammonium hydroxide Substances 0.000 description 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 231100000552 anovulation Toxicity 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 230000001363 autoimmune Effects 0.000 description 1
- HKVFISRIUUGTIB-UHFFFAOYSA-O azanium;cerium;nitrate Chemical compound [NH4+].[Ce].[O-][N+]([O-])=O HKVFISRIUUGTIB-UHFFFAOYSA-O 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 206010013663 drug dependence Diseases 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 239000000262 estrogen Substances 0.000 description 1
- 206010020718 hyperplasia Diseases 0.000 description 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 description 1
- 208000000509 infertility Diseases 0.000 description 1
- 231100000535 infertility Toxicity 0.000 description 1
- 230000036512 infertility Effects 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 201000003631 narcolepsy Diseases 0.000 description 1
- RLOWWWKZYUNIDI-UHFFFAOYSA-N phosphinic chloride Chemical compound ClP=O RLOWWWKZYUNIDI-UHFFFAOYSA-N 0.000 description 1
- 201000000484 premenstrual tension Diseases 0.000 description 1
- 239000000651 prodrug Chemical group 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 229960003387 progesterone Drugs 0.000 description 1
- 239000000186 progesterone Substances 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 208000002815 pulmonary hypertension Diseases 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 231100000872 sexual dysfunction Toxicity 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 230000007781 signaling event Effects 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 208000020685 sleep-wake disease Diseases 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000004014 thioethyl group Chemical group [H]SC([H])([H])C([H])([H])* 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462051735P | 2014-09-17 | 2014-09-17 | |
| US62/051,735 | 2014-09-17 | ||
| US201462052283P | 2014-09-18 | 2014-09-18 | |
| US62/052,283 | 2014-09-18 | ||
| PCT/US2015/050814 WO2016044667A1 (en) | 2014-09-17 | 2015-09-17 | Compounds and methods |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017527598A JP2017527598A (ja) | 2017-09-21 |
| JP2017527598A5 true JP2017527598A5 (enExample) | 2018-10-18 |
| JP6596080B2 JP6596080B2 (ja) | 2019-10-23 |
Family
ID=55533880
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017514842A Active JP6596080B2 (ja) | 2014-09-17 | 2015-09-17 | 化合物および方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US10150774B2 (enExample) |
| EP (2) | EP3193878B1 (enExample) |
| JP (1) | JP6596080B2 (enExample) |
| KR (1) | KR102332957B1 (enExample) |
| CN (1) | CN107106563B (enExample) |
| AU (1) | AU2015317527B2 (enExample) |
| BR (1) | BR112017005533B1 (enExample) |
| CA (1) | CA2961212C (enExample) |
| ES (2) | ES2915200T3 (enExample) |
| HK (1) | HK1243342A1 (enExample) |
| IL (2) | IL292225B2 (enExample) |
| MX (1) | MX385382B (enExample) |
| RU (1) | RU2711442C2 (enExample) |
| WO (1) | WO2016044667A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HK1243342A1 (zh) | 2014-09-17 | 2018-07-13 | Intra-Cellular Therapies, Inc. | 化合物和方法 |
