JP2014516086A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014516086A5 JP2014516086A5 JP2014514930A JP2014514930A JP2014516086A5 JP 2014516086 A5 JP2014516086 A5 JP 2014516086A5 JP 2014514930 A JP2014514930 A JP 2014514930A JP 2014514930 A JP2014514930 A JP 2014514930A JP 2014516086 A5 JP2014516086 A5 JP 2014516086A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- pharmaceutical composition
- compound
- salt form
- condition
- 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 21
- 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 claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 15
- 201000010099 disease Diseases 0.000 claims description 13
- 150000003839 salts Chemical group 0.000 claims description 11
- 239000000186 progesterone Substances 0.000 claims description 10
- 229960003387 progesterone Drugs 0.000 claims description 9
- 208000010877 cognitive disease Diseases 0.000 claims description 8
- 238000011282 treatment Methods 0.000 claims description 8
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 7
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 230000011664 signaling Effects 0.000 claims description 7
- 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 claims description 6
- 208000028698 Cognitive impairment Diseases 0.000 claims description 6
- 206010057671 Female sexual dysfunction Diseases 0.000 claims description 6
- 208000028017 Psychotic disease Diseases 0.000 claims description 6
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims description 6
- 208000018737 Parkinson disease Diseases 0.000 claims description 5
- 208000003532 hypothyroidism Diseases 0.000 claims description 5
- 230000002989 hypothyroidism Effects 0.000 claims description 5
- 201000003631 narcolepsy Diseases 0.000 claims description 5
- 201000000980 schizophrenia Diseases 0.000 claims description 5
- 201000000736 Amenorrhea Diseases 0.000 claims description 4
- 206010001928 Amenorrhoea Diseases 0.000 claims description 4
- 206010003805 Autism Diseases 0.000 claims description 4
- 208000020706 Autistic disease Diseases 0.000 claims description 4
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 102000004076 Dopamine D1 Receptors Human genes 0.000 claims description 4
- 108090000511 Dopamine D1 Receptors Proteins 0.000 claims description 4
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 4
- 208000016620 Tourette disease Diseases 0.000 claims description 4
- 231100000540 amenorrhea Toxicity 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229940011871 estrogen Drugs 0.000 claims description 4
- 239000000262 estrogen Substances 0.000 claims description 4
- 208000000509 infertility Diseases 0.000 claims description 4
- 230000036512 infertility Effects 0.000 claims description 4
- 231100000535 infertility Toxicity 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- 230000007781 signaling event Effects 0.000 claims description 4
- 208000037853 Abnormal uterine bleeding Diseases 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 3
- 206010012289 Dementia Diseases 0.000 claims description 3
- 101001117089 Drosophila melanogaster Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1 Proteins 0.000 claims description 3
- 208000012661 Dyskinesia Diseases 0.000 claims description 3
- 206010014733 Endometrial cancer Diseases 0.000 claims description 3
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 3
- 208000001914 Fragile X syndrome Diseases 0.000 claims description 3
- 208000010412 Glaucoma Diseases 0.000 claims description 3
- 208000023105 Huntington disease Diseases 0.000 claims description 3
- 206010020772 Hypertension Diseases 0.000 claims description 3
- 206010027304 Menopausal symptoms Diseases 0.000 claims description 3
- 206010027339 Menstruation irregular Diseases 0.000 claims description 3
- 208000016285 Movement disease Diseases 0.000 claims description 3
