JPWO2022201097A5 - - Google Patents
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- Publication number
- JPWO2022201097A5 JPWO2022201097A5 JP2023558324A JP2023558324A JPWO2022201097A5 JP WO2022201097 A5 JPWO2022201097 A5 JP WO2022201097A5 JP 2023558324 A JP2023558324 A JP 2023558324A JP 2023558324 A JP2023558324 A JP 2023558324A JP WO2022201097 A5 JPWO2022201097 A5 JP WO2022201097A5
- Authority
- JP
- Japan
- Prior art keywords
- independently selected
- alkyl
- occurrence
- pharma
- acceptable salt
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 103
- 150000003839 salts Chemical class 0.000 claims description 95
- 206010023365 keratopathy Diseases 0.000 claims description 68
- 229910052760 oxygen Inorganic materials 0.000 claims description 64
- 229910052717 sulfur Inorganic materials 0.000 claims description 62
- 125000000217 alkyl group Chemical group 0.000 claims description 58
- 125000000623 heterocyclic group Chemical group 0.000 claims description 58
- 125000005842 heteroatom Chemical group 0.000 claims description 54
- 125000003118 aryl group Chemical group 0.000 claims description 48
- 125000005843 halogen group Chemical group 0.000 claims description 36
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- 208000002193 Pain Diseases 0.000 claims description 35
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 34
- 208000003923 Hereditary Corneal Dystrophies Diseases 0.000 claims description 31
- 206010023332 keratitis Diseases 0.000 claims description 31
- 208000002205 allergic conjunctivitis Diseases 0.000 claims description 30
- 201000001119 neuropathy Diseases 0.000 claims description 30
- 230000007823 neuropathy Effects 0.000 claims description 30
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 30
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 28
- 238000005299 abrasion Methods 0.000 claims description 28
- 206010011005 corneal dystrophy Diseases 0.000 claims description 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 26
- 125000001153 fluoro group Chemical group F* 0.000 claims description 22
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 22
- 208000028006 Corneal injury Diseases 0.000 claims description 20
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 206010015958 Eye pain Diseases 0.000 claims description 16
- 208000022873 Ocular disease Diseases 0.000 claims description 16
- 208000035475 disorder Diseases 0.000 claims description 16
- 201000010666 keratoconjunctivitis Diseases 0.000 claims description 16
- 230000000306 recurrent effect Effects 0.000 claims description 16
- 241000224422 Acanthamoeba Species 0.000 claims description 15
- 206010010741 Conjunctivitis Diseases 0.000 claims description 15
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims description 15
- 206010010996 Corneal degeneration Diseases 0.000 claims description 15
- 206010015084 Episcleritis Diseases 0.000 claims description 15
- 206010015995 Eyelid ptosis Diseases 0.000 claims description 15
- 208000001640 Fibromyalgia Diseases 0.000 claims description 15
- 208000010412 Glaucoma Diseases 0.000 claims description 15
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 15
- 208000003084 Graves Ophthalmopathy Diseases 0.000 claims description 15
- XQFRJNBWHJMXHO-RRKCRQDMSA-N IDUR Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(I)=C1 XQFRJNBWHJMXHO-RRKCRQDMSA-N 0.000 claims description 15
- 201000002287 Keratoconus Diseases 0.000 claims description 15
- 206010065062 Meibomian gland dysfunction Diseases 0.000 claims description 15
- 206010027137 Meibomianitis Diseases 0.000 claims description 15
- 208000023715 Ocular surface disease Diseases 0.000 claims description 15
- 201000002154 Pterygium Diseases 0.000 claims description 15
- 241001303601 Rosacea Species 0.000 claims description 15
- 206010039705 Scleritis Diseases 0.000 claims description 15
- 206010042033 Stevens-Johnson syndrome Diseases 0.000 claims description 15
- 231100000168 Stevens-Johnson syndrome Toxicity 0.000 claims description 15
- 206010044604 Trichiasis Diseases 0.000 claims description 15
