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WO2016010131A1 - Agent prophylactique ou thérapeutique pour la dégénérescence maculaire liée à l'âge - Google Patents

Agent prophylactique ou thérapeutique pour la dégénérescence maculaire liée à l'âge Download PDF

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Publication number
WO2016010131A1
WO2016010131A1 PCT/JP2015/070478 JP2015070478W WO2016010131A1 WO 2016010131 A1 WO2016010131 A1 WO 2016010131A1 JP 2015070478 W JP2015070478 W JP 2015070478W WO 2016010131 A1 WO2016010131 A1 WO 2016010131A1
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Prior art keywords
alkyl group
lower alkyl
formula
halogen atom
age
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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.)
Ceased
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PCT/JP2015/070478
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English (en)
Japanese (ja)
Inventor
篤史 吉田
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Santen Pharmaceutical Co Ltd
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Santen Pharmaceutical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
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Application filed by Santen Pharmaceutical Co Ltd filed Critical Santen Pharmaceutical Co Ltd
Publication of WO2016010131A1 publication Critical patent/WO2016010131A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

Definitions

  • the present invention relates to 3-aminocyclopentanecarboxamide derivatives, in particular the formula (1): Or an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof (hereinafter also referred to as “the present compound”) as an active ingredient.
  • Age-related macular degeneration (hereinafter also referred to as “AMD”) is one of the leading causes of blindness in developed countries, and is mainly seen in elderly people over 50 years old.
  • Age-related macular degeneration is a disease caused by changes associated with aging of the macular, and is roughly classified into wet age-related macular degeneration, atrophic age-related macular degeneration, and early age-related macular degeneration, which are precursor lesions thereof.
  • wet age-related macular degeneration is a disease in which neovascularization occurs in the macular of the elderly from the choroid, causing bleeding or exudative lesions in the retinal pigment epithelium or subretinal, and finally scar tissue.
  • atrophic age-related macular degeneration is a disease accompanied by macular atrophy and drusen accumulation.
  • choroidal neovascularization The pathological condition underlying wet age-related macular degeneration is choroidal neovascularization, which is thought to develop on the basis of age-related changes such as macular retinal pigment epithelial cells, Bruch's membrane, and choroidal blood vessels.
  • age-related changes such as macular retinal pigment epithelial cells, Bruch's membrane, and choroidal blood vessels.
  • choroidal neovascularization is not involved in early age-related macular degeneration and atrophic age-related macular degeneration.
  • Non-Patent Document 1 In atrophic age-related macular degeneration, it is considered that visual acuity decreases due to photoreceptor cell degeneration (cell death) accompanying atrophy, and photoreceptor cell protection is attracting attention as a new treatment method.
  • a 3-aminocyclopentanecarboxamide derivative as a chemokine receptor modulator is disclosed, and a plurality of synthesis examples of the derivative are described.
  • guide_body and the renal protective effect in a diabetic nephropathy rat model are verified (patent document 1).
  • An object of the present invention is to provide a preventive or therapeutic agent for age-related macular degeneration containing a 3-aminocyclopentanecarboxamide derivative as an active ingredient.
  • the present inventors conducted extensive research to search for a new preventive or therapeutic agent for age-related macular degeneration containing a 3-aminocyclopentanecarboxamide derivative as an active ingredient. It has been found that it has excellent angiogenesis inhibitory action and vascular permeability enhancement action in ocular tissues, and this compound has an excellent preventive or therapeutic effect on age-related macular degeneration, particularly exudative age-related macular degeneration. As a result, the present invention has been found.
  • the present invention relates to the following.
  • R 1 represents a hydrogen atom, a lower alkyl group, or a lower alkyl group substituted with a halogen atom
  • R 2 represents a hydrogen atom, a lower alkyl group, or a lower alkyl group substituted with a halogen atom
  • R 3 represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkyl group substituted with a halogen atom
  • R 4 represents a 6-membered nitrogen-containing aromatic ring group which is unsubstituted or substituted with R 5
  • R 5 represents a halogen atom, a lower alkyl group or a lower alkyl group substituted with a halogen atom.
  • an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient is a preventive or therapeutic agent for age-related macular degeneration.
  • R 1 represents a lower alkyl group or a lower alkyl group substituted with a halogen atom
  • R 2 represents a hydrogen atom or a lower alkyl group
  • R 3 represents a lower alkyl group or a lower alkyl group substituted with a halogen atom
  • R 4 represents the formula (2a) or (2b):
  • Indicate R 5 represents a lower alkyl group or a lower alkyl group substituted with a halogen atom
  • a prophylactic or therapeutic agent for age-related macular degeneration comprising a compound, an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.
  • “•” in the formula (2a) or (2b) represents a bonding point with the nitrogen atom to which R 4 is bonded.