- 208000001132 Osteoporosis Diseases 0.000 claims description 3
- 206010036618 Premenstrual syndrome Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 206010038743 Restlessness Diseases 0.000 claims description 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims description 3
- 201000001880 Sexual dysfunction Diseases 0.000 claims description 3
- 208000006011 Stroke Diseases 0.000 claims description 3
- 206010044565 Tremor Diseases 0.000 claims description 3
- 201000010105 allergic rhinitis Diseases 0.000 claims description 3
- 230000036506 anxiety Effects 0.000 claims description 3
- 208000006673 asthma Diseases 0.000 claims description 3
- 208000026106 cerebrovascular disease Diseases 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 206010013663 drug dependence Diseases 0.000 claims description 3
- 201000006828 endometrial hyperplasia Diseases 0.000 claims description 3
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims description 3
- 230000009245 menopause Effects 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 230000016087 ovulation Effects 0.000 claims description 3
- 201000000484 premenstrual tension Diseases 0.000 claims description 3
- 208000002815 pulmonary hypertension Diseases 0.000 claims description 3
- 231100000872 sexual dysfunction Toxicity 0.000 claims description 3
- 230000019491 signal transduction Effects 0.000 claims description 3
- 208000019116 sleep disease Diseases 0.000 claims description 3
- 208000011117 substance-related disease Diseases 0.000 claims description 3
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 2
- 208000005107 Premature Birth Diseases 0.000 claims description 2
- 206010036590 Premature baby Diseases 0.000 claims description 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 2
- 239000000583 progesterone congener Substances 0.000 claims description 2
- 201000004240 prostatic hypertrophy Diseases 0.000 claims description 2
- 208000020016 psychiatric disease Diseases 0.000 claims description 2
- 239000003368 psychostimulant agent Substances 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 206010030043 Ocular hypertension Diseases 0.000 claims 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 230000009529 traumatic brain injury Effects 0.000 claims 2
- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 claims 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims 1
- YFGHCGITMMYXAQ-UHFFFAOYSA-N 2-[(diphenylmethyl)sulfinyl]acetamide Chemical compound C=1C=CC=CC=1C(S(=O)CC(=O)N)C1=CC=CC=C1 YFGHCGITMMYXAQ-UHFFFAOYSA-N 0.000 claims 1
- SJZRECIVHVDYJC-UHFFFAOYSA-N 4-hydroxybutyric acid Chemical compound OCCCC(O)=O SJZRECIVHVDYJC-UHFFFAOYSA-N 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- 208000024254 Delusional disease Diseases 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 206010026749 Mania Diseases 0.000 claims 1
- 208000020186 Schizophreniform disease Diseases 0.000 claims 1
- 239000002269 analeptic agent Substances 0.000 claims 1
- 239000000935 antidepressant agent Substances 0.000 claims 1
- 229940005513 antidepressants Drugs 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229960005309 estradiol Drugs 0.000 claims 1
- 229930182833 estradiol Natural products 0.000 claims 1
- 150000002159 estradiols Chemical class 0.000 claims 1
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 claims 1
- 229960001348 estriol Drugs 0.000 claims 1
- 210000000720 eyelash Anatomy 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 229960001165 modafinil Drugs 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 208000002851 paranoid schizophrenia Diseases 0.000 claims 1