| US11839614B2 (en) | 2018-01-31 | 2023-12-12 | Intra-Cellular Therapies, Inc. | Methods for treating or mitigating cardiotoxicity characterized by inhibition of adenosine A2 signaling and/or adenosine A2 receptor expression |
| WO2019227004A1 (en) * | 2018-05-25 | 2019-11-28 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CA3117148A1 (en) * | 2018-10-21 | 2020-04-30 | Intra-Cellular Therapies, Inc. | Novel uses |
| WO2020146384A1 (en) | 2019-01-07 | 2020-07-16 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2020210614A1 (en) * | 2019-04-12 | 2020-10-15 | Intra-Cellular Therapies, Inc. | Organic compounds |
| MX2022002607A (es) * | 2019-09-03 | 2022-03-25 | Intra Cellular Therapies Inc | Metodos de tratamiento. |
| EP4025202A4 (en) | 2019-09-03 | 2023-08-02 | Intra-Cellular Therapies, Inc. | NOVEL CONNECTIONS |
| US12364695B2 (en) | 2020-06-02 | 2025-07-22 | Intra-Cellular Therapies, Inc. | Methods of treating inflammatory disease |
Family Cites Families (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6032638B2 (ja) | 1976-09-01 | 1985-07-29 | 武田薬品工業株式会社 | ３−アミノピラゾロ〔３，４−ｄ〕ピリミジン誘導体 |
| JPS58500966A (ja) | 1981-04-22 | 1983-06-09 | ビイク グルデン ロンベルク ヒエ−ミツシエ フアブリ−ク ゲゼルシヤフト ミツト ベシユレンクテル ハフツング | 新規ピラゾロ〔３，４−ｄ〕ピリミジン、その製法及びこれを含有する医薬品 |
| US4469868A (en) | 1982-05-24 | 1984-09-04 | Warner-Lambert Company | Alkylimidazo[1,2-c]pyrazolo[3,4-e]pyrimidines |
| US4603203A (en) | 1983-12-14 | 1986-07-29 | Takeda Chemical Industries, Ltd. | 3-aminopyrazolo[3,4-d]pyrimidine derivatives and production thereof |
| US4666908A (en) | 1985-04-05 | 1987-05-19 | Warner-Lambert Company | 5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use |
| NZ238609A (en) | 1990-06-21 | 1993-12-23 | Schering Corp | Polycyclic guanine derivatives; preparation, pharmaceutical compositions, |
| US5202328A (en) | 1991-03-06 | 1993-04-13 | Merck & Co., Inc. | Substituted fused pyrimidinones |
| US5294612A (en) | 1992-03-30 | 1994-03-15 | Sterling Winthrop Inc. | 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof |
| HUT72640A (en) | 1993-02-26 | 1996-05-28 | Schering Corp | 2-benzyl-polycyclic guanine derivatives, pharmaceutical compositions containing them and process for preparing them |
| GB9304919D0 (en) | 1993-03-10 | 1993-04-28 | Celltech Ltd | Chemical compounds |
| GB9315017D0 (en) | 1993-07-20 | 1993-09-01 | Glaxo Lab Sa | Chemical compounds |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US5824683A (en) | 1995-11-28 | 1998-10-20 | Schering Corporation | 2'- 4'-halo- 1,1'-biphenyl!-4-yl!methyl!-5'-methyl-spiro cyclopentane-1,7' (8'H)- 3H! imidazo 2,1-b!purin!-4' (5'H)-ones |
| GB9526245D0 (en) | 1995-12-21 | 1996-02-21 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9622363D0 (en) | 1996-10-28 | 1997-01-08 | Celltech Therapeutics Ltd | Chemical compounds |
| US6057329A (en) | 1996-12-23 | 2000-05-02 | Celltech Therapeutics Limited | Fused polycyclic 2-aminopyrimidine derivatives |
| SE9701398D0 (sv) | 1997-04-15 | 1997-04-15 | Astra Pharma Prod | Novel compounds |
| CZ299633B6 (cs) * | 1997-04-25 | 2008-09-24 | Pfizer Inc. | Pyrazolopyrimidinony, meziprodukty pro jejich výrobu a farmaceutické a veterinární kompozice na jejich bázi |