  • the compound represented by the formula (1) is Formula (1 ′): Indicated by A prophylactic or therapeutic agent for age-related macular degeneration comprising a compound or a pharmaceutically acceptable salt thereof as an active ingredient.
  • R 1 represents methyl
  • R 2 represents a hydrogen atom
  • R 3 represents isopropyl
  • R 4 represents the formula (2b):
  • Indicate R 5 represents trifluoromethyl
  • a prophylactic or therapeutic agent for age-related macular degeneration comprising a compound, an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.
  • ⁇ in the formula (2b) represents a point of attachment to the nitrogen atom to which R 4 is bonded.
  • Another aspect of the present invention is to prevent or treat age-related macular degeneration containing a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.
  • An agent for preventing or treating the age-related macular degeneration is exudative age-related macular degeneration.
  • a choroidal neovascularization inhibitor comprising a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.
  • Another aspect of the present invention is to prevent or treat age-related macular degeneration containing a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. It is a prophylactic or therapeutic agent, or an inhibitor, in which the dosage form is ophthalmic administration, intravitreal administration, subconjunctival administration, intraconjunctival sac administration, subtenon administration or oral administration.
  • Another aspect of the present invention is to prevent or treat age-related macular degeneration containing a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.
  • the agent is a prophylactic or therapeutic agent, or an inhibitor whose dosage form is an eye drop, eye ointment, insertion agent, patch, injection, tablet, fine granule or capsule.
  • the present invention also relates to the following.
  • Another aspect of the present invention is a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof for use in the prevention or treatment of age-related macular degeneration. .
  • Another aspect of the present invention provides a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for preventing or treating age-related macular degeneration. Is the use of salt.
  • Another aspect of the present invention provides age-related macular degeneration comprising a therapeutically effective amount of a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof and an additive.
  • Another aspect of the present invention is a method for preventing or treating age-related macular degeneration, the compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof. Administering an effective amount of a salt.
  • age-related macular degeneration particularly exudative age-related macular, comprising a compound represented by the above formula (1), an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.
  • An agent for preventing or treating degeneration can be provided.
  • Halogen atom means a fluorine atom, a chlorine atom, a bromine atom or an iodine atom.
  • the “lower alkyl group” refers to a linear or branched alkyl group having 1 to 8 carbon atoms, preferably a linear or branched alkyl group having 1 to 6 carbon atoms. Specific examples include methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, n-heptyl, n-octyl, isopropyl, isobutyl, sec-butyl, tert-butyl, isopentyl and the like.
  • lower alkyl group substituted with a halogen atom refers to a lower alkyl group substituted with one or more (eg, 2 or 3) halogen atoms, and the lower alkyl substituted with 3 halogen atoms Groups are preferred. Specific examples include trifluoromethyl and the like. When a plurality of halogen atoms are present, these halogen atoms may be the same or different.
  • the “6-membered nitrogen-containing aromatic ring group” means a monocyclic or polycyclic aromatic ring having 6 ring atoms, at least one of which is a nitrogen atom, An aromatic ring containing 1 or 2 nitrogen atoms is preferred. Specific examples include pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl and the like.
  • the compound contained in the preventive or therapeutic agent for age-related macular degeneration according to the present invention can be produced according to a usual method in the field of synthetic organic chemistry. For example, it can be produced according to the method described in International Publication No. 2010/061329 pamphlet.
  • geometric isomers cis-trans isomers
  • optical isomers enantiomers, diastereomers
  • tautomers of the compound are isolated and purified by usual methods such as column chromatography and HPLC. You can also
  • the compound contained in the preventive or therapeutic agent for age-related macular degeneration according to the present invention has the formula (1): Or an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof.
  • R 1 represents a hydrogen atom, a lower alkyl group, or a lower alkyl group substituted with a halogen atom.
  • R 2 represents a hydrogen atom, a lower alkyl group, or a lower alkyl group substituted with a halogen atom.
  • R 3 represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkyl group substituted with a halogen atom.
  • R 4 represents a 6-membered nitrogen-containing aromatic ring group which is unsubstituted or substituted with R 5 .
  • R 5 represents a halogen atom, a lower alkyl group or a lower alkyl group substituted with a halogen atom.
  • R 1 is preferably a lower alkyl group or a lower alkyl group substituted with a halogen atom, particularly preferably a lower alkyl group, and most preferably methyl.
  • R 2 is preferably a hydrogen atom or a lower alkyl group, and particularly preferably a hydrogen atom.