- 230000001737 promoting effect Effects 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 208000022610 schizoaffective disease Diseases 0.000 claims 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 206010000234 Abortion spontaneous Diseases 0.000 description 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 229940121836 Phosphodiesterase 1 inhibitor Drugs 0.000 description 2
- 208000037765 diseases and disorders Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 208000015994 miscarriage Diseases 0.000 description 2
- 230000035935 pregnancy Effects 0.000 description 2
- 239000000651 prodrug Chemical group 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 208000000995 spontaneous abortion Diseases 0.000 description 2
- NWZSZGALRFJKBT-KNIFDHDWSA-N (2s)-2,6-diaminohexanoic acid;(2s)-2-hydroxybutanedioic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O.NCCCC[C@H](N)C(O)=O NWZSZGALRFJKBT-KNIFDHDWSA-N 0.000 description 1
- YUSCRGFYKCAQHE-HQFNMCNFSA-N (8r,9s,13s,14s,17s)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol;(8r,9s,13s,14s,16r,17r)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,16,17-triol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1.OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 YUSCRGFYKCAQHE-HQFNMCNFSA-N 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000006399 Premature Obstetric Labor Diseases 0.000 description 1
- 206010036600 Premature labour Diseases 0.000 description 1
- 208000005793 Restless legs syndrome Diseases 0.000 description 1
- 238000003975 animal breeding Methods 0.000 description 1
- 230000001363 autoimmune Effects 0.000 description 1
- 238000009395 breeding Methods 0.000 description 1
- 230000001488 breeding effect Effects 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 229940008359 estradiol / estriol Drugs 0.000 description 1
- 229940086018 estradiol / progesterone Drugs 0.000 description 1
- 230000012173 estrus Effects 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- IKDUDTNKRLTJSI-UHFFFAOYSA-N hydrazine monohydrate Substances O.NN IKDUDTNKRLTJSI-UHFFFAOYSA-N 0.000 description 1
- 230000007954 hypoxia Effects 0.000 description 1
- 230000028993 immune response Effects 0.000 description 1
- 238000002513 implantation Methods 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 208000026440 premature labor Diseases 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 238000009256 replacement therapy Methods 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 208000023504 respiratory system disease Diseases 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161495683P | 2011-06-10 | 2011-06-10 | |
| US61/495,683 | 2011-06-10 | ||
| PCT/US2012/041925 WO2012171016A1 (en) | 2011-06-10 | 2012-06-11 | Organic compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016196552A Division JP2017061458A (ja) | 2011-06-10 | 2016-10-04 | 有機化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014516086A JP2014516086A (ja) | 2014-07-07 |
| JP2014516086A5 true JP2014516086A5 (enExample) | 2015-07-30 |
| JP6051210B2 JP6051210B2 (ja) | 2016-12-27 |
Family
ID=47296522
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014514930A Active JP6051210B2 (ja) | 2011-06-10 | 2012-06-11 | 有機化合物 |
| JP2016196552A Pending JP2017061458A (ja) | 2011-06-10 | 2016-10-04 | 有機化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016196552A Pending JP2017061458A (ja) | 2011-06-10 | 2016-10-04 | 有機化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US10561656B2 (enExample) |
| EP (1) | EP2717877B1 (enExample) |
| JP (2) | JP6051210B2 (enExample) |
| WO (1) | WO2012171016A1 (enExample) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006255028B2 (en) | 2005-06-06 | 2012-04-19 | Intra-Cellular Therapies, Inc. | Organic compounds |
| KR20090042227A (ko) | 2006-06-06 | 2009-04-29 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| WO2008070095A1 (en) | 2006-12-05 | 2008-06-12 | Intra-Cellular Therapies, Inc. | Novel uses |