- 208000024998 atopic conjunctivitis Diseases 0.000 claims description 15
- 201000004195 band keratopathy Diseases 0.000 claims description 15
- 208000010217 blepharitis Diseases 0.000 claims description 15
- 201000004781 bullous keratopathy Diseases 0.000 claims description 15
- 208000024908 graft versus host disease Diseases 0.000 claims description 15
- 201000010884 herpes simplex virus keratitis Diseases 0.000 claims description 15
- 201000004614 iritis Diseases 0.000 claims description 15
- 206010023683 lagophthalmos Diseases 0.000 claims description 15
- 201000006417 multiple sclerosis Diseases 0.000 claims description 15
- 208000004296 neuralgia Diseases 0.000 claims description 15
- 206010069732 neurotrophic keratopathy Diseases 0.000 claims description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims description 15
- 201000003004 ptosis Diseases 0.000 claims description 15
- 201000004700 rosacea Diseases 0.000 claims description 15
- 238000001356 surgical procedure Methods 0.000 claims description 15
- 208000011580 syndromic disease Diseases 0.000 claims description 15
- 208000018464 vernal keratoconjunctivitis Diseases 0.000 claims description 15
- 208000005494 xerophthalmia Diseases 0.000 claims description 15
- 206010010984 Corneal abrasion Diseases 0.000 claims description 13
- 201000002002 recurrent corneal erosion Diseases 0.000 claims description 13
- 206010011013 Corneal erosion Diseases 0.000 claims description 12
- 201000004173 Epithelial basement membrane dystrophy Diseases 0.000 claims description 11
- 201000000009 conjunctivochalasis Diseases 0.000 claims description 11
- 230000001684 chronic effect Effects 0.000 claims description 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 9
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 150000001204 N-oxides Chemical class 0.000 claims description 6
- 102000003566 TRPV1 Human genes 0.000 claims description 6
- 101150016206 Trpv1 gene Proteins 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 230000001154 acute effect Effects 0.000 claims description 5
- 230000001667 episodic effect Effects 0.000 claims description 5
- 201000005111 ocular hyperemia Diseases 0.000 claims description 5
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims description 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims description 2
- 239000001301 oxygen Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 23
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 3
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 2
- 210000004379 membrane Anatomy 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 description 23
- 238000000034 method Methods 0.000 description 19
- 125000000753 cycloalkyl group Chemical group 0.000 description 12
- 206010015150 Erythema Diseases 0.000 description 8
- 208000035874 Excoriation Diseases 0.000 description 7
- 238000011065 in-situ storage Methods 0.000 description 5
- 125000003545 alkoxy group Chemical group 0.000 description 4
- 230000003628 erosive effect Effects 0.000 description 4
- 125000003709 fluoroalkyl group Chemical group 0.000 description 4
- 125000004438 haloalkoxy group Chemical group 0.000 description 4
- 230000004075 alteration Effects 0.000 description 3
- 210000002469 basement membrane Anatomy 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 230000004048 modification Effects 0.000 description 3
- 238000006467 substitution reaction Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163166289P | 2021-03-26 | 2021-03-26 | |
| US63/166,289 | 2021-03-26 | ||
| PCT/IB2022/052720 WO2022201097A1 (en) | 2021-03-26 | 2022-03-24 | 1,3-substituted cyclobutyl derivatives and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024510778A JP2024510778A (ja) | 2024-03-11 |
| JPWO2022201097A5 true JPWO2022201097A5 (https=) | 2025-04-01 |
| JP2024510778A5 JP2024510778A5 (https=) | 2025-04-01 |
Family
ID=80999265
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023558324A Pending JP2024510778A (ja) | 2021-03-26 | 2022-03-24 | １，３－置換シクロブチル誘導体及びその使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11845730B2 (https=) |
| EP (1) | EP4313951A1 (https=) |