  • R 3 is preferably a lower alkyl group or a lower alkyl group substituted with a halogen atom, particularly preferably a lower alkyl group, and most preferably isopropyl.
  • R 4 is preferably formula (2a) or (2b), particularly preferably formula (2b).
  • R 5 is preferably a lower alkyl group or a lower alkyl group substituted with a halogen atom, particularly preferably a lower alkyl group substituted with a halogen atom, most preferably trifluoromethyl. It is.
  • the above formula (1) is preferably the formula (1 ′): It is.
  • Specific examples of the compound represented by the above formula (1) or formula (1 ′) include the formula (1a): 1,5-anhydro-2,3-dideoxy-3- ⁇ [(1R, 3S) -3-isopropyl-3-( ⁇ (1S, 4S) -5- [5- (trifluoromethyl)] Pyridazin-3-yl] -2,5-diazabicyclo [2,2,1] hept-2-yl ⁇ carbonyl) cyclopentyl] amino ⁇ -4-O-methyl-D-erythro-pentitol (hereinafter referred to as “Compound 1a Also enantiomers and diastereomers, and mixtures thereof (eg, racemic mixtures, diastereo mixtures, etc.).
  • Specific examples of the compound represented by the formula (1) or the formula (1 ′) include a formula (1b): 1,5-anhydro-2,3-dideoxy-3- ⁇ [(1R, 3S) -3-isopropyl-3-( ⁇ (1S, 4S) -5- [6- (trifluoromethyl)] Pyrimidin-4-yl] -2,5-diazabicyclo [2,2,1] hept-2-yl ⁇ carbonyl) cyclopentyl] amino ⁇ -4-O-methyl-D-erythro-pentitol (hereinafter referred to as “Compound 1b Also enantiomers and diastereomers, and mixtures thereof (eg, racemic mixtures, diastereo mixtures, etc.).
  • the “pharmaceutically acceptable salt” of the compound represented by the above formula (1), (1 ′), (1a) or (1b) includes, for example, a salt with an inorganic acid or a salt with an organic acid. It is done.
  • the inorganic acid include hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, sulfuric acid, phosphoric acid and the like.
  • organic acids include acetic acid, fumaric acid, maleic acid, succinic acid, citric acid, tartaric acid, adipic acid, gluconic acid, glucoheptonic acid, glucuronic acid, terephthalic acid, methanesulfonic acid, lactic acid, hippuric acid, 1, 2 -Ethanedisulfonic acid, isethionic acid, lactobionic acid, oleic acid, pamoic acid, polygalacturonic acid, stearic acid, tannic acid, trifluoromethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, lauryl sulfate, methyl sulfate, naphthalene Examples include sulfonic acid and sulfosalicylic acid.
  • the compound represented by the above formula (1), (1 '), (1a) or (1b) may be in the form of a hydrate or a solvate.
  • crystal polymorph group refers to various crystal forms depending on conditions and states (including the formulated state in this state) such as production, crystallization, and storage of these crystals. It means the crystal form and the whole process at each stage when changing.
  • age-related macular degeneration refers to wet age-related macular degeneration, atrophic age-related macular degeneration, and early age-related macular degeneration as a precursor lesion thereof as described above.
  • this compound When this compound is used for the prevention or treatment of age-related macular degeneration, it can be administered to patients orally or parenterally.
  • oral administration topical administration to the eye (instillation administration) , Intraconjunctival sac administration, intravitreal administration, subconjunctival administration, subtenon administration, etc.), intravenous administration, transdermal administration, and the like.
  • an eye drop or an eye ointment is used, or an injection, particularly a subconjunctival agent, a tenon sac administration agent or an intravitreal administration agent is used. Used.
  • a preparation containing the present compound as an active ingredient is formulated into a dosage form suitable for administration together with a pharmaceutically acceptable additive, if necessary.
  • dosage forms suitable for oral administration include tablets, capsules, granules, powders, and the like.
  • dosage forms suitable for parenteral administration include injections, eye drops, eye ointments, and patches.
  • Agents, gels, intercalating agents and the like can be prepared using conventional techniques widely used in the field.
  • it may be a DDS preparation such as an intraocular implant preparation or a microsphere.
  • a tablet can be prepared by appropriately selecting an excipient, a disintegrant, a binder, a lubricant, a coating agent, a corrigent and the like.
  • the excipient include lactose, glucose, D-mannitol, anhydrous calcium hydrogen phosphate, starch, and sucrose.
  • the disintegrant include carboxymethylcellulose, carboxymethylcellulose calcium, croscarmellose sodium, crospovidone, starch, partially pregelatinized starch, and low-substituted hydroxypropylcellulose.
  • binder examples include hydroxypropyl cellulose, ethyl cellulose, gum arabic, starch, partially pregelatinized starch, polyvinyl pyrrolidone, and polyvinyl alcohol.
  • lubricant examples include magnesium stearate, calcium stearate, talc, hydrous silicon dioxide, and hardened oil.
  • coating agent examples include purified sucrose, hydroxypropylmethylcellulose, hydroxypropylcellulose, methylcellulose, ethylcellulose, polyvinylpyrrolidone and the like.
  • corrigent examples include citric acid, aspartame, ascorbic acid, menthol and the like.
  • injections can be prepared by selecting and using isotonic agents, buffering agents, surfactants, thickeners and the like as necessary.
  • isotonizing agent sodium chloride etc. are mentioned, for example.
  • buffering agent include sodium phosphate.
  • surfactant include polyoxyethylene sorbitan monooleate.
  • thickener include methyl cellulose.
  • the eye drops can be selected and used as necessary from isotonic agents, buffering agents, surfactants, stabilizers, preservatives, etc., and the pH is acceptable for ophthalmic preparations.