| KR20120012831A (ko) | 2007-12-06 | 2012-02-10 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| EP2240028B1 (en) | 2007-12-06 | 2016-07-20 | Intra-Cellular Therapies, Inc. | Pyrazolopyrimidine-4,6-dione derivatives and their use as pharmaceutical |
| EP2367430B1 (en) | 2008-12-06 | 2014-08-13 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP2367431B1 (en) | 2008-12-06 | 2015-08-05 | Intra-Cellular Therapies, Inc. | Organic compounds |
| JP5778582B2 (ja) * | 2008-12-06 | 2015-09-16 | 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 |
| BRPI0922809A2 (pt) | 2008-12-06 | 2018-05-29 | Intracellular Therapies Inc | compostos orgânicos |
| WO2010098839A1 (en) | 2009-02-25 | 2010-09-02 | Intra-Cellular Therapies, Inc. | Pde 1 inhibitors for ophthalmic disorders |
| JP2012526810A (ja) | 2009-05-13 | 2012-11-01 | 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 |
| WO2011153136A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2011153135A1 (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 |
| EP2576551A4 (en) | 2010-05-31 | 2014-04-16 | Intra Cellular Therapies Inc | ORGANIC CONNECTIONS |
| US8633178B2 (en) | 2011-11-23 | 2014-01-21 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
| CA2877146C (en) | 2012-06-18 | 2020-10-20 | Dart Neuroscience (Cayman) Ltd | Substituted thiophene- and furan-fused azolopyrimidine-5-(6h)-one compounds |
| US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
| 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 |
| US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US9801882B2 (en) | 2013-02-17 | 2017-10-31 | Intra-Cellular Therapies, Inc. | Phosphodiesterase-1 inhibitors and their use in treatment of cardiovascular diseases |
| EP2968338B1 (en) | 2013-03-15 | 2019-01-09 | Intra-Cellular Therapies, Inc. | Pde1 inhibitors for use in the treatment and/or prevention of cns injuries, and pns diseases, disorders or injuries |
| KR102240326B1 (ko) | 2013-03-15 | 2021-04-13 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| US9630971B2 (en) | 2013-06-21 | 2017-04-25 | Intra-Cellular Therapies, Inc. | Free base crystals |
| JP6696904B2 (ja) | 2014-01-08 | 2020-05-20 | 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． | 製剤および医薬組成物 |
| EP3145489A1 (en) | 2014-05-22 | 2017-03-29 | TherapeuticsMD, Inc. | Natural combination hormone replacement formulations and therapies |
| EP3157926B1 (en) | 2014-06-20 | 2019-05-15 | Intra-Cellular Therapies, Inc. | Organic compounds |
| RU2016141135A (ru) | 2014-07-29 | 2018-08-28 | Терапьютиксмд, Инк. | Трансдермальный крем |
| US9546175B2 (en) | 2014-08-07 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US10285992B2 (en) | 2014-08-07 | 2019-05-14 | Intra-Cellular Therapies, Inc. | Combinations of PDE1 inhibitors and NEP inhibitors and associated methods |
| US10131671B2 (en) | 2014-08-07 | 2018-11-20 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CA2961212C (en) | 2014-09-17 | 2024-02-06 | Intra-Cellular Therapies, Inc. | Compounds and methods |
| TW201629064A (zh) | 2014-10-10 | 2016-08-16 | Ｈ 朗德貝克公司 | 作爲ｐｄｅ１抑制劑之三唑並吡酮 |
| HK1244427A1 (zh) | 2014-12-06 | 2018-08-10 | Intra-Cellular Therapies, Inc. | 有机化合物 |
| CA2969594A1 (en) | 2014-12-06 | 2016-06-09 | Intra-Cellular Therapies, Inc. | Pde2 inhibiting organic compounds |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
| US10682354B2 (en) | 2016-03-28 | 2020-06-16 | Intra-Cellular Therapies, Inc. | Compositions and methods |
| WO2017173071A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical composition |
| WO2017173044A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd Inc. | Steroid hormone compositions in medium chain oils |
| TWI729109B (zh) | 2016-04-12 | 2021-06-01 | 丹麥商Ｈ 朗德貝克公司 | 作爲PDE1抑制劑的1,5-二氫-4H-吡唑并[3,4-d]嘧啶-4-酮和1,5-二氫-4H-吡唑并[4,3-c]吡啶-4-酮 |
| JP7134168B6 (ja) | 2016-09-12 | 2024-02-02 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 新規使用 |
