<?xml version="1.0"?>
<ownershipDocument>

    <schemaVersion>X0206</schemaVersion>

    <documentType>3</documentType>

    <periodOfReport>2017-03-15</periodOfReport>

    <noSecuritiesOwned>0</noSecuritiesOwned>

    <issuer>
        <issuerCik>0001422142</issuerCik>
        <issuerName>Aerpio Pharmaceuticals, Inc.</issuerName>
        <issuerTradingSymbol>NONE</issuerTradingSymbol>
    </issuer>

    <reportingOwner>
        <reportingOwnerId>
            <rptOwnerCik>0001700917</rptOwnerCik>
            <rptOwnerName>Dugel Pravin</rptOwnerName>
        </reportingOwnerId>
        <reportingOwnerAddress>
            <rptOwnerStreet1>C/O AERPIO PHARMACEUTICALS, INC.</rptOwnerStreet1>
            <rptOwnerStreet2>9987 CARVER ROAD, SUITE 420</rptOwnerStreet2>
            <rptOwnerCity>CINCINNATI</rptOwnerCity>
            <rptOwnerState>OH</rptOwnerState>
            <rptOwnerZipCode>25242</rptOwnerZipCode>
            <rptOwnerStateDescription></rptOwnerStateDescription>
        </reportingOwnerAddress>
        <reportingOwnerRelationship>
            <isDirector>1</isDirector>
            <isOfficer>0</isOfficer>
            <isTenPercentOwner>0</isTenPercentOwner>
            <isOther>0</isOther>
        </reportingOwnerRelationship>
    </reportingOwner>

    <derivativeTable>
        <derivativeHolding>
            <securityTitle>
                <value>Stock Option (Right to Buy)</value>
            </securityTitle>
            <conversionOrExercisePrice>
                <value>1.40</value>
            </conversionOrExercisePrice>
            <exerciseDate>
                <footnoteId id="F1"/>
                <footnoteId id="F2"/>
            </exerciseDate>
            <expirationDate>
                <value>2024-10-22</value>
            </expirationDate>
            <underlyingSecurity>
                <underlyingSecurityTitle>
                    <value>Common Stock</value>
                </underlyingSecurityTitle>
                <underlyingSecurityShares>
                    <value>16742</value>
                </underlyingSecurityShares>
            </underlyingSecurity>
            <ownershipNature>
                <directOrIndirectOwnership>
                    <value>D</value>
                </directOrIndirectOwnership>
            </ownershipNature>
        </derivativeHolding>
    </derivativeTable>

    <footnotes>
        <footnote id="F1">These options were acquired pursuant to an Agreement and Plan of Merger, dated as of March 7, 2017 (the &quot;Merger Agreement&quot;), pursuant to which a wholly-owned subsidiary of the Company merged with and into Aerpio Therapeutics, Inc. (&quot;Aerpio&quot;). Pursuant to the Merger Agreement, the then outstanding shares of Aerpio's common stock and outstanding shares of each series of Aerpio's preferred stock were cancelled and were automatically converted into the right to received shares of the Company's common stock on a 2.3336572-1 basis upon closing of the merger.</footnote>
        <footnote id="F2">(Continued from Footnote 1) This stock option was granted under Aerpio's 2011 Equity Incentive Plan and vests over four (4) years beginning on October 5, 2015, at a rate of twenty-five percent (25%) after 12 months, and in thirty-six (36) equal monthly installments thereafter. This stock option represents options that the Company issued in connection with the merger pursuant to which options to purchase Aerpio common stock were converted into options to purchase the Company's common stock on a 2.3336572-1 basis.</footnote>
    </footnotes>

    <remarks>Exhibit 24.1: Limited Power of Attorney</remarks>

    <ownerSignature>
        <signatureName>/s/ Pravin Dugel</signatureName>
        <signatureDate>2017-03-17</signatureDate>
    </ownerSignature>
</ownershipDocument>