  • isotonic agent include sodium chloride and concentrated glycerin.
  • buffering agent include sodium phosphate and sodium acetate.
  • surfactant include polyoxyethylene sorbitan monooleate, polyoxyl 40 stearate, polyoxyethylene hydrogenated castor oil, and the like.
  • stabilizer include sodium citrate and sodium edetate.
  • the preservative include benzalkonium chloride and paraben.
  • the eye ointment can be prepared using a commonly used base such as white petrolatum, liquid paraffin and the like.
  • the intercalating agent is prepared by crushing and mixing a biodegradable polymer, for example, a biodegradable polymer such as hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxyvinyl polymer, polyacrylic acid and the like, and compressing the powder. And an excipient, a binder, a stabilizer, and a pH adjuster can be used as necessary.
  • a biodegradable polymer for example, a biodegradable polymer such as hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxyvinyl polymer, polyacrylic acid and the like.
  • an excipient, a binder, a stabilizer, and a pH adjuster can be used as necessary.
  • an intraocular implant preparation can be prepared using a biodegradable polymer, for example, a biodegradable polymer such as polylactic acid, polyglycolic acid, lactic acid / glycolic acid copolymer, and hydroxypropylcellulose.
  • a biodegradable polymer such as polylactic acid, polyglycolic acid, lactic acid / glycolic acid copolymer, and hydroxypropylcellulose.
  • the dose of this compound can be appropriately changed according to the dosage form, the severity of the patient's symptoms, age, weight, eye volume, doctor's judgment, etc. 0.01 to 10000 mg per day, preferably 0.1 to 5000 mg, more preferably 0.5 to 2500 mg can be administered in one or several divided doses. For adults, 0.0001 to 2000 mg can be administered once or in several divided doses. In the case of eye drops or intercalating agents, 0.000001 to 10% (w / v), preferably 0.00001 to 1% (w / v), more preferably 0.0001 to 0.1% ( The active ingredient concentration of w / v) can be administered once or several times a day.
  • a patch containing 0.0001 to 2000 mg can be applied to an adult.
  • a patch containing 0.0001 to 2000 mg can be applied to an adult.
  • an intraocular implant preparation 0.0001 to 2000 mg is included for an adult.
  • An intraocular implant formulation can be implanted in the eye.
  • Rats were anesthetized by intramuscular administration of 1 mL / kg of a mixed solution (7: 1) of 5% (W / V) ketamine hydrochloride injection and 2% xylazine hydrochloride injection, and 0.5% (W / V) Tropicamide-0.5% phenylephrine hydrochloride ophthalmic solution was instilled to make mydriasis, and then photocoagulated with a krypton laser photocoagulator.
  • Photocoagulation was performed in the posterior region of the fundus, avoiding thick retinal blood vessels, and focusing on the deep retina at 8 spots per eye (coagulation conditions: spot size 100 ⁇ m, output 100 mW, coagulation time 0.1 seconds). . After photocoagulation, fundus photography was performed to confirm the laser irradiation site.
  • Compound 1b is mixed with 1% (W / V) methylcellulose solution (prepared by dissolving methylcellulose in purified water) to 0.2 and 2 mg / mL, and compound 1b is administered at doses of 1 and 10 mg / kg.
  • the liquid was orally administered twice a day for 7 days including the operation day from the photocoagulation operation day.
  • a 1% (W / V) methylcellulose solution was similarly administered to the base administration group.
  • Inhibition rate (%) ⁇ (A 0 ⁇ A X ) / A 0 ⁇ ⁇ 100
  • a 0 incidence rate of choroidal neovascularization in base administration group
  • a X incidence rate of choroidal neovascularization in drug administration group
  • Compound 1b was shown to inhibit choroidal neovascularization in a laser-induced rat choroidal neovascularization model animal. From the above results, it was shown that the present compound has an excellent angiogenesis inhibitory action in the choroid and has an excellent preventive or therapeutic effect on age-related macular degeneration, particularly wet age-related macular degeneration.
  • formulation example The pharmaceutical agent of the present invention will be described more specifically with formulation examples, but the present invention is not limited to these formulation examples.
  • eye drops having a concentration of 0.05% (w / v) to 1% (w / v) can be prepared.
  • An eye ointment is prepared by adding this compound to uniformly melted white petrolatum and liquid paraffin, mixing them well, and gradually cooling. By changing the amount of this compound added, an eye ointment having a concentration of 0.05% (w / v) to 1% (w / w) can be prepared.
  • Formulation Example 3 1 mg of this compound in 100 mg of tablets Lactose 66.4mg Corn starch 20mg Carboxymethylcellulose calcium 6mg Hydroxypropylcellulose 6mg Magnesium stearate 0.6mg
  • This compound and lactose are mixed in a blender, carboxymethylcellulose calcium and hydroxypropylcellulose are added to the mixture and granulated. The resulting granules are dried and sized, and magnesium stearate is added to the sized granules. Mix and compress with a tableting machine. In addition, tablets with a content of the present compound in 100 mg of 0.1 mg to 50 mg can be prepared by appropriately changing the addition amount of the present compound, carboxymethylcellulose calcium and hydroxypropylcellulose.
  • an injection with a content of the present compound in 10 mL of 2 mg to 200 mg can be prepared.
  • the injection prepared as described above can be administered as an injection for intraocular administration, for example, an intravitreal administration.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

