<?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>0001602474</rptOwnerCik>
            <rptOwnerName>Dalal Anupam</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>

    <nonDerivativeTable>
        <nonDerivativeHolding>
            <securityTitle>
                <value>Common Stock</value>
            </securityTitle>
            <postTransactionAmounts>
                <sharesOwnedFollowingTransaction>
                    <value>7882</value>
                    <footnoteId id="F1"/>
                </sharesOwnedFollowingTransaction>
            </postTransactionAmounts>
            <ownershipNature>
                <directOrIndirectOwnership>
                    <value>I</value>
                </directOrIndirectOwnership>
                <natureOfOwnership>
                    <value>See Footnote</value>
                    <footnoteId id="F2"/>
                </natureOfOwnership>
            </ownershipNature>
        </nonDerivativeHolding>
    </nonDerivativeTable>

    <footnotes>
        <footnote id="F1">These shares 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.</footnote>
        <footnote id="F2">Consists of 7,882 shares of Common Stock owned directly by TWHVP SPV, LLC, or TWHVP. The general partner of TWHVP is Kearny Venture Associates II, LLC or KVA II.  KVA II has the sole voting and investment control over the shares owned by TWHVP and the Managing Members of KVA II have sole voting and investment control over the shares controlled by KVA II.  The Managing Members of KVA II are Caley Castelein, Anupam Dalal and Andrew Jensen.  None of the Managing Members of KVA II has individual voting or investment power with respect to such shares and each disclaims beneficial ownership of such shares except to the extent of any pecuniary interest therein.</footnote>
    </footnotes>

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

    <ownerSignature>
        <signatureName>/s/Anupam Dalal</signatureName>
        <signatureDate>2017-03-17</signatureDate>
    </ownerSignature>
</ownershipDocument>