| WO2018073251A1 (en) | 2016-10-18 | 2018-04-26 | H. Lundbeck A/S | Imidazopyrazinones, pyrazolopyrimidinones and pyrazolopyridinones as pde1 inhibitors |
| AU2017350473A1 (en) | 2016-10-28 | 2019-04-18 | H. Lundbeck A/S | Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders |
| WO2018078042A1 (en) | 2016-10-28 | 2018-05-03 | H. Lundbeck A/S | Combination treatments comprising administration of imidazopyrazinones |
| JP7401442B2 (ja) | 2018-01-31 | 2023-12-19 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 新規使用 |
| MX2020012628A (es) | 2018-05-25 | 2021-01-29 | Intra Cellular Therapies Inc | Compuestos organicos. |
| WO2020210614A1 (en) | 2019-04-12 | 2020-10-15 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP4413980A3 (en) * | 2019-09-03 | 2024-10-30 | Intra-Cellular Therapies, Inc. | Novel compounds |
| US12435093B2 (en) | 2020-05-06 | 2025-10-07 | Intra-Cellular Therapies, Inc. | Free base crystals |
| US12364695B2 (en) | 2020-06-02 | 2025-07-22 | Intra-Cellular Therapies, Inc. | Methods of treating inflammatory disease |
| MX2023008755A (es) * | 2021-01-27 | 2023-08-02 | Intra Cellular Therapies Inc | Cristales de sal. |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US5939419A (en) | 1993-02-26 | 1999-08-17 | Schering-Plough Corporation | 2-benzyl-polycyclic guanine derivatives and process for preparing them |
| GB9315017D0 (en) | 1993-07-20 | 1993-09-01 | Glaxo Lab Sa | 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 |
| SE9701398D0 (sv) | 1997-04-15 | 1997-04-15 | Astra Pharma Prod | Novel compounds |
| 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 |
| US20040014761A1 (en) * | 1997-10-28 | 2004-01-22 | Place Virgil A. | Treatment of female sexual dysfunction with phosphodiesterase inhibitors |
| US6133273A (en) | 1998-05-08 | 2000-10-17 | American Home Products Corporation | Pyrazolopyrimidine-2,4-dione sulfonamides |
| DE19931206A1 (de) | 1999-07-07 | 2001-01-11 | Stief Christian | Arzneimittel zur Erhöhung des cAMP-Spiegels und deren Verwendung |
| 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 |
| HK1049834A1 (zh) | 1999-10-11 | 2003-05-30 | 辉瑞大药厂 | 用作磷酸二酯酶抑制剂的5-(2-取代的-5-杂环基磺酰基吡啶-3-基)-二氢吡唑并[4，3-d]嘧啶-7-酮类化合物 |
| 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 |
| US20020006926A1 (en) | 2000-04-19 | 2002-01-17 | Roylance H. H. | Use of cyclic GMP-specific phosphodiesterase inhibitors for treatment of parkinson's disease |
| WO2002074312A1 (en) | 2001-03-16 | 2002-09-26 | Pfizer Limited | Pyrazolo`4,3-d.pyrimidinone compounds as cgmp pde inhibitors |
| 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 |
| IL160307A0 (en) | 2001-08-31 | 2004-07-25 | Univ Rockefeller | 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 |
| IL163575A0 (en) | 2002-02-21 | 2005-12-18 | Univ Rockefeller | 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 |
| US7153824B2 (en) | 2003-04-01 | 2006-12-26 | Applied Research Systems Ars Holding N.V. | Inhibitors of phosphodiesterases in infertility |
| AR045582A1 (es) | 2003-09-05 | 2005-11-02 | Neurogen Corp | Piridinas pirazinas y pirimidinas heteroarilo fusionadas como ligandos receptores de crf1 |
| US20090298864A1 (en) * | 2005-04-11 | 2009-12-03 | The Trustees Of Columbia University In The City Of New York | Methods for Treating Mild Cognitive Impairment |
| AU2006255028B2 (en) | 2005-06-06 | 2012-04-19 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US20080194592A1 (en) | 2005-08-23 | 2008-08-14 | Intra-Cellular Therapies, Inc. | Organic Compounds |
| KR20090042227A (ko) | 2006-06-06 | 2009-04-29 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| US20070286890A1 (en) | 2006-06-07 | 2007-12-13 | John Garnett Walt | Eyelash applicator and method |
| WO2008063505A1 (en) | 2006-11-13 | 2008-05-29 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2008070095A1 (en) | 2006-12-05 | 2008-06-12 | Intra-Cellular Therapies, Inc. | Novel uses |