　La présente invention se rapporte à un agent prophylactique ou thérapeutique pour la dégénérescence maculaire liée à l'âge, qui contient en tant que principe actif, un composé représenté par la formule (1), un énantiomère ou un diastéréomère de celui-ci, ou un sel pharmacologiquement acceptable de celui-ci (également appelé "ce composé" ci-dessous).
PCT/JP2015/070478 2014-07-17 2015-07-17 Agent prophylactique ou thérapeutique pour la dégénérescence maculaire liée à l'âge Ceased WO2016010131A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2014-146574 2014-07-17
JP2014146574 2014-07-17

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WO2016010131A1 true WO2016010131A1 (fr) 2016-01-21

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JP (1) JP2016029038A (fr)
TW (1) TW201605451A (fr)
WO (1) WO2016010131A1 (fr)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012509931A (ja) * 2008-11-26 2012-04-26 ファイザー・インク ケモカイン受容体モジュレーターとしての３−アミノシクロペンタンカルボキサミド

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012509931A (ja) * 2008-11-26 2012-04-26 ファイザー・インク ケモカイン受容体モジュレーターとしての３−アミノシクロペンタンカルボキサミド

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
SENNLAUB, FLORIAN ET AL.: "CCR2+ monocytes infiltrate atrophic lesions in age-related macular disease and mediate photoreceptor degeneration in experimental subretinal inflammation in Cx3cr1 deficient mice", EMBO MOLECULAR MEDICINE, vol. 5, no. 11, 2013, pages 1775 - 1793 *
XIE, PING ET AL.: "Suppression and regression of choroidal neovascularization in mice by a novel CCR2 antagonist, INCB3344", PLOS ONE, vol. 6, no. 12, 2011, pages 1 - 10 *

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JP2016029038A (ja) 2016-03-03
TW201605451A (zh) 2016-02-16

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