| IT1291372B1 (it) | 1997-05-21 | 1999-01-07 | Schering Plough S P A | Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie |
| US6013621A (en) | 1997-10-17 | 2000-01-11 | The Rockfeller University | Method of treating psychosis and/or hyperactivity |
| GB9722520D0 (en) | 1997-10-24 | 1997-12-24 | Pfizer Ltd | Compounds |
| EP1067123B1 (en) | 1998-03-31 | 2011-01-19 | Kyowa Hakko Kirin Co., Ltd. | Nitrogenous heterocyclic compounds |
| US6133273A (en) | 1998-05-08 | 2000-10-17 | American Home Products Corporation | Pyrazolopyrimidine-2,4-dione sulfonamides |
| GB9907658D0 (en) | 1999-04-06 | 1999-05-26 | Zeneca Ltd | Chemical compounds |
| DE60006541D1 (de) | 1999-06-30 | 2003-12-18 | Merck & Co Inc | Src-kinase hemmende verbindungen |
| CA2376951A1 (en) | 1999-06-30 | 2001-01-04 | Peter J. Sinclair | Src kinase inhibitor compounds |
| DE19931206A1 (de) | 1999-07-07 | 2001-01-11 | Stief Christian | Arzneimittel zur Erhöhung des cAMP-Spiegels und deren Verwendung |
| ES2250186T3 (es) | 1999-09-10 | 2006-04-16 | MERCK & CO., INC. | Inhibidores de tirosina quinasa. |
| CA2379585C (en) | 1999-09-30 | 2006-06-20 | James W. Darrow | Certain alkylene diamine-substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines |
| AU7547900A (en) | 1999-10-11 | 2001-04-23 | Pfizer Inc. | 5-(2-substituted-5-heterocyclylsulphonylpyrid-3-yl)- dihydropyrazolo(4,3-d)pyrimidin-7-ones as phosphodiesterase inhibitors |
| TWI265925B (en) | 1999-10-11 | 2006-11-11 | Pfizer | Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them |
| IL139073A0 (en) | 1999-10-21 | 2001-11-25 | Pfizer | Treatment of neuropathy |
| MY125533A (en) | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US20020006926A1 (en) | 2000-04-19 | 2002-01-17 | Roylance H. H. | Use of cyclic GMP-specific phosphodiesterase inhibitors for treatment of parkinson's disease |
| US6693099B2 (en) | 2000-10-17 | 2004-02-17 | The Procter & Gamble Company | Substituted piperazine compounds optionally containing a quinolyl moiety for treating multidrug resistance |
| BR0208078A (pt) | 2001-03-16 | 2004-03-02 | Pfizer | Compostos pirazol[4,3-d]pirimidinona como inibidores de cgmp pde |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| SE0102315D0 (sv) | 2001-06-28 | 2001-06-28 | Astrazeneca Ab | Compounds |
| ATE395349T1 (de) | 2001-08-28 | 2008-05-15 | Schering Corp | Polycyclische guanin phosphodiesterase inhibitoren |
| AU2002324846B2 (en) * | 2001-08-31 | 2007-05-10 | Childrens Hospital Medical Center | Phosphodiesterase activity and regulation of phosphodiesterase 1-B-mediated signaling in brain |
| CA2465893A1 (en) | 2001-11-09 | 2003-05-22 | Schering Corporation | Polycyclic guanine derivative phosphodiesterase v inhibitors |
| EP1483277A4 (en) | 2002-02-15 | 2007-10-03 | Merckle Gmbh | CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS OF PREPARATION AND USE, AND FORMULATION AND PHARMACEUTICAL APPLICATIONS |
| CA2477253A1 (en) | 2002-02-21 | 2003-09-04 | The Rockefeller University | Compositions and method for regulation of calcium-dependent signalling in brain |
| GB0230045D0 (en) | 2002-12-23 | 2003-01-29 | Glaxo Group Ltd | Compounds |