| EP2240028B1 (en) | 2007-12-06 | 2016-07-20 | Intra-Cellular Therapies, Inc. | Pyrazolopyrimidine-4,6-dione derivatives and their use as pharmaceutical |
| KR20120012831A (ko) | 2007-12-06 | 2012-02-10 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| KR20110103949A (ko) | 2008-12-06 | 2011-09-21 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| JP5778582B2 (ja) | 2008-12-06 | 2015-09-16 | 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 |
| BRPI0922809A2 (pt) | 2008-12-06 | 2018-05-29 | Intracellular Therapies Inc | compostos orgânicos |
| MA32942B1 (fr) | 2008-12-06 | 2012-01-02 | Intra Cellular Therapies Inc | Composes organiques |
| EP2367430B1 (en) | 2008-12-06 | 2014-08-13 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP2367431B1 (en) | 2008-12-06 | 2015-08-05 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2010098839A1 (en) | 2009-02-25 | 2010-09-02 | Intra-Cellular Therapies, Inc. | Pde 1 inhibitors for ophthalmic disorders |
| JP2012526810A (ja) | 2009-05-13 | 2012-11-01 | 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 |
| WO2011043816A1 (en) | 2009-10-08 | 2011-04-14 | Intra-Cellular Therapies, Inc. | Phosphodiesterase 1-targeting tracers and methods |
| 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 |
| EP2576551A4 (en) | 2010-05-31 | 2014-04-16 | Intra Cellular Therapies Inc | ORGANIC CONNECTIONS |
| WO2011153135A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| KR102240326B1 (ko) | 2013-03-15 | 2021-04-13 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| US9630971B2 (en) | 2013-06-21 | 2017-04-25 | Intra-Cellular Therapies, Inc. | Free base crystals |
-
2012
- 2012-06-11 JP JP2014514930A patent/JP6051210B2/ja active Active
- 2012-06-11 WO PCT/US2012/041925 patent/WO2012171016A1/en not_active Ceased
- 2012-06-11 EP EP12796910.3A patent/EP2717877B1/en not_active Not-in-force
- 2012-06-11 US US14/125,017 patent/US10561656B2/en not_active Expired - Fee Related
-
2016
- 2016-10-04 JP JP2016196552A patent/JP2017061458A/ja active Pending
-
2020
- 2020-01-02 US US16/733,174 patent/US20200138820A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014516086A5 (enExample) | ||
| JP2012510991A5 (enExample) | ||
| HRP20131073T1 (hr) | Organski spojevi | |
| JP2017518355A5 (enExample) | ||
| JP6810613B2 (ja) | 有機化合物 | |
| RU2015143672A (ru) | Органические соединения | |
| AU2013248481B2 (en) | Estrogenic components for use in the treatment of neurological disorders. | |
| JP2018184452A (ja) | 置換アシルアニリドおよびそれらの使用方法 | |
| JP2009539872A5 (enExample) | ||
| WO2016209847A1 (en) | C-20 steroid compounds, compositions, and uses thereof to treat traumatic brain injury (tbi), including concussions | |
| RU2325910C2 (ru) | Новые сложные эфиры этоногестрела | |
| HUP0303624A2 (hu) | NEP inhibitor hatású N-fenpropil-ciklopentil-csoporttal szubsztituált glutáramid származékok és ezeket tartalmazó gyógyászati készítmények és eljárás a vegyületek előállítására | |
| CN101516835A (zh) | 选择性雄激素受体调节剂、它们的类似物和衍生物以及它们的用途 | |
| JP2010522714A (ja) | 新規な医薬組成物 | |
| JP2015522025A (ja) | コレステロール生合成阻害剤によるエストロゲン受容体βの誘発および癌の処置方法 | |
| TWI286140B (en) | 9-alpha-substituted estratrienes as selectively active estrogens | |
| UA80703C2 (en) | Pharmaceutical composition comprising etonogestrel esters and use thereof for contraception and hormone replacement therapy | |
| TW201625660A (zh) | Ｃ－２０類固醇化合物、其組成物及用於治療包含震盪之創傷性腦損傷（ｔｂｉ）的用途 | |
| KR20150013596A (ko) | 안드로겐 매개 질환의 예방 또는 치료에 사용하기 위한 프로게스테론 수용체 조절제 | |
| DK159649B (da) | 4-hydroxy-alfa-benzhydrolderivater, fremgangsmaade til fremstilling deraf, farmaceutiske praeparater indeholdende disse, samt fremgangsmaade til fremstilling af disse farmaceutiske praeparater | |
| CN103613631A (zh) | 一种合成烯基叠氮孕酮的方法 | |
| NZ536882A (en) | 9-Alpha-substituted estratrienes as selectively active estrogens |