| JP (1) | JP2024510778A (https=) |
| KR (1) | KR20230162660A (https=) |
| CN (1) | CN117062804A (https=) |
| AR (1) | AR125196A1 (https=) |
| AU (1) | AU2022244467A1 (https=) |
| CA (1) | CA3214066A1 (https=) |
| IL (1) | IL307189A (https=) |
| MX (1) | MX2023011377A (https=) |
| PY (1) | PY2221203A (https=) |
| TW (1) | TW202304864A (https=) |
| UY (1) | UY39681A (https=) |
| WO (1) | WO2022201097A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR125196A1 (es) * | 2021-03-26 | 2023-06-21 | Novartis Ag | Derivados de ciclobutilo 1,3-sustituidos y sus usos |
| WO2024062389A1 (en) * | 2022-09-21 | 2024-03-28 | Bausch + Lomb Ireland Limited | Crystalline polymorph forms of a trpv1 antagonist and formulations thereof |
| US20240148709A1 (en) * | 2022-11-08 | 2024-05-09 | Aisa Pharma, Inc. | Methods of treating eye pain and eye disorders |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004078163A2 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| US6933311B2 (en) * | 2003-02-11 | 2005-08-23 | Abbott Laboratories | Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor |
| US7514562B2 (en) * | 2003-03-07 | 2009-04-07 | Glaxo Group Limited | Urea derivatives and their use as vanilloid receptor antagonists in the treatment of pain |
| GB0412769D0 (en) | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| RU2451014C2 (ru) | 2005-07-22 | 2012-05-20 | Мотида Фармасьютикал Ко., Лтд. | Новое производное гетероциклиден ацетамида |
| EP2050734A1 (en) | 2006-07-13 | 2009-04-22 | Kyowa Hakko Kirin Co., Ltd. | Pentadienamide derivative |
| NZ577980A (en) | 2006-12-27 | 2012-01-12 | Sanofi Aventis | Cycloalkylamine substituted isoquinolone derivatives |
| WO2012072512A1 (en) * | 2010-11-29 | 2012-06-07 | Glaxo Group Limited | N-cyclobutyl-imidazopyridine or -pyrazolopyridine carboxamides as trpv1 antagonists |
| DE102010052781A1 (de) | 2010-11-30 | 2012-05-31 | Trw Automotive Gmbh | Befestigungsvorrichtung und Befestigungsbaugruppe zur Befestigung eines Gasgenerators und Fahrzeuginsassenrückhaltesystem |
| TW201302681A (zh) * | 2011-03-25 | 2013-01-16 | Abbott Lab | Ｔｒｐｖ１拮抗劑 |
| JP2014510768A (ja) * | 2011-04-11 | 2014-05-01 | グラクソ グループ リミテッド | Ｔｒｐｖ１アンタゴニストとしてのｎ−シクロブチルイミダゾピリジンメチルアミン |
| US9747862B2 (en) | 2015-11-02 | 2017-08-29 | Castar, Inc. | Method of immersive rendering for wide field of view |
| US10269906B2 (en) * | 2016-11-30 | 2019-04-23 | Taiwan Semiconductor Manufacturing Co., Ltd. | Semiconductor device having two spacers |
| WO2018151678A1 (en) * | 2017-02-15 | 2018-08-23 | Agency For Science, Technology And Research | Compounds for treatment of cancer and epigenetics |
| US11542248B2 (en) | 2017-06-08 | 2023-01-03 | Kura Oncology, Inc. | Methods and compositions for inhibiting the interaction of menin with MLL proteins |
| AU2019392904B9 (en) | 2018-12-07 | 2022-12-22 | University Of Maryland, Baltimore | Non-ATP/catalytic site p38 mitogen activated protein kinase inhibitors |
| AR125196A1 (es) * | 2021-03-26 | 2023-06-21 | Novartis Ag | Derivados de ciclobutilo 1,3-sustituidos y sus usos |
-
2022
- 2022-03-22 AR ARP220100676A patent/AR125196A1/es unknown
- 2022-03-22 UY UY0001039681A patent/UY39681A/es unknown
- 2022-03-23 PY PY202202221203A patent/PY2221203A/es unknown
- 2022-03-24 JP JP2023558324A patent/JP2024510778A/ja active Pending
- 2022-03-24 EP EP22714016.7A patent/EP4313951A1/en active Pending
- 2022-03-24 CA CA3214066A patent/CA3214066A1/en active Pending
- 2022-03-24 AU AU2022244467A patent/AU2022244467A1/en active Pending
- 2022-03-24 US US17/656,313 patent/US11845730B2/en active Active
- 2022-03-24 WO PCT/IB2022/052720 patent/WO2022201097A1/en not_active Ceased
- 2022-03-24 CN CN202280024266.2A patent/CN117062804A/zh active Pending
- 2022-03-24 TW TW111111060A patent/TW202304864A/zh unknown
- 2022-03-24 KR KR1020237036535A patent/KR20230162660A/ko active Pending
- 2022-03-24 IL IL307189A patent/IL307189A/en unknown
- 2022-03-24 MX MX2023011377A patent/MX2023011377A/es unknown
-
2023
- 2023-10-24 US US18/493,441 patent/US12435040B2/en active Active
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