| EP1613747A1 (en) | 2003-03-31 | 2006-01-11 | Pfizer Products Inc. | Crystal structure of 3 ,5 -cyclic nucleotide phosphodiesterase 1b (pde1b) and uses thereof |
| EA200501548A1 (ru) | 2003-04-01 | 2006-02-24 | Апплайд Резеч Системз Арс Холдинг Н.В. | Ингибиторы фосфодиэстераз при бесплодии |
| CA2537829A1 (en) | 2003-09-05 | 2005-03-17 | Neurogen Corporation | Heteroaryl fused pyridines, pyrazines and pyrimidines as crf1 receptor ligands |
| JP5084725B2 (ja) | 2005-06-06 | 2012-11-28 | 武田薬品工業株式会社 | 有機化合物 |
| US20080194592A1 (en) | 2005-08-23 | 2008-08-14 | Intra-Cellular Therapies, Inc. | Organic Compounds |
| CA2651519A1 (en) | 2006-06-06 | 2007-12-13 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US20070286890A1 (en) | 2006-06-07 | 2007-12-13 | John Garnett Walt | Eyelash applicator and method |
| JP2010509399A (ja) * | 2006-11-13 | 2010-03-25 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
| EP2089034A4 (en) | 2006-12-05 | 2010-07-28 | Intra Cellular Therapies Inc | NEW USES |
| AU2008249750B2 (en) * | 2007-05-11 | 2011-07-14 | Pfizer Inc. | Amino-heterocyclic compounds |
| US8846693B2 (en) | 2007-12-06 | 2014-09-30 | Intra-Cellular Therapies, Inc. | Optionally substituted pyrazolo[3,4-d]pyrimidine-4,6-diones |
| CN104370922A (zh) | 2007-12-06 | 2015-02-25 | 武田药品工业株式会社 | 有机化合物 |
| EP2367431B1 (en) * | 2008-12-06 | 2015-08-05 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US8859564B2 (en) | 2008-12-06 | 2014-10-14 | Intra-Cellular Therapies, Inc. | Pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione derivatives useful as inhibitors of phosphodiesterase 1 |
| EP2358723B1 (en) | 2008-12-06 | 2015-05-13 | Intra-Cellular Therapies, Inc. | 4,5,7,8-tetrahydro-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine compounds as PDE1 inhibitors |
| AU2009322900A1 (en) * | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN102238873A (zh) | 2008-12-06 | 2011-11-09 | 细胞内治疗公司 | 有机化合物 |
| SG171775A1 (en) | 2008-12-06 | 2011-07-28 | Intra Cellular Therapies Inc | Organic compounds |
| US11464781B2 (en) | 2009-02-25 | 2022-10-11 | Intra-Cellular Therapies, Inc. | PDE1 inhibitors for ophthalmic disorders |
| WO2010132127A1 (en) | 2009-05-13 | 2010-11-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP2485771A4 (en) | 2009-10-08 | 2014-11-12 | Intra Cellular Therapies Inc | TRACER AND METHODS TAGGED ON PHOSPHODIESTERASE 1 |
| KR101868165B1 (ko) | 2010-04-22 | 2018-07-19 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| WO2011153136A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| TW201206937A (en) | 2010-05-31 | 2012-02-16 | Intra Cellular Therapies Inc | Organic compounds |
| US9371327B2 (en) | 2010-05-31 | 2016-06-21 | Intra-Cellular Therapies, Inc. | PDE1 inhibitor compounds |
| US9763948B2 (en) | 2010-05-31 | 2017-09-19 | Intra-Cellular Therapies, Inc. | PDE1 inhibitory compounds and methods |
| JP6051210B2 (ja) | 2011-06-10 | 2016-12-27 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 有機化合物 |
| AR091507A1 (es) | 2012-06-21 | 2015-02-11 | Intra Cellular Therapies Inc | SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA |
| KR102240326B1 (ko) | 2013-03-15 | 2021-04-13 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| ES2745819T3 (es) * | 2014-08-07 | 2020-03-03 | Intra Cellular Therapies Inc | Derivados de imidazo[1,2-a]-pirazolo[4,3-e]-pirimidin-4-ona con actividad inhibidora de la PDE1 |
| HK1243342A1 (zh) | 2014-09-17 | 2018-07-13 | Intra-Cellular Therapies, Inc. | 化合物和方法 |
| CN104570148B (zh) * | 2014-12-29 | 2015-09-02 | 河海大学 | 涉水结构物渗漏无热源光纤定位定向系统及监测方法 |
-
2015
- 2015-09-17 HK HK18102919.4A patent/HK1243342A1/zh unknown
- 2015-09-17 WO PCT/US2015/050814 patent/WO2016044667A1/en not_active Ceased
- 2015-09-17 MX MX2017003646A patent/MX385382B/es unknown
- 2015-09-17 JP JP2017514842A patent/JP6596080B2/ja active Active
- 2015-09-17 RU RU2017112989A patent/RU2711442C2/ru active
- 2015-09-17 EP EP15841777.4A patent/EP3193878B1/en active Active
- 2015-09-17 BR BR112017005533-3A patent/BR112017005533B1/pt active IP Right Grant
- 2015-09-17 AU AU2015317527A patent/AU2015317527B2/en active Active
- 2015-09-17 CN CN201580062061.3A patent/CN107106563B/zh active Active
- 2015-09-17 CA CA2961212A patent/CA2961212C/en active Active
- 2015-09-17 US US15/512,005 patent/US10150774B2/en active Active
- 2015-09-17 EP EP20178873.4A patent/EP3725789B1/en active Active
- 2015-09-17 ES ES20178873T patent/ES2915200T3/es active Active
- 2015-09-17 KR KR1020177010409A patent/KR102332957B1/ko active Active
- 2015-09-17 IL IL292225A patent/IL292225B2/en unknown
- 2015-09-17 ES ES15841777T patent/ES2857567T3/es active Active
-
2017
- 2017-03-12 IL IL251107A patent/IL251107B/en unknown
-
2018
- 2018-11-09 US US16/186,272 patent/US20190144460A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017527598A5 (enExample) | ||
| KR102821964B1 (ko) | 치환된 피롤로피리미딘 jak 억제제 및 이의 제조 및 사용 방법 | |
| IL287004B1 (en) | Dosage forms and regimens for amino acid compounds | |
| US12018017B2 (en) | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof | |
| MX386258B (es) | Derivados de 5,7-dihidro-pirrolo-piridina para tratar enfermedades neurologicas y neurodegenerativas | |
| MX2022016276A (es) | Nuevos profarmacos de catecolamina para uso en el tratamiento de la enfermedad de parkinson. | |
| PH12015500294B1 (en) | Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors | |
| WO2017127430A1 (en) | Irak4 inhibiting agents | |
| JP2022531088A (ja) | Ｊａｋ阻害剤としての置換ピロロピリジン | |
| CN105085482B (zh) | 取代的哌嗪化合物及其使用方法和用途 | |
| WO2019090143A1 (en) | Pyrazolyl pyrrolo[2,3-b]pyrimidine-5-carboxylate analogs and methods of making the same | |
| IL285708B1 (en) | Imidazopyridinyl compounds and use thereof for treatment of neurodegenerative disorders | |
| PH12021552375A1 (en) | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders | |
| CN105294554B (zh) | 苯基哌嗪衍生物及其使用方法和用途 | |
| CN105461635B (zh) | 苯基哌嗪衍生物及其使用方法和用途 | |
| JP2021535924A (ja) | 新規なチアゾール誘導体及びその薬学的に許容される塩 | |
| JP2017514867A5 (enExample) | ||
| CN106279153B (zh) | 取代的吲哚化合物及其使用方法和用途 | |
| CN109912514B (zh) | (2-杂芳基胺基苯基)氮杂环衍生物及其用途 | |
| CN106065018B (zh) | 取代的吲哚化合物及其使用方法和用途 | |
| CN105085491B (zh) | 取代的吲哚化合物及其使用方法和用途 | |
| CA3063180A1 (en) | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof | |
| CN108409729B (zh) | 苯基八氢-1H-吡啶并[1,2-a]吡嗪衍生物及其用途 | |
| WO2025008732A1 (en) | Novel compounds as modulators of il17 | |
| CN108069937B (zh) | 苯基哌啶衍生物及其使用方法和用途 |